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新的苯磺酰脲類化合物、其制備方法及其作為除草劑和植物生長調(diào)節(jié)劑的應(yīng)用的制作方法

文檔序號:308544閱讀:2687來源:國知局
專利名稱:新的苯磺酰脲類化合物、其制備方法及其作為除草劑和植物生長調(diào)節(jié)劑的應(yīng)用的制作方法
技術(shù)領(lǐng)域
本發(fā)明涉及除草劑和植物生長調(diào)節(jié)劑,特別是在有用植物中選擇性防除闊葉和禾本科雜草的除草劑。
已知在苯環(huán)上帶有一個氨基的或一個功能化的氨基基團(tuán)的雜環(huán)取代的苯石磺酰脲類化合物具有除草劑和植物生長調(diào)節(jié)劑的性質(zhì)。(EP-A-1515,US-A-4,892,946;US-A-4,981,509;EP-A-116518,US-A-4,664,695和US-A-4,632,695)。
令人驚奇地發(fā)現(xiàn),某些雜環(huán)取代的苯磺酰脲類化合物特別適合于作為除草劑和植物生長調(diào)節(jié)劑。
本發(fā)明的對象是式(Ⅰ)化合物或其鹽
(Ⅰ)
式中
R1是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基、其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、CONH2、C1-C4-烷硫基、CN、CHO、(C1-C6-烷基)-羰基、(C3-C6-環(huán)烷基)-羰基、C1-C4-烷基磺?;?、羧基、(C1-C4-烷氧基)-羰基、(C2-C4-鏈烯氧基)-羰基、(C2-C4-炔氧基)-羰基、NO2、NH2、單一和二-(C1-C6)-烷基氨基的基團(tuán)取代,
R2是CO-R5、COO-R6、CO-SR7、CO-NR8R9、CS-NR10R11、CS-OR12、CS-SR13、SO2R14、SO2NR15R16,
R3是COR17、CO-OR18、CO-NR19R20、CO-SR21、CO-O-N=CR22R23、CSR24、CSSR25、CS-OR26、CS-NR27R28、C(=NR29)R30,
R4是H、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個鹵素取代,
R5是H、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基、其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,或是未取代的或取代的C3-C8-環(huán)烷基、未取代的或取代的苯基、未取代的或取代的雜芳基或苯基-C1-C4-烷基,其苯環(huán)上是未取代的或取代的,
R6是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基、其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代、或C3-C6-環(huán)烷基,它是未取代的或被一個或多個選自鹵素、C1-C4-烷基和C1-C4-烷氧基的基團(tuán)取代、或C3-C6-環(huán)烷基-C1-C3-烷基,
R7類似于R6,
R8是H、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個鹵素基取代、或是(C1-C6-烷氧基)-羰基,或C1-C4-烷氧基,
R9是H、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代、或是CO-R33、CO-OR34、CO-NR35R36、CS-NR35R36、CS-R33或CS-OR34或
R8和R9一起組成一個式-(CH2)4-、-(CH2)5-、-CH2CH2-O-CH2CH2-、-CH2CH2-NH-CH2CH2-的二價基團(tuán),其中后4個基團(tuán)是未取代的或被C1-C4-烷基取代,
R10類似于R8,
R11類似于R9,
R12類似于R6,
R13類似于R6,
R14是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基、其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,
R15類似于R8,
R16是氫、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個鹵素取代,
R17類似于R5,
R18是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基、其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,或是C3-C6-環(huán)烷基,它是未取代的或被一個或多個選自鹵素、C1-C4-烷基和C1-C4-烷氧基的基團(tuán)取代、或是C3-C6-環(huán)烷基-C1-C3-烷基或H,
R19類似于R8,
R20類似于R9,
R21類似于R18,
R22是H、C1-C4-烷基、C3-C5-鏈烯基或C3-C5炔基,
R23是H、C1-C4-烷基、C3-C5-鏈烯基或C3-C5-炔基,
R24類似于R17,
R25類似于R18,
R26類似于R18,
R27類似于R8,
R28類似于R9,
R29是H、OH、NH2、NHR37、N(R37)2、C1-C4-烷基、C1-C4-烷氧基、C2-C4-鏈烯基或C2-C4-炔基,其中后4個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C3-烷氧基和C1-C3-烷硫基的基團(tuán)取代,
R30是H、C1-C6-烷基、C1-C6-烷氧基、C2-C6-鏈烯基、C2-C6-炔基、其中后4個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C3-烷氧基和C1-C3-烷硫基的基團(tuán)取代,
R31是H、C1-C4-烷基,(C1-C4-烷基)-羰基、(C1-C4-烷氧基)-羰基或CHO,
R32分別是H或C1-C4-烷基,
R33類似于R5,
R34類似于R6,
R35,R36分別相互獨(dú)立地是H、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個鹵素取代,
R37是C1-C4-烷基,C2-C4-鏈烯基或C2-C4-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基和C1-C4-烷硫基的基團(tuán)取代,
W是O或S,
X,Y分別相互獨(dú)立地是H、鹵素、C1-C6-烷基,C1-C6-烷氧基或C1-C6-烷硫基,其中后3個基團(tuán)是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基和C1-C4-烷硫基的基團(tuán)取代,或是單一或二-(C1-C4-烷基)-氨基、C3-C6-環(huán)烷基,C3-C5-鏈烯基,C3-C5-烯氧基或C3-C5-炔氧基,和
Z是CH或N。
在式(1)和后面的式中的烷基,烷氧基、鹵代烷基、鹵代烷氧基、烷基氨基和烷硫基以及相應(yīng)的不飽和的和/或在碳骨架上的取代基每個都可是直鏈的或支鏈的。如果未作特別說明,這些基團(tuán)優(yōu)選帶1至4個C原子的碳骨架,或?qū)τ诓伙柡突鶊F(tuán)來說優(yōu)選帶2至4個C原子的基團(tuán)。烷基基團(tuán)及在那些組合含義的基團(tuán)如烷氧基、鹵代烷基等中出現(xiàn)的烷基是指例如甲基、乙基、正-或異丙基、正-,異-,叔-或2-丁基、戊基、己基如正己基、異己基和1,4-二甲基戊基;鏈烯基和炔基具有與烷基相對應(yīng)的、可能的不飽和基團(tuán)的含義,鏈烯基是指例如烯丙基、1-甲基丙-2-烯-1-基、2-甲基-丙-2-烯-1-基、丁-2-烯-1-基、丁-3-烯-1-基、1-甲基-丁-3-烯-1-基和1-甲基丁-2-烯-1-基;炔基是指例如炔丙基、丁-2-炔-1-基、丁-3-炔-1-基、1-甲基-丁-3-炔-1-基。
鹵素是指氟、氯、溴或碘。鹵代-烷基、-烯基和-炔基是指被鹵素、優(yōu)選被氟、氯和/或溴、特別是被氟或氯部分地或全部取代的烷基、鏈烯基或炔基,例如CF3、CHF2、CH2F、CF3-CF2、CH2FCHCl、CCl3、CHCl2、CH2CH2Cl;鹵代烷氧基是例如OCF3、OCHF2、OCH2F、CF3CF2O、OCH2CF3和OCH2CH2Cl。相應(yīng)地這也適合于鹵代烯基和其它被鹵素取代的基團(tuán)。
芳基是指單一、二-或多環(huán)芳香系統(tǒng),例如苯基、萘基、四氫萘基、茚基、茚滿基、戊搭烯基、芴基和類似物,優(yōu)選苯基;芳氧基優(yōu)選與所列舉的芳基相對應(yīng)芳氧基團(tuán),特別是苯氧基。
雜芳基是一個單一、二-或多環(huán)芳香族系統(tǒng),在這個系統(tǒng)中至少1個環(huán)含有一個或多個雜原子,例如吡啶基、嘧啶基、噠嗪基、吡嗪基、噻吩基、噻唑基、噁唑基、呋喃基、吡咯基、吡唑基和咪唑基,但也還包括雙環(huán)的芳香族或芳脂族化合物,例如喹啉基、苯并噁唑基等。
取代的芳基、雜芳基、苯基、芐基或帶有芳香族部分的取代的雙環(huán)基團(tuán)指的是例如一個由未取代的母體衍生的取代基,其中取代基是例如一個或多個、優(yōu)選1、2或3個選自鹵素、烷基、鹵代烷基、烷氧基、鹵代烷氧基、烷硫基、羥基、氨基、硝基、氰基、烷氧基羰基、烷基羰基、甲?;?、氨基甲?;我缓投?烷基氨基羰基、單-或二-烷基氨基、烷基亞磺?;屯榛酋;幕鶊F(tuán),帶C原子的基團(tuán)優(yōu)選帶1至4個C原子、特別是帶1或2個C原子。通常取代基優(yōu)選鹵素例如氟和氯、C1-C4-烷基,優(yōu)選甲基或乙基、C1-C4-鹵代烷基,優(yōu)選三氟甲基、C1-C4-烷氧基,優(yōu)選甲氧基或乙氧基、C1-C4-鹵代烷氧基、硝基和氰基。其中取代基特別優(yōu)選甲基、甲氧基和氯。
需要時取代的苯基是例如萘基,它是未取代的或單-或多取代的,優(yōu)選多至三取代、取代基是相同的或不同的,選自鹵素、C1-C4-烷氧基、C1-C4-鹵代烷基、C1-C4-鹵代烷氧基和硝基,例如鄰位-、間位-和對位-甲苯基、二甲苯基、2-、3-和4-氯代苯基、2-,3-和4-三氟-和-三氯苯基、2,4-、3,5-、2,5-和2,3-二氯代苯基、鄰位-,間位-和對位-甲氧基苯基。
雜芳基優(yōu)選5-或6-元的且含1、2或3個雜原子,優(yōu)選含N、O和S的雜芳基。該基團(tuán)可苯并稠合。這些基團(tuán)是如環(huán)氧乙烷基、吡咯烷基、哌啶基、二氧戊環(huán)基、吡唑基、嗎啉基、呋喃基、四氫呋喃基、吲哚基、喹啉基、嘧啶基、氮雜
基、咪唑基、噻唑基、噻吩基和惡唑基。
本發(fā)明還涉及式(Ⅰ)所包括的所有立體異構(gòu)體及其混合物。式(Ⅰ)所示的這類化合物含有一個或多個不對稱碳原子,或還包括在通式(Ⅰ)沒有特別給定的雙鍵。由它們特定的空間形式所確定的可能的立體異構(gòu)體如對映體、非對映體、Z-和E-異構(gòu)體全部在式(Ⅰ)范疇之內(nèi),可按通常的方法從立體異構(gòu)體的混合物中得到,或通過立體選擇反應(yīng)與應(yīng)用立體化學(xué)純的原料相結(jié)合的方法制備。
式(Ⅰ)化合物可形成鹽,在這些鹽中,-SO2NH-基團(tuán)的或其它酸的氫原子(例如由COOH等)將被一個農(nóng)業(yè)上適用的陽離子取代。這些鹽例如是金屬鹽,特別是堿金屬(例如Na或K鹽)或堿土(金屬)的鹽,或也可是銨鹽或與有機(jī)胺的鹽。同樣也可以將一個酸加成到堿性基團(tuán)和氨基和烷基氨基上成鹽。合適的酸是強(qiáng)無機(jī)酸和有機(jī)酸,例如HCl,HBr,H2SO4或HNO3。
首先,基于高效的除草性能、更好的選擇性和/或更易于制備,下面式(Ⅰ)化合物或它們的鹽是特別有意義的,式中
R1是C1-C4-烷基、C2-C4-鏈烯基或C2-C4-炔基、優(yōu)選C1-C4-烷基、烯丙基或炔丙基或
R2是CO-R5、COOR6、CO-NR8R9、CS-NR10R11、SO2R14或SO2NR15R16或
R3是COR17、COOR18、CONR19R20或CO-ON=CR22R23,優(yōu)選COOR18,或
R4是H或C1-C4-烷基,優(yōu)選H或甲基,或
R5是H、C1-C6-烷基,它是未取代的或被一個或多個鹵素或被C1-C4-烷氧基、C1-C4-烷硫基或NR31R32的基團(tuán)取代,或是C3-C6-環(huán)烷基、未取代的或取代的苯基、未取代的或取代的芐基或未取代的或取代的雜芳基,優(yōu)選H、C1-C6-烷基、C1-C4-鹵代烷基、環(huán)丙基、環(huán)戊基、環(huán)己基、苯基或雜芳基,其中后2個基團(tuán)是未取代的或被一個或多個選自C1-C4-烷基,C1-C4-烷氧基和鹵素的基團(tuán)取代,或
R6是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基、C1-C6-鹵代烷基或C3-C6-環(huán)烷基,優(yōu)選C1-C4-烷基、C1-C4-鹵代烷基、烯丙基、炔丙基或C3-C6-環(huán)烷基,或
R7是C1-C4-烷基,
R8是H、C1-C6-烷基、C1-C4-鹵代烷基、C1-C4-烷氧基或(C1-C4-烷氧基)-羰基,
R9是氫、C1-C6-烷基,它是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基和NR31R32的基團(tuán)取代,或CO-R33,CO-OR34或CO-NR35R36或
R8和R9一起組成一個式-(CH2)4-、-(CH2)5-或-CH2CH2-O-CH2CH2-的二價基團(tuán)或
R14是C1-C6-烷基、C1-C6-鹵代烷基,優(yōu)選C1-C4-烷基或C1-C4-鹵代烷基或
R15,R16分別相互獨(dú)立地是氫或C1-C4-烷基或
R17是氫或C1-C4-烷基、C1-C4-鹵代烷基,C3-C6-環(huán)烷基、苯基或雜芳基,其中后2個基團(tuán)是未取代的或取代的,或
R18是氫、C1-C4-烷基、C2-C6-鏈烯基或C2-C6-炔基,其中后3個基團(tuán)是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,或C3-C6-環(huán)烷基或C3-C6-環(huán)烷基-C1-C3-烷基或
R22是氫或C1-C2-烷基或
R23是氫或C1-C2-烷基或
R29是氫、羥基、氨基、NHCH3、N(CH3)2、C1-C4-烷基或C1-C4-烷氧基,
R30是氫或C1-C4-烷基或
R31相互獨(dú)立地是H或C1-C4-烷基或
R32相互獨(dú)立地是H或C1-C4-烷基或
R33是氫、C1-C4-烷基、C1-C4-鹵代烷基,C3-C6-環(huán)烷基或苯基,它是未取代的或被一個或多個選自鹵素、C1-C4-烷基和C1-C4-烷氧基的基團(tuán)取代,或
R34是C1-C4-烷基、烯丙基、炔丙基或環(huán)烷基或
R35是氫或C1-C4-烷基或
R36是氫或C1-C4-烷基或
X是C1-C4-烷基、C1-C4-烷氧基、C1-C4-鹵代烷基、C1-C4-烷硫基、鹵素或單-或二-(C1-C2-烷基)-氨基,優(yōu)選甲基、乙基、甲氧基、乙氧基、甲硫基、乙硫基、氯、NHCH3或N(CH3)2,或
Y是C1-C4-烷基、C1-C4-烷氧基、C1-C4-鹵代烷基或C1-C4-烷硫基,優(yōu)選甲基、乙基、甲氧基或乙氧基,
或優(yōu)選這樣的式(Ⅰ)化合物或其鹽,即在式(Ⅰ)中連有二個或多個具有前面所列舉的特殊的或優(yōu)選含義的R1至R36基團(tuán)。
優(yōu)選這樣的式(Ⅰ)化合物或其鹽,在式中
R1是甲基、乙基、正丙基、異丙基或烯丙基、
R2是CO-R5、COOR6、CO-NR8R9、CS-NR10R11、SO2R14或SO2NR15R16,
R5是H、C1-C4-烷基、C1-C2-鹵代烷基、環(huán)丙基、苯基、芐基或帶5或6個環(huán)原子的雜芳基,其中后3個基團(tuán)是未取代的或被一個或多個鹵素取代,
R6是C1-C6-烷基、烯丙基、炔丙基或環(huán)丙基,
R8是H、C1-C4-烷基、C1-C4-鹵代烷基或(C1-C4-烷氧基)-羰基,
R9是H或C1-C4-烷基,
R10是H或C1-C4-烷基,
R11是H或C1-C4-烷基,
R14是C1-C4-烷基,
R15是H或C1-C4-烷基和
R16是H或C1-C4-烷基。
特別優(yōu)選的是R5是H、CH3、C2H5、正-或異-丙基、正-、異-、叔-或2-丁基、正戊基、CF3、CH2Cl、CHCl2、CCl3、CH2Br、CH2CCl3、環(huán)丙基、苯基、噻吩基、呋喃基或吡啶基,其中后4個基團(tuán)可被1至3個鹵素原子取代。
本發(fā)明還涉及式(Ⅰ)所示本發(fā)明化合物或其鹽的制備方法,其特征在于,人們可用
a)一個式(Ⅱ)化合物
(Ⅱ)
與一個式(Ⅲ)雜環(huán)氨基甲酸酯反應(yīng),
(Ⅲ)
式中R*需要時是取代的苯基或C1-C4-烷基,或
b)一個式(Ⅳ)的磺?;惽杷狨?
(Ⅳ)
與一個式(Ⅴ)的氨基雜環(huán)化合物反應(yīng),
(Ⅴ)
或,c)一個式(Ⅱ)的化合物與一個式(Ⅹ)的(硫代)異氰酸酯在一種堿的存在下反應(yīng),
(Ⅹ)
其中在上面的式(Ⅱ)至(Ⅴ)和(Ⅹ)中的基團(tuán)R1至R4、W、X、Y和Z具有在式(Ⅰ)中所確定的含義,同時用方法a)和b)將首先得到W=O的式(Ⅰ)化合物。
式(Ⅱ)和(Ⅲ)化合物的反應(yīng)優(yōu)選于一惰性有機(jī)溶劑如二氯甲烷、乙腈、二噁烷或四氫呋喃中堿催化進(jìn)行,反應(yīng)溫度在0℃至、優(yōu)選20℃至溶劑沸點(diǎn)之間。作為堿可用例如有機(jī)胺堿,如1,8-重氮雙環(huán)-〔5.4.0〕十一碳-7-烯(DBU),特別是R*=(取代的)苯基時(參見EP-A-44807),或用三甲基鋁或三乙基鋁,后者特別適合于R*=烷基時使用(參見EP-A-166516)。
磺酰胺(Ⅱ)和磺酰基異氰酸酯(Ⅳ)是新的化合物。它們和它們的制備也是本發(fā)明的對象。
人們可從式(Ⅵ)化合物與一個強(qiáng)酸反應(yīng)得到式(Ⅱ)化合物(參見WO-89/10921)
(Ⅵ)
式中R1、R2和R3的含義如在式(Ⅰ)中所確定。
可用于反應(yīng)的強(qiáng)酸有例如無機(jī)酸,如H2SO4或HCl,或強(qiáng)有機(jī)酸,如三氟醋酸。叔丁基保護(hù)基團(tuán)脫去的反應(yīng)可在-20℃至每個反應(yīng)混合物的回流溫度下進(jìn)行,優(yōu)選的溫度是0℃至40℃。反應(yīng)可在物料或在一惰性溶劑、如二氯甲烷或三氯甲烷中進(jìn)行。
式(Ⅵ)化合物可由與式(Ⅵ)化合物相應(yīng)的式(Ⅵ)化合物(式中R2=H)與合適的親電物質(zhì)、如酰氯、酸酐、異氰酸酯、硫代異氰酸酯、磺酰氯或胺基磺酰氯反應(yīng)得到(參A.L.J.Beckniter in J.Zabicky,“The Chemistry of Amides”,73-185頁,Interscience,New York,1970;E.J.Corey et al.,Tetrahedron Lett.1978,1051;以及
H.J.Saunders,R.J.Slocombe,Chem.Rev.43,203(1948);
S.Ozaki,Chem.Rev.72,457,469(1972);
G.ZolB,Arzneim.-Forsch.33,2(1983);
Houben-Weyl-Hagemann,“MethodenderorganischenChemie”,4.Aufl.Bd.E4,
S.485ff.,ThiemeVerlagStuttgart,1983;
J.Golinsky,M.Mahosza,Synthesis1978,823;
Houben-Weyl-Müller,“MethodenderorganischenChemie”,4.Aufl.Bd.IX,S.338-400und605-622,ThiemeVelagStuttgart,1955;
Houben-Weyl-Klarmann,“MethodenderorganischenChemie”,4,Aufl.Bd.E11/2,S.1020-22,ThiemeVerlagStuttgart,1985;
S.Krishnamurthey,TetrahedronLett.23,3315(1982).).
這里所需要的N-單取代的氨基苯-衍生物,例如式(Ⅵ)的N-烷基氨基苯-衍生物(見式(Ⅵ),R2=H)可通過式(Ⅵ″)的苯胺(=式(Ⅵ),R1=H和R2=H)按標(biāo)準(zhǔn)方法進(jìn)行單烷基化反應(yīng)得到。例如式(Ⅵ″)的苯胺與羧酰氯或羧酸酐的?;磻?yīng)可生成相應(yīng)的N-?;?苯胺。隨后發(fā)生的?;被€原成類似的N-單取代的氨基官能基、如烷基氨基功能基的反應(yīng)是與合適的還原劑如二甲基硫化硼烷-絡(luò)合物進(jìn)行的,反應(yīng)生成式(Ⅵ)的苯胺衍生物(=式(Ⅵ),R2=H),并具有很好的收率;見S.Krish-namurthey,Tetrahedron Lett.23 3315(1982)。
所列舉的式(Ⅵ)的苯胺衍生物(=式(Ⅵ),R1和R2=H)可按文獻(xiàn)中所公布的方法通過式(Ⅶ)的硝基的還原,如在一個合適的催化劑如鈀-碳或阮內(nèi)-鎳催化劑存在下腹用氫進(jìn)行氫化反應(yīng),或通過在乙酸介質(zhì)中用鐵進(jìn)行還原反應(yīng)而得到。
(見.hierzuH.Berrie,G.T.Neuhold,F(xiàn).S.Spring,J.Chem.Soc.1952,2042;M.Freifelder,"CatalyticHydrogenationinOrganicSynthesisProceduresandCommentary”,J.WileyandSons,NewYork(1978),Kap.5).
