CN1333751A - 取代的吡啶除草剂 - Google Patents

取代的吡啶除草剂 Download PDF

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CN1333751A
CN1333751A CN99815786A CN99815786A CN1333751A CN 1333751 A CN1333751 A CN 1333751A CN 99815786 A CN99815786 A CN 99815786A CN 99815786 A CN99815786 A CN 99815786A CN 1333751 A CN1333751 A CN 1333751A
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CN1176907C (zh
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A·埃德蒙兹
C·卢西
K·塞金杰
A·德麦斯马克
K·昆兹
J·谢策尔
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Syngenta Participations AG
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Abstract

式Ⅰ化合物(其中各取代基如权利要求1中定义)及其农药上可耐受的盐M+以及式Ⅰ化合物的所有立体异构体和互变异构体适于用作除草剂。

Description

取代的吡啶除草剂
本发明涉及具有除草活性的新型吡啶酮化合物、其制备、包含这些化合物的组合物以及它们在防治杂草,尤其是防治有用作物中的杂草方面和抑制植物生长方面的用途。
具有除草活性的吡啶酮化合物在例如WO97/46530中已有记载。但现在我们发现了新的具有除草和生长抑制性能的吡啶酮化合物。
因此,本发明涉及式I化合物及其农药上可耐受的盐M+以及式I化合物的所有立体异构体和互变异构体:
Figure A9981578600161
其中p为0或1;R5为C1-C6卤代烷基;R2为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,被C1-C2烷氧基羰基或苯基取代的乙烯基,或者为C2-C6炔基,C2-C6卤代炔基,被三甲基甲硅烷基、羟基、C1-C2烷氧基、C1-C2烷氧基羰基或苯基取代的乙炔基,或者为C3-C6二烯基(allenyl),C3-C6环烷基,被卤素取代的C3-C6环烷基,或者为C1-C6烷氧基,C3-C6链烯氧基,C3-C6炔氧基,C1-C6卤代烷氧基,C3-C6卤代链烯氧基,氰基-C1-C4烷氧基,C1-C4烷氧基-C1-C4烷氧基,C1-C4烷硫基-C1-C4烷氧基,C1-C4烷基亚磺酰基-C1-C4烷氧基,C1-C4烷基磺酰基-C1-C4烷氧基,C1-C4烷氧基羰基-C1-C4烷氧基,C1-C6烷硫基,C1-C6烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷硫基,C1-C6卤代烷基亚磺酰基,C1-C6卤代烷基磺酰基,C1-C4烷氧基羰基-C1-C4烷硫基,C1-C4烷氧基羰基-C1-C4烷基亚磺酰基,C1-C4烷氧基羰基-C1-C4烷基磺酰基,苄基-S(O)n1-,C1-C6烷基氨基,C2-C6二烷基氨基,C1-C6烷基氨基磺酰基,二-(C1-C6烷基氨基)磺酰基,苄氧基,苄基,苯基,苯氧基,苯硫基,苯基亚磺酰基或苯磺酰基,这些含苯基的基团本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,或者R2为OS(O)n2-R21,N(R23)-S(O)n3-R22,氰基,氨基甲酰基,C1-C4烷氧基羰基,甲酰基,卤素,氰硫基,氨基,羟基-C1-C4烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷基-S(O)n4-C1-C4烷基,氰基-C1-C4烷基,C1-C6烷基羰氧基-C1-C4烷基,C1-C4烷氧基羰基-C1-C4烷基,C1-C4烷氧基羰氧基-C1-C4烷基,C1-C4氰硫基-C1-C4烷基,苯甲酰氧基-C1-C4烷基,C2-C6环氧乙烷基(oxiranyl),C1-C4烷基氨基-C1-C4烷基,二-(C1-C4烷基)氨基-C1-C4烷基,C1-C12烷基硫代羰基-C1-C4烷基或甲酰基-C1-C4烷基,或者R2为可以是芳香性或部分饱和并且可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或稠合二环环系,所述环系经由C1-C4亚烷基、-CH=CH-、-C≡C-、-CH2O-、-CH2N(C1-C4烷基)-、-CH2SO-、或-CH2SO2基团与吡啶环键连,且每一环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,巯基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C2-C5烷氧基烷硫基,C3-C5乙酰基烷硫基,C3-C6烷氧基羰基烷硫基,C2-C4氰基烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,二-(C1-C4烷基)氨基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素;R3为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C3-C6环烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷硫基,C1-C6烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷硫基,C1-C6卤代烷基亚磺酰基,C1-C6卤代烷基磺酰基,C1-C6烷基氨基,C2-C6二烷基氨基,C1-C6烷基氨基磺酰基,C2-C6二烷基氨基磺酰基,苯基,苯硫基,苯基亚磺酰基,苯磺酰基或苯氧基,其中的苯基部分本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,或者R3为-N(R23)-S(O)n-R22,氰基,卤素,氨基,C1-C4烷氧基-C1-C4烷基或C1-C4烷基-S(O)n-C1-C4烷基;R4为氢,C1-C6烷基,羟基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6卤代链烯氧基,C3-C6炔氧基,C1-C4烷基羰氧基,C1-C4烷基磺酰氧基,甲苯磺酰氧基,C1-C4烷硫基,C1-C4烷基亚磺酰基,C1-C4烷基磺酰基,C1-C4烷基氨基,C1-C4二烷基氨基,C1-C4烷氧基羰基,C1-C4卤代烷基,甲酰基,氰基,卤素,苯基或苯氧基,其中的苯基部分本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代;或者R4为可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或R3-稠合二环环系,其中所述环系,除非稠合,均直接或经由C1-C4亚烷基、-CH=CH-、-C≡C-、-CH2O-、-CH2N(C1-C4烷基)-、-CH2S-、-CH2SO-、或-CH2SO2-基团与吡啶环键连,且所述环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C1-C4烷氧基-C1-C2烷硫基,C1-C4烷基羰基-C1-C2烷硫基,C1-C4烷氧基羰基-C1-C2烷硫基,氰基-C1-C4烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,二-(C1-C4烷基)氨基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素;R21为C1-C4烷基或C1-C4卤代烷基;R22为C1-C4烷基,C1-C4卤代烷基或二-(C1-C4烷基)氨基;R23、R24、R25彼此独立地为氢或C1-C4烷基;n,n1,n2,n3和n4彼此独立地为0,1或2;Q为Q1
Figure A9981578600191
其中R6、R7、R8和R9彼此独立地为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6炔基,C1-C6烷氧基羰基,C1-C6烷基羰基,C1-C6烷基-S(O)n17,C1-C6烷基-NHS(O)2,C1-C6烷基氨基,二-(C1-C6烷基)氨基,羟基,C1-C6烷氧基,C3-C6链烯氧基,C3-C6炔氧基,羟基-C1-C6烷基,C1-C4烷基磺酰氧基-C1-C6烷基,甲苯磺酰氧基-C1-C6烷基,C1-C6烷氧基-C1-C6烷基,C1-C6烷基-S(O)n4-C1-C6烷基,氰基-C1-C6烷基,C1-C6烷氧基-C1-C6烷氧基,苄氧基-C1-C6烷基,C1-C6烷氧基羰基-C1-C6烷基,C1-C6烷氧基羰氧基-C1-C6烷基,氰硫基-C1-C6烷基,环氧乙烷基,C1-C6烷基氨基-C1-C6烷基,二(C1-C6烷基)氨基-C1-C6烷基,甲酰基-C1-C6烷基,C1-C6烷基肟基(alkyloximo),卤素,氰基,硝基,苯基或被下列基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、氨基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n18、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n5、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)n19N(C1-C4烷基)2、卤素、硝基、COOH或氰基;或者相邻的R6与R7或R8与R9一起表示-(CH2)m-,C(O)O(CH2)n20-或-S(O)n21(CH2)n22-;n5,n17,n18,n19和n21彼此独立地为0,1或2;n20为2或3;n22为2,3或4;m为2,3,4,5,或6;W为氧,S(O)n6,-CR11R12-,-CR63R64CR65R66,-C(O)-或-NR13;R63、R64、R65和R66彼此独立地为氢或C1-C6烷基,或者R65与R7或R9一起形成直接键;n6为0,1或2;R11为氢,C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷硫基-C1-C4烷基,C1-C4烷硫基-C3-C6环烷基,C1-C4烷基羰氧基-C1-C4烷基,C1-C4烷基磺酰氧基-C1-C4烷基,甲苯磺酰氧基-C1-C4烷基,二-(C1-C3烷氧基烷基)甲基,二-(C1-C3烷硫基烷基)甲基,(C1-C3烷氧基烷基)-(C1-C3烷硫基烷基)甲基,C3-C5氧杂环烷基,C3-C5硫杂环烷基,C3-C4二氧杂环烷基,C3-C4二硫杂环烷基,C3-C4氧硫杂环烷基,甲酰基,C1-C4烷氧基羰基,氨基甲酰基,C1-C4烷基氨基羰基,二-(C1-C4烷基)氨基羰基,苯基氨基羰基,苄基氨基羰基或其本身又可以被下述基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、氨基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n21、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n7、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)n20N(C1-C4烷基)、卤素、硝基、COOH或氰基;n7,n20和n21彼此独立地为0,1或2;或者R12与R6或R9一起代表基团-(CH2)o-;o为1,2,3,4或5;R12为氢,C1-C4烷基或C1-C4卤代烷基;或者R12与R11一起代表基团-(CH2)m1;m1为2,3,4,5,或6;R10为羟基,O-M+,卤素,氰基,SCN,OCN,C1-C12烷氧基,C1-C4烷氧基羰基-C1-C4烷氧基,C1-C12烷硫基,C1-C12烷基亚磺酰基,C1-C12烷基磺酰基,C1-C12卤代烷硫基,C1-C12卤代烷基亚磺酰基,C1-C12卤代烷基磺酰基,C1-C6烷氧基-C1-C6烷硫基,C1-C6烷氧基-C1-C6烷基亚磺酰基,C