式(Ⅶ)的芳香磺酰胺可由式(Ⅷ)的磺酸得到。
首先將式(Ⅷ)的磺酸基轉(zhuǎn)化成磺酰氯,例如可按照標(biāo)準(zhǔn)方法如磷酰氯或亞硫酰氯在惰性溶劑如乙腈和/或環(huán)丁砜中與相應(yīng)的磺酸的鉀鹽反應(yīng),或在一個物質(zhì)中通過加熱至回流(參見Houben-Weyl-Klamann,“MethodenderorganischenChemie”,4.Aufl.Bd.EX1/2,S.1067-1073,ThiemeVerlagStuttgart,1985)。
由磺酰氯與叔丁胺于乙醇中反應(yīng)生成式(Ⅶ)磺酰胺,反應(yīng)具有很好的收率(參見WO89/10921中的類似反應(yīng))。
式(Ⅷ)的磺酸是可由商品的2-甲基-5-硝基苯磺酸制備的。
2-甲基-5-硝基苯磺酸通過標(biāo)準(zhǔn)方法進(jìn)行其甲基的氧化反應(yīng),比如與高錳酸鉀反應(yīng)生成羧酸功能基以及需要時繼之進(jìn)行衍生化反應(yīng)如酯化反應(yīng)或形成酰胺,可將R3取代基引入。(參見,Houben-Weyl-Falbe“Methoden der Organischen Chemie”,4.Aufl.Bd.EV/1,Thieme Verlag Stuttgart,1985,S.199-202)。
通過一系列的標(biāo)準(zhǔn)反應(yīng)可得到很多不同的R3基團(tuán)。
*可用羧酸酐或酰氯與胺反應(yīng)得到羧酰胺(參見A.L.J.BeckwithinJ.Zabicky..“TheChemistryofAmides”,S.73-185.Interscience,NewYork1970)。
*可由羧酸和硫醇通過羰基活化反應(yīng),如與二苯基膦酰氯反應(yīng)得到硫代羧酸-S-酯(參見D.Scholz,D.Eigner,Monatsh.Chemie110,759(1979),S.Yamadaet.al.,J.Org.Chem.39,3302(1974);
* 可通過羧酸酯與合適的試劑,如P4S10反應(yīng)制備硫代羧酸-O-酯(參見S.O.Lauresson et.al.,Bull.Soc.Chim.Belg.87,293(1978);T.Nishiwaket.al.,Chem.Lett.1980,401));
*硫代羧酰胺可由羧酰胺經(jīng)“硫化反應(yīng)”如與五硫化磷反應(yīng)得到(Houben-Weyl-Falbe,“MethodenderOrganischenChemie”,4.Aufl.Bd.E5/2,S.1242-1247(和其中所列舉的文獻(xiàn)),Thieme-VerlagStuttgart,1985);
*醛可由羧酸或酯借助于一系列的還原劑而合成(Houben-Weyl-Falbe.“MethodenderOrganischenChemie”,4.Aufl.Bd.E3,S.418ff.,ThiemeVerlagStuttgart,1983)。
*功能化的醛衍生物如肟、肟醚、肼等可由醛與相應(yīng)的胺縮合得到(參見Houben-Weyl-Müller,“MethodenderOrganischenChemie,”4.Aufl.Bd.7/1,S.453-474,ThiemeVerlagStuttgart,1954);
*N-烷氧基-羧酸-酰亞胺-酯可由異羥肟酰溴衍生物和醇化物得到(E.C.Tayler,F(xiàn).Kienzle,J.Org.Chem.36,233(1971);
*羧酸-酰亞胺-酯可由酰氯酰亞胺和相應(yīng)的醇化物得到(參見H.Boehme,O.Müller,Chem.Ber.98,1450(1965);G.Bock,Chem.Ber.100,2870(1967);
*O-?;?肟是通過羧酸酐和酮肟反應(yīng)得到(參見S.Bittner,Y.Knobler,M.Frankel,TetrahedronLett.1965,95);
*異羥肟酸酰胺可由異羥肟酰氯衍生物與胺反應(yīng)得到(參見Houben-Weyl-Müller,“MethodenderOrganischenChemie”,4.Aufl.Bd.10/4,S.209ff.,Thieme-VerlagStuttgart,1968)。
另外,式(Ⅱ)的磺酰胺(式中R1和R2不是氫)可通過式(Ⅸb)所示的相應(yīng)的磺酰氯的氨基分解反應(yīng)得到,
它還可以由磺酸(Ⅸa)通過所列舉的標(biāo)準(zhǔn)方法(用所列舉的由(Ⅷ)生成(Ⅶ)的反應(yīng))很容易得到。
化合物(Ⅸa)還可由硝基苯磺酸(Ⅷ)通過下列反應(yīng)得到,
(1)類似于(Ⅶ)還原的還原反應(yīng),
(2)N-烷基化反應(yīng),和
(3)N-?;磻?yīng),
最后一個正如(Ⅵ)的制備反應(yīng)。
按照方法a),化合物(Ⅱ)的反應(yīng)所需的、式(Ⅲ)所示的氨基甲酸酯在文獻(xiàn)中有記載或可用類似于已知的方法制備(參見EP-A-70804或US-A-4,480,101)。
制備方法b)中,可用的式(Ⅳ)和(Ⅴ)所示的化合物可由所列舉的式(Ⅲ)和(Ⅷ)所示的化合物按照或類似于通常的方法制備。
式(Ⅳ)所示的苯基磺?;惽杷狨タ捎妙愃朴贓P-A-184385的方法由式(Ⅱ)所示的化合物與例如光氣反應(yīng)制備。
式(Ⅳ)化合物與氨基雜環(huán)化合物(Ⅴ)的反應(yīng)優(yōu)選在一惰性的非質(zhì)子溶劑如二噁烷、乙腈或四氫呋喃中、于0℃至溶劑沸點(diǎn)之間的溫度下進(jìn)行。
式(Ⅹ)的(硫代)異氰酸酯可按文獻(xiàn)中公布的方法制備(參見EP-A-232067,EP-A-166516)。
式(Ⅹ)化合物與式(Ⅱ)氨磺酰的反應(yīng)是在-10℃至100℃之間、優(yōu)選20至80℃之間,于一惰性的非質(zhì)子溶劑如丙酮或乙腈中,并在一個合適的堿如三乙基胺或碳酸鉀存在下進(jìn)行。
式(Ⅰ)化合物的鹽優(yōu)選在一惰性溶劑如水、甲醇、丙酮、二氯甲烷、四氫呋喃、甲苯或庚烷中,于0℃至100℃溫度下制備。制備本發(fā)明化合物的鹽所用的合適的堿是例如堿性碳酸鹽,如碳酸鉀、堿金屬-或堿土金屬氫氧化物、氨或一個合適的胺堿,如三乙基胺或乙醇胺。適合于成鹽的酸是例如HCl、HBr、H2SO4或HNO3。
前面制備方法中所提到的“惰性溶劑”是指那些在每一個反應(yīng)條件之下呈惰性的溶劑,而并非是在任何反應(yīng)條件下都必須呈惰性。
本發(fā)明的式(Ⅰ)化合物或其鹽對在農(nóng)業(yè)上具有重要經(jīng)濟(jì)意義的單子葉和雙子葉有害植物具有優(yōu)良的、廣譜的除草作用。用本發(fā)明的有效成分也可有效地防除那些以塊莖、根或其它存活期長的繁殖器官繁殖的難以防除的多年生雜草。至于在播種前、發(fā)芽前或發(fā)芽后施用無關(guān)緊要。這里列舉一些可用本發(fā)明化合物控制的單子葉和雙子葉雜草的代表,但不限于此。
可有效地防治的單子葉雜草有例如野燕麥、毒麥、看麥娘、
草、稗草、馬唐、狗尾草以及一年生的莎草類和每年生的冰草、狗牙根、白茅及蜀黍,還有多年生的莎草類。
可有效地防治的雙子葉一年生雜草有例如豬殃殃、紫花地丁、婆婆納、野芝麻、繁縷、莧、歐白芥、牽牛、母菊、苘麻、黃花稔以及多年生的田旋花、薊屬、酸模和蒿。
在水稻田特定栽培條件下出現(xiàn)的一些雜草如
菇、澤瀉、荸薺、扁桿藨草以及莎草也可用本發(fā)明的化合物有效地防除。
本發(fā)明的化合物也可以在發(fā)芽前作土壤表面處理,以完全阻止雜草發(fā)芽或者控制雜草只能長至子葉階段,使其停止繼續(xù)生長,三至四周后完全死亡。
如果在雜草出苗之后用有效成分施用于植物的綠色部分,施藥后雜草迅速停止生長,并使之停留在施藥時的生長階段或在施藥后一定時間死亡。用這種方式可使那些對農(nóng)作物有害的雜草盡早或永久地失去競爭力。
本發(fā)明的化合物雖已被證實(shí)對單子葉和雙子葉雜草具有優(yōu)良的除草活性,但它們對那些具有重要經(jīng)濟(jì)意義的農(nóng)作物如小麥、大麥、黑麥、水稻、玉米、甜菜、棉花和大豆影響很小或完全無害。正因?yàn)槿绱耍景l(fā)明的化合物適合于在農(nóng)作物中進(jìn)行選擇性除草。
此外還證實(shí)本發(fā)明化合物對農(nóng)作物具有顯著的生長調(diào)節(jié)作用。它能影響植物自身的物質(zhì)轉(zhuǎn)化;因此可以有目的地使之影響植物的內(nèi)含物質(zhì),也可以用它控制植物的株型和脫水干燥使之更易于收獲。它還可以調(diào)節(jié)和抑制植物瘋長,而不會使植物死亡。這種生長抑制作用對許多單子葉和雙子葉農(nóng)作物十分重要,因?yàn)榻璐丝梢詼p少或完全阻止倒伏。
本發(fā)明的化合物可制備成可濕性粉劑,乳油,可噴灑的溶液,粉劑或常規(guī)劑型的顆粒劑供使用。所以本發(fā)明的對象還包括用式(Ⅰ)化合物或其鹽制備的具有除草和植物生長調(diào)節(jié)性能的制劑。
式(Ⅰ)化合物可根據(jù)其有關(guān)生物學(xué)(或)化學(xué)-物理參數(shù)加工成不同的劑型。比如可考慮加工的劑型是可濕性粉劑(WP),水溶性粉劑(SP),水溶性濃縮物,乳油(EC),水包油和油包水的乳化液(EW),可噴灑的溶液,懸浮濃縮物(SC),以油或水為基質(zhì)的分散劑,可與油相混的溶液膠懸液(CS),粉劑(DP),浸漬劑,撒播和土壤中施用的顆粒劑,微型顆粒劑,噴灑顆粒劑,沉降顆粒劑和吸附顆粒劑(GR),在水中可分散的顆粒劑(WG),水溶性顆粒劑(SG),超低量劑型,微膠囊劑和蠟劑。
上述劑型基本上是已知的,在有些著述中已有介紹,如
Winnacker-Küchler,“ChemischeTechnologie”,
Band7,C.HauserVerlagMünchen,4.Aufl.1986,WadevanValkenburg,“PesticideFormulations”,MarcelDekker,N.Y.,1973;K.Martens,“SprayDrying”Handbook,3rdEd.1979,G.GoodwinLtd.London.
一些必要的助劑物質(zhì)如惰性物質(zhì)、表面活性劑、溶劑以及其它一些添加劑也都是已知的。在下述文獻(xiàn)中有介紹,如
Watkins,“HandbookofInsecticideDustDiluent
andCarriers”,2ndEd.,DarlandBooks,CaldwellN.J.,H.v.Olphen,“IntroductiontoClayColloidChemistry”;2ndEd.,J.Wiley&Sons,N.Y.;C.Marsden,
“SolventsGuide”;2ndEd.,Interscience,N.Y.1963;McCutcheon's“DetergentsandEmulsifiersAnnual”,MCPubl.Corp.,RidgewoodN.J.;SisleyandWood,“EncyclopediaofSurfaceActiveAgents”,Chem.Publ.Co.Inc.,N.Y.1964;
Schoenfeldt,“GrenzflaechenaktiveAethylenoxidaddukte”,Wiss.Verlagsgesell.,Stuttgart1976;Winnacker-Küchler,“ChemischeTechnologie”,Band7,C.HauserVerlagMünchen,4.Aufl.1986.]
在這些劑型的基礎(chǔ)上,它們可與其它的農(nóng)藥有效成分如殺蟲劑、殺螨劑、除草劑、殺菌劑、安全劑、肥料和/或植物生長調(diào)節(jié)劑混配。例如它可以加工成一種成品制劑形式或罐裝混合物的形式。
在水中可均勻分散的可濕性粉劑除了含有有效成分、一種稀釋劑或惰性物質(zhì)外,還含有離子型和/或非離子型的面活性劑(潤濕劑,分散劑),例如聚氧乙基化的烷基酚類、聚氧乙基化的脂肪醇類、聚氧乙基化的脂肪胺類、脂肪醇聚乙二醇醚硫酸酯、烷基磺酸酯或烷基苯磺酸酯類、木質(zhì)素磺酸鈉、2,2-二萘基甲烷-6,6-二磺酸鈉、二丁基萘磺酸鈉或油酰甲基?;撬徕c。可濕性粉劑的制備是將例如除草有效成分在常規(guī)的設(shè)備如錘式磨,鼓風(fēng)磨,氣流粉碎磨中磨細(xì),同時或繼之與劑型助劑物質(zhì)混合。
乳油是將有效成分溶解在一有機(jī)溶劑如丁醇、環(huán)己酮、二甲基甲酰胺、二甲苯或高沸點(diǎn)的芳香族或烴類或有機(jī)溶劑的混合物中,并添加一種或多種離子型和/或非離子型表面活性劑(乳化劑)制備而成。可作為乳化劑使用的例如烷基磺酸鈣鹽如十二烷基苯磺酸鈣或非離子型乳化劑如脂肪酸聚乙二醇酯、烷基芳基聚乙二醇醚、脂肪醇聚乙二醇醚、環(huán)氧丙烷-環(huán)氧乙烷縮合產(chǎn)物、烷基聚醚、脫水山梨醇酯如脫水山梨醇脂肪酸酯或聚氧乙撐脫水山梨醇酯如聚氧乙撐脫水山梨醇脂肪酸酯。
粉劑是將有效成分與細(xì)顆粒的呈分散狀的固體物質(zhì)如滑石、天然粘土如高嶺土、皂土、葉蠟石或硅藻土經(jīng)磨粉加工而成。
懸浮濃縮物可以以水或油為基質(zhì)。它可以用例如商業(yè)上常用的球磨機(jī)通過濕磨,需要時添加入表面活性劑(如上面別的劑型加工中所提到的)制備而成。
乳油例如水包油的乳油(EW)是借助于攪拌器、膠體磨和/或靜止混合器、在加入液體有機(jī)溶劑、有時還加入上面的劑型加工中所提到的表面活性劑一起加工而成。
顆粒劑的制備是將有效成分噴灑在具有吸附性能的顆粒狀惰性物質(zhì)表面或是將有效成分用聚乙烯醇、聚丙烯酸鈉這些粘合劑或礦物油粘附到砂子、高嶺土等載體表面或顆粒狀惰性物質(zhì)的表面。也可以用通常制造顆粒肥料的方法將某些合適的有效成分加工成顆粒劑。需要時也可與肥料混在一起加工。
水中可分散的顆粒劑通常按常規(guī)方法如噴灑干燥,流化床造粒,塔式造粒,用高速混合機(jī)混合和擠壓而無需固體惰性載體的方法制備。
農(nóng)業(yè)化學(xué)制劑通常含有0.1至99%(重量)、特別是0.1至95%(重量)的式(Ⅰ)有效成分或其鹽。
可濕性粉劑含有效成分的濃度例如大約為10至90(重量),其余部分由常用的一些劑型助劑物質(zhì)組成。乳油中有效成分濃度大約為1至90%優(yōu)選5至80%(重量)。粉劑含有效成分1至30%,優(yōu)選至少為5-20%(重量)。可噴灑的溶液含有效成分大約為0.05至80%、優(yōu)選2至50%(重量)。水中可分散的顆粒劑其有效成分含量部分取決于有效成分化合物是呈液體或固體以及使用什么樣的顆粒助劑物質(zhì)、填料等。水中可分散顆粒中有效成分含量在1至95%(重量)之間,優(yōu)選在10至80%(重量)之間。
此外,所列舉的有效成分的劑型中需要時還可含有常用的粘結(jié)劑、潤濕劑、分散劑、乳化劑、滲透劑、防腐劑、抗凍劑和溶劑、填料、載體和顏料物質(zhì)、消泡劑、蒸發(fā)抑制劑和調(diào)節(jié)pH值及粘度的物質(zhì)。
在混劑或罐裝混合物中可與本發(fā)明有效成分配對的是一些已知的有效成分,例如,它們是記載在如Weedresearch26,441-445(1986),或“ThepesticideManual”,9thedition,TheBritishcropprotectioncouncil,1990/91,Bracknell,England,和其中所列舉的文獻(xiàn)中。在文獻(xiàn)中公布的可與式(Ⅰ)化合物混用的有效成分列舉如下(注解化合物是用國際標(biāo)準(zhǔn)化組織(ISO)規(guī)定的“通用名”或用其化學(xué)名稱,必要時給出其常用代號)。
乙基乙草胺;三氟羧草醚;aclonifen;AKH7088,即〔〔〔1-〔5-〔2-氯-4-(三氟甲基)-苯氧基〕-2-硝基苯〕-2-甲氧基乙叉〕-氧基〕-乙酸和-乙酸甲酯;雜草鎖;alloxydim;莠去凈;amidosulfuron;氨三唑;氨基磺酸銨;anilofos;磺草靈;莠去津;丙氮草凈;氯炔草靈;BAS516H,即5-氟-2-苯基-4H-3,1-苯并噁嗪-4-酮;除草靈;乙丁氟樂靈;benfuresate;芐嘧磺隆;砜草磷;苯達(dá)松;benzofenap;benzofluor;新燕靈;benzthiazuron;bialaphos;甲酯除草醚;丁溴定;bromobutide;溴酚肟;溴草腈;bromuron;buminafos;busoxinone;丁草鎖;butamifos;butenachlor;丁硫咪唑酮;丁樂靈;異丁草丹;草威安;烯草安;硫烯草丹;CGA184927即2-〔4-(5-氯-3-氟-2-吡啶基)-氧基〕-苯氧基〕-丙酸和其2-丙酯;;chlomethoxyfen;豆科畏;chlorazifop-butyl;pirifenop-butyl;氯溴隆;炔草靈;伐草克;氯甲丹;殺草敏;chlorimimuronethyl;草枯醚;綠麥隆;氯醚隆;氯苯胺靈;綠磺隆;敵草索;氯草硫安;噁庚草烷;cinosulfuron;clethodim;廣滅靈,clomeprop;cloproxydim;clopyralid;丙腈津;環(huán)己丹;cycloxydim;環(huán)辛隆;苯草快;環(huán)丙津;環(huán)茂安;2,4-滴丁酸;茅草枯;甜草靈;敵草凈;二氯烯丹;麥草畏;敵草腈;dichlorprop;2,4-滴苯丙酸甲酯;diethatyl;甲氧醚隆;離子草吡唑;diflufenican;dimefuron;菌核凈;戊草凈;dimethazone;dimethipin;dimetrasulfuron;cinosulfuron;敵樂胺;地樂酚;特樂酚;草乃敵;殺草凈;敵草快;dithiopyr;敵草隆;二硝甲酚;eglinazine-ethyl;EL-177,即5-氰基-1-(1,1-二甲基乙基)-N-甲基-3H-吡唑-4-羧酰胺;除草靈;丙草丹;esprocarb;烯氟樂靈;ethametsulfuron-methyl;ethidimuron;ethiozin;甜菜呋;F5231,即N-〔2-氯-4-氟-5-〔4-(3-(氟代丙基)-4,5-二氫-5-氧代-1H-四唑-1-基〕-乙烷磺酰胺;F6258,即1-〔5-(N-甲磺酰基)-氨基-2,4-二氯代苯基〕-3-甲基-4-二氟甲基-1,2,4-三唑-5-酮;2,4,5-涕丙酸;fenoxan,S.clomazon;2,4,5-涕丙酸乙酯;去草隆;草氟安;flazasulfuron;吡氟禾草靈和它的酯衍生物;氯氟樂靈;flumesulam;N-〔2,6-二氟苯基〕-5-甲基-(1,2,4)-勻三唑并〔1,5a〕嘧啶-2-磺酰胺;伏草隆;flumipropyn;氟甲消草醚;fluoroglycofen-ethyl;fluridone;flurochloridone;氟草定;flurtamone;氟磺胺草醚;調(diào)節(jié)磷;furyloxyfen;glufosinate;草甘膦;halosaten;吡氟乙草靈和它的酯衍生物;環(huán)嗪酮;HW52,即N-(2,3-二氯代苯基)-4-(乙氧基甲氧基)-苯酰胺;imazamethabenz-methyl;imazapyr;imazaquin;imazethamethapyr;普殺特;imazosulfuron;碘草腈;異丁咪啉酮;異丙樂靈;異丙隆;isouron;isoxaberr,isoxapyrifop;特威隆;克闊樂;環(huán)草啶;利谷隆;2甲4氯;2甲4氯丁酸;2甲4氯丙酸;mefenacet;mefluidid;甲苯嗪;metazachlor;噻唑隆;硫威鈉;定草噁;去草酮;甲基沙草隆;莠谷隆;甲氧毒草安;甲氧隆;賽克嗪;metsutfuron-methyl;抑芽丹;環(huán)草丹;草庚安;moncarbamide;dihydrogensulfate;綠谷隆;滅草隆;MT128,即6-氯-N-(3-氯-2-丙烯基)-5-甲基-N-苯基-3-噠嗪胺;MT5950,即N-〔3-氯-4-(1-甲基乙基)-苯基〕-2-甲基戊酰胺;naproanilide;萘丙安;抑草生;NC310,即4-(2,4-二氯苯甲酰)-1-甲基-5-芐基氧基吡唑;丁敵隆;nicosulfuron;nipyraclophen;磺樂靈;除草醚;nitrofluorfen;norflurazon;orbencarb;磺胺樂靈;松草噁;乙氧氟甲草醚;離子對草快;克草丹;二甲戊樂靈;perfluidone;甲二威靈;phenisopham;毒草定;哌草磷;piributicarb;pirifenop-butyl;丙草胺;primisulfuron-methyl;procyazine;prodiamine;環(huán)丙氟樂靈;proglinazine-ethyl;撲草通;撲草凈;毒草安;敵稗;propaquizafop和它的酯衍生物;撲滅津;苯胺靈;炔敵稗;甲硫基磺樂靈;prosulfocarb;丁炔毒草安;pyrazolinate;殺草敏;pyrazosulfuron-ethyl;pyrazoxyfen;噠草特;快殺稗;quinmerac;quinofop和它的酯衍生物;quizalofop和它的酯衍生物;喹禾靈;quizalofop-p-tefuryl;renriduron;沙草隆;S275,即2-〔4-氯-2-氟-5-(2-丙基氧基)-苯基〕-4,5,6,7-四氫-2H-吲唑;S482,即2-〔7-氟-3,4-二氫-3-氧代-4-(2-丙基)-2H-1,4-苯并噁嗪-6-基〕-4,5,6,7-四氫-1H-異吲哚-1,3-(2H)-二酮;另丁通;sethoxydim;環(huán)己隆;西瑪津;西瑪凈;SN106279,即2-〔7-氯-4-(三氟-甲基)-苯氧基〕-2-萘基〕-氧基〕-丙酸和其甲酯;sulfometuron-methyl;sulfazuron;flazasulfuron;三氯乙酸;tebutam;丁噻隆;特氯啶;芽根靈;特丁通;特丁津;特丁草凈;TFH450,即N,N-二乙基-3-〔(2-乙基-6-甲基苯基)-磺?;?1H-1,2,4-三唑-1-羧酰胺;thiazafluron;thifensulfuron-methyl;禾草丹;tiocarbazil;tralkoxydim;三氯烯丹;triasulfuron;triazofenamide;tribenuron-methyl;乙氯草定;tridiphane;草達(dá)津;氟樂靈;三甲隆;衛(wèi)農(nóng);WL110547,即5-苯氧基-1-〔3-(三氟甲基)-苯基〕-1H-四唑。
以常規(guī)商品形式提供的劑型應(yīng)用時,用常規(guī)方式稀釋,例如可濕性粉劑,乳油,分散液和水中可分散的顆粒劑是用水稀釋。粉劑,土壤和撒播顆粒劑以及可噴灑的溶液在使用前通常不再用惰性物稀釋。
式(Ⅰ)化合物的用量隨外界條件如溫度、濕度、所用除草劑的種類而變化。它可在很大范圍內(nèi)變化,例如在0.001-10.0公斤/公頃之間或用更多的有效成分,優(yōu)選的用量在0.005至5公斤/公頃。
A化學(xué)制備例
a)2-羧基-硝基苯磺酸
在2小時內(nèi),于80℃之下將400.0g(2.53mol)的高錳酸鉀分次加入到含106.0g(0.40Mol)的2-甲基-5-硝基-苯磺酸和80.0g(0.58Mol)碳酸鉀于1300ml水中形成的溶液中。反應(yīng)溫度維持在80℃至95℃之間。然后再攪拌4小時,濾出生成的固體物質(zhì)。濾液用濃HCl酸化(pH=1)。用布氏漏斗抽濾沉淀下來的無色的2-羧基-5-硝基-苯磺酸,并在約50℃/100Torr下干燥,得到82.0g標(biāo)題化合物(理論收率的83.7%)。其熔點(diǎn)>300℃。
b)2-甲氧基羰基-5-硝基-苯磺酸
在3小時內(nèi)將由190.0g(0.77Mol)2-羧基-5-硝基-苯磺酸、10ml二甲基甲酰胺和250ml(3.43Mol)亞硫酰氯組成的懸浮液沸騰加熱。通過過濾分離掉不溶的部分后濃縮濾液。向濃縮后的殘?jiān)械渭?00ml(4.94Mol)的甲醇。加完甲醇后將反應(yīng)混合物冷卻至0℃。濾出沉淀的固體物質(zhì)并干燥。得到70.9g(理論收率的35.3%)無色的結(jié)晶狀2-甲氧基羰基-5-硝基-苯磺酸,其熔點(diǎn)92-94℃。
在蒸發(fā)器中蒸發(fā)出母液中的揮發(fā)部分得到第二部分(62.5g,理論值的31.1%)。
c)2-甲氧基羰基-5-硝基-苯磺酰氯
在強(qiáng)烈攪拌下,向含70.9g(0.27Mol)2-甲氧基羰基-5-硝基-苯磺酸的300ml甲醇中小心地加入由17.3g(0.27Mol)KOH(88%)和100ml甲醇組成的溶液。冷卻到0℃后,濾出生成的鹽,干燥,接著使之懸浮于150ml環(huán)丁砜、150ml乙腈和10ml二甲基甲酰胺中。滴加入100ml(1.07Mol)的磷酰氯后,混合物加熱沸騰2.5小時,接著倒入冰水中。沉淀的2-甲氧基羰基-5-硝基-苯磺酰氯(60.1g,理論值的70%)用布氏漏斗抽濾并減壓蒸去殘余的溶劑,產(chǎn)物的熔點(diǎn)86-88℃。
d)N-叔丁基-2-甲氧基羰基-5-硝基-苯磺酰胺
在0℃下向含34.4g(0.12Mol)2-甲氧基羰基-5-硝基-苯磺酰氯的200ml乙酸乙酯和250ml乙醇中緩慢滴加50ml(0.48Mol)叔丁胺。反應(yīng)液于室溫下攪拌10分鐘。加入500ml水后,有無色固體物質(zhì)結(jié)晶析出。經(jīng)過濾和干燥,得到28.1g(89%)的N-叔丁基-2-甲氧基羰基-5-硝基-苯磺酰胺,其熔點(diǎn)121-124℃。
e)N-叔丁基-5-氨基-2-甲氧基羰基-苯磺酰胺
25.08g(0.079mol)N-叔丁基-2-甲氧基羰基-5-硝基-苯磺酰胺溶在1000ml甲醇中。添加入0.5gPd-c(10%)催化劑后,混合物在氫氣氛下(1atm.)搖動直至氫氣吸收結(jié)束。分離掉催化劑后蒸去劑。殘?jiān)蒙倭恳宜嵋阴噭?。得到N-叔丁基-5-氨基-2-甲氧基羰基-苯磺酰胺(18.3g;理論值的80.9%),它193℃下熔化。
f)N-叔丁基-5-甲?;被?2-甲氧基羰基-苯磺酰胺
在0℃下將6.5ml甲酸小心地加到13ml醋酸酐中。繼之混合物在50-60℃下加熱2小時。在0℃下滴加入由16.0g(0.056mol)N-叔丁基-5-氨基-2-甲氧基羰基-苯磺酰胺和50ml二甲基甲酰胺組成的溶液。從冰水浴中拿出后,在室溫下攪拌4小時。然后反應(yīng)混合物溶在800ml乙酸乙酯中,并用3×150ml水洗滌。有機(jī)相用硫酸鎂干燥并蒸掉溶劑,殘?jiān)谝宜嵋阴?庚烷中重結(jié)晶。得到N-叔丁基-5-甲酰基氨基-2-甲氧基羰基苯磺酰胺(14.23g,理論值的82%),在113-114℃時熔化。
g)N-叔丁基-2-甲氧基羰基-5-甲基氨基-苯磺酰胺
9.92g(0.032mol)N-叔丁基-5-甲?;被?2-甲氧基羰基苯磺酰胺溶于50mlCHCl3中,繼之在0℃下加入5ml(0.053mol)的二甲基硫-硼烷-絡(luò)合物。在0℃下放置1小時和在室溫下3小時后,反應(yīng)混合物被冷卻至0℃。添加30ml甲醇后,用水洗滌混合物。有機(jī)相經(jīng)硫酸鎂干燥并蒸去溶劑后,得到9.23g(理論值的98%)N-叔丁基-2-甲氧基羰基-5-甲基氨基苯磺酰胺。熔點(diǎn)120-124℃。
h)N-叔丁基-5-〔N-(乙氧基羰基氨基-硫代羰基)-甲基氨基〕-2-甲氧基羰基-苯磺酰胺
1.20g(4.0mmol)N-叔丁基-2-甲氧基羰基-5-甲基氨基-苯磺酰胺溶在5ml無水二甲基甲酰胺中,并加入0.6g(4.3mmol)95%的乙氧基羰基芥子油。在室溫下放置3小時后混合物溶于乙酸乙酯中,并用1N鹽酸和水洗滌。有機(jī)相用硫酸鎂干燥后蒸去溶劑。殘?jiān)蒙倭恳宜嵋阴ト芙猓?25℃下用庚烷使其沉淀。抽濾并干燥后得到1.29g(理論值的75%)無色的N-叔丁基-5-〔N-(乙氧基羰基氨基-硫代羰基)-甲胺基-2-甲氧基羰基-苯磺酰胺。熔點(diǎn)110℃。
i)5-〔N-(乙氧基羰基氨基-硫代羰基)-甲氨基〕-2-甲氧基-羰基苯磺酰胺
1.05g(2.4mmol)N-叔丁基-5-〔N-(乙氧基羰基氨基硫代羰基)-N-甲基-氨基〕-2-甲氧基羰基-苯磺酰胺于室溫下在15ml三氟乙酸中攪拌18小時。繼之在12Torr/50℃下蒸去揮發(fā)組分。殘?jiān)眉妆綉腋?。?2Torr/50℃重新濃縮懸浮液后,得到一高粘度的殘?jiān)?0.85g,理論值的93%),它無須再純化,便可直接反應(yīng)生成相應(yīng)的磺酰脲化合物(參見例j)。
j)N-〔(4,6-二甲氧基嘧啶-2-基)-氨基羰基〕-5-〔N-(乙氧基羰基氨基-硫代羰基)-甲基氨基〕-2-甲氧基羰基-苯磺酰胺(見表例2192)
向含0.69g(1.84mmol)5-〔N-(乙氧基羰基氨基硫代羰基)-甲基氨基〕-2-甲氧基羰基-苯磺酰胺和0.55g(1.99mmol)4,6-二甲氧基-2-苯氧羰基氨基-嘧啶在5ml乙腈中的懸浮液中加入1.2mlDBU。在室溫下攪拌17小時后蒸去溶劑。殘?jiān)盟芙獠⒂靡颐严礈?。水相用濃鹽酸酸化(pH=1),出現(xiàn)無色固體沉淀。濾出沉淀,用少量甲醇攪拌。得到0.61g(理論值的60%)N-〔(4-二甲氧基-嘧啶-2-基)-氨基羰基〕-5-〔N-(乙氧基羰基氨基-硫代羰基)-甲基氨基〕-2-甲氧基羰基-苯磺酰胺。熔點(diǎn)144-145℃。
k)5-(N-乙酰基-甲基氨基)-N-〔4,6-二甲氧基-嘧啶-2-基)-氨基羰基〕-2-甲氧基羰基苯磺酰胺(見表1,例89)
向含0.75g(2.6mmol)5-(N-乙?;?甲基氨基)-2-甲氧基羰基苯磺酰胺和0.73g(2.6mmol)4,6-二甲氧基-2-(苯氧基羰基氨基)-嘧啶的10ml CH3CN中加入0.45ml DBU。按類似于例j)的步驟處理,得到0.59g所要的磺酰脲類化合物,熔點(diǎn)197℃。
l)2-甲氧基羰基-5-(N-甲氧基羰基-N-甲基氨基)-苯磺?;惽杷狨?br> 將5.0g2-甲氧基羰基-5-(N-甲氧基羰基-N-甲基氨基)-苯磺酰胺懸浮于17ml1,2-二氯乙烷中。添加4ml亞硫酰氯后,反應(yīng)混合物加熱沸騰5小時,冷卻至室溫后,加入0.3ml吡啶,向反應(yīng)混合物中導(dǎo)入光氣,溶液加熱回流4小時。反應(yīng)混合物經(jīng)濃縮后得到6.3g油狀物,它可直接用于后面的反應(yīng)(例m,n,o)。
m)2-甲氧基羰基-5-(N-甲氧基羰基-N-甲基氨基)-N〔(4,6-二甲基嘧啶-2-基)-氨基羰基〕-苯磺酰胺(見表1,例1,183)
向含0.8g2-氨基-4,6-二甲基嘧啶的20ml二氯乙烷中加入由2.1g2-甲氧基羰基-5-(N-甲氧基羰基甲基氨基)-苯磺酰基異氰酸酯(例1)和20ml二氯乙烷組成的溶液。在40℃下攪拌8小時后濃縮反應(yīng)混合物。殘?jiān)?N鹽酸和甲醇逐漸地強(qiáng)烈地?cái)嚢琛5玫?.47g所要的固體泡沫狀的磺酰脲類化合物
1H-NMR(DMSO,80MHz)δ(ppm)=2,5(s,6H,2CH3),3,3(s,3H,N-CH3),3,7(s,3H,O-CH3),3,9(s,3H,OCH3),7,0(s,1H,HPyrimidin),7,8(s,2H,3-H,und 4-H),8,1(s,1H,6-H),10,6(s,1H,NH),13,3(s,1H,SO2-NH).
n)N-〔(4-氯-6-甲氧基嘧啶-2-基)-氨基羰基〕-2-甲氧基羰基-5-(N-甲氧基羰基-N-甲基氨基)-苯磺酰胺(見表1,例1.185)
類似于例m),使0.9g2-氨基-4-氯-6-甲氧基嘧啶與2.1g2-甲氧基羰基-5-(N-甲氧基羰基-N-甲基氨基)-苯磺?;惽杷狨?例1))反應(yīng)。得到0.45g所要的固體泡沫狀磺酰脲類化合物;
1H-NMR(DMSO,80MHz)δ(ppm)=3,3(s,3H,N-CH3),3,7(s,3H,O-CH3),3,8(s,3H,O-CH3),4,0(s,3H,O-CH3),6,8(s,1H,HPyrimidin),7,7(s,2H,3-H,und 4-H),10,9(s,1H,NH),12,0(s,1H,SO2-NH).
o)N-〔N-(4-甲氧基-6-甲基三唑-2-基)氨基羰基〕-2-甲氧基羰基-5-(N-甲氧基羰基-N-甲基-氨基)-苯磺酰胺(見表1,例1.180)
類似于例m),使0.8g2-氨基-4-甲氧基-6-甲基三唑與2.1g2-甲氧基羰基-5-(N-甲氧基羰基-N-甲基氨基)-苯磺酰基異氰酸酯(例1))反應(yīng)。得到0.47g固體泡沫狀的所要的磺酰脲類化合物;
1H-NMR(DMSO,80MHz)δ(ppm)=2,4(s,3H,CH3),3,3(s,3H,N-CH3),3,7(s,3H,OCH3),3,8(s,3H,OCH3),4,0(s,3H,O-CH3),7,8(s,2H,3-H,4-H),8,1(s,1H,6-H),11,0(s,1H,NH),12,3(s,14,SO2NH).
用與例a)至o)相類似的方法可得到在表1中所述的其它化合物。
表1中所用的縮寫如下
No.=實(shí)施例號
Ep.=熔點(diǎn)(以℃表示)
Me=甲基
Et=乙基
Pr=丙基
n-Pr=正丙基
i-Pr=異丙基
c-Pr=環(huán)丙基
Bu=丁基
Ph=苯基
表1
No. R1R2R3R4X Y Z Fp.
1 Me CO-CH2-OMe CO2Me H OMe OMe CH
2Et″″″″″″
3 Me COCH2NHCO2″ ″ ″ ″ ″
Me
4 Me COCH2SMe ″ ″ ″ ″ ″
5″″″Me″″″
6″″″HOMeMeN
7″″″″MeMeCH
8Et″″″″″″
9″″″″OMe″N
10″″″″OMeOMeN
11MeCHO″″OMeOMeCH177-182
12″″″″OMeOMeN
13″″″″OMeMeN
14″″″″OMeMeCH
15 ″ ″ ″ ″ NMe2OCH2CF3N
16″″″″MeMeCH
17″″″″MeMeN
18″″″″ClOMeCH
19″″″MeOMeOMeCH
20″″″MeOMeMeN
21 ″ ″ CO2Et H OMe OMe CH
22″″″″OMeClCH
23″″″″MeMeCH
24″″″″OMeMeN
25 ″ ″ ″ ″ NMe2OCH2CF3N
26″″″MeOMeOMeCH
27″″″MeOMeMeN
No. R1R2R3R4X Y Z Fp.
28 ″ ″ CO2-n-Pr H OMe OMe CH
29″″″″OMeOMeN
30″″″″OMeMeN
31″″″″MeMeCH
32″″″″OMeClCH
33″″″MeMeOMeN
34″″″MeOMeOMeCH
35 Me CHO CO2-i-Pr H OMe OMe CH
36″″″″OMeOMeN
37″″″″OMeMeN
38″″″″OMeClCH
39″″″″MeMeCH
40 ″ ″ ″ ″ SMe NEt2N
41 ″ ″ CO2-i-Pr Me OMe Me N
42″″″MeOMeOMeCH
43 Me CHO CO2-烯丙基 H OMe OMe CH
44 Et CHO CO2Me H OMe OMe CH
45″″″″OMeMeN
46″″″″MeMeCH
47″″″″ClOMeCH
48″″″MeOMeOMeCH
49″″″MeOMeMeN
50 ″ ″ CO2Et H OMe OMe CH
51″″″″OMeMeCH
52″″″″ClOMeCH
53″″″″OMeMeN
54″″″MeOMeOMeCH
55″″″MeOMeMeN
56 ″ ″ CO2-n-Pr H OMe OMe CH
57″″″″OMeMeN
58″″″″OMeClCH
59″″″″MeMeCH
60″″″MeOMeOMeCH
61″″″MeOMeMeN
62 ″ ″ CO2-i-Pr H OMe OMe CH
63″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
64″″″″MeMeCH
65″″″MeOMeMeN
66 n-Pr CHO CO2Me H OMe OMe CH
67″″″″OMeClCH
68″″″″MeMeCH
69″″″″OMeMeN
70″″″MeOMeOMeCH
71″″″MeOMeMeN
72 n-Pr ″ CO2Et H OMe Me N
73″″″″OMeOMeCH
74″″″″MeMeCH
75 ″ ″ CO2n-Pr ″ OMe OMe CH
76 i-Pr ″ CO2Me H OMe OMe CH
77″″″″OMeMeN
78″″″″MeMeCH
79″″″″ClOMeN
80″″″MeOMeMeN
81″″″MeOMeOMeCH
82 烯丙基 ″ CO2Me H OMe OMe CH
83″″″″OMeClCH
84″″″″MeMeCH
85″″″″OMeMeN
86 ″ ″ CO2Et ″ OMe OMe CH
87 ″ ″ CO2n-Pr ″ OMe OMe CH
88 ″ ″ CO2i-Pr ″ OMe OMe CH
89 Me CO-CH3CO2Me ″ OMe OMe CH 197℃
90″″″″OMeOMeN
91″″″″OMeMeN
92″″″″OMeMeCH
93 ″ ″ ″ ″ NMe2OCH2CF3N
94″″″″MeMeCH
95″″″″MeMeN
96″″″″ClOMeCH
97″″″MeOMeOMeCH
98″″″MeOMeMeN
99 ″ ″ CO2Et H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
100″″″″OMeClCH
101″″″″MeMeCH
102″″″″OMeMeN
103 ″ ″ ″ ″ NMe2OCH2CF3N
104″″″MeOMeOMeCH
105″″″MeOMeMeN
106 ″ ″ CO2-n-Pr H OMe OMe CH
107″″″″OMeOMeN
108″″″″OMeMeN
109″″″″MeMeCH
110″″″″OMeClCH
111″″″MeMeOMeN
112″″″MeOMeOMeCH
113 Me COCH3CO2-i-Pr H OMe OMe CH
114″″″″OMeOMeN
115″″″″OMeMeN
116″″″″OMeClCH
117″″″″MeMeCH
118 ″ ″ ″ ″ SMe NEt2N
119 ″ ″ CO2-i-Pr Me OMe Me N
120″″″MeOMeOMeCH
121 Me COCH3CO2-烯丙基 H OMe OMe CH
122 Et ″ CO2Me H OMe OMe CH
123″″″″OMeMeN
124″″″″MeMeCH
125″″″″ClOMeCH
126″″″MeOMeOMeCH
127″″″MeOMeMeN
128 ″ ″ CO2Et H OMe OMe CH
129″″″″OMeMeCH
130″″″″ClOMeCH
131″″″″OMeMeN
132″″″MeOMeOMeCH
133″″″MeOMeMeN
134 ″ ″ CO2-n-Pr H OMe OMe CH
135″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
136″″″″OMeClCH
137″″″″MeMeCH
138″″″MeOMeOMeCH
139″″″MeOMeMeN
140 ″ ″ CO2-i-Pr H OMe OMe CH
141″″″″OMeMeN
142″″″″MeMeCH
143″″″MeOMeMeN
144 n-Pr CO-CH3CO2Me H OMe OMe CH 160℃
145″″″″OMeClCH
146″″″″MeMeCH
147″″″″OMeMeN
148″″″MeOMeOMeCH
149″″″MeOMeMeN
150 n-Pr ″ CO2Et H OMe Me N
151″″″″OMeOMeCH
152″″″″MeMeCH
153 ″ ″ CO2-n-Pr ″ OMe OMe CH
154 i-Pr ″ CO2Me H OMe OMe CH
155″″″″OMeMeN
156″″″″MeMeCH
157″″″″ClOMeN
158″″″MeOMeMeN
159″″″MeOMeOMeCH
160 烯丙基 ″ CO2Me H OMe OMe CH
161″″″″OMeClCH
162″″″″MeMeCH
163″″″″OMeMeN
164 ″ ″ CO2Et H OMe OMe CH
165 ″ ″ CO2-n-Pr ″ OMe OMe CH
166 ″ ″ CO2-i-Pr ″ OMe OMe CH
167 Me COCH2CH3CO2Me H OMe OMe CH
168″″″″OMeOMeN
169″″″″SMeMeN
170″″″″OMeMeN
171″″″″OMeMeCH
No. R1R2R3R4X Y Z Fp.
172 ″ ″ ″ ″ NMe2OCH2CF3N
173″″″″MeMeCH
174″″″″MeMeN
175″″″″ClOMeCH
176″″″MeOMeOMeCH
177 ″ ″ CO2Me Me OMe Me N
178 ″ ″ CO2Et H OMe OMe CH
179″″″″OMeClCH
180″″″″MeMeCH
181″″″″OMeMeN
182 ″ ″ ″ ″ NMe2OCH2CF3N
183″″″MeOMeOMeCH
184″″″MeOMeMeN
185 ″ ″ CO2-n-Pr H OMe OMe CH
186″″″″OMeOMeN
187″″″″OMeMeN
188″″″″MeMeCH
189″″″″OMeClCH
190″″″MeMeOMeN
191″″″″OMeOMeCH
192 Me COCH2CH3CO2-i-Pr H OMe OMe CH
193″″″″OMeOMeN
194″″″″OMeMeN
195″″″″OMeClCH
196″″″″MeMeCH
197 ″ ″ ″ ″ SMe NEt2N
198″″″MeOMeMeN
199″″″″OMeOMeCH
200 Me COCH2CH3CO2-烯丙基 H OMe OMe CH
201 Et ″ CO2-Me H OMe OMe CH
202″″″″OMeMeN
203″″″″MeMeCH
204″″″″ClOMeCH
205″″″MeOMeOMeCH
206″″″″OMeMeN
207 ″ ″ CO2-Et H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
208″″″″OMeMeCH
209″″″″ClOMeCH
210″″″″OMeMeN
211″″″MeOMeOMeCH
212″″″″″MeN
213 ″ ″ CO2-n-Pr H OMe OMe CH
214″″″″OMeMeN
215″″″″OMeClCH
216″″″″MeMeCH
217″″″MeOMeOMeCH
218″″″″OMeMeN
219 ″ ″ CO2-i-Pr H OMe OMe CH
220″″″″OMeMeN
221″″″″MeMeCH
222″″″MeOMeMeN
223 n-Pr COCH2CH3CO2Me H OMe OMe CH
224″″″″OMeClCH
225″″″″MeMeCH
226″″″″OMeMeN
227″″″MeOMeOMeCH
228″″″MeOMeMeN
229 n-Pr ″ CO2Et H OMe Me N
230″″″″OMeOMeCH
231″″″″MeMeCH
232 ″ ″ CO2-n-Pr ″ OMe OMe CH
233 i-Pr ″ CO2Me H OMe OMe CH
234″″″″OMeMeN
235″″″″MeMeCH
236″″″″ClOMeN
237″″″MeOMeMeN
238″″″MeOMeOMeCH
239 烯丙基 ″ CO2Me H OMe OMe CH
240″″″″OMeClCH
241″″″″MeMeCH
242″″″″OMeMeN
243 ″ ″ CO2Et H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
244 ″ ″ CO2-n-Pr ″ OMe OMe CH
245 ″ ″ CO2-i-Pr ″ OMe OMe CH
246 Me CO-n-Pr CO2Me H OMe OMe CH
247″″″″OMeOMeN
248″″″″OMeMeN
249″″″″OMeMeCH
250 ″ ″ ″ ″ NMe2OCH2CF3N
251″″″″MeMeCH
252″″″″MeMeN
253″″″″ClOMeCH
254″″″MeOMeOMeCH
255″″″MeOMeMeN
256 ″ ″ CO2Et H OMe OMe CH
257″″″″OMeClCH
258″″″″MeMeCH
259″″″″OMeMeN
260 ″ ″ ″ ″ NMe2OCH2CF3N
261″″″MeOMeOMeCH
262″″″MeOMeMeN
263 ″ ″ CO2-n-Pr H OMe OMe N
264″″″″OMeOMeCH
265 Me CO-n-Pr CO2-n-Pr H OMe OMe CH
266″″″″OMeOMeN
267″″″″OMeClCH
268″″″MeMeOMeN
269″″″MeOMeOMeCH
270 Me CO-n-Pr CO2-i-Pr H OMe OMe CH
271″″″″OMeOMeN
272″″″″OMeMeN
273″″″″OMeClCH
274″″″″MeMeCH
275 ″ ″ ″ ″ SMe NEt2N
276 ″ ″ CO2-i-Pr Me OMe Me N
277″″″MeOMeOMeCH
278 Me ″ CO2-烯丙基 H OMe OMe CH
279 Et ″ CO2Me H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
280″″″″OMeMeN
281″″″″MeMeCH
282″″″″ClOMeCH
283″″″MeOMeOMeCH
284″″″MeOMeMeN
285 ″ ″ CO2Et H OMe OMe CH
286″″″″OMeMeCH
287″″″″ClOMeCH
288″″″″OMeMeN
289″″″MeOMeOMeCH
290″″″MeOMeMeN
291 ″ ″ CO2-n-Pr H OMe OMe CH
292″″″″OMeMeN
293″″″″OMeClCH
294″″″″MeMeCH
295″″″MeOMeOMeCH
296″″″MeOMeMeN
297 ″ ″ CO2-i-Pr H OMe OMe CH
298″″″″OMeMeN
299 n-Pr CO-n-Pr CO2-Me H OMe OMe CH
300″″″″OMeClCH
301″″″″MeMeCH
302″″″″OMeMeN
303″″″MeOMeOMeCH
304″″″MeOMeMeN
305 n-Pr ″ CO2Et H OMe Me N
306″″″″OMeOMeCH
307″″″″MeMeCH
308 ″ ″ CO2-n-Pr ″ OMe OMe CH
309 i-Pr ″ CO2Me H OMe OMe CH
310″″″″OMeMeN
311″″″″MeMeCH
312″″″″ClOMeN
313″″″MeOMeMeN
314″″″MeOMeOMeCH
315 烯丙基 ″ CO2-Me H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
316″″″″OMeClCH
317″″″″MeMeCH
318″″″″OMeMeN
319 ″ ″ CO2Et H OMe OMe CH
320 ″ ″ CO2-n-Pr ″ OMe OMe CH
321 ″ ″ CO2-i-Pr ″ OMe OMe CH
322 Me CO-i-Pr CO2-Me H OMe OMe CH
323″″″″OMeOMeN
324″″″″″MeN
325″″″″″″CH
326 ″ ″ ″ ″ NMe2OCH2CF3N
327″″″″MeMeCH
328″″″″MeMeN
329″″″″ClOMeCH
330″″″MeOMeOMeCH
331″″″″″MeN
332 ″ ″ CO2-Et H OMe OMe CH
333″″″″″ClCH
334″″″″MeMeCH
335″″″″OMeMeN
336 ″ ″ ″ ″ NMe2OCH2CF3N
337″″″MeOMeOMeCH
338″″″″OMeMeN
339 ″ ″ CO2-n-Pr H OMe OMe CH
340″″″″″″N
341″″″″OMeMeN
342″″″″MeMeCH
343″″″″OMeClCH
344″″″MeMeOMeN
345″″″″OMeOMeCH
346 Me CO-i-Pr CO2-i-Pr H OMe OMe CH
347″″″″″″N
348″″″″OMeMeN
349″″″″OMeClCH
350″″″″MeMeCH
351 ″ ″ ″ ″ SMe NEt2N
45
No. R1R2R3R4X Y Z Fp.
352 ″ ″ CO2-i-Pr Me OMe Me N
353″″″″OMeOMeCH
354 Me COCHMe2CH2CHCH2H OMe OMe CH
355 Et ″ CO2-Me H OMe OMe CH
356″″″HOMeMeN
357″″″″MeMeCH
358″″″″ClOMeCH
359″″″MeOMeOMeCH
360″″″″OMeMeN
361 ″ ″ CO2-Et H OMe OMe CH
362″″″″OMeMeCH
363″″″″ClOMeCH
364″″″″OMeMeN
365″″″MeOMeOMeCH
366″″″″″MeN
367 ″ ″ CO2-n-Pr H OMe OMe CH
368″″″″OMeMeN
369″″″″OMeClCH
370″″″″MeMeCH
371″″″MeOMeOMeCH
372″″″″OMeMeN
373 ″ ″ CO2-i-Pr H OMe OMe CH
374″″″″OMeMeN
375″″″″MeMeCH
376″″″MeOMeMeN
377 n-Pr CO-i-Pr CO2-Me H OMe OMe CH
378″″″″″ClCH
379″″″″MeMeCH
380″″″″OMeMeN
381″″″MeOMeOMeCH
382″″″″OMeMeN
383 n-Pr ″ CO2-Et H ″ Me N
384″″″″″OMeCH
385″″″″MeMeCH
386 ″ ″ CO2-n-Pr ″ OMe OMe CH
387 i-Pr ″ CO2-Me H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
388″″″″OMeMeN
389″″″″MeMeCH
390″″″″ClOMeN
391″″″MeOMeMeN
392″″″″″OMeCH
393 烯丙基 ″ CO2-Me H OMe OMe CH
394″″″″″ClCH
395″″″″MeMeCH
396″″″″OMeMeN
397 ″ ″ CO2-Et H OMe OMe CH
398 ″ ″ CO2-n-Pr ″ OMe OMe CH
399 ″ ″ CO2-i-Pr ″ ″ ″ ″
400 Me CO-t-Bu CO2-Me H OMe OMe CH
401″″″″″OMeN
402″″″″″MeN
403″″″″″″CH
404 ″ ″ ″ ″ NMe2OCH2CF3N
405″″″″MeMeCH
406″″″″″″N
407″″″″ClOMeCH
408″″″MeOMeOMeCH
409″″″″″MeN
410 ″ ″ CO2-Et H OMe OMe CH
411″″″″″ClCH
412″″″″MeMeCH
413″″″″OMeMeN
414 ″ ″ ″ ″ NMe2OCH2CF3N
415″″″MeOMeOMeCH
416″″″″OMeMeN
417 ″ ″ CO2-n-Pr H OMe OMe CH
418″″″″″″N
419″″″″OMeMeN
420″″″″MeMeCH
421″″″″OMeClCH
422″″″MeMeOMeN
423″″″″OMeOMeCH
No. R1R2R3R4X Y Z Fp.
424 Me CO-t-Bu CO2-i-Pr H OMe OMe CH
425″″″″″″N
426″″″″HMeN
427″″″″OMeClCH
428″″″″MeMeCH
429 ″ ″ ″ ″ SMe NEt2N
430 ″ ″ CO2-i-Pr Me OMe Me N
431″″″EtOMeOMeCH
432 Me ″ CO2-烯丙基 H OMe OMe CH
433 Et ″ CO2-Me H OMe OMe CH
434″″″HOMeMeN
435″″″″MeMeCH
436″″″″ClOMeCH
437″″″MeOMeOMeCH
438″″″″OMeMeN
439 ″ ″ CO2-Et H OMe OMe CH
440″″″″OMeMeCH
441″″″″ClOMeCH
442″″″″OMeMeN
443″″″MeOMeOMeCH
444″″″″″MeN
445 ″ ″ CO2-n-Pr H OMe OMe CH
446″″″″OMeMeN
447″″″″OMeClCH
448″″″″MeMeCH
449″″″MeOMeOMeCH
450″″″″OMeMeN
451 ″ ″ CO2-iPr H OMe OMe CH
452″″″″OMeMeN
453″″″″MeMeCH
454″″″MeOMeMeN
455 n-Pr CO-t-Bu CO2-Me H OMe OMe CH
456″″″″OMeClCH
457″″″″MeMeCH
458″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
459″″″MeOMeOMeCH
460 n-Pr ″ CO2-Et Me OMe Me N
461 n-Pr ″ CO2-Et H OMe Me N
462″″″″OMeOMeCH
463″″″″MeMeCH
464 i-Pr ″ CO2-Me ″ OMe OMe CH
465i-Pr″″MeOMeOMeCH
466″″″HOMeMeN
467″″″″MeMeCH
468″″″″ClOMeN
469″″″MeOMeMeN
470烯丙基″″HOMeOMeCH
471″″″HOMeClCH
472″″″″OMeMeN
473″″″″MeMeCH
474 ″ ″ CO2-Et H OMe OMe CH
475 ″ ″ CO2-n-Pr H OMe OMe CH
476 ″ ″ CO2-i-Pr H OMe OMe CH
477 Me CO-環(huán)丙基 CO2-Me H OMe OMe CH 161℃
478″″″″″OMeN
479″″″″″MeN
480″″″″″″CH
481 ″ ″ ″ ″ NMe2OCH2CF3N
482″″″″MeMeCH
483″″″″″″N
484″″″″ClOMeCH
485″″″MeOMeOMeCH
486″″″″″MeN
487 ″ ″ CO2-Et H OMe OMe CH
488″″″″″ClCH
489″″″″MeMeCH
490″″″″OMeMeN
491 ″ ″ ″ ″ NMe2OCH2CF3N
492″″″MeOMeOMeCH
493″″″″OMeMeN
494 ″ ″ CO2-n-Pr H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
495″″″″″″N
496″″″″OMeMeN
497″″″″MeMeCH
498″″″″OMeClCH
499″″″MeMeOMeN
500″″″″OMeOMeCH
501 Me CO-環(huán)丙基 CO2-i-Pr H OMe OMe CH
502″″″″″″N
503″″″″OMeMeN
504″″″″OMeClCH
505″″″″MeMeCH
506 ″ ″ ″ ″ SMe NEt2N
507 ″ ″ CO2-i-Pr Me OMe Me N
508″″″″OMeOMeCH
509 Me ″ CO2-烯丙基 H OMe OMe CH
510 Et ″ CO2-Me H OMe OMe CH
511″″″HOMeMeN
512″″″″MeMeCH
513″″″″ClOMeCH
514″″″MeOMeOMeCH
515″″″″OMeMeN
516 ″ ″ CO2-Et H OMe OMe CH
517″″″″MeMeCH
518″″″″ClOMeCH
519″″″″OMeMeN
520″″″MeOMeOMeCH
521″″″″″MeN
522 ″ ″ CO2-n-Pr H OMe OMe CH
523″″″″OMeMeN
524″″″″OMeClCH
525″″″″MeMeCH
526″″″MeOMeOMeCH
527″″″″OMeMeN
528 ″ ″ CO2-i-Pr H OMe OMe CH
529″″″″OMeMeN
530″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
531″″″MeOMeMeN
532 n-Pr CO-環(huán)丙基 CO2-Me H OMe OMe CH
533″″″″″ClCH
534″″″″MeMeCH
535″″″″OMeMeN
536″″″MeOMeOMeCH
537″″″″OMeMeN
538 n-Pr ″ CO2-Et H ″ ″ N
539″″″″″OMeCH
540″″″″MeMeCH
541 ″ ″ CO2-n-Pr ″ OMe OMe CH
542 i-Pr ″ CO2-Me H OMe OMe CH
543″″″″OMeMeN
544″″″″MeMeCH
545″″″″ClOMeN
546″″″MeOMeMeN
547″″″″″OMeCH
548 烯丙基 ″ CO2-Me H OMe OMe CH
549″″″″″ClCH
550″″″″MeMeCH
551″″″″OMeMeN
552 ″ ″ CO2-Et H OMe OMe CH
553 ″ ″ CO2-n-Pr H OMe OMe CH
554 ″ ″ CO2-i-Pr H OMe OMe CH
555 Me CO-n-C5H11CO2-Me H OMe OMe CH
556″″″″OMeOMeN
557″″″″″MeN
558″″″″″″CH
559 ″ ″ ″ ″ NMe2OCH2CF3N
560″″″″MeMeCH
561″″″″″″N
562″″″″ClOMeCH
563″″″MeOMeOMeCH
564″″″″″MeN
565 ″ ″ CO2-Et H OMe OMe CH
566″″″″″ClCH
No. R1R2R3R4X Y Z Fp.