1-C6烷氧基-C1-C6烷基磺酰基,C2-C12链烯硫基,C2-C12链烯基亚磺酰基,C2-C12链烯基磺酰基,C2-C12炔硫基,C2-C12炔基亚磺酰基,C2-C12炔基磺酰基,C2-C12卤代链烯硫基,C2-C12卤代链烯基亚磺酰基,C2-C12卤代链烯基磺酰基,C1-C4烷氧基羰基-C1-C4烷硫基,C1-C4烷氧基羰基-C1-C4烷基亚磺酰基,C1-C4烷氧基羰基-C1-C4烷基磺酰基,(C1-C4烷氧基)2P(O)O,C1-C4烷基-(C1-C4烷氧基)P(O)O,H(C1-C4烷氧基)P(O)O,R14R15N,R14R15NNH,R16R17NC(O)O-,R16R17NC(O)NH-,C1-C12烷基-S(O)2NR18,C1-C4卤代烷基-S(O)2NR19,C1-C12烷基-S(O)2O,C1-C4卤代烷基-S(O)2O,C1-C18烷基羰氧基,其中的烷基基团可以被卤素、C1-C6烷氧基、C1-C6烷硫基或氰基取代,或者为C2-C18链烯基羰氧基,C2-C18炔基羰氧基,C3-C6环烷基羰氧基,C1-C12烷氧基羰氧基,C1-C12烷硫基羰氧基,C1-C12烷基硫代氨基甲酰基,C1-C6烷基-NH(CS)N(C1-C6烷基)-NH-,二-C1-C6烷基-N(CS)N(C1-C6烷基)-NH-,苄氧基,苄硫基,苄基亚磺酰基,苄基磺酰基,苯氧基,苯硫基,苯基亚磺酰基,苯基磺酰基,苯磺酰基氨基,苯磺酰氧基或苯甲酰氧基,其中的苯基基团部分本身又可被下述基团取代:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷硫基、C1-C4烷基亚磺酰基、C1-C4烷基磺酰基、C1-C4烷基-S(O)2O、C1-C4卤代烷硫基、C1-C4卤代烷基亚磺酰基、C1-C4卤代烷基磺酰基、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)2N(C1-C4烷基)、卤素、硝基或氰基;或者R10为基团Ar1-硫基,Ar2-亚磺酰基,Ar3-磺酰基,-OCO-Ar4或NH-Ar5,其中Ar1、Ar2、Ar3、Ar4和Ar5彼此独立地为可以是芳香性或部分饱和的并且可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或稠合二环环系,且对于每一环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,巯基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C2-C5烷氧基烷硫基,C3-C5乙酰基烷硫基,C3-C6烷氧基羰基烷硫基,C2-C4氰基烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,二-(C1-C4烷基)氨基,卤素,氰基,硝基,苯基和苄硫基,其中的苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮上的取代基不能为卤素;R14、R15、R16、R17和R18彼此独立地为氢或C1-C6烷基;n8,n9,n10,n11,n12,n13和n14彼此独立地为0,1或2;R13为氢,C1-C4烷基,C1-C4烷硫基-C1-C4羰基,C1-C4烷基亚磺酰基-C1-C4羰基,C1-C4烷基磺酰基-C1-C4羰基,C1-C4烷氧基羰基,C1-C4烷基羰基,苯基羰基,或者为其本身还可以被下述基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n15、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n16、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)2N(C1-C4烷基)、卤素、硝基或氰基;以及n15和n16彼此独立地为0,1或2。
取代基定义中的烷基基团可以是直链的或支链的,并且例如为甲基、乙基、正丙基、异丙基、正丁基、仲丁基、异丁基、叔丁基、戊基、己基、庚基、辛基、壬基、癸基、十一烷基和十二烷基以及它们的支链异构体。烷氧基、链烯基和炔基基团则由上述烷基基团衍生得到。链烯基和炔基基团可以是单-或多不饱和的。
亚烷基基团例如-(CH2)m-、-(CH2)m1-或-(CH2)o-可以被一个或多个甲基基团取代,优选这些亚烷基基团在每种情况下是未取代的。这同样适用于-C(O)O(CH2)n20-和-S(O)n21(CH2)n22-基团,并且也适用于所有含有C3-C6-环烷基-、C3-C5氧杂环烷基-、C3-C5硫杂环烷基-、C3-C4二氧杂环烷基-、C3-C4二硫杂环烷基-、C3-C4氧硫杂环烷基的基团。
卤素通常指氟、氯、溴或碘。类似地,这也适用于处于其它组合含义如卤代烷基或卤代苯基中的卤素。
具有1-6个碳原子链长的卤代烷基例如为氟甲基、二氟甲基、三氟甲基、氯甲基、二氯甲基、三氯甲基、2,2,2-三氟乙基、1-氟乙基、2-氟乙基、2-氯乙基、2-氟丙-2-基、五氟乙基、1,1-二氟-2,2,2-三氯乙基、2,2,3,3-四氟乙基和2,2,2-三氯乙基、五氟乙基、七氟正丙基、全氟正己基;R2、R3、尤其是R5定义中的卤代烷基优选为三氯甲基、氟甲基、二氯氟甲基、二氟氯甲基、二氟甲基、三氟甲基、五氟乙基或七氟正丙基。
合适的卤代烷基是指单卤代-或多卤代的链烯基,其中的卤素指氟、氯、溴和碘,尤其是氟和氯,所述基团例如1-氯乙烯基、2-氯乙烯基、2,2-二氟乙烯基、2,2-二氟丙-1-烯-2-基、2,2-二氯乙烯基、3-氟丙-1-烯基、氯丙-1-烯-1-基、3-溴丙-1-烯-1-基、2,3,3-三氟丙-2-烯-1-基、2,3,3-三氯丙-2-烯-1-基和4,4,4-三氟丁-2-烯-1-基。在单卤代、二卤代或三卤代的C2-C6链烯基中,优选链长为2-5个碳原子的链烯基。
合适的卤代炔基例如为单卤代-或多卤代的炔基,其中的卤素指溴,碘且尤其是氟和氯,例如3-氟丙炔基、3-氯丙炔基、3-溴丙炔基、3,3,3-三氟丙炔基和4,4,4-三氟丁-2-炔-1-基。在单卤代或多卤代的炔基基团中,优选链长为2-5个碳原子的炔基。
单卤代或多卤代的C3-C6环烷基例如为2,2-二氯环丙基、2,2-二溴环丙基、2,2,3,3-四氟环丁基或2,2-二氟-3,3-二氯环丁基基团。
烷氧基基团优选具有1-6个碳原子的链长。烷氧基例如是指甲氧基、乙氧基、丙氧基、异丙氧基、正丁氧基、异丁氧基、仲丁氧基和叔丁氧基以及戊氧基和己氧基异构体;优选甲氧基和乙氧基。烷基羰基优选为乙酰基或丙酰基。烷氧基羰基例如为甲氧基羰基、乙氧基羰基、丙氧基羰基、异丙氧基羰基、正丁氧基羰基、异丁氧基羰基、仲丁氧基羰基或叔丁氧基羰基;优选甲氧基羰基、乙氧基羰基或叔丁氧基羰基。卤代烷氧基优选具有1-6个碳原子的链长。
卤代烷氧基例如为氟甲氧基、二氟甲氧基、三氟甲氧基、2,2,2-三氟乙氧基、1,1,2,2-四氟乙氧基、1-氟乙氧基、2-氟乙氧基、2-氯乙氧基、2,2-二氟乙氧基和2,2,2-三氯乙氧基;优选氟甲氧基、二氟甲氧基、2-氯乙氧基和三氟甲氧基。
烷硫基优选具有1-8个碳原子的链长。烷硫基例如为甲氧基、乙硫基、丙硫基、异丙硫基、正丁硫基、异丁硫基、仲丁硫基或叔丁硫基,优选甲硫基和乙硫基。烷基亚磺酰基例如为甲基亚磺酰基、乙基亚磺酰基、丙基亚磺酰基、异丙基亚磺酰基、正丁基亚磺酰基、异丁基亚磺酰基、仲丁基亚磺酰基、叔丁基亚磺酰基;优选甲亚磺酰基和乙亚磺酰基。
烷基磺酰基例如为甲磺酰基、乙磺酰基、丙磺酰基、异丙磺酰基、正丁基磺酰基、异丁基磺酰基、仲丁基磺酰基或叔丁基磺酰基;优选甲磺酰基和乙磺酰基。
烷基氨基例如为甲基氨基、乙基氨基、正丙基氨基、异丙基氨基或丁基氨基异构体。二烷基氨基例如为二甲氨基、甲基乙基氨基、二乙基氨基、正丙基甲基氨基、二丁基氨基和二-异丙基氨基。优选的烷基氨基具有1-4个碳原子链长。烷氧基烷基优选具有1-6个碳原子。烷氧基烷基例如为甲氧基甲基、甲氧基乙基、乙氧基甲基、乙氧基乙基、正丙氧基甲基、正丙氧基乙基、异丙氧基甲基或异丙氧基乙基。烷硫基烷基优选具有1-6个碳原子。烷硫基烷基例如为甲硫基甲基、甲硫基乙基、乙硫基甲基、乙硫基乙基、正丙硫基甲基、正丙硫基乙基、异丙硫基甲基、异丙硫基乙基、丁硫基甲基、丁硫基乙基或丁硫基丁基。
苯基本身以及作为诸如苯氧基、苄基、苄氧基、苯甲酰基、苯硫基、苯基烷基、苯氧基烷基或甲苯磺酰基之类取代基的一部分可以是单取代或多取代形式。在这种情况下,取代基位于邻位、间位或对位的任何位置上。
二烯基(allenyl)例如为CH2=C=CH2、CH2=CH-CH2-CH=CH2、CH2=CH-CH2-CH2-CH=CH2或CH2=CH-CH2-CH=CH-CH3
本发明还涉及盐M+,它们可以由式I化合物,特别是其中R10为O-M+的那些式I化合物与(并且优选)胺、碱金属碱、碱土金属碱或季铵碱形成。在作为成盐物的碱金属碱和碱土金属碱中,必须强调下列碱:锂、钠、钾、镁或钙的氢氧化物,特别是钠或钾的氢氧化物。适于形成铵盐的胺实例包括氨以及伯-、仲-和叔-C1-C18烷基胺、C1-C4羟烷基胺和C2-C4-烷氧基烷基胺,例如甲胺、乙胺、正丙胺、异丙胺、丁胺的四种异构体、正戊胺、异戊胺、己胺、庚胺、辛胺、壬胺、癸胺、十五碳烷胺、十六碳烷胺、十七碳烷胺、十八碳烷胺、甲乙胺、甲基异丙基胺、甲基己基胺、甲基壬基胺、甲基十五烷基胺、甲基十八烷基胺、乙基丁基胺、乙基庚基胺、乙基辛基胺、己基庚基胺、己基辛基胺、二甲基胺、二乙基胺、二正丙基胺、二异丙基胺、二正丁基胺、二正戊基胺、二异戊基胺、二己基胺、二庚基胺、二辛基胺、乙醇胺、正丙醇胺、异丙醇胺、N,N-二乙醇胺、N-乙基丙醇胺、N-丁基乙醇胺、烯丙胺、正丁烯基-2-胺、正戊烯基-2-胺、2,3-二甲基丁烯基-2-胺、二丁烯基-2-胺、正己烯基-2-胺、丙二胺、三甲基胺、三乙基胺、三正丙基胺、三异丙基胺、三正丁基胺、三异丁基胺、三仲丁基胺、三正戊基胺、甲氧基乙胺和乙氧基乙胺;杂环胺,例如吡啶、喹啉、异喹啉、吗啉、哌啶、吡咯烷、二氢吲哚、喹宁环和氮杂;伯芳胺,例如苯胺、甲氧基苯胺、乙氧基苯胺、邻-、间-和对-二甲基苯胺、苯二胺、萘胺和邻-、间-和对-氯苯胺;但是特别优选三乙胺、异丙胺和二异丙基胺。适于成盐的季铵碱实例例如为[N(RaRbRcRd)]+OH-,其中Ra,Rb,Rc和Rd彼此独立地为C1-C4烷基。具有其它阴离子的其它适宜四烷基铵碱例如通过阴离子交换反应得到。M+优选代表铵盐(特别是NH4 +)或碱金属(特别是钾或钠)。
式I化合物可以以各种互变异构形式存在,例如当R10为羟基时以优选的式I′和I形式存在:
Figure A9981578600261
式I化合物中,优选这些化合物及其农药上可耐受的盐M+以及式I化合物的所有立体异构体和互变异构体,其中:p为0;R5为C1-C6卤代烷基;R2为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C3-C6环烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷硫基,C1-C6烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷硫基,C1-C6卤代烷基亚磺酰基,C1-C6卤代烷基磺酰基,苄基-S(O)n1-,C1-C6烷基氨基,C2-C6二烷基氨基,C1-C6烷基氨基磺酰基,C2-C6-二烷基氨基磺酰基,苯基,苯氧基,苯硫基,苯基亚磺酰基或苯磺酰基,其中的苯基基团本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,或者为OS(O)n2-R21,N(R23)-S(O)n3-R22,氰基,卤素,氨基,C1-C4烷氧基-C1-C4烷基,C1-C4烷基-S(O)n4-C1-C4烷基,氰基-C1-C4烷基或C1-C4烷氧基-C1-C4烷氧基;R3为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C3-C6环烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷硫基,C1-C6烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷硫基,C1-C6卤代烷基亚磺酰基,C1-C6卤代烷基磺酰基,C1-C6烷基氨基,C2-C6二烷基氨基,C1-C6烷基氨基磺酰基,C2-C6二烷基氨基磺酰基,苯基,苯硫基,苯基亚磺酰基,苯磺酰基或苯氧基,其中的苯基部分本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,或者为-N(R23)-S(O)n-R22,氰基,卤素,氨基,C1-C4烷氧基-C1-C4烷基或C1-C4烷基-S(O)n-C1-C4烷基;R4为氢,C1-C6烷基,C1-C4烷氧基,C1-C4卤代烷氧基,C1-C4烷基羰氧基,C1-C4烷硫基,C1-C4烷基亚磺酰基,C1-C4烷基磺酰基,C1-C4卤代烷基,甲酰基,氰基,卤素,苯基或苯氧基,其中的苯基部分本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代;或者R4为可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或R3-稠合二环环系,其中所述环系经由C1-C4亚烷基与吡啶环键连,且所述环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C1-C4烷氧基-C1-C2烷硫基,C1-C4烷基羰基-C1-C2烷硫基,C1-C4烷氧基羰基-C1-C2烷硫基,氰基-C1-C4烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,C2-C4二烷基氨基磺酰基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取,而且杂环中氮原子上的取代基不能为卤素;R21和R22彼此独立地为C1-C4烷基或C1-C4卤代烷基;R23、R24和R25彼此独立地为氢或C1-C4烷基;n,n1,n2,n3和n4彼此独立地为0,1或2;Q为Q1 