567″″″″MeMeCH
568″″″″OMeMeN
569 ″ ″ ″ ″ NMe2OCH2CF3N
570″″″MeOMeOMeCH
571″″″″OMeMeN
572 ″ ″ CO2-n-Pr H OMe OMe CH
573″″″″″″N
574″″″″OMeMeN
575″″″″MeMeCH
576″″″″OMeClCH
577″″″MeMeOMeN
578″″″″OMeOMeCH
579 Me CO-n-C5H11CO2-i-Pr H OMe OMe CH
580″″″″″″N
581″″″″HMeN
582″″″″OMeClCH
583″″″″MeMeCH
584 ″ ″ ″ ″ SMe NEt2N
585 ″ ″ CO2-i-Pr Me OMe Me N
586″″″″OMeOMeCH
587 Me ″ CO2-烯丙基 H OMe OMe CH
588 Et ″ CO2-Me H OMe OMe CH
589″″″HOMeMeN
590″″″″MeMeCH
591″″″″ClOMeCH
592″″″MeOMeOMeCH
593″″″″OMeMeN
594 ″ ″ CO2-Et H OMe OMe CH
595″″″″OMeMeCH
596″″″″ClOMeCH
597″″″″OMeMeN
598″″″MeOMeOMeCH
599″″″″″MeN
600 ″ ″ CO2-n-Pr H OMe OMe CH
601″″″″OMeMeN
602″″″″OMeClCH
No. R1R2R3R4X Y Z Fp.
603″″″″MeMeCH
604″″″MeOMeOMeCH
605″″″″OMeMeN
606 ″ ″ CO2-i-Pr H OMe OMe CH
607″″″″OMeMeN
608″″″″MeMeCH
609″″″MeOMeMeN
610 n-Pr CO-n-C5H11CO2-Me H OMe OMe CH
611″″″″″ClCH
612″″″″MeMeCH
613″″″″OMeMeN
614″″″MeOMeOMeCH
615″″″″OMeMeN
616 n-Pr ″ CO2-Et H OMe Me N
617″″″″″OMeCH
618″″″″MeMeCH
619 ″ ″ CO2-n-Pr ″ OMe OMe CH
620 i-Pr ″ CO2-Me H OMe OMe CH
621″″″″OMeMeN
622″″″″MeMeCH
623″″″″ClOMeN
624″″″MeOMeN
625″″″″″OMeCH
626 烯丙基 ″ CO2-Me H OMe OMe CH
627″″″″″ClCH
628″″″″MeMeCH
629″″″″OMeMeN
630 ″ ″ CO2-Et H OMe OMe CH
631 ″ ″ CO2-n-Pr ″ ″ ″ CH
632 ″ ″ CO2-i-Pr ″ ″ ″ ″
633 Me CO-CHMeEt CO2-Me H OMe OMe CH
634″″″″″OMeN
635″″″″″MeN
636″″″″″″CH
637 ″ ″ ″ ″ NMe2OCH2CF3N
638″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
639″″″″″″N
640″″″″ClOMeCH
641″″″MeOMeOMeCH
642″″″″″MeN
643 ″ ″ CO2-Et H OMe OMe CH
644″″″″″ClCH
645″″″″MeMeCH
646″″″″OMeMeN
647 ″ ″ ″ ″ NMe2OCH2CF3N
648″″″MeOMeOMeCH
649″″″″OMeMeN
650 ″ ″ CO2-n-Pr H OMe OMe CH
651″″″″″″N
652″″″″OMeMeN
653″″″″MeMeCH
654″″″″OMeClCH
655″″″MeMeOMeN
656″″″″OMeOMeCH
657 Me COCHMeEt CO2-i-Pr H OMe OMe CH
658″″″″″″N
659″″″″OMeMeN
660″″″″OMeClCH
661″″″″MeMeCH
662 ″ ″ ″ ″ SMe NEt2N
663 ″ ″ CO2-i-Pr Me OMe Me N
664″″″″OMeOMeCH
665 Me ″ CO2-烯丙基 H OMe OMe CH
666 Et ″ CO2-Me H OMe OMe CH
667″″″HOMeMeN
668″″″″MeMeCH
669″″″″ClOMeCH
670″″″MeOMeOMeCH
671″″″″OMeMeN
672 ″ ″ CO2-Et H OMe OMe CH
673″″″″OMeMeCH
674″″″″ClOMeCH
No. R1R2R3R4X Y Z Fp.
675″″″″OMeMeN
676″″″MeOMeOMeCH
677″″″″″MeN
678 ″ ″ CO2-n-Pr H OMe OMe CH
679″″″″OMeMeN
680″″″″OMeClCH
681″″″″MeMeCH
682″″″MeOMeOMeCH
683″″″″OMeMeN
684 ″ ″ CO2-i-Pr H OMe OMe CH
685″″″″OMeMeN
686″″″″MeMeCH
687″″″MeOMeMeN
688 n-Pr CO-CHMeEt CO2-Me H OMe OMe CH
689″″″″″ClCH
690″″″″MeMeCH
691″″″″OMeMeN
692″″″MeOMeOMeCH
693″″″″OMeMeN
694 n-Pr ″ CO2-Et H ″ ″ N
695″″″″″OMeCH
696″″″″MeMeCH
697 ″ ″ CO2-n-Pr ″ OMe OMe CH
698 i-Pr ″ CO2-Me H OMe OMe CH
699″″″″OMeMeN
700″″″″MeMeCH
701″″″″ClOMeN
702″″″MeOMeMeN
703″″″″″OMeCH
704 烯丙基 ″ CO2-Me H OMe OMe CH
705″″″″″ClCH
706″″″″MeMeCH
707″″″″OMeMeN
708 ″ ″ CO2-Et H OMe OMe CH
709 ″ ″ CO2-n-Pr ″ ″ ″ CH
710 ″ ″ CO2-i-Pr ″ ″ ″ CH
No. R1R2R3R4X Y Z Fp.
711 Me
CO2-Me H OMe OMe CH
712""""OMeOMeN
713"""""MeN
714""""""CH
715 " " " " NMe2OCH2CF3N
716""""MeMeCH
717""""""N
718""""ClOMeCH
719"""MeOMeOMeCH
720"""""MeN
721 " " CO2-Et H OMe OMe CH
722"""""ClCH
723""""MeMeCH
724""""OMeMeN
725 " " " " NMe2OCH2CF3N
726"""MeOMeOMeCH
727""""OMeMeN
728 " " CO2-n-Pr H OMe OMe CH
729""""""N
730""""OMeMeN
731""""MeMeCH
732""""OMeClCH
733"""MeMeOMeN
734""""OMeOMeCH
735 Me
CO2-i-Pr H OMe OMe CH
736""""""N
737""""OMeMeN
738""""OMeClCH
739""""MeMeCH
740 " " " " SMe NEt2N
741 " " CO2-i-Pr Me OMe Me N
742""""OMeOMeCH
743 Me " CO2-烯丙基 H OMe OMe CH
744 Et " CO2-Me H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
745"""HOMeMeN
746""""MeMeCH
747""""ClOMeCH
748"""MeOMeOMeCH
749""""OMeMeN
750 " " CO2-Et H OMe OMe CH
751""""OMeMeCH
752""""ClOMeCH
753""""OMeMeN
754"""MeOMeOMeCH
755"""""MeN
756 " " CO2-n-Pr H OMe OMe CH
757""""OMeMeN
758""""OMeClCH
759""""MeMeCH
760"""MeOMeOMeCH
761""""OMeMeN
762 " " CO2-i-Pr H OMe OMe CH
763""""OMeMeN
764""""MeMeCH
765"""MeOMeMeN
766 n-Pr
CO2-Me H OMe OMe CH
767"""""ClCH
768""""MeMeCH
769""""OMeMeN
770"""MeOMeOMeCH
771""""OMeMeN
772 n-Pr " CO2-Et H OMe OMe N
773"""""OMeCH
774""""MeMeCH
775 " " CO2-n-Pr " OMe OMe CH
776 i-Pr " CO2-Me H OMe OMe CH
777""""OMeMeN
778""""MeMeCH
779""""ClOMeN
No. R1R2R3R4X Y Z Fp.
780"""MeOMeMeN
781"""""OMeCH
782 烯丙基 " CO2-Me H OMe OMe CH
783"""""ClCH
784""""MeMeCH
785""""OMeMeN
786 " " CO2-Et H OMe OMe CH
787 " " CO2-n-Pr " " " "
788 " " CO2-i-Pr " " " "
789 Me
CO2Me H OMe OMe CH
790"""""OMeN
791"""""MeN
792""""""CH
793 " " " " NMe2OCH2CF3N
794""""MeMeCH
795""""""N
796""""ClOMeCH
797"""MeOMeOMeCH
798"""""MeN
799 " " CO2-Et H OMe OMe CH
800"""""ClCH
801""""MeMeCH
802""""OMeMeN
803 " " " " NMe2OCH2CF3N
804"""MeOMeOMeCH
805""""OMeMeN
806 " " CO2-n-Pr H OMe OMe CH
807""""""N
808""""OMeMeN
809""""MeMeCH
810""""OMeClCH
811"""MeMeOMeN
812""""OMeOMeCH
813 Me " CO2-i-Pr H OMe OMe CH
814""""""N
No. R1R2R3R4X Y Z Fp.
815″″″″OMeMeN
816″″″″OMeClCH
817″″″″MeMeCH
818 ″ ″ ″ ″ SMe NEt2N
819 ″ ″ CO2-i-Pr Me OMe Me N
820″″″″OMeOMeCH
821 Me ″ CO2-烯丙基 H OMe OMe CH
822 Et ″ CO2-Me H OMe OMe CH
823″″″HOMeMeN
824″″″″MeMeCH
825″″″″ClOMeCH
826″″″MeOMeOMeCH
827″″″″OMeMeN
828 ″ ″ CO2-Et H OMe OMe CH
829″″″″OMeMeCH
830″″″″ClOMeCH
831″″″″OMeMeN
832″″″MeOMeOMeCH
833″″″″″MeN
834 ″ ″ CO2-n-Pr H OMe OMe CH
835″″″″OMeMeN
836″″″″OMeClCH
837″″″″MeMeCH
838″″″MeOMeOMeCH
839″″″″OMeMeN
840 ″ ″ CO2-i-Pr H OMe OMe CH
841″″″″OMeMeN
842″″″″MeMeCH
843″″″MeOMeMeN
844 n-Pr ″ CO2-Me H OMe OMe CH
845″″″″″ClCH
846″″″″MeMeCH
847″″″″OMeMeN
848″″″MeOMeOMeCH
849″″″″OMeMeN
850 n-Pr ″ CO2-Et H ″ ″ N
No. R1R2R3R4X Y Z Fp.
851"""""OMeCH
852""""MeMeCH
853 " " CO2-n-Pr " OMe OMe CH
854 i-Pr " CO2-Me H OMe OMe CH
855""""OMeMeN
856""""MeMeCH
857""""ClOMeN
858"""MeOMeMeN
859"""""OMeCH
860 烯丙基 " CO2-Me H OMe OMe CH
861"""""ClCH
862""""MeMeCH
863""""OMeMeN
864 " " CO2-Et H OMe OMe CH
865 " " CO2-n-Pr H OMe OMe CH
866 " " CO2-i-Pr " " " CH
867 Me
CO2-Me H OMe OMe CH
868"""""OMeN
869"""""MeN
870""""""CH
871 " " " " NMe2OCH2CF3N
872""""MeMeCH
873"""""ClN
874""""ClOMeCH
875"""MeOMeOMeCH
876"""""MeN
877 " " CO2-Et H OMe OMe CH
878"""""ClCH
879""""MeMeCH
880""""OMeMeN
881 " " " " NMe2OCH2CF3N
882"""MeOMeOMeCH
883""""OMeMeN
884 " " CO2-n-Pr H OMe OMe CH
885""""""N
No. R1R2R3R4X Y Z Fp.
886″″″″OMeMeN
887″″″″MeMeCH
888″″″″OMeClCH
889″″″MeMeOMeN
890″″″″OMeOMeCH
891 Me ″ CO2-i-Pr H OMe OMe CH
892″″″″″″N
893″″″″HMeN
894″″″″OMeClCH
895″″″″MeMeCH
896 ″ ″ ″ ″ SMe NEt2N
897 ″ ″ CO2-i-Pr Me OMe Me N
898″″″″OMeOMeCH
899 Me ″ CO2-烯丙基 H OMe OMe CH
900 Et ″ CO2-Me H OMe OMe CH
901″″″HOMeMeN
902″″″″MeMeCH
903″″″″ClOMeCH
904″″″MeOMeOMeCH
905″″″″OMeMeN
906 ″ ″ CO2-Et H OMe OMe CH
907″″″″OMeMeCH
908″″″″ClOMeCH
909″″″″OMeMeN
910″″″MeOMeOMeCH
911″″″″″MeN
912 ″ ″ CO2-n-Pr H OMe OMe CH
913″″″″OMeMeN
914″″″″OMeClCH
915″″″″MeMeCH
916″″″MeOMeOMeCH
917″″″″OMeMeN
918 ″ ″ CO2-i-Pr H OMe OMe CH
919″″″″OMeMeN
920″″″″MeMeCH
921″″″MeOMeMeN
No. R1R2R3R4X Y Z Fp.
922 n-Pr " CO2-Me H OMe OMe CH
923"""""ClCH
924""""MeMeCH
925""""OMeMeN
926"""MeOMeOMeCH
927""""OMeMeN
928 n-Pr " CO2-Et H " " N
929"""""OMeCH
930""""MeMeCH
931 " " CO2-n-Pr " OMe OMe CH
932 i-Pr " CO2-Me H OMe OMe CH
933""""OMeMeN
934""""MeMeCH
935""""ClOMeN
936"""MeOMeMeN
937"""""OMeCH
938 烯丙基 " CO2-Me H OMe OMe CH
939"""""ClCH
940""""MeMeCH
941""""OMeMeN
942 " " CO2-Et H OMe OMe CH
943 " " CO2-n-Pr " " " CH
944 " " CO2-i-Pr " " " "
945 Me
CO2-Me H OMe OMe CH
946"""""OMeN
947"""""MeN
948""""""CH
949 " " " " NMe2OCH2CF3N
950""""MeMeCH
951""""""N
952""""ClOMeCH
953"""MeOMeOMeCH
954"""""MeN
955 " " CO2-Et H OMe OMe CH
956"""""ClCH
No. R1R2R3R4X Y Z Fp.
957""""MeMeCH
958""""OMeMeN
959 " " " " NMe2OCH2CF3N
960"""MeOMeOMeCH
961""""OMeMeN
962 " " CO2-n-Pr H OMe OMe CH
963""""""N
964""""OMeMeN
965""""MeMeCH
966""""OMeClCH
967"""MeMeOMeN
968""""OMeOMeCH
969 Me
CO2-i-Pr H OMe OMe CH
970""""""N
971""""HMeN
972""""OMeClCH
973""""MeMeCH
974 " " " " SMe NEt2N
975 " " CO2-i-Pr Me OMe Me N
976""""OMeOMeCH
977 Me " CO2-烯丙基 H OMe OMe CH
978 Et " CO2-Me H OMe OMe CH
979"""HOMeMeN
980""""MeMeCH
981""""ClOMeCH
982"""MeOMeOMeCH
983""""OMeMeN
984 " " CO2-Et H OMe OMe CH
985""""OMeMeCH
986""""ClOMeCH
987""""OMeMeN
988"""MeOMeOMeCH
989"""""MeN
990 " " CO2-n-Pr H OMe OMe CH
991""""OMeMeN
No. R1R2R3R4X Y Z Fp.
992″″″″OMeClCH
993″″″″MeMeCH
994″″″MeOMeOMeCH
995″″″″OMeMeN
996 ″ ″ CO2-i-Pr H OMe OMe CH
997″″″″OMeMeN
998″″″″MeMeCH
999″″″MeOMeMeN
1.000 n-Pr ″ CO2-Me H OMe OMe CH
1.001″″″″″ClCH
1.002″″″″MeMeCH
1.003″″″″OMeMeN
1.004″″″MeOMeOMeCH
1.005″″″″OMeMeN
1.006 n-Pr ″ CO2-Et H ″ ″ N
1.007″″″″ClOMeCH
1.008″″″″MeMeCH
1.009 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.010 i-Pr ″ CO2-Me H OMe OMe CH
1.011″″″″OMeMeN
1.012″″″″MeMeCH
1.013″″″″ClOMeN
1.014″″″MeOMeMeN
1.015″″″″″OMeCH
1.016 烯丙基 ″ CO2-Me H OMe OMe CH
1.017″″″″″ClCH
1.018″″″″MeMeCH
1.019″″″″OMeMeN
1.020 ″ ″ CO2-Et H OMe OMe CH
1.021 ″ ″ CO2-n-Pr ″ ″ ″ CH
1.022 ″ ″ CO2-i-Pr ″ ″ ″ CH
1.023 Me CO-Ph CO2-Me H OMe OMe CH
1.024″″″″″OMeN
1.025″″″″″MeN
1.026″″″″OMe″CH
1.027 ″ ″ ″ ″ NMe2OCH2CF3N
No. R1R2R3R4X Y Z Fp.
1.028″″″″MeMeCH
1.029″″″″″″N
1.030″″″″ClOMeCH
1.031″″″MeOMeOMeCH
1.032″″″″″MeN
1.033 ″ ″ CO2-Et H OMe OMe CH
1.034″″″″″ClCH
1.035″″″″MeMeCH
1.036″″″″OMeMeN
1.037 ″ ″ ″ ″ NMe2OCH2CF3N
1.038″″″MeOMeOMeCH
1.039″″″″OMeMeN
1.040 ″ ″ CO2-n-Pr H OMe OMe CH
1.041″″″″″″N
1.042″″″″OMeMeN
1.043″″″″MeMeCH
1.044″″″″OMeClCH
1.045″″″MeMeOMeN
1.046″″″″OMeOMeCH
1.047 Me CO-Ph CO2-i-Pr OMe OMe OMe CH
1.048″″″″″″N
1.049″″″″OMeMeN
1.050″″″″OMeClCH
1.051″″″″MeMeCH
1.052 ″ ″ ″ ″ SMe NEt2N
1.053 ″ ″ CO2-i-Pr Me OMe Me N
1.054″″″″OMeOMeCH
1.055 Me ″ CO2-烯丙基 H OMe OMe CH
1.056 Et ″ CO2-Me H OMe OMe CH
1.057″″″HOMeMeN
1.058″″″″MeMeCH
1.059″″″″ClOMeCH
1.060″″″MeOMeOMeCH
1.061″″″″OMeMeN
1.062 ″ ″ CO2-Et H OMe OMe CH
1.063″″″″OMeMeCH
No. R1R2R3R4X Y Z Fp.
1.064″″″″ClOMeCH
1.065″″″″OMeMeN
1.066″″″MeOMeOMeCH
1.067″″″″″MeN
1.068 ″ ″ CO2-n-Pr H OMe OMe CH
1.069″″″″OMeMeN
1.070″″″″OMeClCH
1.071″″″″MeMeCH
1.072″″″MeOMeOMeCH
1.073″″″″OMeMeN
1.074 ″ ″ CO2-i-Pr H OMe OMe CH
1.075″″″″OMeMeN
1.076″″″MeOMeMeN
1.077 n-Pr CO-Ph CO2-Me H OMe OMe CH
1.078″″″″″ClCH
1.079″″″″MeMeCH
1.080″″″″OMeMeN
1.081″″″MeOMeOMeCH
1.082″″″″OMeMeN
1.083 n-Pr ″ CO2-Et H ″ ″ N
1.084″″″″″OMeCH
1.085″″″″MeMeCH
1.086 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.087 i-Pr ″ CO2-Me H OMe OMe CH
1.088″″″″OMeMeN
1.089″″″″MeMeCH
1.090″″″″ClOMeN
1.091″″″MeOMeMeN
1.092″″″″″OMeCH
1.093 烯丙基 ″ CO2-Me H OMe OMe CH
1.094″″″″″ClCH
1.095″″″″MeMeCH
1.096″″″″OMeMeN
1.097 ″ ″ CO2-Et H OMe OMe CH
1.098 ″ ″ CO2-n-Pr H OMe OMe CH
1.099 ″ ″ CO2-i-Pr ″ ″ ″ CH
No. R1R2R3R4X Y Z Fp.
1.100 Me
CO2-Me H OMe OMe CH
1.101"""""OMeN
1.102"""""MeN
1.103""""""CH
1.104 " " " " NMe2OCH2CF3N
1.105""""MeMeCH
1.106""""""N
1.107""""ClOMeCH
1.108"""MeOMeOMeCH
1.109"""""MeN
1.110 " " CO2-Et H OMe OMe CH
1.111"""""ClCH
1.112""""MeMeCH
1.113""""OMeMeN
1.114 " " " " NMe2OCH2CF3N
1.115"""MeOMeOMeCH
1.116""""OMeMeN
1.117 " " CO2-n-Pr H OMe OMe CH
1.118""""""N
1.119""""OMeMeN
1.120""""MeMeCH
1.121""""OMeClCH
1.122"""MeMeOMeN
1.123""""OMeOMeCH
1.124 Me " CO2-i-Pr H OMe OMe CH
1.125""""""N
1.126""""HMeN
1.127""""OMeClCH
1.128""""MeMeCH
1.129 " " " " SMe NEt2N
1.130 " " CO2-i-Pr Me OMe Me N
1.131""""OMeOMeCH
1.132 Me " CO2-烯丙基 H OMe OMe CH
1.133 Et " CO2-Me H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
1.134"""HOMeMeN
1.135""""MeMeCH
1.136""""ClOMeCH
1.137"""MeOMeOMeCH
1.138""""OMeMeN
1.139 " " CO2-Et H OMe OMe CH
1.140""""OMeMeCH
1.141""""ClOMeCH
1.142""""OMeMeN
1.143"""MeOMeOMeCH
1.144"""""MeN
1.145 " " CO2-n-Pr H OMe OMe CH
1.146""""OMeMeN
1.147""""OMeClCH
1.148""""MeMeCH
1.149"""MeOMeOMeCH
1.150"""MeOMeMeN
1.151 " " CO2-i-Pr H OMe OMe CH
1.152""""OMeMeN
1.153""""MeMeCH
1.154"""MeOMeMeN
1.155 n-Pr
CO2-Me H OMe OMe CH
1.156"""""ClCH
1.157""""MeMeCH
1.158""""OMeMeN
1.159"""MeOMeOMeCH
1.160""""OMeMeN
1.161 n-Pr " CO2-Et H OMe Me N
1.162"""""OMeCH
1.163""""MeMeCH
1.164 " " CO2-n-Pr " OMe OMe CH
1.165 i-Pr " CO2-Me H OMe OMe CH
1.166""""OMeMeN
1.167""""MeMeCH
No. R1R2R3R4X Y Z Fp.
1.168″″″″ClOMeN
1.169″″″MeOMeMeN
1.170″″″″″OMeCH
1.171 烯丙基 ″ CO2-Me H OMe OMe CH
1.172″″″″″ClCH
1.173″″″″MeMeCH
1.174″″″″OMeMeN
1.175 ″ ″ CO2-Et H OMe OMe CH
1.176 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.177 ″ ″ CO2-i-Pr H OMe OMe CH
1.178 Me CO-OMe CO2-Me H OMe OMe CH 128℃
1.179″″″″″OMeN
1.180″″″″″MeNs.Bsp.o)
1.181″″″″″″CH89-101
1.182 ″ ″ ″ ″ NMe2OCH2CF3N
1.183″″″″MeMeCHs.Bsp.m)
1.184″″″″″″N
1.185″″″″ClOMeCHs.Bsp.n)
1.186″″″MeOMeOMeCH150-154
1.187″″″″″MeN
1.188 ″ ″ CO2-Et H OMe OMe CH
1.189″″″″″ClCH
1.190″″″″MeMeCH
1.191″″″″OMeMeN
1.192 ″ ″ ″ ″ NMe2OCH2CF3N
1.193″″″MeOMeOMeCH
1.194″″″″OMeMeN
1.195 ″ ″ CO2-n-Pr H OMe OMe CH
1.196″″″″″″N
1.197″″″″OMeMeN
1.198″″″″MeMeCH
1.199″″″″OMeClCH
1.200″″″MeMeOMeN
1.201″″″″OMeOMeCH
1.202 Me CO-OMe CO2-i-Pr H OMe OMe CH
1.203″″″″″″N
No. R1R2R3R4X Y Z Fp.
1.204″″″″OMeMeN
1.205″″″″OMeClCH
1.206″″″″MeMeCH
1.207 ″ ″ ″ ″ SMe NEt2N
1.208 ″ ″ CO2-i-Pr Me OMe Me N
1.209″″″″OMeOMeCH
1.210 Me ″ CO2-烯丙基 H OMe OMe CH
1.211 Et ″ CO2-Me H OMe OMe CH
1.212″″″HOMeMeN
1.213″″″″MeMeCH
1.214″″″″ClOMeCH
1.215″″″MeOMeOMeCH
1.216″″″″OMeMeN
1.217 ″ ″ CO2-Et H OMe OMe CH
1.218″″″″OMeMeCH
1.219″″″″ClOMeCH
1.220″″″″OMeMeN
1.221″″″MeOMeOMeCH
1.222″″″″″MeN
1.223 ″ ″ CO2-n-Pr H OMe OMe CH
1.224″″″″OMeMeN
1.225″″″″OMeClCH
1.226″″″″MeMeCH
1.227″″″MeOMeOMeCH
1.228″″″″OMeMeN
1.229 ″ ″ CO2-i-Pr H OMe OMe CH
1.230″″″″OMeMeN
1.231″″″″MeMeCH
1.232″″″MeOMeMeN
1.233 n-Pr CO-OMe CO2-Me H OMe OMe CH
1.234″″″″″ClCH
1.235″″″″MeMeCH
1.236″″″″OMeMeN
1.237″″″MeOMeOMeCH
1.238″″″″OMeMeN
1.239 n-Pr ″ CO2-Et H OMe Me N
No. R1R2R3R4X Y Z Fp.
1.240″″″″″OMeCH
1.241″″″″MeMeCH
1.242 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.243 i-Pr ″ CO2-Me H OMe OMe CH
1.244″″″″OMeMeN
1.245″″″″MeMeCH
1.246″″″″ClOMeN
1.247″″″MeOMeMeN
1.248″″″″″OMeCH
1.249 烯丙基 ″ CO2-Me H OMe OMe CH
1.250″″″″″ClCH
1.251″″″″MeMeCH
1.252″″″″OMeMeN
1.253 ″ ″ CO2-Et H OMe OMe CH
1.254 ″ ″ CO2-n-Pr ″ ″ ″ ″
1.255 ″ ″ CO2-i-Pr ″ ″ ″ CH
1.256 Me CO-OEt CO2-Me H OMe OMe CH
1.257″″″″″OMeN
1.258″″″″″MeN
1.259″″″″″″CH
1.260 ″ ″ ″ ″ NMe2OCH2CF3N
1.261″″″″MeMeCH
1.262″″″″″″N
1.263″″″″ClOMeCH
1.264″″″MeOMeOMeCH
1.265″″″″″MeN
1.266 ″ ″ CO2-Et H OMe OMe CH
1.267″″″″″ClCH
1.268″″″″MeMeCH
1.269″″″″OMeMeN
1.270 ″ ″ ″ ″ NMe2OCH2CF3N
1.271″″″MeOMeOMeCH
1.272″″″″OMeMeN
1.273 ″ ″ CO2-n-Pr H OMe OMe CH
1.274″″″″″″N
1.275″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
1.276″″″″MeMeCH
1.277″″″″OMeClCH
1.278″″″MeMeOMeN
1.279″″″″OMeOMeCH
1.280 Me CO-OEt CO2-i-Pr H OMe OMe CH
1.281″″″″″″N
1.282″″″″OMeMeN
1.283″″″″OMeClCH
1.284″″″″MeMeCH
1.285 ″ ″ ″ ″ SMe NEt2N
1.286 ″ ″ CO2-i-Pr Me OMe Me N
1.287″″″″OMeOMeCH
1.288 Me ″ CO2-烯丙基 H OMe OMe CH
1.289 Et ″ CO2-Me H OMe OMe CH
1.290″″″HOMeMeN
1.291″″″″MeMeCH
1.292″″″″ClOMeCH
1.293″″″MeOMeOMeCH
1.294″″″″OMeMeN
1.295 ″ ″ CO2-Et H OMe OMe CH
1.296″″″″OMeMeCH
1.297″″″″ClOMeCH
1.298″″″″OMeMeN
1.299″″″MeOMeOMeCH
1.300″″″″″MeN
1.301 ″ ″ CO2-n-Pr H OMe OMe CH
1.302″″″″OMeMeN
1.303″″″″OMeClCH
1.304″″″″MeMeCH
1.305″″″MeOMeOMeCH
1.306″″″″OMeMeN
1.307 ″ ″ CO2-i-Pr H OMe OMe CH
1.308″″″″OMeMeN
1.309″″″″MeMeCH
1.310″″″MeOMeMeN
1.311 n-Pr CO-OEt CO2-Me H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
1.312″″″″″ClCH
1.313″″″″MeMeCH
1.314″″″″OMeMeN
1.315″″″MeOMeOMeCH
1.316″″″″OMeMeN
1.317 n-Pr ″ CO2-Et H ″ ″ N
1.318″″″″″OMeCH
1.319″″″″MeMeCH
1.320 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.321 i-Pr ″ CO2-Me H OMe OMe CH
1.322″″″″OMeMeN
1.323″″″″MeMeCH
1.324″″″″ClOMeN
1.325″″″MeOMeMeN
1.326″″″″″OMeCH
1.327 烯丙基 ″ CO2-Me H OMe OMe CH
1.328″″″″″ClCH
1.329″″″″MeMeCH
1.330″″″″OMeMeN
1.331 ″ ″ CO2-Et H OMe OMe CH
1.332 ″ ″ CO2-n-Pr H OMe OMe CH
1.333 ″ ″ CO2-i-Pr ″ ″ ″ ″
1.334 Me CO-O-i-Pr CO2-Me H OMe OMe CH
1.335″″″″″OMeN
1.336″″″″″MeN
1.337″″″″″″CH
1.338 ″ ″ ″ ″ NMe2OCH2CF3N
1.339″″″″MeMeCH
1.340″″″″″″N
1.341″″″″ClOMeCH
1.342″″″MeOMeOMeCH
1.343″″″″″MeN
1.344 ″ ″ CO2-Et H OMe OMe CH
1.345″″″″″ClCH
1.346″″″″MeMeCH
1.347″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
1.348 ″ ″ ″ ″ NMe2OCH2CF3N
1.349″″″MeOMeOMeCH
1.350″″″″OMeMeN
1.351 ″ ″ CO2-n-Pr H OMe OMe CH
1.352″″″″″″N
1.353″″″″OMeMeN
1.354″″″″MeMeCH
1.355″″″″OMeClCH
1.356″″″MeMeOMeN
1.357″″″″OMeOMeCH
1.358 Me CO-O-i-Pr CO2-i-Pr H OMe OMe CH
1.359″″″″″″N
1.360″″″″HMeN
1.361″″″″OMeClCH
1.362″″″″MeMeCH
1.363 ″ ″ ″ ″ SMe NEt2N
1.364 ″ ″ CO2-i-Pr Me OMe Me N
1.365″″″″OMeOMeCH
1.366 Me ″ CO2-烯丙基 H OMe OMe CH
1.367 Et ″ CO2-Me H OMe OMe CH
1.368″″″HOMeMeN
1.369″″″″MeMeCH
1.370″″″″ClOMeCH
1.371″″″MeOMeOMeCH
1.372″″″″OMeMeN
1.373 ″ ″ CO2-Et H OMe OMe CH
1.374″″″″OMeMeCH
1.375″″″″ClOMeCH
1.376″″″″OMeMeN
1.377″″″MeOMeOMeCH
1.378″″″″″MeN
1.379 ″ ″ CO2-n-Pr H OMe OMe CH
1.380″″″″OMeMeN
1.381″″″″OMeClCH
1.382″″″″MeMeCH
1.383″″″MeOMeOMeCH
No. R1R2R3R4X Y Z Fp.
1.384″″″″OMeMeN
1.385 ″ ″ CO2-i-Pr H OMe OMe CH
1.386″″″″OMeMeN
1.387″″″″MeMeCH
1.388″″″MeOMeMeN
1.389 n-Pr CO-O-i-Pr CO2-Me H OMe OMe CH
1.390″″″″″ClCH
1.391″″″″MeMeCH
1.392″″″″OMeMeN
1.393″″″MeOMeOMeCH
1.394″″″″OMeMeN
1.395 n-Pr ″ CO2-Et H ″ ″ N
1.396″″″″″OMeCH
1.397″″″″MeMeCH
1.398 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.399 i-Pr ″ CO2-Me H OMe OMe CH
1.400″″″″OMeMeN
1.401″″″″MeMeCH
1.402″″″″ClOMeN
1.403″″″MeOMeMeN
1.404″″″″″OMeCH
1.405 烯丙基 ″ CO2-Me H OMe OMe CH
1.406″″″″″ClCH
1.407″″″″MeMeCH
1.408″″″″OMeMeN
1.409 ″ ″ CO2-Et H OMe OMe CH
1.410 ″ ″ CO2-n-Pr ″ ″ ″ CH
1.411 ″ ″ CO2-i-Pr ″ ″ ″ CH
1.412 Me CO-O-n-Pr CO2-Me H OMe OMe CH
1.413″″″″″OMeN
1.414″″″″″MeN
1.415″″″″″″CH
1.416 ″ ″ ″ ″ NMe2OCH2CF3N
1.417″″″″MeMeCH
1.418″″″″″″N
1.419″″″″ClOMeCH
No. R1R2R3R4X Y Z Fp.
1.420″″″MeOMeOMeCH
1.421″″″″″MeN
1.422 ″ ″ CO2-Et H OMe OMe CH
1.423″″″″″ClCH
1.424″″″″MeMeCH
1.425″″″″OMeMeN
1.426 ″ ″ ″ ″ NMe2OCH2CF3N
1.427″″″MeOMeOMeCH
1.428″″″″OMeMeN
1.429 ″ ″ CO2-n-Pr H OMe OMe CH
1.430″″″″″″N
1.431″″″″OMeMeN
1.432″″″″MeMeCH
1.433″″″″OMeClCH
1.434″″″MeMeOMeN
1.435″″″″OMeOMeCH
1.436 Me CO-O-n-Pr CO2-i-Pr H OMe OMe CH
1.437″″″″″″N
1.438″″″″OMeMeN
1.439″″″″OMeClCH
1.440″″″″MeMeCH
1.441 ″ ″ ″ ″ SMe NEt2N
1.442 ″ ″ CO2-i-Pr Me OMe Me N
1.443″″″″OMeOMeCH
1.444 Me ″ CO2-烯丙基 H OMe OMe CH
1.445 Et ″ CO2-Me H OMe OMe CH
1.446″″″HOMeMeN
1.447″″″″MeMeCH
1.448″″″″ClOMeCH
1.449″″″MeOMeOMeCH
1.450″″″″OMeMeN
1.451 ″ ″ CO2-Et H OMe OMe CH
1.452″″″″OMeMeCH
1.453″″″″ClOMeCH
1.454″″″″OMeMeN
1.455″″″MeOMeOMeCH
No. R1R2R3R4X Y Z Fp.
1.456″″″″″MeN
1.457 ″ ″ CO2-n-Pr H OMe OMe CH
1.458″″″″OMeMeN
1.459″″″″OMeClCH
1.460″″″″MeMeCH
1.461″″″MeOMeOMeCH
1.462″″″″OMeMeN
1.463 ″ ″ CO2-i-Pr H OMe OMe CH
1.464″″″″OMeMeN
1.465″″″″MeMeCH
1.466″″″MeOMeMeN
1.467 n-Pr CO-O-n-Pr CO2-Me H OMe OMe CH
1.468″″″″″ClCH
1.469″″″″MeMeCH
1.470″″″″OMeMeN
1.471″″″MeOMeOMeCH
1.472″″″″OMeMeN
1.473 n-Pr ″ CO2-Et H ″ ″ N
1.474″″″″″OMeCH
1.475″″″″MeMeCH
1.476 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.477 i-Pr ″ CO2-Me H OMe OMe CH
1.478″″″″OMeMeN
1.479″″″″MeMeCH
1.480″″″″ClOMeN
1.481″″″MeOMeMeN
1.482″″″″″OMeCH
1.483 烯丙基 ″ CO2-Me H OMe OMe CH
1.484″″″″″ClCH
1.485″″″″MeMeCH
1.486″″″″OMeMeN
1.487 ″ ″ CO2-Et H OMe OMe CH
1.488 ″ ″ CO2-n-Pr ″ ″ ″ CH
1.489 ″ ″ CO2-i-Pr ″ ″ ″ CH
1.490 Me CO-O-烯丙基 CO2-Me H OMe OMe CH
1.491″″″″″OMeN
No. R1R2R3R4X Y Z Fp.
1.492″″″″″MeN
1.493″″″″″″CH
1.494 ″ ″ ″ ″ NMe2OCH2CF3N
1.495″″″″MeMeCH
1.496″″″″″″N
1.497″″″″ClOMeCH
1.498″″″MeOMeOMeCH
1.499″″″″″MeN
1.500 ″ ″ CO2-Et H OMe OMe CH
1.501″″″″″ClCH
1.502″″″″MeMeCH
1.503″″″″OMeMeN
1.504 ″ ″ ″ ″ NMe2OCH2CF3N
1.505″″″MeOMeOMeCH
1.506″″″″OMeMeN
1.507 ″ ″ CO2-n-Pr H OMe OMe CH
1.508″″″″″″N
1.509″″″″OMeMeN
1.510″″″″MeMeCH
1.511″″″″OMeClCH
1.512″″″MeMeOMeN
1.513″″″″OMeOMeCH
1.514 Me CO-O-烯丙基 CO2-i-Pr H OMe OMe CH
1.515″″″″″″N
1.516″″″″HMeN
1.517″″″″OMeClCH
1.518″″″″MeMeCH
1.519 ″ ″ ″ ″ SMe NEt2N
1.520 ″ ″ CO2-i-Pr Me OMe Me N
1.521″″″″OMeOMeCH
1.522 Me ″ CO2-烯丙基 H OMe OMe CH
1.523 Et ″ CO2-Me H OMe OMe CH
1.524″″″HOMeMeN
1.525″″″″MeMeCH
1.526″″″″ClOMeCH
1.527″″″MeOMeOMeCH
No. R1R2R3R4X Y Z Fp.
1.528″″″″OMeMeN
1.529 ″ ″ CO2-Et H OMe OMe CH
1.530″″″″OMeMeCH
1.531″″″″ClOMeCH
1.532″″″″OMeMeN
1.533″″″MeOMeOMeCH
1.534″″″″″MeN
1.535 ″ ″ CO2-n-Pr H OMe OMe CH
1.536″″″″OMeMeN
1.537″″″″OMeClCH
1.538″″″″MeMeCH
1.539″″″MeOMeOMeCH
1.540″″″″OMeMeN
1.541 ″ ″ CO2-i-Pr H OMe OMe CH
1.542″″″″OMeMeN
1.543″″″″MeMeCH
1.544″″″MeOMeMeN
1.545 n-Pr CO-O-烯丙基 CO2-Me H OMe OMe CH
1.546″″″″″ClCH
1.547″″″″MeMeCH
1.548″″″″OMeMeN
1.549″″″MeOMeOMeCH
1.550″″″″OMeMeN
1.551 n-Pr ″ CO2-Et H ″ ″ N
1.552″″″″″OMeCH
1.553″″″″MeMeCH
1.554 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.555 i-Pr ″ CO2-Me H OMe OMe CH
1.556″″″″OMeMeN
1.557″″″″MeMeCH
1.558″″″″ClOMeN
1.559″″″MeOMeMeN
1.560″″″″″OMeCH
1.561 烯丙基 ″ CO2-Me H OMe OMe CH
1.562″″″″″ClCH
1.563″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
1.564″″″″OMeMeN
1.565 ″ ″ CO2-Et H OMe OMe CH
1.566 ″ ″ CO2-n-Pr ″ ″ ″ CH
1.567 ″ ″ CO2-i-Pr ″ ″ ″ CH
1.568 Me CO-NH-Et CO2-Me H OMe OMe CH
1.569″″″″″OMeN
1.570″″″″″MeN
1.571″″″″″″CH
1.572 ″ ″ ″ ″ NMe2OCH2CF3N
1.573″″″″MeMeCH
1.574″″″″″″N
1.575″″″″ClOMeCH
1.576″″″MeOMeOMeCH
1.577″″″″″MeN
1.578 ″ ″ CO2-Et H OMe OMe CH
1.579″″″″″ClCH
1.580″″″″MeMeCH
1.581″″″″OMeMeN
1.582 ″ ″ ″ ″ NMe2OCH2CF3N
1.583″″″MeOMeOMeCH
1.584″″″″OMeMeN
1.585 ″ ″ CO2-n-Pr H OMe OMe CH
1.586″″″″″″N
1.587″″″″OMeMeN
1.588″″″″MeMeCH
1.589″″″″OMeClCH
1.590″″″MeMeOMeN
1.591″″″″OMeOMeCH
1.592 Me CO-NHEt CO2-i-Pr H OMe OMe CH
1.593″″″″″″N
1.594″″″″OMeMeN
1.595″″″″OMeClCH
1.596″″″″MeMeCH
1.597 ″ ″ ″ ″ SMe NEt2N
1.598 ″ ″ CO2-i-Pr Me OMe Me N
1.599″″″″OMeOMeCH
No. R1R2R3R4X Y Z Fp.
1.600 Me ″ CO2-烯丙基 H OMe OMe CH
1.601 Et ″ CO2-Me H OMe OMe CH
1.602″″″HOMeMeN
1.603″″″″MeMeCH
1.604″″″″ClOMeCH
1.605″″″MeOMeOMeCH
1.606″″″″OMeMeN
1.607 ″ ″ CO2-Et H OMe OMe CH
1.608″″″″OMeMeCH
1.609″″″″ClOMeCH
1.610″″″″OMeMeN
1.611″″″MeOMeOMeCH
1.612″″″″″MeN
1.613 ″ ″ CO2-n-Pr H OMe OMe CH
1.614″″″″OMeMeN
1.615″″″″OMeClCH
1.616″″″″MeMeCH
1.617″″″MeOMeOMeCH
1.618″″″″OMeMeN
1.619 ″ ″ CO2-i-Pr H OMe OMe CH
1.620″″″″OMeMeN
1.621″″″″MeMeCH
1.622″″″MeOMeMeN
1.623 n-Pr CO-NHEt CO2-Me H OMe OMe CH
1.624″″″″″ClCH
1.625″″″″MeMeCH
1.626″″″″OMeMeN
1.627″″″MeOMeOMeCH
1.628″″″″OMeMeN
1.629 n-Pr ″ CO2-Et H ″ ″ N
1.630″″″″″OMeCH
1.631″″″″MeMeCH
1.632 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.633 i-Pr ″ CO2-Me H OMe OMe CH
1.634″″″″OMeMeN
1.635″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
1.636″″″″ClOMeN
1.637″″″MeOMeMeN
1.638″″″″″OMeCH
1.639 烯丙基 ″ CO2-Me H OMe OMe CH
1.640″″″″″ClCH
1.641″″″″MeMeCH
1.642″″″″OMeMeN
1.643 ″ ″ CO2-Et H OMe OMe CH
1.644 ″ ″ CO2-n-Pr ″ ″ ″ CH
1.645 ″ ″ CO2-i-Pr ″ ″ ″ CH
1.646 Me CO-NHPr CO2-Me H ″ ″ CH
1.647″″″″″OMeN
1.648″″″″″MeN
1.649″″″″″″CH
1.650 ″ ″ ″ ″ NMe2OCH2CF3N
1.651″″″″MeMeCH
1.652″″″″″″N
1.653″″″″ClOMeCH
1.654″″″MeOMeOMeCH
1.655″″″″″MeN
1.656 ″ ″ CO2-Et H OMe OMe CH
1.657″″″″″ClCH
1.658″″″″MeMeCH
1.659″″″″OMeMeN
1.660 ″ ″ ″ ″ NMe2OCH2CF3N
1.661″″″MeOMeOMeCH
1.662″″″″OMeMeN
1.663 ″ ″ CO2-n-Pr H OMe OMe CH
1.664″″″″″″N
1.665″″″″OMeMeN
1.666″″″″MeMeCH
1.667″″″″OMeClCH
1.668″″″MeMeOMeN
1.669″″″″OMeOMeCH
1.670 Me CONHPr CO2-i-Pr H OMe OMe CH
1.671″″″″″″N
No. R1R2R3R4X Y Z Fp.
1.672″″″″OMeMeN
1.673″″″″OMeClCH
1.674″″″″MeMeCH
1.675 ″ ″ ″ ″ SMe NEt2N
1.676 ″ ″ CO2-i-Pr Me OMe Me N
1.677″″″″OMeOMeCH
1.678 Me ″ CO2-烯丙基 H OMe OMe CH
1.679 Et ″ CO2-Me H OMe OMe CH
1.680″″″HOMeMeN
1.681″″″″MeMeCH
1.682″″″″ClOMeCH
1.683″″″MeOMeOMeCH
1.684″″″″OMeMeN
1.685 ″ ″ CO2-Et H OMe OMe CH
1.686″″″″OMeMeCH
1.687″″″″ClOMeCH
1.688″″″″OMeMeN
1.689″″″MeOMeOMeCH
1.690″″″″″MeN
1.691 ″ ″ CO2-n-Pr H OMe OMe CH
1.692″″″″OMeMeN
1.693″″″″OMeClCH
1.694″″″″MeMeCH
1.695″″″MeOMeOMeCH
1.696″″″″OMeMeN
1.697 ″ ″ CO2-i-Pr H OMe OMe CH
1.698″″″″OMeMeN
1.699″″″″MeMeCH
1.700″″″MeOMeMeN
1.701 n-Pr ″ CO2Me H OMe OMe CH
1.702″″″″″ClCH
1.703″″″″MeMeCH
1.704″″″″OMeMeN
1.705″″″MeOMeOMeCH
1.706″″″″OMeMeN
1.707 n-Pr ″ CO2-Et H ″ ″ N
No. R1R2R3R4X Y Z Fp.
1.708″″″″″OMeCH
1.709″″″″MeMeCH
1.710 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.711 i-Pr ″ CO2-Me H OMe OMe CH
1.712″″″″OMeMeN
1.713″″″″MeMeCH
1.714″″″″ClOMeN
1.715″″″MeOMeMeN
1.716″″″″″OMeCH
1.717 烯丙基 ″ CO2-Me H OMe OMe CH
1.718″″″″″ClCH
1.719″″″″MeMeCH
1.720″″″″OMeMeN
1.721 ″ ″ CO2-Et H OMe OMe CH
1.722 ″ ″ CO2-n-Pr ″ ″ ″ CH
1.723 ″ ″ CO2-i-Pr ″ ″ ″ CH
1.724 Me CONH.烯丙基 CO2-Me H OMe OMe CH
1.725″″″″″OMeN
1.726″″″″″MeN
1.727″″″″″″CH
1.728 ″ ″ ″ ″ NMe2OCH2CF3N
1.729″″″″MeMeCH
1.730″″″″″″N
1.731″″″″ClOMeCH
1.732″″″MeOMeOMeCH
1.733″″″″″MeN
1.734 ″ ″ CO2-Et H OMe OMe CH
1.735″″″″″ClCH
1.736″″″″MeMeCH
1.737″″″″OMeMeN
1.738 ″ ″ ″ ″ NMe2OCH2CF3N
1.739″″″MeOMeOMeCH
1.740″″″″OMeMeN
1.741 ″ ″ CO2-n-Pr H OMe OMe CH
1.742″″″″″″N
1.743″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
1.744″″″″MeMeCH
1.745″″″″OMeCHCH
1.746″″″MeMeOMeN
1.747″″″″OMeOMeCH
1.748 Me CONH.烯丙基 CO2-i-Pr H OMe OMe CH
1.749″″″″″″N
1.750″″″″OMeMeN
1.751″″″″OMeClCH
1.752″″″″MeMeCH
1.753 ″ ″ ″ ″ SMe NEt2N
1.754 ″ ″ CO2-i-Pr Me OMe Me N
1.755″″″″OMeOMeCH
1.756 Me ″ CO2-烯丙基 H OMe OMe CH
1.757 Et ″ CO2-Me H OMe OMe CH
1.758″″″HOMeMeN
1.759″″″″MeMeCH
1.760″″″″ClOMeCH
1.761″″″MeOMeOMeCH
1.762″″″″OMeMeN
1.763 ″ ″ CO2-Et H OMe OMe CH
1.764″″″″OMeMeCH
1.765″″″″ClOMeCH
1.766″″″″OMeMeN
1.767″″″MeOMeOMeCH
1.768″″″″″MeN
1.769 ″ ″ CO2-n-Pr H OMe OMe CH
1.770″″″″OMeMeN
1.771″″″″OMeClCH
1.772″″″″MeMeCH
1.773″″″MeOMeOMeCH
1.774″″″″OMeMeN
1.775 ″ ″ CO2-i-Pr H OMe OMe CH
1.776″″″″OMeMeN
1.777″″″″MeMeCH
1.778″″″MeOMeMeN
1.779 n-Pr CO-NH烯丙基 CO2-Me H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
1.780″″″″″ClCH
1.781″″″″MeMeCH
1.782″″″″OMeMeN
1.783″″″MeOMeOMeCH
1.784″″″″OMeMeN
1.785 n-Pr ″ CO2-Et H OMe Me N
1.786″″″″″OMeCH
1.787″″″″MeMeCH
1.788 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.789 i-Pr ″ CO2-Me H OMe OMe CH
1.790″″″″OMeMeN
1.791″″″″MeMeCH
1.792″″″″ClOMeN
1.793″″″MeOMeMeN
1.794″″″″″OMeCH
1.795 烯丙基 ″ CO2-Me H OMe OMe CH
1.796″″″″″ClCH
1.797″″″″MeMeCH
1.798″″″″OMeMeN
1.799 ″ ″ CO2-Et H OMe OMe CH
1.800 ″ ″ CO2-n-Pr ″ ″ ″ ″
1.801 ″ ″ CO2-i-Pr ″ ″ ″ ″
1.802 Me CS-NHMe CO2-Me H OMe OMe CH
1.803″″″″″OMeN
1.804″″″″″MeN
1.805″″″″″″CH
1.806 ″ ″ ″ ″ NMe2OCH2CF3N
1.807″″″″MeMeCH
1.808″″″″″″N
1.809″″″″ClOMeCH
1.810″″″MeOMeOMeCH
1.811″″″″″MeN
1.812 ″ ″ CO2-Et H OMe OMe CH
1.813″″″″″ClCH
1.814″″″″MeMeCH
1.815″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
1.816 ″ ″ ″ ″ NMe2OCH2CF3N
1.817″″″MeOMeOMeCH
1.818″″″″OMeMeN
1.819 ″ ″ CO2-n-Pr H OMe OMe CH
1.820″″″″″″N
1.821″″″″OMeMeN
1.822″″″″MeMeCH
1.823″″″″OMeClCH
1.824″″″MeMeOMeN
1.825″″″″OMeOMeCH
1.826 Me CS-NHMe CO2-i-Pr H OMe OMe CH
1.827″″″″″″N
1.828″″″″OMeMeN
1.829″″″″OMeClCH
1.830″″″″MeMeCH
1.831 ″ ″ ″ ″ SMe NEt2N
1.832 ″ ″ CO2-i-Pr Me OMe Me N
1.833″″″″OMeOMeCH
1.834 Me ″ CO2-烯丙基 H OMe OMe CH
1.835 Et ″ CO2-Me H OMe OMe CH
1.836″″″HOMeMeN
1.837″″″″MeMeCH
1.838″″″″ClOMeCH
1.839″″″MeOMeOMeCH
1.840″″″″OMeMeN
1.841 ″ ″ CO2-Et H OMe OMe CH
1.842″″″″OMeMeCH
1.843″″″″ClOMeCH
1.844″″″″OMeMeN
1.845″″″MeOMeOMeCH
1.846″″″″″MeN
1.847 ″ ″ CO2-n-Pr H OMe OMe CH
1.848″″″″OMeMeN
1.849″″″″OMeClCH
1.850″″″″MeMeCH
1.851″″″MeOMeOMeCH
No. R1R2R3R4X Y Z Fp.