其中R6、R7、R8和R9彼此独立地为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6炔基,C1-C6烷氧基羰基,C1-C6烷基-S(O)n17,C1-C6烷基-NHS(O)2,C1-C6烷基氨基,二-(C1-C6烷基)氨基,羟基,C1-C6烷氧基,C3-C6链烯氧基,C3-C6炔氧基,羟基-C1-C6烷基,C1-C4烷基磺酰氧基-C1-C6烷基,甲苯磺酰氧基-C1-C6烷基,卤素,氰基,硝基,苯基或被下列基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、氨基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n18、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n5、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)n19N(C1-C4烷基)、卤素、硝基、COOH或氰基;或者相邻的R6与R7或R8与R9一起表示-(CH2)m-;n5,n17,n18和n19彼此独立地为0,1或2;m为2,3,4,5,或6;W为氧,S(O)n6,-CR11R12-,-C(O)-或-NR13-;n60,1或2;R11为氢,C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷硫基-C1-C4烷基,C1-C4烷基羰氧基-C1-C4烷基,C1-C4烷基磺酰氧基-C1-C4烷基,甲苯磺酰氧基-C1-C4烷基,二-(C1-C3烷氧基烷基)甲基,二-(C1-C3烷硫基烷基)甲基,(C1-C3烷氧基烷基)-(C1-C3烷硫基烷基)甲基,C3-C5氧杂环烷基,C3-C5硫杂环烷基,C3-C4二氧杂环烷基,C3-C4二硫杂环烷基,C3-C4氧硫杂环烷基,甲酰基,C1-C4烷氧基羰基或其本身又可以被下述基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、氨基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n21、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n7、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)n20N(C1-C4烷基)、卤素、硝基、COOH或氰基;n7,n20和n21彼此独立地为0,1或2;或者R12与R9一起代表基团-(CH2)o-;o为1,2,3,4或5;R12为氢,C1-C4烷基或C1-C4卤代烷基;或者R12与R11一起代表基团-(CH2)m1;m1为2,3,4,5,或6;R10为羟基,O-M+,卤素,C1-C12烷氧基,C1-C12烷基羰氧基,C2-C4链烯基羰氧基,C3-C6环烷基羰氧基,C1-C12烷氧基羰氧基,C1-C12烷基羰氧基,R23R24N-C(O)O,C1-C12烷基S(O)n8-,C1-C4卤代烷基-S(O)n9-,C2-C12-链烯基S(O)n10-,C2-C12卤代链烯基S(O)n11-,C2-C12炔基S(O)n12-;苄氧基,苯氧基,苯硫基,苯基亚磺酰基或苯磺酰基,其中的苯基基团部分本身又可被下述基团取代:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n13、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n14、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)2N(C1-C4烷基)、卤素、硝基或氰基,或者为C1-C4烷基-S(O)2O,苯基-S(O)2O,(C1-C4烷氧基)2P(O)O,C1-C4烷基(C1-C4烷氧基)P(O)O,或H(C1-C4烷氧基)P(O)O;n8,n9,n10,n11,n12,n13和n14彼此独立地为0,1或2;R13为氢,C1-C4烷基,C1-C4烷氧基羰基或其本身又可以被下述基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n15、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n16、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)2N(C1-C4烷基)、卤素、硝基或氰基;n15和n16彼此独立地为0,1或2。
在优选的一组式I化合物中,R10为卤素,氰硫基,C1-C12烷硫基,C1-C12烷基亚磺酰基,C1-C12烷基磺酰基,C1-C12卤代烷硫基,C1-C12卤代烷基亚磺酰基,C1-C12卤代烷基磺酰基,C1-C12链烯硫基,C2-C12链烯基亚磺酰基,C2-C12链烯基磺酰基,C2-C12卤代链烯硫基,C2-C12卤代链烯基亚磺酰基,C2-C12卤代链烯基磺酰基,C2-C12炔硫基,C2-C12炔基亚磺酰基,C2-C12炔基磺酰基,C1-C4烷氧基羰基-C1-C2烷硫基,C1-C4烷氧基羰基-C1-C2烷基亚磺酰基,C1-C4烷氧基羰基-C1-C2烷基磺酰基,C1-C8烷基-S(O)2NH,C1-C8卤代烷基-S(O)2NH,C1-C8烷基-S(O)2O,C1-C18烷基羰氧基,C2-C18链烯基羰氧基,C3-C6环烷基羰氧基,C1-C12烷氧基羰氧基,C1-C12烷硫基羰氧基,R16R17NC(O)O-,R16R17NC(S)O-,苄硫基,苄基亚磺酰基,苄基磺酰基,苯硫基,苯基亚磺酰基,苯基磺酰基,苯磺酰氧基或苯甲酰氧基,其中各苯基基团部分本身又可如权利要求1所述被取代;或者为基团Ar1-硫基,Ar1-亚磺酰基,Ar1-磺酰基,其中的Ar1为可以是芳香性或部分饱和的并且可以含有1-2个选自氮、氧和硫的杂原子的五-或六元单环环系,并且该环系本身又可如 1所述被取代;或者为噻吩基羰氧基或呋喃基羰氧基,这两个基团本身又可以被甲基或卤素取代,或者为其本身又可如权利要求1所述被取代的吡啶基羰氧基。
而且,在优选的式I化合物中,R10还为羟基或O-M+
必须强调的其它式I化合物为这些,其中W为氧,-CR11R12-或-C(O)-,特别是当W为-CR11R12-的情形下,a)R6为氢,甲基,乙基,氰基,甲氧基羰基,乙氧基羰基,甲硫基,甲亚磺酰基,甲磺酰基或甲氧基;并且R7、R8、R9、R11和R12彼此独立地为氢,C1-C4烷基,C1-C3卤代烷基,C2-C3链烯基或C2-C3炔基,或b)相邻的R6与R7和/或R8与R9一起表示-(CH2)m-,-C(O)O(CH2)2-或-S(O)n21(CH2)3-;或c)R6为氢,甲基,乙基,甲氧基羰基,乙氧基羰基,甲硫基,甲亚磺酰基,甲磺酰基或甲氧基,并且R12与R9一起表示-(CH2)o-的化合物。
此外,优选的数组式I化合物为这些化合物,其中:W为氧且R6、R7、R8和R9彼此独立地为氢或C1-C3烷基;或者W为-C(O)-且R6、R7、R8和R9彼此独立地为C1-C3烷基;或者R2为氢且R3为甲基;或者R2为甲基,乙基,正丙基,异丙基,乙烯基,甲氧基甲基,甲氧基羰氧基甲基,乙氧基羰氧基甲基,乙酰氧基甲基,丙酰氧基甲基,氯甲基,溴甲基,氟甲基,二氟甲基,三氟甲基或氰基甲基。
必须强调的其它式I化合物为这些化合物,其中R4为氢或甲基,或者R5为三氟甲基,二氟氯甲基,五氟乙基,七氟丙基或二氟甲基。
在另一组优选的式I化合物中,R3为氢,R2为C1-C4烷基,C1-C3卤代烷基,环丙基,C2-C3链烯基,C2-C3卤代链烯基,C2-C3炔基,丙二烯基(allenyl),C1-C2烷氧基-C1-C2烷基,C1-C2烷硫基-C1-C2烷基,氰基-C1-C2烷基,C1-C2烷氧基羰基-C1-C2烷基,C1-C4烷基羰氧基-C1-C2烷基,C1-C3烷氧基,C1-C3卤代烷氧基,烯丙氧基,炔丙氧基,C1-C3烷硫基,C1-C3烷基亚磺酰基或氰基。
其中Q为基团Q1的式I化物可以应用本领域公知的方法(例如EP-A-0353187和EP-A-0316491中所述的方法)制备,例如通过:a)在碱存在下,使式III化合物:
其中R2、R3、R4和R5具有式I给出的含义,且X为离去基团,例如卤素或氰基,与式II化合物在惰性有机溶剂中反应:
其中R6、R7、R8、R9和W具有式I给出的含义,生成式IV化合物:随后异构化后者,例如在碱和催化量的二甲氨基吡啶(DMAP)或氰化物源存在下进行;或者b)在碱和偶联剂存在下,使式XVI化合物:
Figure A9981578600322
其中R2、R3、R4和R5具有式I给出的含义与式II化合物在惰性有机溶剂中反应:
Figure A9981578600323
其中R6、R7、R8、R9和W具有式I给出的含义,生成式IV化合物:
Figure A9981578600324
随后如路线a)所述异构体后者。
下面的反应流程I详细说明了式I化合物的制备。反应流程1路线a):
Figure A9981578600331
路线b):
Figure A9981578600332
基团Q1中R10为羟基的式I化合物优选按照该反应流程进行制备。按照反应流程1,路线a)制备其中Q为基团Q1且R10为羟基的式I化合物用的起始物质为式III羧酸衍生物,其中X为离去基团例如卤素(如碘、溴、尤其是氯)、N-氧化邻苯二甲酰亚胺或N,O-二甲基羟基氨基或活化酯部分,例如(由二环己基碳二亚胺(DCC)与相应的羧酸形成)或
Figure A9981578600342
(由N-乙基-N′-(3-二甲氨基丙基)碳二亚胺(EDC)与相应的羧酸形成)。在碱例如烷基胺(优选三乙胺)或芳香胺(例如吡啶或4-二甲氨基吡啶(DMAP))存在下,这些式III化合物与式II二酮衍生物在惰性有机溶剂例如卤代烃(如二氯甲烷)、腈(如乙腈)、或芳烃(如甲苯)中反应,产生式IV的异构烯醇醚。该酯化反应在0℃-110℃下成功进行。
式IV的酯衍生物异构成式I二酮衍生物(其中R10为OH)的反应可以按照例如EP-A-0353187或EP-A-0316491的类似方法在碱和催化量DMAP或催化量的氰化物源(例如丙酮合氰化氢或氰化钾)存在下进行,其中的碱例如为烷基胺(如三乙胺)、碳酸盐(如碳酸钾)。这两步反应可以就地进行,无需分离中间体IV,特别是在使用式III氰化物(X=氰基)或者在有催化量丙酮合氰化氢或氰化钾存在的情况下更是如此。
按照反应流程1,路线b),所需的式I二酮化合物(其中R10为羟基)例如可以类似Chem.Lett.1975,1045所述制得,即在碱例如烷基胺(如三乙胺)和偶联剂(例如碘化2-氯-1-甲基吡啶鎓)存在下,在惰性溶剂例如卤代烃(如二氯甲烷)、腈(如乙腈)或芳烃(如甲苯)中用式II二酮衍生物酯化式XVI羧酸。依据所用溶剂,该酯化反应在0℃-110℃的温度下成功进行,并且如路线a)所述首先生成式IV的异构酯,后者可如路线a)所述进行异构化,例如在碱和催化量的DMAP,或氰化物源存在下,异构产生所需的式I二酮衍生物(R10=羟基)。