1.852″″″″OMeMeN
1.853 ″ ″ CO2-i-Pr H OMe OMe CH
1.854″″″″OMeMeN
1.855″″″″MeMeCH
1.856″″″MeOMeMeN
1.857 n-Pr CS-NHMe CO2-Me H OMe OMe CH
1.858″″″″″ClCH
1.859″″″″MeMeCH
1.860″″″″OMeMeN
1.861″″″MeOMeOMeCH
1.862″″″″OMeMeN
1.863 n-Pr ″ CO2-Et H ″ ″ N
1.864″″″″″OMeCH
1.865″″″″MeMeCH
1.866 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.867 i-Pr ″ CO2-Me H OMe OMe CH
1.868″″″″OMeMeN
1.869″″″″MeMeCH
1.870″″″″ClOMeN
1.871″″″MeOMeMeN
1.872″″″″″OMeCH
1.873 烯丙基 ″ CO2-Me H OMe OMe CH
1.874″″″″″ClCH
1.875″″″″MeMeCH
1.876″″″″OMeMeN
1.877 ″ ″ CO2-Et H OMe OMe CH
1.878 ″ ″ CO2-n-Pr H OMe OMe CH
1.879 ″ ″ CO2-i-Pr ″ ″ ″ ″
1.880 Me CS-NHEt CO2-Me H OMe OMe CH
1.881″″″″″OMeN
1.882″″″″″MeN
1.883″″″″″″CH
1.884 ″ ″ ″ ″ NMe2OCH2CF3N
1.885″″″″MeMeCH
1.886″″″″″″N
1.887″″″″ClOMeCH
No. R1R2R3R4X Y Z Fp.
1.888″″″MeOMeOMeCH
1.889″″″″″MeN
1.890 ″ ″ CO2-Et H OMe OMe CH
1.891″″″″″ClCH
1.892″″″″MeMeCH
1.893″″″″OMeMeN
1.894 ″ ″ ″ ″ NMe2OCH2CF3N
1.895″″″MeOMeOMeCH
1.896″″″″OMeMeN
1.897 ″ ″ CO2-n-Pr H OMe OMe CH
1.898″″″″″″N
1.899″″″″OMeMeN
1.900″″″″MeMeCH
1.901″″″″OMeClCH
1.902″″″MeMeOMeN
1.903″″″″OMeOMeCH
1.904 Me CS-NHEt CO2-i-Pr H OMe OMe CH
1.905″″″″″″N
1.906″″″″OMeMeN
1.907″″″″OMeClCH
1.908″″″″MeMeCH
1.909 ″ ″ ″ ″ SMe NEt2N
1.910 ″ ″ CO2-i-Pr Me OMe Me N
1.911″″″″OMeOMeCH
1.912 Me ″ CO2-烯丙基 H OMe OMe CH
1.913 Et ″ CO2-Me H OMe OMe CH
1.914″″″HOMeMeN
1.915″″″″MeMeCH
1.916″″″″ClOMeCH
1.917″″″MeOMeOMeCH
1.918″″″″OMeMeN
1.919 ″ ″ CO2-Et H OMe OMe CH
1.920″″″″″MeCH
1.921″″″″ClOMeCH
1.922″″″″OMeMeN
1.923″″″MeOMeOMeCH
No. R1R2R3R4X Y Z Fp.
1.924″″″″″MeN
1.925 ″ ″ CO2-n-Pr H OMe OMe CH
1.926″″″″OMeMeN
1.927″″″″OMeClCH
1.928″″″″MeMeCH
1.929″″″MeOMeOMeCH
1.930″″″″OMeMeN
1.931 ″ ″ CO2-i-Pr H OMe OMe CH
1.932″″″″OMeMeN
1.933″″″″MeMeCH
1.934″″″MeOMeMeN
1.935 n-Pr CS-NHEt CO2-Me H OMe OMe CH
1.936″″″″″ClCH
1.937″″″″MeMeCH
1.938″″″″OMeMeN
1.939″″″MeOMeOMeCH
1.940″″″″OMeMeN
1.941 n-Pr ″ CO2-Et H ″ ″ N
1.942″″″″″OMeCH
1.943″″″″MeMeCH
1.944 ″ ″ CO2-n-Pr ″ OMe OMe CH
1.945 i-Pr ″ CO2-Me H OMe OMe CH
1.946″″″″OMeMeN
1.947″″″″MeMeCH
1.948″″″″ClOMeN
1.949″″″MeOMeMeN
1.950″″″″″OMeCH
1.951 烯丙基 ″ CO2-Me H OMe OMe CH
1.952″″″″″ClCH
1.953″″″″MeMeCH
1.954″″″″OMeMeN
1.955 ″ ″ CO2-Et H OMe OMe CH
1.956 ″ ″ CO2-n-Pr ″ ″ ″ CH
1.957 ″ ″ CO2-i-Pr ″ ″ ″ CH
1.958 Me CS-NH-n-Pr CO2-Me H OMe OMe CH
1.959″″″″″OMeN
No. R1R2R3R4X Y Z Fp.
1.960″″″″″MeN
1.961″″″″″″CH
1.962 ″ ″ ″ ″ NMe2OCH2CF3N
1.963″″″″MeMeCH
1.964″″″″″″N
1.965″″″″ClOMeCH
1.966″″″MeOMeOMeCH
1.967″″″″″MeN
1.968 ″ ″ CO2-Et H OMe OMe CH
1.969″″″″″ClCH
1.970″″″″MeMeCH
1.971″″″″OMeMeN
1.972 ″ ″ ″ ″ NMe2OCH2CF3N
1.973″″″MeOMeOMeCH
1.974″″″″OMeMeN
1.975 ″ ″ CO2-n-Pr H OMe OMe CH
1.976″″″″″″N
1.977″″″″OMeMeN
1.978″″″″MeMeCH
1.979″″″″OMeClCH
1.980″″″MeMeOMeN
1.981″″″″OMeOMeCH
1.982 Me CS-NH-n-Pr CO2-i-Pr H OMe OMe CH
1.983″″″″″″N
1.984″″″″OMeMeN
1.985″″″″OMeClCH
1.986″″″″MeMeCH
1.987 ″ ″ ″ ″ SMe NEt2N
1.988 ″ ″ CO2-i-Pr Me OMe Me N
1.989″″″″OMeOMeCH
1.990 Me ″ CO2-烯丙基 H OMe OMe CH
1.991 Et ″ CO2-Me H OMe OMe CH
1.992″″″HOMeMeN
1.993″″″″MeMeCH
1.994″″″″ClOMeCH
1.995″″″MeOMeOMeCH
No. R1R2R3R4X Y Z Fp.
1.996″″″″OMeMeN
1.997 ″ ″ CO2-Et H OMe OMe CH
1.998″″″″OMeMeCH
1.999″″″″ClOMeCH
2.000″″″″OMeMeN
2.001″″″MeOMeOMeCH
2.002″″″″″MeN
2.003 ″ ″ CO2-n-Pr H OMe OMe CH
2.004″″″″OMeMeN
2.005″″″″OMeClCH
2.006″″″″MeMeCH
2.007″″″MeOMeOMeCH
2.008″″″″OMeMeN
2.009 ″ ″ CO2-i-Pr H OMe OMe CH
2.010″″″″OMeMeN
2.011″″″″MeMeCH
2.012″″″MeOMeMeN
2.013 n-Pr CS-NH-n-Pr CO2-Me H OMe OMe CH
2.014″″″″″ClCH
2.015″″″″MeMeCH
2.016″″″″OMeMeN
2.017″″″MeOMeOMeCH
2.018″″″″OMeMeN
2.019 n-Pr ″ CO2-Et H ″ ″ N
2.020″″″″″OMeCH
2.021″″″″MeMeCH
2.022 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.023 i-Pr ″ CO2-Me H ″ ″ CH
2.024″″″″″MeN
2.025″″″″MeMeCH
2.026″″″″ClOMeN
2.027″″″MeOMeMeN
2.028″″″″″OMeCH
2.029 烯丙基 ″ CO2-Me H OMe OMe CH
2.030″″″″″ClCH
2.031″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
2.032″″″″OMeMeN
2.033 ″ ″ CO2-Et H OMe OMe CH
2.034 ″ ″ CO2-n-Pr ″ ″ ″ CH
2.035 ″ ″ CO2-i-Pr ″ ″ ″ CH
2.036 Me CS-NH-i-Pr CO2-Me H OMe OMe CH
2.037″″″″″OMeN
2.038″″″″″MeN
2.039″″″″″″CH
2.040 ″ ″ ″ ″ NMe2OCH2CF3N
2.041″″″″MeMeCH
2.042″″″″″″N
2.043″″″″ClOMeCH
2.044″″″MeOMeOMeCH
2.045″″″″″MeN
2.046 ″ ″ CO2-Et H OMe OMe CH
2.047″″″″″ClCH
2.048″″″″MeMeCH
2.049″″″″OMeMeN
2.050 ″ ″ ″ ″ NMe2OCH2CF3N
2.051″″″MeOMeOMeCH
2.052″″″″OMeMeN
2.053 ″ ″ CO2-n-Pr H OMe OMe CH
2.054″″″″″″N
2.055″″″″OMeMeN
2.056″″″″MeMeCH
2.057″″″″OMeClCH
2.058″″″MeMeOMeN
2.059″″″″OMeOMeCH
2.060 Me CS-NH-i-Pr CO2-i-Pr H OMe OMe CH
2.061″″″″″″N
2.062″″″″OMeMeN
2.063″″″″OMeClCH
2.064″″″″MeMeCH
2.065 ″ ″ ″ ″ SMe NEt2N
2.066 ″ ″ CO2-i-Pr Me OMe Me N
2.067″″″″OMeOMeCH
No. R1R2R3R4X Y Z Fp.
2.068 Me ″ CO2-烯丙基 H OMe OMe CH
2.069 Et ″ CO2-Me H OMe OMe CH
2.070″″″HOMeMeN
2.071″″″″MeMeCH
2.072″″″″ClOMeCH
2.073″″″MeOMeOMeCH
2.074″″″″OMeMeN
2.075 ″ ″ CO2-Et H OMe OMe CH
2.076″″″″OMeMeCH
2.077″″″″ClOMeCH
2.078″″″″OMeMeN
2.079″″″MeOMeOMeCH
2.080″″″″″MeN
2.081 ″ ″ CO2-n-Pr H OMe OMe CH
2.082″″″″OMeMeN
2.083″″″″OMeClCH
2.084″″″″MeMeCH
2.085″″″MeOMeOMeCH
2.086″″″″OMeMeN
2.087 ″ ″ CO2-i-Pr H OMe OMe CH
2.088″″″″OMeMeN
2.089″″″″MeMeCH
2.090″″″MeOMeMeN
2.091 n-Pr CS-NH-i-Pr CO2-Me H OMe OMe CH
2.092″″″″″ClCH
2.093″″″″MeMeCH
2.094″″″″OMeMeN
2.095″″″MeOMeOMeCH
2.096″″″″OMeMeN
2.097 n-Pr ″ CO2-Et H ″ ″ N
2.098″″″″″OMeCH
2.099″″″″MeMeCH
2.100 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.101 i-Pr ″ CO2-Me H OMe OMe CH
2.102″″″″OMeMeN
2.103″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
2.104″″″″ClOMeN
2.105″″″MeOMeMeN
2.106″″″″″OMeCH
2.107 烯丙基 ″ CO2-Me H OMe OMe CH
2.108″″″″″ClCH
2.109″″″″MeMeCH
2.110″″″″OMeMeN
2.111 ″ ″ CO2-Et H OMe OMe CH
2.112 ″ ″ CO2-n-Pr ″ ″ ″ CH
2.113 ″ ″ CO2-i-Pr ″ ″ ″ CH
2.114 Me CS-NH-烯丙基 CO2-Me H OMe OMe CH
2.115″″″″″OMeN
2.116″″″″″MeN
2.117″″″″″″CH
2.118 ″ ″ ″ ″ NMe2OCH2CF3N
2.119″″″″MeMeCH
2.120″″″″″″N
2.121″″″″ClOMeCH
2.122″″″MeOMeOMeCH
2.123″″″″″MeN
2.124 ″ ″ CO2-Et H OMe OMe CH
2.125″″″″″ClCH
2.126″″″″MeMeCH
2.127″″″″OMeMeN
2.128 ″ ″ ″ ″ NMe2OCH2CF3N
2.129″″″MeOMeOMeCH
2.130″″″″OMeMeN
2.131 ″ ″ CO2-n-Pr H OMe OMe CH
2.132″″″″″″N
2.133″″″″OMeMeN
2.134″″″″MeMeCH
2.135″″″″OMeClCH
2.136″″″MeMeOMeN
2.137″″″″OMeOMeCH
2.138 Me CS-NH.烯丙基 CO2-i-Pr H OMe OMe CH
2.139″″″″″″N
No. R1R2R3R4X Y Z Fp.
2.140″″″″HMeN
2.141″″″″OMeClCH
2.142″″″″MeMeCH
2.143 ″ ″ ″ ″ SMe NEt2N
2.144 ″ ″ CO2-i-Pr Me OMe Me N
2.145″″″″OMeOMeCH
2.146 Me ″ CO2-烯丙基 H OMe OMe CH
2.147 Et ″ CO2-Me H OMe OMe CH
2.148″″″HOMeMeN
2.149″″″″MeMeCH
2.150″″″″ClOMeCH
2.151″″″MeOMeOMeCH
2.152″″″″OMeMeN
2.153 ″ ″ CO2-Et H OMe OMe CH
2.154″″″″OMeMeCH
2.155″″″″ClOMeCH
2.156″″″″OMeMeN
2.157″″″MeOMeOMeCH
2.158″″″″″MeN
2.159 ″ ″ CO2-n-Pr H OMe OMe CH
2.160″″″″OMeMeN
2.161″″″″OMeClCH
2.162″″″″MeMeCH
2.163″″″MeOMeOMeCH
2.164″″″″OMeMeN
2.165 ″ ″ CO2-i-Pr H OMe OMe CH
2.166″″″″OMeMeN
2.167″″″″MeMeCH
2.168″″″MeOMeMeN
2.169 n-Pr CS-NH.烯丙基 CO2-Me H OMe OMe CH
2.170″″″″″ClCH
2.171″″″″MeMeCH
2.172″″″″OMeMeN
2.173″″″MeOMeOMeCH
2.174″″″″OMeMeN
2.175 n-Pr ″ CO2-Et H ″ ″ N
No. R1R2R3R4X Y Z Fp.
2.176″″″″″OMeCH
2.177″″″″MeMeCH
2.178 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.179 i-Pr ″ CO2-Me H OMe OMe CH
2.180″″″″OMeMeN
2.181″″″″MeMeCH
2.182″″″″ClOMeN
2.183″″″MeOMeMeN
2.184″″″″″OMeCH
2.185 烯丙基 ″ CO2-Me H OMe OMe CH
2.186″″″″″ClCH
2.187″″″″MeMeCH
2.188″″″″OMeMeN
2.189 ″ ″ CO2-Et H OMe OMe CH
2.190 ″ ″ CO2-n-Pr ″ ″ ″ CH
2.191 ″ ″ CO2-i-Pr ″ ″ ″ CH
2.192 Me CS-NH-CO2Et CO2-Me H OMe OMe CH 144-
145℃
2.193″″″″″OMeN
2.194″″″″″MeN
2.195″″″″″″CH
2.196 ″ ″ ″ ″ NMe2OCH2CF3N
2.197″″″″MeMeCH
2.198″″″″″″N
2.199″″″″ClOMeCH
2.200″″″MeOMeOMeCH
2.201″″″″″MeN
2.202 ″ ″ CO2-Et H OMe OMe CH
2.203″″″″″ClCH
2.204″″″″MeMeCH
2.205″″″″OMeMeN
2.206 ″ ″ ″ ″ NMe2OCH2CF3N
2.207″″″MOMeOMeCH
2.208″″″″OMeMeN
2.209 ″ ″ CO2-n-Pr H OMe OMe CH
2.210″″″″″″N
No. R1R2R3R4X Y Z Fp.
2.211″″″″OMeOMeN
2.212″″″″MeMeCH
2.213″″″″OMeClCH
2.214″″″MeMeOMeN
2.215″″″″OMeOMeCH
2.216 Me CS-NH-CO2Et CO2-i-Pr H OMe OMe CH
2.217″″″″″″N
2.218″″″″OMeMeN
2.219″″″″OMeClCH
2.220″″″″MeMeCH
2.221 ″ ″ ″ ″ SMe NEt2N
2.222 ″ ″ CO2-i-Pr Me OMe Me N
2.223″″″″OMeOMeCH
2.224 Me ″ CO2-烯丙基 H OMe OMe CH
2.225 Et ″ CO2-Me H OMe OMe CH
2.226″″″HOMeMeN
2.227″″″″MeMeCH
2.228″″″″ClOMeCH
2.229″″″MeOMeOMeCH
2.230″″″″OMeMeN
2.231 ″ ″ CO2-Et H OMe OMe CH
2.232″″″″OMeMeCH
2.233″″″″ClOMeCH
2.234″″″″OMeMeN
2.235″″″MeOMeOMeCH
2.236″″″″″MeN
2.237 ″ ″ CO2-n-Pr H OMe OMe CH
2.238″″″″OMeMeN
2.239″″″″OMeClCH
2.240″″″″MeMeCH
2.241″″″MeOMeOMeCH
2.242″″″″OMeMeN
2.243 ″ ″ CO2-i-Pr H OMe OMe CH
2.244″″″″OMeMeN
2.245″″″″MeMeCH
2.246″″″MeOMeMeN
No. R1R2R3R4X Y Z Fp.
2.247 n-Pr CS-NH-CO2Et CO2-Me H OMe OMe CH
2.248″″″″″ClCH
2.249″″″″MeMeCH
2.250″″″″OMeMeN
2.251″″″MeOMeOMeCH
2.252″″″″OMeMeN
2.253 n-Pr ″ CO2-Et H ″ ″ N
2.254″″″″″OMeCH
2.255″″″″MeMeCH
2.256 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.257 i-Pr ″ CO2-Me H OMe OMe CH
2.258″″″″OMeMeN
2.259″″″″MeMeCH
2.260″″″″ClOMeN
2.261″″″MeOMeMeN
2.262″″″″″OMeCH
2.263 烯丙基 ″ CO2-Me H OMe OMe CH
2.264″″″″″ClCH
2.265″″″″MeMeCH
2.266″″″″OMeMeN
2.267 ″ ″ CO2-Et H OMe OMe CH
2.268 ″ ″ CO2-n-Pr H OMe OMe CH
2.269 ″ ″ CO2-i-Pr ″ ″ ″ CH
2.270 Me SO2NHMe CO2-Me H OMe OMe CH117-
118℃
2.271″″″″″OMeN
2.272″″″″″MeN
2.273″″″″″″CH
2.274 ″ ″ ″ ″ NMe2OCH2CF3N
2.275″″″″MeMeCH
2.276″″″″″″N
2.277″″″″ClOMeCH
2.278″″″MeOMeOMeCH
2.279″″″″″MeN
2.280 ″ ″ CO2-Et H OMe OMe CH
2.281″″″″″ClCH
No. R1R2R3R4X Y Z Fp.
2.282″″″″MeMeCH
2.283″″″″OMeMeN
2.284 ″ ″ ″ ″ NMe2OCH2CF3N
2.285″″″MeOMeOMeCH
2.286″″″″OMeMeN
2.287 ″ ″ CO2-n-Pr H OMe OMe CH
2.288″″″″″″N
2.289″″″″OMeMeN
2.290″″″″MeMeCH
2.291″″″″OMeClCH
2.292″″″MeMeOMeN
2.293″″″″OMeOMeCH
2.294 Me SO2-NHMe CO2-i-Pr H OMe OMe CH
2.295″″″″″″N
2.296″″″″OMeMeN
2.297″″″″MeMeCH
2.298″″″″MeMeCH
2.299 ″ ″ ″ ″ SMe NEt2N
2.300 ″ ″ CO2-i-Pr Me OMe Me N
2.301″″″″OMeOMeCH
2.302 Me ″ CO2-烯丙基 H OMe OMe CH
2.303 Et ″ CO2-Me H OMe OMe CH
2.304″″″HOMeMeN
2.305″″″″MeMeCH
2.306″″″″ClOMeCH
2.307″″″MeOMeOMeCH
2.308″″″″OMeMeN
2.309 ″ ″ CO2-Et H OMe OMe CH
2.310″″″″OMeMeCH
2.311″″″″ClOMeCH
2.312″″″″OMeMeN
2.313″″″MeOMeOMeCH
2.314″″″″″MeN
2.315 ″ ″ CO2-n-Pr H OMe OMe CH
2.316″″″″OMeMeN
2.317″″″″OMeClCH
No. R1R2R3R4X Y Z Fp.
2.318″″″″MeMeCH
2.319″″″MeOMeOMeCH
2.320″″″″OMeMeN
2.321 ″ ″ CO2-i-Pr H OMe OMe CH
2.322″″″″OMeMeN
2.323″″″″MeMeCH
2.324″″″MeOMeMeN
2.325 n-Pr SO2NHMe CO2-Me H OMe OMe CH
2.326″″″″″ClCH
2.327″″″″MeMeCH
2.328″″″″OMeMeN
2.329″″″MeOMeOMeCH
2.330″″″″OMeMeN
2.331 n-Pr ″ CO2-Et H ″ ″ N
2.332″″″″″OMeCH
2.333″″″″MeMeCH
2.334 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.335 i-Pr ″ CO2-Me H OMe OMe CH
2.336″″″″OMeMeN
2.337″″″″MeMeCH
2.338″″″″ClOMeN
2.339″″″MeOMeMeN
2.340″″″″″OMeCH
2.341 烯丙基 ″ CO2-Me H OMe OMe CH
2.342″″″″″ClCH
2.343″″″″MeMeCH
2.344″″″″OMeMeN
2.345 ″ ″ CO2-Et H OMe OMe CH
2.346 ″ ″ CO2-n-Pr H OMe OMe CH
2.347 ″ ″ CO2-i-Pr ″ ″ ″ CH
2.348 Me SO2NMe2CO2-Me H OMe OMe CH
2.349″″″″″OMeN
2.350″″″″″MeN
2.351″″″″″″CH
2.352 ″ ″ ″ ″ NMe2OCH2CF3N
2.353″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
2.354″″″″″″N
2.355″″″″ClOMeCH
2.356″″″MeOMeOMeCH
2.357″″″″″MeN
2.358 ″ ″ CO2-Et H OMe OMe CH
2.359″″″″″ClCH
2.360″″″″MeMeCH
2.361″″″″OMeMeN
2.362 ″ ″ ″ ″ NMe2OCH2CF3N
2.363″″″MeOMeOMeCH
2.364″″″″OMeMeN
2.365 ″ ″ CO2-n-Pr H OMe OMe CH
2.366″″″″″″N
2.367″″″″OMeMeN
2.368″″″″MeMeCH
2.369″″″″OMeClCH
2.370″″″MeMeOMeN
2.371″″″″OMeOMeCH
2.372 Me SO2NMe2CO2-i-Pr H OMe OMe CH
2.373″″″″″″N
2.374″″″″OMeMeN
2.375″″″″OMeClCH
2.376″″″″MeMeCH
2.377 ″ ″ ″ ″ SMe NEt2N
2.378 ″ ″ CO2-i-Pr Me OMe Me N
2.379″″″″OMeOMeCH
2.380 Me ″ CO2-烯丙基 H OMe OMe CH
2.381 Et ″ CO2-Me H OMe OMe CH
2.382″″″HOMeMeN
2.383″″″″MeMeCH
2.384″″″″ClOMeCH
2.385″″″MeOMeOMeCH
2.386″″″″OMeMeN
2.387 ″ ″ CO2-Et H OMe OMe CH
2.388″″″″OMeMeCH
2.389″″″″ClOMeCH
No. R1R2R3R4X Y Z Fp.
2.390″″″″OMeMeN
2.391″″″MeOMeOMeCH
2.392″″″″″MeN
2.393 ″ ″ CO2-n-Pr H OMe OMe CH
2.394″″″″OMeMeN
2.395″″″″OMeClCH
2.396″″″″MeMeCH
2.397″″″MeOMeOMeCH
2.398″″″″OMeMeN
2.399 ″ ″ CO2-i-Pr H OMe OMe CH
2.400″″″″OMeMeN
2.401″″″″MeMeCH
2.402″″″MeOMeMeN
2.403 n-Pr SO2-NMe2CO2-Me H OMe OMe CH
2.404″″″″″ClCH
2.405″″″″MeMeCH
2.406″″″″OMeMeN
2.407″″″MeOMeOMeCH
2.408″″″″OMeMeN
2.409 n-Pr ″ CO2-Et H OMe Me N
2.410″″″″″OMeCH
2.411″″″″MeMeCH
2.412 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.413 i-Pr ″ CO2-Me H OMe OMe CH
2.414″″″″OMeMeN
2.415″″″″MeMeCH
2.416″″″″ClOMeN
2.417″″″MeOMeMeN
2.418″″″″″OMeCH
2.419 烯丙基 ″ CO2-Me H OMe OMe CH
2.420″″″″″ClCH
2.421″″″″MeMeCH
2.422″″″″OMeMeN
2.423 ″ ″ CO2-Et H OMe OMe CH
2.424 ″ ″ CO2-n-Pr H OMe OMe CH
2.425 ″ ″ CO2-i-Pr ″ ″ ″ CH
No. R1R2R3R4X Y Z Fp.
2.426 Me CHO
H OMe OMe CH
2.427"""HOMeMeN
2.428""""MeMeCH
2.429 " CO-CH3" " OMe OMe CH
2.430""""OMeMeN
2.431""""MeMeCH
2.432 " COCH2CH3" " OMe OMe CH
2.433EtCHO""""CH
2.434Pr"""""CH
2.435 Et COCH3" " " " CH
2.436Pr"""""CH
2.437 Et COCH2CH3" " " " CH
2.438 Me
" " " " CH
2.439 Me CO2Me " " " " CH
2.440Et"""""CH
2.441Pr"""""CH
2.442MeCO-NHEt""""CH
2.443Et"""""CH
2.444Pr"""""CH
2.445 Me CHO
H OMe OMe CH
2.446"""HOMeMeN
2.447""""MeMeCH
2.448 " CO-CH3" " OMe OMe CH
2.449""""OMeMeN
2.450""""MeMeCH
2.451 " COCH2CH3" " OMe OMe CH
2.452EtCHO""""CH
2.453Pr"""""CH
2.454 Et COCH3" " " " CH
2.455Pr"""""CH
2.456 Et COCH2CH3" " " " CH
No. R1R2R3R4X Y Z Fp.
2.457 Me
" " " " CH
2.458 Me CO2Me " " " " CH
2.459Et"""""CH
2.460Pr"""""CH
2.461MeCO-NHEt""""CH
2.462Et"""""CH
2.463Pr"""""CH
2.464 Me CHO CO2-N=CHMe2H OMe OMe CH
2.465"""HOMeMeN
2.466""""MeMeCH
2.467 " CO-CH3" " OMe OMe CH
2.468""""OMeMeN
2.469""""MeMeCH
2.470 " COCH2CH3" " OMe OMe CH
2.471EtCHO""""CH
2.472Pr"""""CH
2.473 Et COCH3" " " " CH
2.474Pr"""""CH
2.475 Et COCH2CH3" " " " CH
2.476 Me
" " " " CH
2.477 Me CO2Me " " " " CH
2.478Et"""""CH
2.479Pr"""""CH
2.480MeCO-NHEt""""CH
2.481Et"""""CH
2.482Pr"""""CH
2.483 Me CHO CO2CH2CH2Cl H OMe OMe CH
2.484""""OMeMeN
2.485""""MeMeCH
2.486 " CO-CH3" " OMe OMe CH
2.487""""OMeMeN
2.488""""MeMeCH
2.489 " COCH2CH3" " OMe OMe CH
No. R1R2R3R4X Y Z Fp.