反应流程I(路线a)中的式III活化羧酸衍生物(其中X为离去基团,例如卤素(如溴、碘或者特别是氯))可用已知的标准方法制备,例如下列文献中所述的方法:C.Ferri“Reaktionen der organischenSynthese”[“有机合成反应”],Georg Thieme Verlag,Stuttgart,1978,p.460之后。该反应由下述反应流程2说明。反应流程2
Figure A9981578600351
按照反应流程2,其中X具有上述含义的式III化合物的制备例如使用卤化剂,例如亚硫酰卤(如亚硫酰氯或亚硫酰溴);卤化磷或磷酰卤(如五氯化磷或磷酰氯,或五溴化磷或三溴氧化磷);或草酰卤(如草酰氯),或使用能形成活化酯的式XVII的试剂,例如N,N′-二环己基碳二亚胺(DCC)或N-乙基-N′-(3-二甲氨基丙基)碳二亚胺(EDC)。作为卤化剂的式XVII化合物中的X含义实例为离去基团,例如卤素(如氟、溴或碘,特别是氯),并且W1例如为PCl2,SOCl,SOBr,或ClCOCO。
反应优选在催化量的N,N-二甲基甲酰胺存在下在惰性有机溶剂中于-20℃至反应混合物的回流温度下,优选在40-150℃进行,其中所述的惰性有机溶剂例如为脂族、卤代脂族、芳族或卤代芳族烃,如正己烷、苯、甲苯、二甲苯、二氯甲烷、1,2-二氯乙烷或氯苯。这类反应通常是已知的,并且各种不同的离去基团X在文献中均有记载。
其中R10不为羟基或卤素的式I化合物可以利用文献中公知的转化方法制备,例如以其中R10为羟基的化合物为原料,在适当碱存在下使用合适的酰氯通过酰化或甲氨酰化方法制备,或者通过对其中R10为卤素的式I氯化物进行亲核取代制备,而其中的式I氯化物也可以通过按照已知方法与氯化剂如光气、亚硫酰氯或草酰氯反应制得。在这种情况下,所用化合物的实例为适当取代的胺,或者直接为羟胺,或者为烷基磺酰胺、硫醇、硫酚类、酚类、Ar5-NH2或Ar1-SH,其中需要有碱如5-乙基-2-甲基吡啶、二异丙基乙胺、三乙胺、碳酸氢钠、乙酸钠或碳酸钾存在。
其中R10包含硫基的式I化合物可以按照与已知标准方法类似的方式,例如使用过酸(如间-氯过苯甲酸(m-CPBA)或过乙酸)氧化生成相应的式I砜和亚砜。硫原子的氧化程度(SO-或SO2-)可以根据氧化剂的用量加以控制。
所产生的其中R10不为羟基的式I衍生物同样也能够以各种异构形式存在,如果需要的话,可以分离它们成纯净形式。因此本发明还涉及所有这些立体异构体。这些异构体的实例为下面的式I*,I**和I***,其中Q为基团Q1(同样可参见上文第11页的说明与结构图)。
Figure A9981578600361
考虑到吡啶基或Q部分的化学性质,式I范围内的所有其它化合物均可以很容易地制得。
式I终产物的分离可以按照常规方式通过浓缩或蒸发溶剂,进而在它们难以溶解的溶剂如醚、芳烃或氯化烃中重结晶或研制固体残渣完成,或者通过蒸馏或利用柱色谱和适宜的洗脱剂完成。
另外,专业技术人员也都熟悉为避免副反应而适当进行的某些反应的次序。当没有进行分离纯净异构体的定向合成时,所得产物可以是两种或多种异构体的混合物。这些异构体可以用本领域公知的方法拆分。
其中n为1的式I化合物,亦即相应的式IN-氧化物,可以通过其中n为0的式I化合物与适当氧化剂(例如H2O2-脲加合物)在酸酐(如三氟乙酸酐)存在下反应合成。
其中R位于吡啶氮的邻位,并且代表1-氯-C1-C2烷基,1-羟基-C1-C2烷基,1-(C1-C6烷基羰氧基)-C1-C2烷基,1-苯甲酰氧基-C1-C2烷基,1-(C1-C4烷氧基羰氧基)-C1-C2烷基,1-(C1-C4烷硫基)-C1-C2烷基,1-(C1-C4烷基亚磺酰基)-C1-C2烷基,1-(C1-C4烷基磺酰基)-C1-C2烷基,1-氰硫基-C1-C2烷基,1-氰基-C1-C2烷基的式I化合物,还可以通过例如在已知反应条件下加热式I的N-氧化物制备,例如在甲苯磺酰氯存在下进行(参见例如Parham,W.E.;Sloan,K.B.;Reddy,K.R.;Olson,P.E.;JOrg Chem(有机化学杂志)1973,38,927),或者在酸酐存在下进行(参见例如Konno,K.;Hashimoto,K.;Shirahama,H.;Matsumoto,T.;Heterocycles 1986,24,2169),并且如果合适的话,随后进一步反应所得产物。这些反应次序可以用下述实例加以说明。
其中R位于吡啶氮的邻位,且尤其是代表1-溴-C1-C2烷基,1-氯-C1-C2烷基,1-氟-C1-C2烷基,1,1-二溴甲基,1,1-二氯甲基,甲酰基,1-(C1-C4烷硫基)-C1-C2烷基,1-(C1-C4烷基亚磺酰基)-C1-C2烷基,1-(C1-C4烷基磺酰基)-C1-C2烷基,1-氰硫基-C1-C2烷基或1-氰基-C1-C2烷基的式I化合物,也可以通过例如在已知的卤化反应条件下氧化其中R10尤其是氯、C1-C4烷氧基羰氧基或苯甲酰基羰氧基的式I化合物制备,例如在光和游离基引发剂(例如过氧化苯甲酰)存在下用N-溴代琥珀酰亚胺或N-氯代琥珀酰亚胺进行,生成1-溴或1-氯、1,1-二溴或1,1-二氯化合物,随后再次官能化后者,得到相应衍生物。这些反应次序也可以借助下列实例加以说明。
式I化合物还可以如下合成:在-100至-20℃(优选-70至-50℃)的温度下,在惰性溶剂(例如四氢呋喃)中使其中p为0而R2为C1-C6烷基的式I化合物与适当碱例如二异丙基氨化锂或正丁基锂反应,生成相应的双阴离子物。专业技术人员懂得如何通过亲电取代,例如使用氯甲酸酯来转化这些负碳离子物。这一反应次序可参照下述实例说明:
考虑到吡啶基或Q部分的化学性质,式I范围内的其它化合物可用适当的亲电子试剂制备。
式IIIa化合物是新的,并且具体讲这些化合物用于式I化合物的制备,因而它们构成了本发明的进一步主题:其中R501为C1-C6卤代烷基;R301为氢;R401为氢或C1-C6烷基;并且R201为C1-C6烷基,C1-C6卤代烷基-C1-C4烷基,C2-C6链烯基,C2-C6卤代链烯基,或C1-C2烷氧基羰基-或苯基-取代的乙烯基,C2-C6炔基或C2-C6卤代炔基;或者为三甲基甲硅烷基-、羟基-、C1-C2烷氧基-、C1-C2烷氧基羰基-或苯基-取代的乙炔基,或C3-C6二烯基;或者为C3-C6环烷基,卤代C3-C6环烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷基-S(O)n4-C1-C4烷基,氰基-C1-C4烷基,C1-C4烷氧基羰基-C1-C4烷基,C1-C4氰硫基,环氧乙烷基,C1-C4烷基氨基-C1-C4烷基,C1-C4二烷基氨基-C1-C4烷基,羟基-C1-C4烷基,C1-C12烷硫基羰基-C1-C4烷基或甲酰基-C1-C4烷基,或者R201为可以是芳香性或部分饱和的并且可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或稠合二环环系,所述环系经由C1-C4亚烷基、-CH=CH-、-C≡C-、-CH2O-、-CH2N(C1-C4烷基)-、-CH2S-、-CH2SO-或-CH2SO2-基团与吡啶环键连,且每一环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,巯基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C2-C5烷氧基烷硫基,C3-C5乙酰基烷硫基,C3-C6烷氧基羰基烷硫基,C2-C4氰基烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,二-(C1-C4烷基)氨基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素;以及X为卤素或氰基。
式XVIa化合物是新的,并因此构成了本发明的另一主题:其中R201,R301,R401和R501具有上述含义,但条件是当R501为三氟甲基、同时R301和R401均为氢时,则R201不为C1-C6烷基。
式Q1(或式II)的化合物是已知的,并且可以按照例如下列文献所述的类似方法制备:J.Org.Chem.(1977),42,1163-9,英国专利申请GB2205316,DE3902818,GB8706557,DE4434987,WO9213821和Aust.J.Chem.(1976),29(11),2525-31,Chem.Commun.(1998),(16),1691-1692.
式XVI(或XVIa和XVIb)的化合物按照与已知方法(例如Heterocycles,46,129(1997)或Helvetica Chimica Acta71,596(1988)中所述的方法)类似的方法合成,并且其特征在于:a)在碱例如芳香胺(如吡啶)存在下,用式VI化合物:
Figure A9981578600412
其中R501为C1-C6卤代烷基,酰化式V化物:
Figure A9981578600413
其中R301为氢;R401为氢,C1-C6烷基或苯基,其中苯基基团本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代;或者R401为可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或稠合二环环系,所述环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C1-C4烷氧基-C1-C2烷硫基,C1-C4烷基羰基-C1-C2烷硫基,C1-C4烷氧基羰基-C1-C2烷硫基,氰基-C1-C4烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素;以及R14为C1-C14烷基;生成式VII化合物:
Figure A9981578600421
其中R301,R401,R501和R14具有上述含义,然后在有机溶剂,例如卤代烃(如二氯甲烷)、腈(如乙腈)中,利用氨将其中的烷氧基交换为氨基。所得式VIII化合物:
Figure A9981578600422
随后与式IX化合物进行缩合反应:
Figure A9981578600431
其中R201为C1-C6烷基,C1-C6卤代烷基-C1-C4烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C3-C6环烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷基-S(O)n4-C1-C4烷基,氰基-C1-C4烷基,C1-C4烷氧基羰基-C1-C4烷基,C1-C4烷氧基羰氧基-C1-C4烷基,C1-C4氰硫基-C1-C4烷基,环氧乙烷基,C1-C4烷基氨基-C1-C4烷基,二(C1-C4)烷基氨基-C1-C4烷基或甲酰基-C1-C4烷基;或者R201为基团Ar6-C1-C4烷基,其中的Ar6为可以是芳香性或部分饱和的并且可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或稠合二环环系,其中每一环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,巯基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C2-C5烷氧基烷硫基,C3-C5乙酰基烷硫基,C3-C6烷氧基羰基烷硫基,C2-C4氰基烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,二-(C1-C4烷基)氨基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素,且R14具有上述含义,其后水解所生成的式Xa化合物:
Figure A9981578600432
得到式XVIa化合物:
Figure A9981578600441
其中R201,R301,R401和R501具有上述含义;或者b)使其中R14具有上述含义的式XI化合物:
Figure A9981578600442
与式XII化合物进行缩合反应:
Figure A9981578600443
并且氯化(例如使用POCl3)所生成的式XIII化合物:
Figure A9981578600444
其中R3,R4和R5具有上述含义,且R14为C1-C4烷基,得到式XIV化合物:
Figure A9981578600445
其中R3,R4,R5和R14具有上述含义,随后在碱存在下将这一化合物与式XV亲核试剂反应:
Z-R15(XV)其中Z为SH,OH或氨基,且R15为C1-C6烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,C1-C6烷基磺酰基,C1-C6卤代烷基,苯基或苄基,其中的苯基部分本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,或者为C1-C4烷氧基-C1-C4烷基,C1-C4烷硫基-C1-C4烷基,C1-C4烷基亚磺酰基-C1-C4烷基,C1-C4烷基磺酰基-C1-C4烷基,C1-C4烷基磺酰基或二-(C1-C4烷基)氨基磺酰基,或者R15为可以是芳香性或部分饱和的并且可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或稠合二环环系,其中每一环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,巯基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C2-C5烷氧基烷硫基,C3-C5乙酰基烷硫基,C3-C6烷氧基羰基烷硫基,C2-C4氰基烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,(CH2)nR7,NR8R9,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素,得到式Xb化合物:其中R14,R15,R3,R4,R5和Z具有上述含义,随后水解所得化合物,生成式XVIb的化合物:
Figure A9981578600461
其中R15,R3,R4,R5和Z具有上述含义。
其中Z-R15中的Z为氧且R15为C1-C6烷基,C3-C6链烯基,C3-C6炔基,C1-C6卤代烷基,C3-C6卤代链烯基,氰基-C1-C4烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷硫基-C1-C4烷基或C1-C4烷氧基羰基-C1-C4烷基的化合物也可以以XIII为起始原料通过用相应的烷基化剂L-R15XVa直接烷基化制备,其中的L为离去基团,如氯、溴、碘、甲磺酰氧基或甲苯磺酰氧基。
其中Z-R15为氟的式XVIb化合物的制备是在极性非质子传递溶剂例如乙腈、二甲基甲酰胺或环丁砜存在下由式XIV化合物与氟化钾以及,如果合适的话,催化量的18-冠-6反应完成。其中Z-R15为氢的式XVIc化合物则是通过在适当溶剂中还原式XIV中的氯基团制得,例如在适当金属催化剂存在下用氢还原或用甲酸铵还原。下面的反应流程3和4详细描述了式XVI或XVIa、XVIb和XVIc的化合物的制备。反应流程3
Figure A9981578600471
反应流程4
Figure A9981578600481
其中R2为溴甲基,氰基甲基,氰硫基甲基,C2-C6链烯基,C2-C6卤代链烯基,C1-C2烷氧基羰基-或苯基-取代的乙烯基,C2-C6炔基,C2-C6卤代炔基,三甲基甲硅烷基-、羟基-、C1-C2烷氧基-、C1-C2烷氧基羰基-或苯基-取代的乙炔基,C3-C6二烯基,C3-C6环烷基或单-或多-卤代C3-C6环烷基的式XVId化合物例如可以按照反应流程4a中所示的公知转化方法制备。反应流程4a
其中R501为CF2Cl的式XVIa中间体的制备如流程3所述,或者通过其中R501为三氯甲基的式Xa化合物与氢氟酸在加压容器中于0-220℃(优选60-200℃)的温度下反应完成。
其中R501为CHF2的式XVIa化合物可如流程3所述制备,或者按下所述制备:在催化量偶氮-异丁腈存在下,在惰性溶剂如甲苯或苯中于25-120℃(优选80-120℃)下加热式Xa化合物(其中R301、R401、R14和R201具有上述含义,且R501为CF2Cl)与三丁基氢化锡或1,1,1,3,3,3-六甲基-2-(三甲基甲硅烷基)丙硅烷,随后水解生成的化合物,得到其中R501为CHF2的式XVIa化合物。
其中R201、R301、R401和R501具有上述含义的式XVIa化合物也可以如下制备:通过亲核取代使其中R14、R301、R401和R501具有上述含义而R201为CH2Cl的式Xc化合物发生反应,例如使用碱金属碘化物在惰性溶剂中进行所述反应,生成相应的碘化物,或者使用气态氢溴酸在低级羧酸如冰乙酸中进行反应,得到相应的溴衍生物(例如按照US-3974166所述方法)或者使用碱金属氟化物在偶极溶剂如环丁砜中进行反应,得到相应的氟衍生物,或者,为了制备烷氧基基团Xd,在碱如氢化钠或碱土金属氧化物或碱土金属碳酸盐存在下使卤素衍生物Xc与醇或酚反应,或者直接与碱金属醇盐在惰性溶剂如二甲基甲酰胺中反应,或者在过量与要引入基团相对应的醇ROH存在下于-5至160℃下进行,或者,为了制备相应的芳香或脂族硫醚Xe,类似于上文所述,在-10-150℃下,在惰性溶剂中使卤化物Xc与脂族或芳族硫醇在碱如氢化钠存在下反应,或者与硫醇的碱金属盐反应,或者,为了制备相应的亚磺酰基或磺酰基衍生物Xe,在惰性溶剂如二氯甲烷中与氧化剂如间-氯过苯甲酸或高碘酸钠或过硼酸钠进行反应,其中温度的控制是本领域已知的,它取决于氧化的程度(例如,对于n=1,温度为-30℃-+50℃;而对于n=2,则温度为-20℃-+100℃),从而得到Xf,或者,为了制备式Xg的氰基亚甲基衍生物,使式Xc的卤化物与碱金属氰化物或四烷基氰化铵或氰化铜在惰性溶剂如二氯甲烷、四氢呋喃或二甲基甲酰胺中于0℃-220℃下反应。
式XVIa化合物(R501=CF2Cl)以及式Xc、Xd、Xe、Xf和Xg中间体的制备用下述反应流程5、6和7详细说明。反应流程5反应流程6
Figure A9981578600512
反应流程7
为了制备按照R201(Z-R15)-R501的定义而官能化的式X和XVI的所有其它化合物,多种已知的标准方法都是合适的,例如烷基化、卤化、酰化、酰胺化、肟化、氧化及还原,但适宜制备方法的选择取决于中间体中取代基的性质(反应性)。
形成式I化合物的反应宜在非质子传递惰性有机溶剂中进行。这类溶剂为烃例如苯、甲苯、二甲苯或环己烷,氯代烃如二氯甲烷、三氯甲烷、四氯化碳或氯代苯,醚如乙醚、乙二醇二甲醚、二甘醇二甲醚、四氢呋喃或二噁烷,腈如乙腈或丙腈,酰胺如N,N-二甲基甲酰胺、N,N-二乙基甲酰胺或N-甲基吡咯烷酮。反应温度优选为-20℃至+120℃。在某些情况下,反应是轻微放热的,通常它们可以在室温下进行。为了缩短反应时间或者为了起动反应,可以将反应混合物迅速加热到沸点。通过加入几滴碱作为反应催化剂同样可以缩短反应时间。合适的碱特别是叔胺例如三甲胺、三乙胺、喹宁环、1,4-二氮杂二环[2.2.2]辛烷、1,5-二氮杂二环[4.3.0]壬-5-烯或1,5-二氮杂二环[5.4.0]十一碳-7-烯。但是也可以使用无机碱例如氢化物如氢化钠或氢化钙、氢氧化物如氢氧化钠或氢氧化钾、碳酸盐如碳酸钠和碳酸钾、或碳酸氢盐如碳酸氢钾和碳酸氢钠作为碱。按照常规方式,通过浓缩和/或蒸发溶剂,可以分离出式I的化合物,并且可以通过重结晶或者在不易溶解的溶剂例如醚、芳香烃或氯代烃中研制固体残留物或而加以纯化。
就本发明的式I化合物或含有它们的组合物来说,使用它们的适宜方法包括所有农业上常规施用方法,例如芽前施用、芽后施用和种子处理以及各种方法和技术例如活性组分的受控释放。为此,使活性组份的溶液吸附到矿物颗粒载体或聚合物颗粒(脲/醛树脂)上,然后干燥。如果合适的话,可以另外包衣(包衣颗粒),使得活性组份能在特定的时间内以受控方式释出。
式I化合物可以以原有形式即合成得到形式用作除草剂。但优选将它们按常规方式与加工配制领域惯常使用的赋型剂一起配制成例如乳油、可直接喷洒或可稀释的溶液、稀乳液、可湿性粉剂、可溶性粉剂、撒粉剂、颗粒剂或微囊剂形式。例如在WO97/34485的第9-13页描述了这些制剂。根据预定目的和周围环境选择施用方法(例如喷洒、雾化、撒粉、湿润、散布或倾倒)以及组合物的类型。
制剂即包含式I活性组份或包含至少一种式I活性组分以及一种或多种固体或液体制剂用助剂的组合物、制品或产物可以按照常规方式制备,例如通过把活性组份与制剂用助剂如溶剂或固体载体致密混合和/或研磨。另外,在制备制剂时也可以使用表面活性化合物(表面活性剂)。例如在WO97/34485的第6页中给出的溶剂和固体载体实例。
根据所配制的式I活性组分的性质,合适的表面活性化合物是具有良好的乳化性、分散性和湿润性的非离子型、阳离子型和/或阴离子型表面活性剂和表面活性剂的混合物。
例如在WO97/34485的第7和8页中列出了合适的阴离子型、非离子型和阳离子型表面活性剂实例。
此外,特别是在“McCutcheon洗涤剂和乳化剂年报”(McCutcheon’s Detergents and Emulsifiers Annual)MC PublishingCorp.,Ridgewood New Jersey,1981,Stache,H.,“Tensid-Taschenbuch”[“表面活性剂指南”],Carl Hanser Verlag,Munich/Vienna,1981和M.和J.Ash,“表面活性剂大全”(Encyclopedia of Surfactants),Vol.I-III,Chemical PublishingCo.,New York,1980-81中描述的制剂加工技术中常用的表面活性剂也适用于配制本发明的除草组合物。
除草组合物一般含有0.1-99%重量、尤其是0.1-95%重量的除草剂,1-99.9%重量、尤其是5-99.8%重量的固体或液体加工助剂和0-25%重量特别是0.1-25%重量的表面活性剂。虽然更优选市售产品形式的浓缩物组合物,但最终使用者往往要使用稀释制剂。组合物还可以包含其它添加剂,例如稳定剂如环氧化或非环氧化的植物油(环氧化的椰子油、油菜油或大豆油)、消泡剂如硅油、防腐剂、粘度调节剂、结合剂、增粘剂以及肥料或其它活性组份。
通常,式I活性成分按0.001-4kg/公顷,特别是0.005-2kg/公顷的施用量施于植物或其周围环境。达到所需效果的需要剂量可以通过试验确定。它取决于作用的类型、栽培植物和杂草的发育阶段以及施用(地点、时间和方法),并且根据这些参数可以在很宽的范围内变化。
式I化合物具有优越的除草和抑制生长的性能,从而使得它们能够用于有用作物,特别是谷类、棉花、大豆、甜菜、甘蔗、栽培作物、油菜、玉米和稻,以及用于非选择性的杂草防除。“作物”应当理解为还包括利用常规繁殖方法或基因工程技术产生的能耐受除草剂的作物。要防除的杂草可以是单子叶或双子叶杂草,例如繁缕属、豆瓣菜属、剪股颍属、马唐属、燕麦属、狗尾草属、白芥属、黑麦草属、茄属、稗属、莞草属、雨久花属、慈姑属、雀麦属、看麦娘属、石茅高粱、筒轴茅属、莎草属、苘麻属、黄花稔属、苍耳属、苋属、藜属、番薯属、茼蒿属、猪殃殃属、堇菜属和婆婆纳属。
下列实施例用于更详细说明本发明,但本发明并不局限于此。制备实施例:实施例H1:制备3-羟基-4,4-二甲基-2-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-2-烯酮(化合物A2-B24):
将6.68g(0.0305mol)2-甲基-6-三氟甲基烟酸甲酯(按照Heterocycles,46,129(1997)中所述制得)溶于250ml甲醇/水(3∶1混合物),在22℃下分批加入1.92g(0.046mol)氢氧化锂水合物。22℃反应4小时后,将反应混合物倒入乙酸乙酯和2N盐酸内,水洗有机相三次,硫酸钠干燥并蒸发,进而用少量己烷研制残留物。过滤后得到5.69g(90%理论产率)2-甲基-6-三氟甲基烟酸,熔点147-149℃。
将所得2-甲基-6-三氟甲基烟酸(1.026g,0.005mol)溶于20ml草酰氯。加入三滴二甲基甲酰胺,回流混合物1小时。然后用旋转蒸发器浓缩混合物,并将残留物(2-甲基-6-三氟甲基烟酰氯)溶于100ml二氯甲烷。在0℃下加入1.6ml(0.0115mol)三乙胺和0.7g(0.005mol)4,4-二甲基环己烷-1,3-二酮。22℃下反应2小时后,利用真空旋转蒸发器除去溶剂,进而将残留物溶于55ml乙腈,加入0.15ml(0.0016mol)丙酮合氰化氢和0.79ml(0.0057mol)三乙胺使中间体发生重排反应。室温搅拌反应溶液4小时后进行蒸发。硅胶层析剩余的浆状物,以甲苯、乙醇、二噁烷、三乙胺以及水组成的混合物(100∶40∶20∶20∶5体积份)洗脱,得到浅黄色粘性油状物(Rf=0.39,上述混合物作为流动相),进而将其溶于二氯甲烷,依次用75ml 5%盐酸和75ml水洗涤。蒸发硫酸钠干燥过的有机溶液至干,得到1.05g(63%)纯净3-羟基-4,4-二甲基-2-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-2-烯酮,白色结晶体,熔点75-77℃。1H NMR(d6-DMSO,δin ppm):1.342,s,6H:2.088,t,J9Hz,2H:2.685,s,3H:2.982,t,J9Hz,2H:8.030,d,J8.1Hz,1H:8.094,d,(J,8.1Hz),1H.实施例H2:制备5-甲基-5-三氟甲基环己烷-1,3-二酮(化合物H-B1066):