2.490EtCHO"""""
2.491Pr""""""
2.492 Et COCH3" " " " "
2.493Pr""""""
2.494 Et COCH2CH3" " " " "
2.495 Me
" " " " "
2.496 Me CO2Me " " " " "
2.497Et""""""
2.498Pr""""""
2.499MeCO-NHEt"""""
2.500Et""""""
2.501Pr""""""
2.502 Me CHO CO2(CH2)2OMe H OMe OMe CH
2.503"""HOMeMeN
2.504""""MeMeCH
2.505 " CO-CH3" " OMe OMe CH
2.506""""OMeMeN
2.507""""MeMeCH
2.508 " COCH2CH3" " OMe OMe CH
2.509EtCHO"""""
2.510Pr""""""
2.511 Et COCH3" " " " "
2.512Pr""""""
2.513 Et COCH2CH3" " " " "
2.514 Me
" " " " "
2.515 Me CO2Me " " " " "
2.516Et""""""
2.517Pr""""""
2.518MeCO-NHEt"""""
2.519Et""""""
2.520Pr""""""
2.521 Me CHO CO2CH2CCl3H OMe OMe CH
2.522"""HOMeMeN
No. R1R2R3R4X Y Z Fp.
2.523""""MeMeCH
2.524 " CO-CH3" " OMe OMe CH
2.525""""OMeMeN
2.526""""MeMeCH
2.527 " COCH2CH3" " OMe OMe CH
2.528EtCHO"""""
2.529Pr""""""
2.530 Et COCH3" " " " "
2.531Pr""""""
2.532 Et COCH2CH3" " " " "
2.533 Me
" " " " "
2.534 Me CO2Me " " " " "
2.535Et""""""
2.536Pr""""""
2.537MeCO-NHEt"""""
2.538Et""""""
2.539Pr""""""
2.540 Me CHO CO2CH2C≡CH H OMe OMe CH
2.541"""HOMeMeN
2.542""""MeMeCH
2.543 " CO-CH3" " OMe OMe CH
2.544""""OMeMeN
2.545""""MeMeCH
2.546 " COCH2CH3" " OMe OMe CH
2.547EtCHO"""""
2.548Pr""""""
2.549 Et COCH3" " " " "
2.550Pr""""""
2.551 Et COCH2CH3" " " " "
2.552 Me
" " " " "
2.553 Me CO2Me " " " " "
2.554Et""""""
2.555Pr""""""
2.556MeCO-NHEt"""""
No. R1R2R3R4X Y Z Fp.
2.557Et″″″″″″
2.558Pr″″″″″″
2.559 Me SO2Et CO2Me H OMe OMe CH
2.560″″″″″OMeN
2.561″″″″″MeN
2.562″″″″″″CH
2.563 ″ ″ ″ ″ NMe2OCH2CF3N
2.564″″″″MeMeCH
2.565″″″″″″N
2.566″″″″ClOMeCH
2.567″″″MeOMeOMeCH
2.568″″″″″MeN
2.569 ″ ″ CO2Et H OMe OMe CH
2.570″″″″″ClCH
2.571″″″″MeMeCH
2.572″″″″OMeMeN
2.573 ″ ″ ″ ″ NMe2OCH2CF3N
2.574″″″MeOMeOMeCH
2.575″″″″OMeMeN
2.576 ″ ″ CO2-n-Pr H OMe OMe CH
2.577″″″″″″N
2.578″″″″OMeMeN
2.579″″″″MeMeCH
2.580″″″″OMeClCH
2.581″″″MeMeOMeN
2.582″″″″OMeOMeCH
2.583 Me SO2Et CO2-i-Pr H OMe OMe CH
2.584″″″″″″N
2.585″″″″OMeMeN
2.586″″″″OMeClCH
2.587″″″″MeMeCH
2.588 ″ ″ ″ ″ SMe NEt2N
2.589 ″ ″ CO2-i-Pr Me OMe Me N
2.590″″″″OMeOMeCH
2.591 Me ″ CO2-烯丙基 H OMe OMe CH
2.592 Et ″ CO2Me H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
2.593″″″HOMeMeN
2.594″″″″MeMeCH
2.595″″″″ClOMeCH
2.596″″″MeOMeOMeCH
2.597″″″″OMeMeN
2.598 ″ ″ CO2Et H OMe OMe CH
2.599″″″″OMeMeCH
2.600″″″″ClOMeCH
2.601″″″″OMeMeN
2.602″″″MeOMeOMeCH
2.603″″″″″MeN
2.604 ″ ″ CO2-n-Pr H OMe OMe CH
2.605″″″″OMeMeN
2.606″″″″OMeClCH
2.607″″″″MeMeCH
2.608″″″MeOMeOMeCH
2.609″″″″OMeMeN
2.610 ″ ″ CO2-i-Pr H OMe OMe CH
2.611″″″″OMeMeN
2.612″″″″MeMeCH
2.613″″″MeOMeMeN
2.614 n-Pr SO2Et CO2Me H OMe OMe CH
2.615″″″″″ClCH
2.616″″″″MeMeCH
2.617″″″″OMeMeN
2.618″″″MeOMeOMeCH
2.619″″″″OMeMeN
2.620 n-Pr ″ CO2Et H ″ ″ N
2.621″″″″″OMeCH
2.622″″″″MeMeCH
2.623 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.624 i-Pr ″ CO2Me H ″ ″ CH
2.625″″″″″MeN
2.626″″″″MeMeCH
2.627″″″″ClOMeN
2.628″″″MeOMeMeN
No. R1R2R3R4X Y Z Fp.
2.629″″″″″OMeCH
2.630 烯丙基 ″ CO2Me H OMe OMe CH
2.631″″″″″ClCH
2.632″″″″MeMeCH
2.633″″″″OMeMeN
2.634 ″ ″ CO2-Et H OMe OMe CH
2.635 ″ ″ CO2-n-Pr H OMe OMe CH
2.636 ″ ″ CO2-i-Pr ″ ″ ″ CH
2.637 Me SO2CH2Cl CO2-Me H OMe OMe CH
2.638″″″″″OMeN
2.639″″″″″MeN
2.640″″″″″″CH
2.641 ″ ″ ″ ″ NMe2OCH2CF3N
2.642″″″″MeMeCH
2.643″″″″″″N
2.644″″″″ClOMeCH
2.645″″″MeOMeOMeCH
2.646″″″″″MeN
2.647 ″ ″ CO2-Et H OMe OMe CH
2.648″″″″″ClCH
2.649″″″″MeMeCH
2.650″″″″OMeMeN
2.651 ″ ″ ″ ″ NMe2OCH2CF3N
2.652″″″MeOMeOMeCH
2.653″″″″OMeMeN
2.654 ″ ″ CO2-n-Pr H OMe OMe CH
2.655″″″″″″N
2.656″″″″OMeMeN
2.657″″″″MeMeCH
2.658″″″″OMeClCH
2.659″″″MeMeOMeN
2.660″″″″OMeOMeCH
2.661 Me SO2CH2Cl CO2-i-Pr H OMe OMe CH
2.662″″″″″″N
2.663″″″″OMeMeN
2.664″″″″OMeClCH
No. R1R2R3R4X Y Z Fp.
2.665″″″″MeMeCH
2.666 ″ ″ ″ ″ SMe NEt2N
2.667 ″ ″ CO2-i-Pr Me OMe Me N
2.668″″″″OMeOMeCH
2.669 Me ″ CO2-烯丙基 H OMe OMe CH
2.670 Et ″ CO2-Me H OMe OMe CH
2.671″″″HOMeMeN
2.672″″″″MeMeCH
2.673″″″″ClOMeCH
2.674″″″MeOMeOMeCH
2.675″″″″OMeMeN
2.676 ″ ″ CO2-Et H OMe OMe CH
2.677″″″″OMeMeCH
2.678″″″″ClOMeCH
2.679″″″″OMeMeN
2.680″″″MeOMeOMeCH
2.681″″″″″MeN
2.682 ″ ″ CO2-n-Pr H OMe OMe CH
2.683″″″″OMeMeN
2.684″″″″OMeClCH
2.685″″″″MeMeCH
2.686″″″MeOMeOMeCH
2.687″″″″″MeN
2.688 ″ ″ CO2i-Pr H OMe OMe CH
2.689″″″″OMeMeN
2.690″″″″MeMeCH
2.691″″″MeOMeMeN
2.692 n-Pr SO2CH2Cl CO2-Me H OMe OMe CH
2.693″″″″″ClCH
2.694″″″″MeMeCH
2.695″″″″OMeMeN
2.696″″″MeOMeOMeCH
2.697″″″″″MeN
2.698 n-Pr ″ CO2-Et H ″ ″ N
2.699″″″″″OMeCH
2.700″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
2.701 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.702 i-Pr ″ CO2-Me H OMe OMe CH
2.703″″″″OMeMeN
2.704″″″″MeMeCH
2.705″″″″ClOMeN
2.706″″″MeOMeMeN
2.707″″″″″OMeCH
2.708 烯丙基 ″ CO2-Me H OMe OMe CH
2.709″″″″″ClCH
2.710″″″″MeMeCH
2.711″″″″OMeMeN
2.712 ″ ″ CO2-Et H OMe OMe CH
2.713 ″ ″ CO2-n-Pr ″ ″ ″ CH
2.714 ″ ″ CO2-i-Pr ″ ″ ″ CH
2.715 Me SO2CH3CO2-Me H OMe OMe CH 119℃
2.716″″″″″OMeN
2.717″″″″″MeN
2.718″″″″″″CH
2.719 ″ ″ ″ ″ NMe2OCH2CF3N
2.720″″″″MeMeCH
2.721″″″″″″N
2.722″″″″ClOMeCH
2.723″″″MeOMeOMeCH
2.724″″″″″MeN
2.725 ″ ″ CO2-Et H OMe OMe CH
2.726″″″″″ClCH
2.727″″″″MeMeCH
2.728″″″″OMeMeN
2.729 ″ ″ ″ ″ NMe2OCH2CF3N
2.730″″″MeOMeOMeCH
2.731″″″″OMeMeN
2.732 ″ ″ CO2-n-Pr H OMe OMe CH
2.733″″″″″″N
2.734″″″″OMeMeN
2.735″″″″MeMeCH
2.736″″″″OMeClCH
No. R1R2R3R4X Y Z Fp.
2.737″″″MeMeOMeN
2.738″″″″OMeOMeCH
2.739 Me SO2Me CO2-i-Pr H OMe OMe CH
2.740″″″″″″N
2.741″″″″OMeMeN
2.742″″″″OMeClCH
2.743″″″″MeMeCH
2.744 ″ ″ ″ ″ SMe NEt2N
2.745 ″ ″ CO2-i-Pr Me OMe Me N
2.746″″″″OMeOMeCH
2.747 Me ″ CO2-烯丙基 H OMe OMe CH
2.748 Et ″ CO2-Me H OMe OMe CH
2.749″″″HOMeMeN
2.750″″″″MeMeCH
2.751″″″″ClOMeCH
2.752″″″MeOMeOMeCH
2.753″″″″OMeMeN
2.754 ″ ″ CO2-Et H OMe OMe CH
2.755″″″″OMeMeCH
2.756″″″″ClOMeCH
2.757″″″″OMeMeN
2.758″″″MeOMeOMeCH
2.759″″″″″MeN
2.760 ″ ″ CO2-n-Pr H OMe OMe CH
2.761″″″″OMeMeN
2.762″″″″OMeClCH
2.763″″″″MeMeCH
2.764″″″MeOMeOMeCH
2.765″″″″OMeMeN
2.766 ″ ″ CO2-i-Pr H OMe OMe CH
2.767″″″″OMeMeN
2.768″″″″MeMeCH
2.769″″″MeOMeMeN
2.770 n-Pr SO2Me CO2-Me H OMe OMe CH
2.771″″″″″ClCH
2.772″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
2.773″″″″OMeMeN
2.774″″″MeOMeOMeCH
2.775″″″″OMeMeN
2.776 n-Pr ″ CO2-Et H ″ ″ N
2.777″″″″″OMeCH
2.778″″″″MeMeCH
2.779 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.780 i-Pr ″ CO2-Me H OMe OMe CH
2.781″″″″OMeMeN
2.782″″″″MeMeCH
2.783″″″″ClOMeN
2.784″″″MeOMeMeN
2.785″″″″″OMeCH
2.786 烯丙基 ″ CO2-Me H OMe OMe CH
2.787″″″″″ClCH
2.788 烯丙基 ″ CO2-Me H OMe OMe CH
2.789″″″″″ClCH
2.790″″″″MeMeCH
2.791″″″″OMeMeN
2.792 ″ ″ CO2-Et H OMe OMe CH
2.793 ″ ″ CO2-n-Pr ″ ″ ″ CH
2.794 ″ ″ CO2-i-Pr ″ ″ ″ CH
2.795 Me CONH- CO2-Me H OMe OMe CH
CH2CH2Cl
2.796″″″″″OMeN
2.797″″″″″MeN
2.798″″″″″″CH
2.799 ″ ″ ″ ″ NMe2OCH2CF3N
2.800″″″″MeMeCH
2.801″″″″″″N
2.802″″″″ClOMeCH
2.803″″″MeOMeOMeCH
2.804″″″″″MeN
2.805 ″ ″ CO2-Et H OMe OMe CH
2.806″″″″″ClCH
2.807″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
2.808″″″″OMeMeN
2.809 ″ ″ ″ ″ NMe2OCH2CF3N
2.810″″″MeOMeOMeCH
2.811″″″″OMeMeN
2.812 ″ ″ CO2-n-Pr H OMe OMe CH
2.813″″″″″″N
2.814″″″″OMeMeN
2.815″″″″MeMeCH
2.816″″″″OMeClCH
2.817″″″MeMeOMeN
2.818″″″″OMeOMeCH
2.819 Me CO- CO2-i-Pr H OMe OMe CH
NHCH2CH2Cl
2.820″″″″″″N
2.821″″″″OMeMeN
2.822″″″″OMeClCH
2.823″″″″MeMeCH
2.824 ″ ″ ″ ″ SMe NEt2N
2.825 ″ ″ CO2-i-Pr Me OMe Me N
2.826″″″″OMeOMeCH
2.827 Me ″ CO2-烯丙基 H OMe OMe CH
2.828 Et ″ CO2-Me H OMe OMe CH
2.829″″″HOMeMeN
2.830″″″″MeMeCH
2.831″″″″ClOMeCH
2.832″″″MeOMeOMeCH
2.833″″″″OMeMeN
2.834 ″ ″ CO2-Et H OMe OMe CH
2.835″″″″OMeMeCH
2.836″″″″ClOMeCH
2.837″″″″OMeMeN
2.838″″″MeOMeOMeCH
2.839″″″″″MeN
2.840 ″ ″ CO2-n-Pr H OMe OMe CH
2.841″″″HOMeMeN
2.842″″″″OMeClCH
No. R1R2R3R4X Y Z Fp.
2.843″″″″MeMeCH
2.844″″″MeOMeOMeCH
2.845″″″″OMeMeN
2.846 ″ ″ CO2-i-Pr H OMe OMe CH
2.847″″″HOMeMeN
2.848″″″″MeMeCH
2.849″″″MeOMeMeN
2.850 n-Pr CO-NH- CO2-Me H OMe OMe CH
CH2CH2Cl
2.851″″″″″ClCH
2.852″″″″MeMeCH
2.853″″″″OMeMeN
2.854″″″MeOMeOMeCH
2.855″″″″OMeMeN
2.856 n-Pr ″ CO2-Et H ″ ″ N
2.857″″″″″OMeCH
2.858″″″″MeMeCH
2.859 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.860 i-Pr ″ CO2-Me H OMe OMe CH
2.861″″″″OMeMeN
2.862″″″″MeMeCH
2.863″″″″ClOMeN
2.864″″″MeOMeMeN
2.865″″″″″OMeCH
2.866 烯丙基 ″ CO2-Me H OMe OMe CH
2.867″″″″″ClCH
2.868″″″″MeMeCH
2.869″″″″OMeMeN
2.870 ″ ″ CO2-Et H OMe OMe CH
2.871 ″ ″ CO2-n-Pr ″ ″ ″ CH
2.872 ″ ″ CO2-i-Pr ″ ″ ″ CH
2.873 Me CO-OCH2-CCl3CO2-Me H OMe OMe CH
2.874″″″″″OMeN
2.875″″″″″MeN
2.876″″″″″″CH
2.877 ″ ″ ″ ″ NMe2OCH2CF3N
No. R1R2R3R4X Y Z Fp.
2.878″″″″MeMeCH
2.879″″″″″″N
2.880″″″″ClOMeCH
2.881″″″MeOMeOMeCH
2.882″″″″″MeN
2.883 ″ ″ CO2-Et H OMe OMe CH
2.884″″″″″ClCH
2.885″″″″MeMeCH
2.886″″″″OMeMeN
2.887 ″ ″ ″ ″ NMe2OCH2CF3N
2.888″″″MeOMeOMeCH
2.889″″″″OMeMeN
2.890 ″ ″ CO2-n-Pr H OMe OMe CH
2.891″″″″″″N
2.892″″″″OMeMeN
2.893″″″″MeMeCH
2.894″″″″OMeClCH
2.895″″″MeMeOMeN
2.896″″″″OMeOMeCH
2.897 Me CO-OCH2CCl3CO2-i-Pr H OMe OMe CH
2.898″″″″″″N
2.899″″″″OMeMeN
2.900″″″″OMeClCH
2.901″″″″MeMeCH
2.902 ″ ″ ″ ″ SMe NEt2N
2.903 ″ ″ CO2-i-Pr Me OMe Me N
2.904″″″″OMeOMeCH
2.905 Me ″ CO2-烯丙基 H OMe OMe CH
2.906 Et ″ CO2-Me H OMe OMe CH
2.907″″″HOMeMeN
2.908″″″″MeMeCH
2.909″″″″ClOMeCH
2.910″″″MeOMeOMeCH
2.911″″″″OMeMeN
2.912 ″ ″ CO2-Et H OMe OMe CH
2.913″″″″OMeMeCH
No. R1R2R3R4X Y Z Fp.
2.914″″″″ClOMeCH
2.915″″″″OMeMeN
2.916″″″MeOMeOMeCH
2.917″″″″″MeN
2.918 ″ ″ CO2-n-Pr H OMe OMe CH
2.919″″″″OMeMeN
2.920″″″″OMeClCH
2.921″″″″MeMeCH
2.922″″″MeOMeOMeCH
2.923″″″″OMeMeN
2.924 ″ ″ CO2-i-Pr H OMe OMe CH
2.925″″″″OMeMeN
2.926″″″″MeMeCH
2.927″″″MeOMeMeN
2.928 n-Pr CO-OCH2CCl3CO2-Me H OMe OMe CH
2.929″″″″″ClCH
2.930″″″″MeMeCH
2.931″″″″OMeMeN
2.932″″″MeOMeOMeCH
2.933″″″″OMeMeN
2.934 n-Pr ″ CO2-Et H OMe Me N
2.935″″″″″OMeCH
2.936″″″″MeMeCH
2.937 ″ ″ CO2-n-Pr ″ OMe OMe CH
2.938 i-Pr ″ CO2-Me H OMe OMe CH
2.939″″″″OMeMeN
2.940″″″″MeMeCH
2.941″″″″ClOMeN
2.942″″″MeOMeMeN
2.943″″″″″OMeCH
2.944 烯丙基 ″ CO2-Me H OMe OMe CH
2.945″″″″″ClCH
2.946″″″″MeMeCH
2.947″″″″OMeMeN
2.948 ″ ″ CO2-Et H OMe OMe CH
2.949 ″ ″ CO2-n-Pr H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
2.950 ″ ″ CO2-i-Pr ″ ″ ″ CH
2.951 Me COCH2Br CO2-Me H OMe OMe CH
2.952″″″″″OMeN
2.953″″″″″MeN
2.954″″″″″″CH
2.955 ″ ″ ″ ″ NMe2OCH2CF3N
2.956″″″″MeMeCH
2.957″″″″″″N
2.958″″″″ClOMeCH
2.959″″″MeOMeOMeCH
2.960″″″″″MeN
2.961 ″ ″ CO2-Et H OMe OMe CH
2.962″″″″″ClCH
2.963″″″″MeMeCH
2.964″″″″OMeMeN
2.965 ″ ″ ″ ″ NMe2OCH2CF3N
2.966″″″MeOMeOMeCH
2.967″″″″OMeMeN
2.968 ″ ″ CO2-n-Pr H OMe OMe CH
2.969″″″″″″N
2.970″″″″OMeMeN
2.971″″″″MeMeCH
2.972″″″″OMeClCH
2.973″″″MeMeOMeN
2.974″″″″OMeOMeCH
2.975 Me COCH2Br CO2-i-Pr H OMe OMe CH
2.976″″″″″″N
2.977″″″″HMeN
2.978″″″″OMeClCH
2.979″″″″MeMeCH
2.980 ″ ″ ″ ″ SMe NEt2N
2.981 ″ ″ CO2-i-Pr Me OMe Me N
2.982″″″″OMeOMeCH
2.983 Me ″ CO2-烯丙基 H OMe OMe CH
2.984 Et ″ CO2-Me H OMe OMe CH
2.985″″″HOMeMeN
No. R1R2R3R4X Y Z Fp.
2.986″″″″MeMeCH
2.987″″″″ClOMeCH
2.988″″″MeOMeOMeCH
2.989″″″″OMeMeN
2.990 ″ ″ CO2-Et H OMe OMe CH
2.991″″″″OMeMeCH
2.992″″″″ClOMeCH
2.993″″″″OMeMeN
2.994″″″MeOMeOMeCH
2.995″″″″″MeN
2.996 ″ ″ CO2-n-Pr H OMe OMe CH
2.997″″″″OMeMeN
2.998″″″″OMeClCH
2.999″″″″MeMeCH
3.000″″″MeOMeOMeCH
3.001″″″″OMeMeN
3.002 ″ ″ CO2-i-Pr H OMe OMe CH
3.003″″″″OMeMeN
3.004″″″″MeMeCH
3.005″″″MeOMeMeN
3.006 n-Pr COCH2Br CO2-Me H OMe OMe CH
3.007″″″″″ClCH
3.008″″″″MeMeCH
3.009″″″″OMeMeN
3.010″″″MeOMeOMeCH
3.011″″″″OMeMeN
3.012 n-Pr ″ CO2-Et H ″ ″ N
3.013″″″″″OMeCH
3.014″″″″MeMeCH
3.015 ″ ″ CO2-n-Pr ″ OMe OMe CH
3.016 i-Pr ″ CO2-Me H OMe OMe CH
3.017″″″″OMeMeN
3.018″″″″MeMeCH
3.019″″″″ClOMeN
3.020″″″MeOMeMeN
3.021″″″″″OMeCH
No. R1R2R3R4X Y Z Fp.
3.022 烯丙基 ″ CO2-Me H OMe OMe CH
3.023″″″″″ClCH
3.024″″″″MeMeCH
3.025″″″″OMeMeN
3.026 ″ ″ CO2-Et H OMe OMe CH
3.027 ″ ″ CO2-n-Pr ″ ″ ″ CH
3.028 ″ ″ CO2-i-Pr ″ ″ ″ CH
3.029 Me COCCl3CO2-Me H OMe OMe CH
3.030″″″″″OMeN
3.031″″″″″MeN
3.032″″″″″″CH
3.033 ″ ″ ″ ″ NMe2OCH2CF3N
3.034″″″″MeMeCH
3.035″″″″″″N
3.036″″″″ClOMeCH
3.037″″″MeOMeOMeCH
3.038″″″″″MeN
3.039 ″ ″ CO2-Et H OMe OMe CH
3.040″″″″″ClCH
3.041″″″″MeMeCH
3.042″″″″OMeMeN
3.043 ″ ″ ″ ″ NMe2OCH2CF3N
3.044″″″MeOMeOMeCH
3.045″″″″OMeMeN
3.046 ″ ″ CO2-n-Pr H OMe OMe CH
3.047″″″″″″N
3.048″″″″OMeMeN
3.049″″″″MeMeCH
3.050″″″″OMeClCH
3.051″″″MeMeOMeN
3.052″″″″OMeOMeCH
3.053 Me COCCl3CO2-i-Pr H OMe OMe CH
3.054″″″″″″N
3.055″″″″OMeMeN
3.056″″″″OMeClCH
3.057″″″″MeMeCH
No. R1R2R3R4X Y Z Fp.
3.058 ″ ″ ″ ″ SMe NEt2N
3.059 ″ ″ CO2-i-Pr Me OMe Me N
3.060″″″″OMeOMeCH
3.061 Me ″ CO2-烯丙基 H OMe OMe CH
3.062 Et ″ CO2-Me H OMe OMe CH
3.063″″″HOMeMeN
3.064″″″″MeMeCH
3.065″″″″ClOMeCH
3.066″″″MeOMeOMeCH
3.067″″″″OMeMeN
3.068 ″ ″ CO2-Et H OMe OMe CH
3.069″″″″OMeMeCH
3.070″″″″ClOMeCH
3.071″″″″OMeMeN
3.072″″″MeOMeOMeCH
3.073″″″″″MeN
3.074 ″ ″ CO2-n-Pr H OMe OMe CH
3.075″″″″OMeMeN
3.076″″″″OMeClCH
3.077″″″″MeMeCH
3.078″″″MeOMeOMeCH
3.079″″″″OMeMeN
3.080 ″ ″ CO2-i-Pr H OMe OMe CH
3.081″″″″OMeMeN
3.082″″″″MeMeCH
3.083″″″MeOMeMeN
3.084 n-Pr COCCl3CO2-Me H OMe OMe CH
3.085″″″″″ClCH
3.086″″″″MeMeCH
3.087″″″″OMeMeN
3.088″″″MeOMeOMeCH
3.089″″″″OMeMeN
3.090 n-Pr ″ CO2-Et H ″ ″ N
3.091″″″″″OMeCH
3.092″″″″MeMeCH
3.093 ″ ″ CO2-n-Pr ″ OMe OMe CH
No. R1R2R3R4X Y Z Fp.
3.094 i-Pr ″ CO2-Me H OMe OMe CH
3.095″″″″OMeMeN
3.096″″″″MeMeCH
3.097″″″″ClOMeN
3.098″″″MeOMeMeN
3.099″″″″″OMeCH
3.100 烯丙基 ″ CO2-Me H OMe OMe CH
3.101″″″″″ClCH
3.102″″″″MeMeCH
3.103″″″″OMeMeN
3.104 ″ ″ CO2-Et H OMe OMe CH
3.105 ″ ″ CO2-n-Pr ″ ″ ″ CH
3.106 ″ ″ CO2-i-Pr ″ ″ ″ CH
3.107 Me COCHCl2CO2-Me H OMe OMe CH
3.108″″″″″OMeN
3.109″″″″″MeN
3.110″″″″″″CH
3.111 ″ ″ ″ ″ NMe2OCH2CF3N
3.112″″″″MeMeCH
3.113″″″″″″N
3.114″″″″ClOMeCH
3.115″″″MeOMeOMeCH
3.116″″″″″MeN
3.117 ″ ″ CO2-Et H OMe OMe CH
3.118″″″″″ClCH
3.119″″″″MeMeCH
3.120″″″″OMeMeN
3.121 ″ ″ ″ ″ NMe2OCH2CF3N
3.122″″″MeOMeOMeCH
3.123″″″″OMeMeN
3.124 ″ ″ CO2-n-Pr H OMe OMe CH
3.125″″″″″″N
3.126″″″″OMeMeN
3.127″″″″MeMeCH
3.128″″″″OMeClCH
3.129″″″MeMeOMeN
No. R1R2R3R4X Y Z Fp.