往40ml乙醇中投入0.64g钠,接着加入3.23ml乙酰乙酸甲酯和4.9g 4,4,4-三氟-3-甲基丁-2-烯酸异丙酯,并在沸腾状态下加热混合物18小时。在将混合物分配到稀盐酸与乙酸乙酯之内后,蒸发混合物。剩余的2-甲基-4,6-二氧代-2-三氟甲基环己烷羧酸甲酯粗品进而在9.1g氢氧化钠存在下于甲醇与水的混合液中沸腾水解。混合物随后用盐酸酸化,并用新鲜乙酸乙酯提取。经重结晶(乙酸乙酯)后得到纯净5-甲基-5-三氟甲基环己烷-1,3-二酮,熔点150-152℃。实施例H3:制备2-羟基-1-甲氧基-5-甲基-4-氧代环己-2-烯羧酸甲酯(实施例H-B1069):
向65ml二甲亚砜中加入30%35.8g甲醇钠溶液,接着在30-35℃、20分钟内用16.7g 3-甲基-3-丁烯-2-酮和32.4g甲氧基丙二酸二甲酯处理。35℃搅拌混合物1小时,然后用盐酸酸化,并用二氯甲烷重复提取。水洗有机相,然后干燥并浓缩。用热乙酸乙酯和己烷结晶得到2-羟基-1-甲氧基-5-甲基-4-氧代环己-2-烯羧酸甲酯纯品,熔点117-117.5℃。实施例H4:制备2-羟基-1-甲氧基-5-甲基-3-(2-甲基-6-三氟甲基吡啶-3-羰基)-4-氧代环己-2-烯羧酸甲酯(化合物A2-B1069):
向2.14g 2-羟基-1-甲氧基-5-甲基-4-氧代环己-2-烯羧酸甲酯和2.02g三乙胺在30ml乙腈中的混合物内加入2.23g新鲜2-甲基-6-三氟甲基烟酰氯。大约30分钟后,加入0.065g氰化钾,搅拌混合物18小时。在pH为2的情形下,将混合物随后分配到水与乙酸乙酯之间,硫酸镁干燥并蒸发。硅胶过滤(流动相:乙酸乙酯/甲醇/三乙胺85∶10∶5)得粘性油状2-羟基-1-甲氧基-5-甲基-3-(2-甲基-6-三氟甲基吡啶-3-羰基)-4-氧代环己-2-烯羧酸甲酯纯品。实施例H5:制备3-羟基-4-甲氧基-6-甲基-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-2-烯酮(化合物A2-B1070):
用0.586g氢氧化钾处理1.4g 2-羟基-1-甲氧基-5-甲基-3-(2-甲基-6-三氟甲基吡啶-3-羰基)-4-氧代环己-2-烯羧酸甲酯的二噁烷/水(5∶3)溶液,并搅拌所得混合物3小时。随后酸化混合物(pH3),用新鲜乙酸乙酯提取。类似实施例H4所述,将粗产物通过色谱纯化。得到3-羟基-4-甲氧基-6-甲基-2-(2-甲基-6-三氟甲基-吡啶-3-羰基)环己-2-烯酮粘性油状物(根据1H-NMR,它为3种互变异构体的混合物)。实施例H6:5-氯-2,2,6,6-四甲基-4-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-4-烯-1,3-二酮(化合物A2-B1105)和6-[氯-(2-甲基-6-三氟甲基吡啶-3-基)亚甲基]-2,2,4,4-四甲基环己烷-1,3,5-三酮:
向18.5g(50mmol)5-羟基-2,2,6,6-四甲基-4-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-4-烯-1,3-二酮(化合物A2-B354)在50ml二氯甲烷中的溶液内加入7.0g(55mmol)草酰氯;接着加入5滴二甲基甲酰胺,缓慢加热混合物至沸点。大约30分钟后,在不再有气体逸出的情形下蒸发混合物,产物通过加正己烷结晶。所得主产物为纯净的5-氯-2,2,6,6-四甲基-4-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-4-烯-1,3-二酮,m.p.119.5-120℃。进一步通过HPLC分离母液(使用5-10%乙酸乙酯/己烷),得到异构体6-[氯-(2-甲基-6-三氟甲基吡啶-3-基)亚甲基]-2,2,4,4-四甲基环己烷-1,3,5-三酮,m.p.92.5-93℃。实施例H7:5-氯-2,2,6,6-四甲基-4-(2-甲基-1-氧-6-三氟甲基吡啶-3-羰基)环己-4-烯-1,3-二酮(化合物A1210-B1105):
-10℃下,在20ml二氯乙烷中用0.94g(10mmol)过氧化氢/脲加合物和1.89g(9mmol)三氟乙酸酐处理1.94g(5mmol)5-氯-2,2,6,6-四甲基-4-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-4-烯-1,3-二酮。搅拌下,温热反应混合物至室温,在这一温度下进一步保持4小时。然后将混合物分配到乙酸乙酯与pH为5的水之间,用氯化钠溶液洗涤并蒸发。通过硅胶过滤得到的残留物为纯净的5-氯-2,2,6,6-四甲基-4-(2-甲基-1-氧-6-三氟甲基吡啶-3-羰基)环己-4-烯-1,3-二酮,熔点145.5-146℃。实施例H8:4-(2-溴甲基-6-三氟甲基吡啶-3-羰基)-5-氯-2,2,6,6-四甲基环己-4-烯-1,3-二酮(化合物A1029-B1105):
在催化量过氧化二苯甲酰存在下,在10ml四氯化碳中回流0.39g(1mmol)5-氯-2,2,6,6-四甲基-4-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-4-烯-1,3-二酮与0.20g(1.1mmol)N-溴代琥珀酰亚胺。反应平息之后,滤除所产生的琥珀酰亚胺,将粗产物通过柱色谱纯化(流动相:乙酸乙酯/己烷1∶4)。从而得到4-(2-溴甲基-6-三氟甲基吡啶-3-羰基)-5-氯-2,2,6,6-四甲基环己-4-烯-1,3-二酮纯品,熔点94.5-95℃。实施例H9:乙酸2-(2-乙酰氧基甲基-6-三氟甲基吡啶-3-羰基)-4,4,6,6-四甲基-3,5-二氧代环己-1-烯基酯(化合物A1099-B1107):
在3ml乙酐存在下,回流0.4g(1mmol)5-氯-2,2,6,6-四甲基-4-(2-甲基-1-氧-6-三氟甲基吡啶-3-羰基)环己-4-烯-1,3-二酮(实施例H7)25分钟。然后浓缩混合物,进而分配到乙酸乙酯与pH为6.5的碳酸氢钠溶液之间。将粗产物通过硅胶加以分离(流动相:乙酸乙酯/己烷1∶4),从而得到油状乙酸2-(2-乙酰氧基甲基-6-三氟甲基吡啶-3-羰基)-4,4,6,6-四甲基-3,5-二氧代环己-1-烯基酯纯品,1H-NMR(CDCl3):7.98d,CH,7.72d,CH,5.62s,CH2,2.22和2.202x OAc,1.58,s,2x CH3,1.44ppm,s,2x CH3.实施例H10:5-羟基-2-甲基-4-(2-甲基-6-三氟甲基吡啶-3-羰基)-二环[4.1.0]庚-4-烯-3-酮(化合物A2-D109)和3-羟基-7-甲基-2-(2-甲基-6-三氟甲基吡啶-3-羰基)环庚-2.6-二烯酮(化合物A2-F5):
室温下,在2∶1的二噁烷/水混合液中搅拌0.82g(2mmol)反式-5-羟基-2-甲基-4-(2-甲基-6-三氟甲基吡啶-3-羰基)-3-氧代二环[4.1.0]庚-4-烯-2-羧酸乙酯(化合物A2-D111)与0.254g(4.5mmol)氢氧化钾至所有起始原料反应完全为止。然后加入乙酸乙酯,用4N HCl酸化混合物至pH3,在40℃下加热该两相混合物大约1小时。水相用氯化钠饱和,然后分离弃之。蒸发乙酸乙酯提取物至干,硅胶层析所得产物(流动相:乙酸乙酯/己烷1∶2)。分离得到的第一个馏分为3-羟基-7-甲基-2-(2-甲基-6-三氟甲基吡啶-3-羰基)环庚-2,6-二烯酮,为纯净的互变异构体混合物,1H-NMR(CDCl3):17.72和17.08,2s,OH,7.6-7.45,2芳香H,6.68和6.62,2t,CH,2.84,m,2.63,m,2.52,m,4H,2.62和2.54,2s,CH3,2.03和1.77ppm,2s,CH3.随后用100%乙酸乙酯洗脱,得到第二个馏分,即5-羟基-2-甲基-4-(2-甲基-6-三氟甲基吡啶-3-羰基)二环[4.1.0]庚-4-烯-3-酮的异构体和互变异构体混合物,1H-NMR(CDCl3):尤其为17.62和17.48,2s,OH,7.6-7.45,2芳香H,2.54,m,2.48,2s CH3,1.22和1.14,2d,CH3,1.00-0.05ppm,2H.实施例H11:5-羟基-2-甲亚磺酰基-2-甲基-4-(2-甲基-6-三氟甲基吡啶-3-羰基)二环[4.1.0]庚-4-烯-3-酮(化合物A2-D114):
在0.56g高碘酸钠存在下,50℃温热0.87g(2.3mmol)5-羟基-2-甲基-2-甲硫基(methylsulfanyl)-4-(2-甲基-6-三氟甲基吡啶-3-羰基)二环[4.1.0]庚-4-烯-3-酮(化合物A2-D113)在8ml甲醇中的溶液3小时。然后将混合物分配到乙酸乙酯与氯化钠溶液之间,浓缩,并将粗产物通过色谱纯化(流动相:乙酸乙酯/甲醇19∶1)。得到纯净的5-羟基-2-甲亚磺酰基-2-甲基-4-(2-甲基-6-三氟甲基吡啶-3-羰基)二环[4.1.0]庚-4-烯-3-酮,为互变异构体与异构体混合物,熔点159.5-160℃.实施例H12:2-丙-2-炔基氧基-6-三氟甲基烟酸(化合物A1025):
在催化量18-冠-6醚存在下,在40ml二甲基甲酰胺与80ml乙腈的混合液中加热47g(0.2mol)2-氧代-6-三氟甲基-1,2-二氢吡啶-3-羧酸、20ml(0.25mol)炔丙基溴和43g(0.31mol)碳酸钾到75℃。5小时后,将混合物分配到乙酸乙酯与氯化钠饱和溶液之间。粗产物通过硅胶柱过滤(使用15%乙酸乙酯/己烷)。所得油状形式的主要组分为纯净2-丙-2-炔基氧基-6-三氟甲基烟酸乙酯;1H-NMR(CDCl3):8.31,d,CH,7.38,d,CH,5.13,d,CH2,4.41,q,CH2,2.48,t,CCH,1.41 ppm,t,CH3.
将36.3g(0.13mol)该产物与11.5g(0.17mol)氢氧化钾在50ml水与50ml二噁烷中的溶液一同搅拌16小时。经酸化及乙酸乙酯提取之后,得到结晶2-丙-2-炔基氧基-6-三氟甲基烟酸;1H-NMR(CDCl3):10.0,b,OH,8.53,d,CH,7.44,d,CH,5.22,d,CH2,2.54ppm,t,CCH.实施例H13:2-甲硫基-6-三氟甲基烟酸(化合物A15):
35℃下,将9.4g(40mmol)2-氧代-6-三氟甲基-1,2-二氢吡啶-3-羧酸加到21.7g三溴化磷(80mmol)的1M二氯甲烷溶液内。然后蒸除溶剂,缓慢加热反应混合物至沸点(大约175℃)。18小时后,冷却化合物到0℃,加二氯甲烷稀释,并与pH1.8的冰水一同搅拌。然后用碳酸钠冷溶液以及15%氯化钠溶液洗涤有机相,硫酸镁干燥并浓缩。残留物为2-溴-6-三氟甲基烟酸乙酯油状物;1H-NMR(CDCl3):8.20,d,CH,7.72d,CH,4.46,q,CH2,1.42ppm,t,CH3,熔点164-166℃。
将1.0g(3.4mmol)该产物溶于少量乙腈,在催化量15-冠-5醚存在下与0.26g甲硫醇钠(3.4mmol)一起加热45分钟到70℃。然后将已冷却至室温的溶液用0.22g(5.5mmol)氢氧化钠和5ml水处理,继续搅拌3小时。随后用少量乙醚除去中性组分,调节水相的pH到2.5,用乙酸乙酯提取两次。由此得到2-甲硫基-6-三氟甲基烟酸结晶产物;1H-NMR(CDCl3):8.46,d,CH,7.43,d,CH,2.58ppm,s,SCH3.实施例H14:2-甲磺酰基氨基-6-三氟甲基烟酸(化合物A1203):
向0.24g 55%氢化钠/油的四氢呋喃悬浮液内加入0.52g甲磺酰胺。待氢气逸出停止后,加入1.5g(5mmol)2-溴-6-三氟甲基烟酸乙酯、0.3g(5.2mmol)氟化钾和催化量冠醚以及5ml N-甲基吡咯烷酮,在沸腾状态下加热混合物18小时。然后将反应混合物分配到乙酸乙酯与水之间,除去有机中性组分。调节水相的pH至2.9,用新鲜乙酸乙酯提取三次,干燥并浓缩。自乙醚/己烷中得到结晶产物2-甲磺酰基氨基-6-三氟甲基烟酸乙酯;1H-NMR(CDCl3):10.48,s,NH,8.49,d,CH,7.38,d,CH,4.45,q,CH2,3.51,s,SO2CH3,1.42ppm,t,CH3.
利用0.22g(3.9mmol)氢氧化钾在二噁烷/水1∶1中的溶液室温水解0.43g(1.4mmol)上述产物。然后将溶液酸化至pH2.5,用乙酸乙酯提取处理,从而得到2-甲磺酰基氨基-6-三氟甲基烟酸结晶;1H-NMR(d6-DMSO):8.62,d,CH,7.72,d,CH,3.52ppm,s,SO2CH3.实施例H15:溴化(3-甲氧基羰基-6-三氟甲基吡啶-2-基甲基)三苯基磷鎓:
在催化量α,α-偶氮(aza)异丁腈存在和150瓦的灯照射下,将50g(0.23mol) 2-甲基-6-三氟甲基烟酸甲酯和49g(0.28mol)N-溴代琥珀酰亚胺在500ml四氯化碳中50℃加热90分钟。滤去沉淀出的琥珀酰亚胺,然后利用柱色谱(流动相:乙酸乙酯/己烷1∶15)分离得到主要组分2-溴甲基-6-三氟甲基烟酸甲酯产物,1H-NMR(CDCl3):4.01,s,3H;5.03,s,2H;7.72,d(J8.2Hz),1H;8.43ppm,d,(J8.2Hz),1H.将25.6g(35mmol)上述产物溶于甲苯,用10.6g(40mmol)三苯膦处理。沸腾加热混合物2小时后,冷却得到纯净的溴化(3-甲氧基羰基-6-三氟甲基吡啶-2-基甲基)三苯基磷鎓晶体,熔点215-217℃.实施例H16:2-乙烯基-6-三氟甲基烟酸(化合物A21)和2-(2,2-二氯环丙基)-6-三氟甲基烟酸(化合物A1092):
室温下,将5.7g(10mmol)溴化(3-甲氧基羰基-6-三氟甲基吡啶-2-基甲基)三苯基磷鎓溶于25ml氯仿与2.1g(20mmol)碳酸钠构成的两相体系,在10ml水存在下与1.7g(20mmol)甲醛的35%水溶液反应。1.5小时后,分出有机相并通过硅胶过滤。得到2-乙烯基-6-三氟甲基烟酸甲酯油状物,1H-NMR(CDCl3):8.31,d,CH,7.10,dd,CH,7.09,d,CH,6.68,dd,CH,5.68,dd,CH,3.97ppm,s,OCH3.
取0.97g(4.1mmol)该产物再次溶于氯仿,在剧烈搅拌和有90mg溴化苄基三甲铵存在下与6ml 50%氢氧化钠溶液反应。20小时后,分出有机相,浓缩并通过HPLC纯化(流动相:乙酸乙酯/己烷1∶4)。从而得到2-(2,2-二氯环丙基)-6-三氟甲基烟酸甲酯纯品,1H-NMR(CDCl3):8.50,d,CH,7.70,d,CH,4.08,s,OCH3,3.68,dd,CH,2.64,dd,CH,2.05ppm,dd,CH.
水解上述酯,从而得到2-乙烯基-6-三氟甲基烟酸,1H-NMR(CDCl3):8.40,d,CH,7.22,dd,CH,7.09,d,CH,6.68,dd,CH,5.58ppm,dd,CH,和2-(2,2-二氯环丙基)-6-三氟甲基烟酸,1H-NMR(CDCl3):8.64,d,CH,7.23,d,CH,3.78,dd,CH,2.67,dd,CH,2.08ppm,dd,CH.实施例H17:2-丙-1,2-二烯基-6-三氟甲基烟酸(A1096)和2-(3-氯丙烯基)-6-三氟甲基烟酸(化合物A1095):
剧烈搅拌下,使6.7g(11mmol)溴化((3-甲氧基羰基-6-三氟甲基吡啶-2-基)甲基)三苯基磷鎓与2ml 45%氯乙醛水溶液(14mmol)和1.5g(14mmol)碳酸钠在20ml氯仿与7ml水构成的两相体系中反应。2小时后,分出有机溶液,用半饱和氯化钠溶液洗涤。产物通过硅胶分离(流动相:乙酸乙酯/己烷1∶4)。分离得到的第一馏分为2-丙-1,2-二烯基-6-三氟甲基烟酸甲酯,1H-NMR(CDCl3):7.62,m,CH,7.55,d,CH,7.32,d,CH,7.04,d,CH,7.02,m,CH,3.98ppm,s,OCH3,分离得到的第二馏分为2-(3-氯丙烯基)-6-三氟甲基烟酸甲酯,1H-NMR(CDCl3):8.85,d,CH,7.65,dd,7.58,d,CH,CH,7.28,dd,CH,4.32,d,CH2Cl,3.98ppm,s,OCH3.
水解上述酯,得到2-丙-1,2-二烯基-6-三氟甲基烟酸,m.p.194-196℃,和2-(3-氯丙烯基)-6-三氟甲基烟酸,m.p.137-138℃.实施例H18:2-氯-4-甲基-6-三氟甲基烟酸(化合物A1205):
在加压容器中,在5.8ml二氯磷酸苯酯存在下170℃加热7.5g(0.03mol)(3-乙氧基羰基)-4-甲基-6-三氟甲基)-吡啶-2-酮3小时。冷却后,反应溶液直接通过短硅胶柱过滤(流动相:乙酸乙酯/己烷1∶9),得到油状产物2-氯-4-甲基-6-三氟甲基吡啶-3-基乙基酯。在氢氧化钾水溶液存在下,在二噁烷中40℃水解后者。酸化至pH2.7后,用乙酸乙酯提取,得2-氯-4-甲基-6-三氟甲基烟酸结晶产物:1H-NMR(CDCl3):9.55,b,OH,7.55,s,1H;3.80,s,CH3,2.56ppm.s.CH3.实施例H19:4-甲基-6-三氟甲基烟酸(化合物A531):
向0.55g 10% Pd/C在20ml甲醇中的悬浮液内加入3.0g(16.8mmol)2-氯-4-甲基-6-三氟甲基吡啶-3-基乙基酯,并分两批加入总量为5g的甲酸铵,然后室温搅拌混合物24小时。反应混合物随后通过Celite过滤,分配到乙酸乙酯与氯化钠溶液之内。层析纯化(流动相1∶9)得到油状形式4-甲基-6-三氟甲基吡啶-3-基乙基酯:按照上述方法水解得到4-甲基-6-三氟甲基烟酸:1H-NMR(CDCl3):9.32,s,1H,7.62,s,1H,2.79ppm,s,CH3.实施例H20:5-甲基-5-甲硫基二环[4.1.0]庚烷-2,4-二酮(化合物H-D113):
0℃下,向13.4g(0.1mol)2-甲基巯基丙酸甲酯的30ml四氢呋喃溶液中加入1M双(三甲基甲硅烷基)氨化锂(16.7g,0.1mol)的四氢呋喃溶液。搅拌化合物1小时后,在20分钟内逐滴加入11.8g(0.1mol)5-氯戊-3-烯-2-酮,加料期间应保证温度仍为0℃。进一步搅拌混合物30分钟后,加入冰水,混合物用盐酸酸化,进而用乙酸乙酯提取。层析粗产物(乙酸乙酯/己烷15/85)。从而得到2-(2-乙酰基环丙基)-2-甲硫基丙酸甲酯,1H-NMR(CDCl3):3.74,s,OCH3,2.19和2.14,2s,SCH3,2.12.和2.00,2s,CH3,2.2-1.9,1H,1.3,s,CH3,1.3-1.0ppm,2H,系3∶7异构体混合物。
将2.45g(11mmol)富含高极性异构体的上述产物与溶在甲苯/二甲基甲酰胺19∶1混合物中的4.5g(25mmol)30%乙醇钠溶液一起115℃加热90分钟。混合物然后吸收到乙酸乙酯内,用pH3的稀盐酸洗涤。分离出的残留物通过硅胶纯化(流动相:乙酸乙酯/己烷1∶2)。从而得到异构体I5-甲基-5-甲硫基二环[4.1.0]庚烷-2,4-二酮,1H-NMR(CDCl3):3.48,d,CH,3.00,d,CH,2.21,m,CH,1.94,m,CH,1.86,s,CH3,1.57,s,CH3,1.44,m,CH,1.04ppm,m,CH。
由富含非极性异构体的产物得到异构体II5-甲基-5-甲硫基二环[4.1.0]庚烷-2,4-二酮,1H-NMR(CDCl3):3.78,d,CH,3.14d,CH,2.22,m,CH,1.93,m,CH,2.08,s,CH3,1.58,s,CH3,1.6-1.4ppm,2H.实施例H21:4-甲基环庚-4-烯-1,3-二酮(化合物H-F5):
在5g阮氏镍存在下,将1.0g(5.4mmol)5-甲基-5-甲硫基二环[4.1.0]庚烷-2,4-二酮异构体II在15ml甲醇中常压氢化90分钟。浓缩混合物并通过硅胶纯化(流动相:乙酸乙酯/己烷1∶1),得到4-甲基环庚-4-烯-1,3-二酮油状物,1H-NMR(CDCl3):6.84,m,CH,3.94,s,CH2,2.77,m,CH2,2.59,m,CH2,1.88ppm,s,CH3.实施例H22:2-氧杂螺[4.5]癸烷-1,6,8-三酮(化合物H-E16):
冷却氢化钠(55%油分散物,27.5mmol)在70ml无水四氢呋喃中的悬浮液到-20℃,随后逐滴加入2-酰基丁内酯(2.69ml,25mmol)的5ml四氢呋喃溶液。在此温度下搅拌反应混合物1小时后,于-20℃滴加丙烯酸甲酯(4.5ml,50mmol)的四氢呋喃溶液进行处理。其后温热反应混合物至室温,搅拌8小时。混合物然后倒入冰水内,用2N盐酸酸化至pH1。经乙酸乙酯提取、硫酸钠干燥和真空浓缩后,将产物通过快速色谱纯化(洗脱剂:乙酸乙酯/乙酸1∶1)。从而得到白色粉末形式2-氧杂螺[4.5]癸烷-1,6,8-三酮,熔点145-148℃.实施例H23:螺[2.5]辛烷-4,6-二酮(化合物H-Cl):
将3.4g氢化钠(55%油悬浮物,78.0mmol)加到11叔丁醇内,室温搅拌此混合物数分钟。然后加入2-酰基丁内酯(100g,0.78mol),反应混合物在大约30℃下用丙烯酸甲酯(67.2g,0.78mmol)处理3.5小时。将反应混合物吸收到乙醚内,依次用75ml磷酸二氢钠饱和溶液、水以及氯化钠饱和溶液洗涤,硫酸钠干燥并浓缩。从而得到162g无色油状物3-(3-乙酰基-2-氧代四氢呋喃-3-基)丙酸甲酯,该产物无需进一步纯化可直接使用。
将2.0g(9.3mmol)上述产物和2.1g碘化钠(14.0mmol)溶于10ml1,3-二甲基-2-咪唑烷酮,210℃加热此溶液3小时。冷却后,将反应混合物倒入磷酸二氢钠稀水溶液内,用乙醚提取,硫酸钠干燥并浓缩。从而得到3-(1-乙酰基环丙基)丙酸甲酯无色油状物。
将74.5g 3-(1-乙酰基环丙基)丙酸甲酯(0.32mol)溶于11四氢呋喃,并将该溶液在室温下用14.3g氢化钠(55%油悬浮物,0.32mol)分批处理。1小时后,反应混合物用200ml二甲基甲酰胺稀释,然后温热到70℃。8小时后,真空除去四氢呋喃,残留物倒入2N盐酸内,用乙醚提取。硫酸钠干燥有机相并浓缩,经硅胶柱层析(二氯甲烷∶甲醇9∶1作为洗脱剂)得到螺[2.5]辛烷-4,6-二酮,系白色结晶,熔点116-118℃。实施例H24:2-(4,6-二甲氧基嘧啶-2-基硫基甲基)-6-三氟甲基烟酸(化合物A1088):
在30ml乙腈和1.63g(11.83mmol)K2CO3中加入2.0g(7.89mmol)2-氯甲基-6-三氟甲基烟酸甲酯(类似Heterocycles,46,129(1997)所述,在三氟乙酸存在下,在甲苯中加热4-氯-3-氧代丁酸甲酯与4-氨基-1,1,1-三氟丁-3-烯-2-酮制得),与1.49g(8.67mmol)4,6-二甲氧基嘧啶-2-硫醇在室温下反应。4小时后,将混合物倒入乙酸乙酯/水中,移出乙酸乙酯相,水相用乙酸乙酯再提取。合并的乙酸乙酯相用硫酸钠干燥,浓缩并在乙酸乙酯/己烷中重结晶,从而得2-(4,6-二甲氧基嘧啶-2-基硫基甲基)-6-三氟甲基烟酸甲酯白色结晶,熔点123-124℃。
水解(类似实施例H1)上述酯,从而得到白色结晶2-(4,6-二甲氧基嘧啶-2-基硫基甲基)-6-三氟甲基烟酸,熔点157-158℃。1H-NMR(CDCl3):3.96,s,6H;3.99,s,3H;5.03,s,2H;5.72,s,1H;7.66,d(J,8.1Hz),1H;8.40ppm,d(J,8.1Hz),1H.实施例H25:2-氰基甲基-6-三氟甲基烟酸(化合物A1103):
在270mg四丁基硫酸氢铵存在下,使2.0g(7.89mmol)2-氯甲基-6-三氟甲基烟酸甲酯与565mg(8.67mmol)氰化钾在20ml乙腈/水混合液(1∶1)中反应。反应结束后,将混合物倒入水中,用乙酸乙酯提取。乙酸乙酯相用硫酸钠干燥,浓缩后得到的粗产物进而用HPLC纯化(乙酸乙酯∶己烷为洗脱剂)。从而得到610mg(32%理论产率)2-氰甲基-6-三氟甲基烟酸甲酯油状物。1H-NMR(CDCl3):3.96,s,3H;4.38,s,2H;7.72,d(J,8.1Hz),1H;8.48ppm,d(J,8.1Hz),1H.