3.130″″″″OMeOMeCH
3.131 Me COCHCl2CO2-i-Pr H OMe OMe CH
3.132″″″″″″N
3.133″″″″OMeMeN
3.134″″″″OMeClCH
3.135″″″″MeMeCH
3.136 ″ ″ ″ ″ SMe NEt2N
3.137 ″ ″ CO2-i-Pr Me OMe Me N
3.138″″″″OMeOMeCH
3.139 Me ″ CO2-烯丙基 H OMe OMe CH
3.140 Et ″ CO2-Me H OMe OMe CH
3.141″″″HOMeMeN
3.142″″″″MeMeCH
3.143″″″″ClOMeCH
3.144″″″MeOMeOMeCH
3.145″″″″OMeMeN
3.146 ″ ″ CO2-Et H OMe OMe CH
3.147″″″″OMeMeCH
3.148″″″″ClOMeCH
3.149″″″″OMeMeN
3.150″″″MeOMeOMeCH
3.151″″″″″MeN
3.152 ″ ″ CO2-n-Pr H OMe OMe CH
3.153″″″″OMeMeN
3.154″″″″OMeClCH
3.155″″″″MeMeCH
3.156″″″MeOMeOMeCH
3.157″″″″OMeMeN
3.158 ″ ″ CO2-i-Pr H OMe OMe CH
3.159″″″″OMeMeN
3.160″″″″MeMeCH
3.161″″″MeOMeMeN
3.162 n-Pr COCHCl2CO2-Me H OMe OMe CH
3.163″″″″″ClCH
3.164″″″″MeMeCH
3.165″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
3.166″″″MeOMeOMeCH
3.167″″″″OMeMeN
3.168 n-Pr ″ CO2-Et H ″ ″ N
3.169″″″″″OMeCH
3.170″″″″MeMeCH
3.171 ″ ″ CO2-n-Pr ″ OMe OMe CH
3.172 i-Pr ″ CO2-Me H OMe OMe CH
3.173″″″″OMeMeN
3.174″″″″MeMeCH
3.175″″″″ClOMeN
3.176″″″MeOMeMeN
3.177″″″″″OMeCH
3.178 烯丙基 ″ CO2-Me H OMe OMe CH
3.179″″″″″ClCH
3.180″″″″MeMeCH
3.181″″″″OMeMeN
3.182 ″ ″ CO2-Et H OMe OMe CH
3.183 ″ ″ CO2-n-Pr ″ ″ ″ CH
3.184 ″ ″ CO2-i-Pr ″ ″ ″ CH
3.185 Me COCH2Cl CO2-Me H OMe OMe CH
3.186″″″″″OMeN
3.187″″″″″MeN
3.188″″″″″″CH
3.189 ″ ″ ″ ″ NMe2OCH2CF3N
3.190″″″″MeMeCH
3.191″″″″″″N
3.192″″″″ClOMeCH
3.193″″″MeOMeOMeCH
3.194″″″″″MeN
3.195 ″ ″ CO2-Et H OMe OMe CH
3.196″″″″″ClCH
3.197″″″″MeMeCH
3.198″″″″OMeMeN
3.199 ″ ″ ″ ″ NMe2OCH2CF3N
3.200″″″MeOMeOMeCh
3.201″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
3.202 ″ ″ CO2-n-Pr H OMe OMe CH
3.203″″″″″″N
3.204″″″″OMeMeN
3.205″″″″MeMeCH
3.206″″″″OMeClCH
3.207″″″MeMeOMeN
3.208″″″″OMeOMeCH
3.209 Me COCH2Cl CO2-i-Pr H OMe OMe CH
3.210″″″″″″N
3.211″″″″OMeMeN
3.212″″″″OMeClCH
3.213″″″″MeMeCH
3.214 ″ ″ ″ ″ SMe NEt2N
3.215 ″ ″ CO2-i-Pr Me OMe Me N
3.216″″″″OMeOMeCH
3.217 Me ″ CO2-烯丙基 H OMe OMe CH
3.218 Et ″ CO2-Me H OMe OMe CH
3.219″″″HOMeMeN
3.220″″″″MeMeCH
3.221″″″″ClOMeCH
3.222″″″MeOMeOMeCH
3.223″″″″OMeMeN
3.224 ″ ″ CO2-Et H OMe OMe CH
3.225″″″″OMeMeCH
3.226″″″″ClOMeCH
3.227″″″″OMeMeN
3.228″″″MeOMeOMeCH
3.229″″″″″MeN
3.230 ″ ″ CO2-n-Pr H OMe OMe CH
3.231″″″″OMeMeN
3.232″″″″OMeClCH
3.233″″″″MeMeCH
3.234″″″MeOMeOMeCH
3.235″″″″OMeMeN
3.236 ″ ″ CO2-i-Pr H OMe OMe CH
3.237″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
3.238″″″″MeMeCH
3.239″″″MeOMeMeN
3.240 n-Pr COCH2Cl CO2-Me H OMe OMe CH
3.241″″″″″ClCH
3.242″″″″MeMeCH
3.243″″″″OMeMeN
3.244″″″MeOMeOMeCH
3.245″″″″OMeMeN
3.246 n-Pr ″ CO2-Et H ″ ″ N
3.247″″″″″OMeCH
3.248″″″″MeMeCH
3.249 ″ ″ CO2-n-Pr ″ OMe OMe CH
3.250 i-Pr ″ CO2-Me H OMe OMe CH
3.251″″″″OMeMeN
3.252″″″″MeMeCH
3.253″″″″ClOMeN
3.254″″″MeOMeMeN
3.255″″″″″OMeCH
3.256 烯丙基 ″ CO2-Me H OMe OMe CH
3.257″″″″″ClCH
3.258″″″″MeMeCH
3.259″″″″OMeMeN
3.260 ″ ″ CO2-Et H OMe OMe CH
3.261 ″ ″ CO2-n-Pr ″ ″ ″ CH
3.262 ″ ″ CO2-i-Pr ″ ″ ″ CH
3.263 Me COCF3CO2Me H OMe OMe CH
3.264″″″″″OMeN
3.265″″″″″MeN
3.266″″″″″″CH
3.267 ″ ″ ″ ″ NMe2OCH2CF3N
3.268″″″″MeMeCH
3.269″″″″″″N
3.270″″″″ClOMeCH
3.271″″″MeOMeOMeCH
3.272″″″″″MeN
3.273 ″ ″ CO2-Et H OMe OMe CH
No. R1R2R3R4X Y Z Fp.
3.274″″″″″ClCH
3.275″″″″MeMeCH
3.276″″″″OMeMeN
3.277 ″ ″ ″ ″ NMe2OCH2CF3N
3.278″″″MeOMeOMeCH
3.279″″″″OMeMeN
3.280 ″ ″ CO2-n-Pr H OMe OMe CH
3.281″″″″″″N
3.282″″″″OMeMeN
3.283″″″″MeMeCH
3.284″″″″OMeClCH
3.285″″″MeMeOMeN
3.286″″″″OMeOMeCH
3.287 Me COCF3CO2-i-Pr H OMe OMe CH
3.288″″″″″″N
3.289″″″″OMeMeN
3.290″″″″OMeClCH
3.291″″″″MeMeCH
3.292 ″ ″ ″ ″ SMe NEt2N
3.293 ″ ″ CO2-i-Pr Me OMe Me N
3.294″″″″OMeOMeCH
3.295 Me ″ CO2-烯丙基 H OMe OMe CH
3.296 Et ″ CO2-Me H OMe OMe CH
3.297″″″HOMeMeN
3.298″″″″MeMeCH
3.299″″″″ClOMeCH
3.300″″″MeOMeOMeCH
3.301″″″″OMeMeN
3.302 ″ ″ CO2-Et H OMe OMe CH
3.303″″″″OMeMeCH
3.304″″″″ClOMeCH
3.305″″″″OMeMeN
3.306″″″MeOMeOMeCH
3.307″″″″″MeN
3.308 ″ ″ CO2-n-Pr H OMe OMe CH
3.309″″″″OMeMeN
No. R1R2R3R4X Y Z Fp.
3.310″″″″OMeClCH
3.311″″″″MeMeCH
3.312″″″MeOMeOMeCH
3.313″″″″OMeMeN
3.314 ″ ″ CO2-i-Pr H OMe OMe CH
3.315″″″″OMeMeN
3.316″″″″MeMeCH
3.317″″″MeOMeMeN
3.318 n-Pr COCF3CO2-Me H OMe OMe CH
3.319″″″″″ClCH
3.320″″″″MeMeCH
3.321″″″″OMeMeN
3.322″″″MeOMeOMeCH
3.323″″″″OMeMeN
3.324 n-Pr ″ CO2-Et H ″ ″ N
3.325″″″″″OMeCH
3.326″″″″MeMeCH
3.327 ″ ″ CO2-n-Pr ″ OMe OMe CH
3.328 i-Pr ″ CO2-Me H OMe OMe CH
3.329″″″″OMeMeN
3.330″″″″MeMeCH
3.331″″″″ClOMeN
3.332″″″MeOMeMeN
3.333″″″″″OMeCH
3.334 烯丙基 ″ CO2-Me H OMe OMe CH
3.335″″″″″ClCH
3.336″″″″MeMeCH
3.337″″″″OMeMeN
3.338 ″ ″ CO2-Et H OMe OMe CH
3.339″″n-Pr″″″CH
3.340″″i-Pr″″″CH
3.341 Me COCH3CHO ″ ″ ″ CH
3.342 ″ CO2CH3″ ″ ″ ″ CH
3.343 ″ COCH3CO-CH3″ ″ ″ CH
3.344 ″ CO2CH3″ ″ ″ ″ CH
3.345 ″ CO-CH3CO-S-i-Pr ″ ″ ″ CH
No. R1R2R3R4X Y Z Fp.
3.346 ″ CO2Et ″ ″ ″ ″ CH
3.347 ″ CHO CONMe2″ ″ ″ CH
3.348″″″″OMeMeN
3.349 ″ COCH3″ ″ OMe OMe CH
3.350 ″ ″ CONH2″ ″ ″ CH
3.351 ″ COCH3CS-NMe2″ OMe OMe CH
3.352 ″ CO2Et ″ ″ ″ ″ CH
3.353 ″ CO-CH2CH3″ ″ ″ ″ CH
3.354 ″ CO2Me CS-O-i-Pr ″ ″ ″ CH
3.355″CHO″″″″CH
3.356 ″ ″ C(=N-NMe2)H ″ ″ ″ CH
3.357 Me CO-CH3C(=N-OMe)OMe H OMe OMe CH
3.358 ″ CO2CH3H ″ ″ ″ CH
3.359″CHO″″″″CH
3.360″″C(=NOH)H″″″CH
3.361 ″ CO2Me ″ ″ ″ ″ CH
3.362 ″ COCH3C(=NOMe)H ″ ″ ″ CH
3.363 ″ ″ CO2H ″ ″ ″ CH
3.364 ″ CO2Me ″ ″ ″ ″ CH
3.365 ″ COCH3C(=N-Et)OMe ″ ″ ″ CH
3.366″″C(=N-i-Pr)H″″″CH
3.367 ″ CO2CH2CH2Cl COOMe H OMe OMe CH 141-143
3.368″″″H″″CH123-126
B.劑型制備例
a)粉劑10份重的一種式(Ⅰ)化合物與90份重的滑石粉或惰性物質(zhì)混合,在錘式破碎機(jī)中磨碎。
b)可濕性粉劑25份重的一種式(Ⅰ)化合物和64份重充作惰性材料的含高嶺土的石英粉、10份重木質(zhì)素磺酸鉀和1份重的油酰甲基牛磺酸鈉用作潤濕劑和分散劑,上述混合物在棒式破碎機(jī)中研磨加工。
c)水中易分散的分散體濃縮劑20份重的一種式(Ⅰ)化合物、6份重的烷基酚聚乙二醇醚(
Triton X 207)、3份重異十三烷醇聚乙二醇醚(8EO)和71份重石蠟礦物油(沸點(diǎn)范圍大約在255-277℃以下),上述混合物在球磨機(jī)內(nèi)磨至顆粒在5微米以下。
d)乳油15份重一種式(Ⅰ)化合物,75份重環(huán)己酮作為溶劑和10份重乙氧基化的壬基酚作為乳化劑。
e)在水中可分散的顆粒劑組成如下
75份重一種式(Ⅰ)化合物
10份重木質(zhì)素磺酸鈣
5份重月桂基硫酸鈉
3份重聚乙烯醇
7份重高嶺土
將上述各組份混合,在棒式破碎機(jī)中磨碎,粉狀物質(zhì)在流化床上通過把水作為造粒液體噴灑造粒。
f)在水中可分散的顆粒劑組成如下
25份重一種式(Ⅰ)化合物
5份重2,2-二萘基甲烷-6,6-二磺酸鈉
2份重油酰基甲基?;撬徕c
1份重聚乙烯醇
17份重碳酸鈣和
50份重水
將上述組份在膠體磨中勻漿、預(yù)磨碎,繼之在球磨機(jī)中進(jìn)一步研磨,再將所得到的懸浮物在噴霧塔中通過一種單級噴頭噴霧并干燥。
c.生物學(xué)防治實(shí)例
1.芽前除草效果
單子葉和雙子葉雜草的種子或塊根置于盛砂質(zhì)粘土的塑料盆中,上面用壤土復(fù)蓋。將本發(fā)明化合物的可濕性粉劑或乳油加水稀釋成懸浮液或乳化液,加水稀釋至藥液量為600-800升/公頃,然后按不同施藥劑量對盆栽表層土壤進(jìn)行復(fù)蓋式噴灑處理。噴藥處理后將塑料盆放入溫室內(nèi),維持適宜于雜草生長的溫室條件。3至4周后與未施藥對照組比較,用目測評估方法評價供試植物發(fā)芽或發(fā)芽后植株受害情況。試驗(yàn)結(jié)果表明本發(fā)明化合物是一個防治單子葉和雙子葉雜草的優(yōu)良廣譜性芽前除草劑。例如表1中例號為89、477、1.178、1.180、1.182、1.183、1.185、1.186、2.192、2.270、2.715、3.367和3.386的化合物對有害植物如歐白芥、南苘蒿、野燕麥、狗尾草、稗草和毒麥作芽前除草,當(dāng)用量為每公頃0.3kg或更少一些時,表現(xiàn)出了優(yōu)良的除草效果。
2.芽后除草效果
單子葉和雙子葉雜草的種子或塊根置于盛砂質(zhì)粘土的塑料盆中,上面用壤土復(fù)蓋后置于有利于生長的溫室中培育,播種三周后至供試植物長至3葉期時用藥劑處理。
本發(fā)明化合物的可濕性粉劑或乳油用水稀釋至相當(dāng)于600-800升/公頃藥液量,用不同劑量噴灑處理供試植株的綠色部分,然后將供試植物置于最佳生長條件的溫室內(nèi)3于4周,與未施藥的對照組相比較,評價制劑的效果。
本發(fā)明制劑是一種防治重要經(jīng)濟(jì)作物中的單子葉和雙子葉雜草的優(yōu)良廣譜性芽后除草劑。例如表1中的例號為89、477、1.178、1.180、1.182、1.183、1.185、1.186、2.192、2.270、2.715、3.367和3.368的化合物對于有害植物如歐白芥、狗尾草、稗草、毒麥、南苘蒿和野燕麥作芽后除草,當(dāng)其用量為每公頃0.3kg或更少一些時,表現(xiàn)出優(yōu)良的除草效果。
3.農(nóng)作物對藥劑的承受能力
在室溫內(nèi)還要進(jìn)行下面的試驗(yàn),即將大量的農(nóng)作物和雜草的種子置于盛砂質(zhì)粘土的盆內(nèi),上面用壤土覆蓋。
其中一部分盆子立即按上面1中所述方法處理,其余部分置于溫室中至供試植物長至2-3片真葉期,按上面2中所述方法用不同劑量噴灑處理,給藥處理后在溫室中放置4至5周,通過目測評價可以確證,本發(fā)明化合物無論作芽前或芽后處理,即使在高劑量下對兩葉期的大豆、棉花、油菜、甜菜和馬鈴薯這些農(nóng)作物沒有藥害。此外本發(fā)明有些化合物對禾本科農(nóng)作物如大麥、小麥、黑麥、高粱、小米或水稻還有保護(hù)作用。所以,式(Ⅰ)化合物是可以在農(nóng)作物中施用的高選擇性除草劑。
權(quán)利要求
1、式(1)化合物或其鹽,
式中
R1是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基、其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、CONH2、C1-C4-烷硫基、CN、CHO、(C1-C6-烷基)-羰基、(C3-C6-環(huán)烷基)-羰基、C1-C4-烷基磺酰基、羧基、(C1-C4-烷氧基)-羰基、(C2-C4-鏈烯氧基)-羰基、(C2-C4-炔氧基)-羰基、NO2、NH2、單-和二-(C1-C6)-烷基氨基的基團(tuán)取代,
R2是CO-R5、COO-R6、CO-SR7、CO-NR8R9、CS-NR10R11、CS-OR12、CS-SR13、SO2R14、SO2NR15R16,
R3是COR17、CO-OR18、CO-NR19R20、CO-SR21、CO-O-N=CR22R23、CSR24、CSSR25、CS-OR26、CS-NR27R28、C(=NR29)R30,
R4是H、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個鹵素取代,
R5是H、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,或是未取代的或取代的C3-C8-環(huán)烷基、未取代的或取代的苯基、未取代的或取代的雜芳基或苯基-C1-C4-烷基,其苯環(huán)上是未取代的或取代的,
R6是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,或C3-C6-環(huán)烷基,它是未取代的或被一個或多個選自鹵素、C1-C4-烷基和C1-C4-烷氧基的基團(tuán)取代,或C3-C6-環(huán)烷基-C3-C3-烷基,
R7類似于R6,
R8是H、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代或被一個或多個鹵素取代,或是(C1-C6-烷氧基)-羰基或C1-C4烷氧基,
R9是H、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,或是CO-R33、CO-OR34、CO-NR35R36、CS-R33或CS-OR34或
R8和R9一起組成一個式-(CH2)4-、-(CH2)5-、-CH2CH2-O-CH2CH2-、-CH2CH2-NH-CH2CH2-的二價基團(tuán),其中后4個基團(tuán)是未取代的或被C1-C4-烷基取代,
R10類似于R8,
R11類似于R9,
R12類似于R6,
R13類似于R6,
R14是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,
R15類似于R8,
R16是氫、C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個鹵素取代,
R17類似于R5,
R18是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,或是C3-C6-環(huán)烷基,它是未取代的或被一個或多個選自鹵素、C1-C4-烷基和C1-C4-烷氧基的基團(tuán)取代,或是C3-C6-環(huán)烷基-C1-C3-烷基或H,
R19類似于R8,
R20類似于R9,
R21類似于R18,
R22是H、C1-C4-烷基、C3-C5-鏈烯基或C3-C5-炔基,
R23是H、C1-C4-烷基、C3-C5-鏈基或C3-C5-炔基,
R24類似于R17,
RR18是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基,其中后3個基團(tuán)分別相互獨(dú)立地是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,或是C3-C6-環(huán)烷基,它是未取代的或被一個或多個選自鹵素、C1-C4-烷基和C1-C4-烷氧基的基團(tuán)取代,或是C3-C6-環(huán)烷基-C1-C3-烷基或H,
R19類似于R8,
R20類似于R9,
R21類似于R18,
R22是H、C1-C4-烷基、C3-C5-鏈烯基或C3-C5-炔基,
R23是H、C1-C4-烷基、C3-C5-鏈基或C3-C5-炔基,
2、根據(jù)權(quán)利要求1的化合物或其鹽,其特征在于,
R1是C1-C4-烷基、C2-C4-鏈烯基或C2-C4-炔基,或
R2是CO-R5、COOR6、CO-NR8R9、CS-NR10R11、SO2R14或SO2NR15R16或
R3是COR17、COOR18、CONR19R20或CO-ON=CR22R23,或
R4是H或C1-C4-烷基,或
R5是H、C1-C6-烷基,它是未取代的或被一個或多個鹵素或被C1-C4-烷氧基、C1-C4-烷硫基或NR31R32的基團(tuán)取代,或是C3-C6-環(huán)烷基,未取代的或取代的苯基、未取代的或取代的芐基或未取代的或取代的雜芳基,其中后2個基團(tuán)是未取代的或被一個或多個選自C1-C4-烷基,C1-C4-烷氧基和鹵素的基團(tuán)取代,或
R6是C1-C6-烷基、C2-C6-鏈烯基、C2-C6-炔基、C1-C6-鹵代烷基或C3-C6-環(huán)烷基,或
R7是C1-C4-烷基,
R8是H、C1-C6-烷基、C1-C4-鹵代烷基、C1-C4-烷氧基或(C1-C4-烷氧基)-羰基、
R9是氫、C1-C6-烷基,它是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基和NR31R32的基團(tuán)取代,或CO-R33、CO-OR34或CO-NR35R36或
R8和R9一起組成一個式-(CH2)4-、-(CH2)5-或-CH2CH2-O-CH2CH2-的二價基團(tuán)或
R14是C1-C6-烷基、C1-C6-鹵代烷基,或
R15,R16分別相互獨(dú)立地是氫或C1-C4-烷基或
R17是氫或C1-C4-烷基、C1-C4-鹵代烷基、C3-C6-環(huán)烷基、苯基或雜芳基,其中后2個基團(tuán)是未取代的或取代的,或
R18是氫、C1-C4-烷基、C2-C6-鏈烯基或C2-C6-炔基,其中后3個基團(tuán)是未取代的或被一個或多個選自鹵素、C1-C4-烷氧基、C1-C4-烷硫基和NR31R32的基團(tuán)取代,或C3-C6-環(huán)烷基或C3-C6-環(huán)烷基-C1-C3-烷基或
R22是氫或C1-C2-烷基或
R23是氫或C1-C2-烷基或
R29是氫、羥基、氨基、NHCH3、N(CH3)2、C1-C4-烷基或C1-C4-烷氧基,
R30是氫或C1-C4-烷基或
R31相互獨(dú)立地是H或C1-C4-烷基或
R32相互獨(dú)立地是H或C1-C4-烷基或
R33是氫、C1-C4-烷基、C1-C4-鹵代烷基、C3-C6環(huán)烷基或苯基,它是未取代的或被一個或多個選自鹵素、C1-C4-烷基和C1-C4-烷氧基的基團(tuán)取代,或
R34是C1-C4-烷基、烯丙基、炔丙基或環(huán)烷基或
R35是氫或C1-C4-烷基或
R36是氫或C1-C4-烷基或
X是C1-C4-烷基、C1-C4-烷氧基、C1-C4-鹵代烷基、C1-C4-烷硫基、鹵素或單一或二-(C1-C2-烷基)-氨基,或
Y是C1-C4-烷基、C1-C4-烷氧基、C1-C4-鹵代烷基或C1-C4-烷硫基,
或是這樣的式(Ⅰ)化合物或其鹽,即在式(Ⅰ)中連有二個或多個具有前面所列舉的優(yōu)選含義的R1至R36基團(tuán)。
3、根據(jù)權(quán)利要求1或2的化合物或其鹽,其特征在于,
R1是甲基、乙基、正丙基、異丙基或烯丙基,
R2是CO-R5、COOR6、CO-NR8R9、CS-NR10R11、SO2R14或SO2NR15R16,
R5是H、C1-C4-烷基、C1-C2-鹵代烷基,環(huán)丙基、苯基、芐基或帶5或6個環(huán)原子的雜芳基,其中后3個基團(tuán)是未取代的或被一個或多個鹵素原子取代,
R6是C1-C4-烷基、烯丙基、炔丙基或環(huán)丙基,
R8是H、C1-C4-烷基、C1-C4-鹵代烷基或(C1-C4-烷氧基)-羰基,
R9是H或C1-C4-烷基,
R10是H或C1-C4-烷基,
R11是H或C1-C4-烷基,
R14是C1-C4-烷基,
R15是H或C1-C4-烷基和
R16是H或C1-C4-烷基。
4、式(Ⅰ)化合物或其鹽的制備方法,其特征在于,可以用
a)一個式(Ⅱ)化合物
(Ⅱ)
與一個式(Ⅲ)雜環(huán)氨基甲酸酯反應(yīng),
(Ⅲ)
式中R*需要時是取代的苯基或C1-C4-烷基,或
b)一個式(Ⅳ)的磺?;惽杷狨?br> (Ⅳ)
與一個式(Ⅴ)的氨基雜環(huán)化合物反應(yīng),
(Ⅴ)
或,c)一個式(Ⅱ)的化合物與一個式(Ⅹ)的(硫代)異氰酸酯在一種堿的存在下反應(yīng),
(Ⅹ)
其中,在上面的式(Ⅱ)至(Ⅴ)和(Ⅹ)中的基團(tuán)R1至R4、W、X、Y和Z具有式(Ⅰ)中新確定的含義,且用方法a)和b)將首先得到W=O的式(Ⅰ)化合物。
5、除草劑或植物生長調(diào)節(jié)劑,其特征在于,它含有根據(jù)權(quán)利要求1至3中一項(xiàng)的式(Ⅰ)化合物和常用的劑型助劑物質(zhì)。
6、根據(jù)權(quán)利要求1至3中一項(xiàng)的式(Ⅰ)化合物作為除草劑和植物生長調(diào)節(jié)劑的應(yīng)用。
7、防除有害植物或植物生長調(diào)節(jié)的方法,其特征在于,人們可以施用根據(jù)權(quán)利要求1至3中一項(xiàng)的一個有效作用劑量的式(Ⅰ)化合物或其鹽于植物、植物部分或農(nóng)業(yè)或工業(yè)所利用的土地。
8、式(Ⅱ)化合物
(Ⅱ)
式中
R1、R2和R3的含義如權(quán)利要求1、2或3中式(Ⅰ)中所確定。
9、式(Ⅳ)化合物
(Ⅳ)
式中
R1、R2和R3的含義如權(quán)利要求1、2或3的式(Ⅰ)中所確定。
全文摘要
新的苯磺酰脲類化合物,它的制備以及它們作為除草劑和植物生長調(diào)節(jié)劑的應(yīng)用。
文檔編號A01N47/36GK1087631SQ9311974
公開日1994年6月8日 申請日期1993年10月30日 優(yōu)先權(quán)日1992年10月31日
發(fā)明者G·施納博, L·威爾姆斯, K·保爾, H·比倫格 申請人:赫徹斯特股份公司
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