采用上文早已描述过的类似方法进行水解,从而得到2-氰甲基-6-三氟甲基烟酸黄色晶体,熔点152-153℃。1H-NMR(CDCl3):4.18,s,2H;7.72,d(J,8.1Hz),1H;8.52ppm,d(J,8.1Hz),1H.实施例H26:3-(6-二氟甲基-2-甲基吡啶-3-羰基)-2-羟基-1-甲基-4-氧代环己-2-烯羧酸甲酯(化合物A124-B34):
在0.18ml(0.62mmol)三(三甲基甲硅烷基)硅烷存在下,在8ml甲苯中于120℃加热200mg(0.516mmol)3-[6-(氯二氟甲基)-2-甲基吡啶-3-羰基]-2-羟基-1-甲基-4-氧代环己-2-烯羧酸甲酯(化合物A94-B34)3小时。硅胶层析剩余的粘性残留物。将用甲苯、乙醇、二噁烷、三乙胺与水的混合液(100∶40∶20∶20∶5,体积比)洗脱得到的浅黄色粘性油状物溶于二氯甲烷,依次用盐酸水溶液和水洗涤。蒸发经硫酸钠干燥后的有机溶液,得140mg(73%)3-(6-二氟甲基-2-甲基吡啶-3-羰基)-2-羟基-1-甲基-4-氧代环己-2-烯羧酸甲酯纯品,系浅黄色油状物。1H-NMR(CDCl3):1.28,s,3H;1.79-1.97,m,1H;2.39-2.46,m,1H;2.43,s,3H;2.69,dt(J,19.2和4.8Hz),1H;2.82-2.92,m,1H;3.67,s,3H;6.55,t,(J,55.5Hz),1H;7.43,d(J,7.8Hz),1H;7.49,d(J,7.8Hz),1H;17.20ppm,br s,1H.实施例H27:3-羟基-2-(2-甲基-1-氧-6-三氟甲基吡啶-3-羰基)环己-2-烯酮(化合物A1210-B1):
将16.1g(0.054mol)3-羟基-2-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-2-烯酮(实施例A2-B1)和10.2g(0.11mol)脲/过氧化氢复合物溶于150ml二氯甲烷,随后在25℃下加入22.1ml(0.162mol)三氟乙酸酐。25℃搅拌反应混合物14小时后,倒入乙酸乙酯和水中,水洗有机相两次,硫酸钠干燥并浓缩。硅胶层析残留物(洗脱剂∶乙酸乙酯/甲醇9/1)。得到2.4g(14%)所需产物,白色结晶(m.p.117-119℃).
1H-NMR(d6-DMSO):1.98,m,2H;2.30,s,3H;2.60,t(J,7.25Hz),4H:7.32,d(J,9.8Hz),1H;7.92ppm,d(J,9.8Hz),1H.实施例H28:2-(2-甲基-6-三氟甲基吡啶-3-羰基)-3-苯硫基环己-2-烯酮(化合物A2-B1102):
将4.0g(0.0134mol)3-羟基-2-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-2-烯酮(化合物A2-B1)悬浮于25ml草酰氯,随后逐滴加入0.1ml二甲基甲酰胺。待大量气体逸出停止后,在45℃浴温下保持混合物1.5小时,其后浓缩,并将残留物(3-氯-2-(2-甲基-6-三氟甲基吡啶-3-羰基)-环己-2-烯酮)溶于60ml二氯甲烷。在0-5℃下加入三乙胺(3.7ml,0.0268mol)、二甲氨基吡啶(160mg,1.34mmol)以及1.5ml(0.0147mol)苯硫酚。22℃反应20小时后,浓缩反应混合物,进而通过硅胶纯化(己烷/乙酸乙酯5∶1)。用己烷研制得纯净2-(2-甲基-6-三氟甲基吡啶-3-羰基)-3-苯硫基环己-2-烯酮,白色结晶体,熔点124-125℃.1H-NMR(CDCl3):1.99,m,2H;2.41,m 4H;2.80,s,3H;2.60:7.40-7.60,m,6H;7.80ppm,d(J,8.2Hz),1H.实施例H29:3-苯磺酰基-2-(2-甲基-6-三氟甲基吡啶-3-羰基)环己-2-烯酮(化合物A2-B1104):
将上面得到的0.8g(0.00204mol)2-(2-甲基-6-三氟甲基吡啶-3-羰基)-3-苯硫基环己-2-烯酮溶于30ml二氯甲烷,随后在25℃逐滴加入1.39ml过乙酸(39%乙酸,0.00816mol)。25℃反应4小时后,将反应混合物倒入乙酸乙酯与水内,水洗有机相,硫酸钠干燥并浓缩,残留物用少量己烷和乙酸乙酯研制。过滤得到0.72g(84%理论产率)3-苯磺酰基-2-(2-甲基-6-三氟甲基-吡啶-3-羰基)环己-2-烯酮,白色结晶,熔点165-167℃.
1H-NMR(CDCl3):2.30,m,2H;2.55,t(J,7Hz),2H;2.71,m,2H;3.05,s,3H;:7.40-7.80,m,4H;7.80-8.05ppm,m,3H.实施例H30:6-二氟甲基-2-甲基烟酸(化合物A124):
在430mg(0.26mol)三(三甲基甲硅烷基)硅烷存在下,在150ml甲苯中120℃加热6.1g(0.026mol)6-(氯二氟甲基)-2-甲基烟酸甲酯(后者按照Heterocycles,46,129(1997)所述的类似方法,在三氟乙酸存在下,在甲苯中加热3-氧代丁酸甲酯与4-氨基-1-氯-1,1-二氟丁-3-烯-2-酮制得)。1.5小时后,浓缩反应混合物,进而通过硅胶纯化(己烷/乙酸乙酯13∶1)。得到3.8g(73%理论产率)6-二氟甲基-2-甲基烟酸甲酯,系无色油状物。
水解(类似于实施例H1)上述酯,从而得到白色结晶形式6-二氟甲基-2-甲基烟酸,熔点135-136℃.
1H-NMR(CDCl3):2.68,s,3H;6.583,t(J,55.2Hz),1H;:7.54,d(J,8.1Hz),1H;7.54ppm,d(J,8.1Hz),1H.实施例H31:6-(氯二氟甲基)-2-甲基烟酸(化合物A-94):
在加压容器中冷却5.0g(18.62mmol)2-甲基-6-三氯甲基烟酸甲酯(类似Heterocycles,46,129(1997)所述制得)至-40℃,随后在此温度下加入35g(1.75mol)蒸馏过的氢氟酸。200℃加热混合物10小时(压力大约55巴)。冷却后,利用气体-洗涤系统解除压力。抽吸除去HF,其后将反应混合物倒入乙酸乙酯/冰中。分出乙酸乙酯相,水相用乙酸乙酯再提取。然后水洗合并的乙酸乙酯相,硫酸钠干燥并浓缩,残留物进而用少量己烷和乙酸乙酯研制。过滤得到2.2g(53%理论产率)6-氯二氟甲基-2-甲基烟酸,浅绿色结晶,熔点134-135℃。1H-NMR(CDCl3):2.987,s,3H;7.64,d(J,8.1Hz),1H;8.513ppm,d(J,8.1Hz),1H.实施例H32:2-[2-(4,6-二甲氧基嘧啶-2酰基甲基)-6-三氟甲基吡啶-3-羰基]-3-羟基环己-2-烯酮(化合物A1090-B1):
将100mg 2-[2-(4,6-二甲氧基嘧啶-2-基硫基甲基)-6-三氟甲基吡啶-3-羰基]-3-羟基环己-2-烯酮(化合物A1088-B1)溶于二氯甲烷,随后在25℃下逐滴加入0.3ml过乙酸(39%乙酸溶液)。25℃反应15小时后,将反应混合物倒入乙酸乙酯与水中,有机相用水洗涤、硫酸钠干燥并浓缩。从而得到95mg树脂状2-[2-(4,6-二甲氧基嘧啶-2-磺酰基甲基)-6-三氟甲基吡啶-3-羰基]-3-羟基环己-2-烯酮。1H-NME(CDCl3):3.79,s,6H;3.91,s,3H;4.99,s,2H;6.09,s,1H;7.52,d(J,9Hz),1H;7.68ppm,d(J,9Hz),1H.
下列各表中,Ph代表苯基,且CC代表乙炔基。表1:式XVId化合物:化合物序号      R2         R3  R4  R5  pA1              H            H    H    CF3 0A2            CH3           H    H    CF3 0A3            CH3CH2       H    H    CF3 0A4            (CH3)2CH     H    H    CF3 0A5            (CH3)3C      H    H    CF3 0A6            环丙基          H    H    CF3 0A7            CH3(CH2)2   H    H    CF3 0化合物序号    R2                       R3  R4  R5      pA8            CH3OCH2                 H    H    CF3     0A9            CH3O(CH2)2             H    H    CF3     0A10           Ph                         H    H    CF3     0A11           PhO                        H    H    CF3     0A12           PhS                        H    H    CF3     0A13           PhSO                       H    H    CF3     0A14           PhSO2                    H    H    CF3     0A15           CH3S                     H    H    CF3     0A16           CH3SO                    H    H    CF3     0A17           CF3                      H    H    CF3     0A18           F2CH                     H    H    CF3     0A19           HCC                       H    H    CF3     0A20           CH3CC                    H    H    CF3     0A21           CH2=CH                  H    H    CF3     0A22           CH2=CHCH2              H    H    CF3     0A23           CH3SO2N(CH3)           H    H    CF3     0A24           (CH3)2N                 H    H    CF3     0A25           (CH3)2NSO2             H    H    CF3     0A26           ClCH2                    H    H    CF3     0A27           CH3SCH2                 H    H    CF3     0A28           CH3SOCH2                H    H    CF3     0A29           CH3SO2CH2              H    H    CF3     0A30           [1.2.4]-三唑-1-基甲基      H    H    CF3     0A31           CH3                      CF3  H    CH3     0A32           CH3                      CH3  H    CF3     0A33           H                          H    H    CF3CF2 0A34           CH3                       H    H    CF3CF2 0A35           CH3CH2                   H    H    CF3CF2 0A36           环丙基                      H    H    CF3CF2 0A37           (CH3)3C                  H    H    CF3CF2 0A38           (CH3)2CH                 H    H    CF3CF2 0A39           CH3(CH2)2               H    H    CF3CF2 0A40           CH3OCH2                  H    H    CF3CF2 0化合物序号   R2                      R3  R4     R5      pA41          CH3O(CH2)2            H    H    CF3CF2    0A42          Ph                        H    H    CF3CF2    0A43          PhO                       H    H    CF3CF2    0A44          PhS                       H    H    CF3CF2    0A45          PhSO                      H    H    CF3CF2    0A46          PhSO2                    H    H    CF3CF2    0A47          CH3S                     H    H    CF3CF2    0A48          CH3SO                    H    H    CF3CF2    0A49          CF3                      H    H    CF3CF2    0A50          F2CH                     H    H    CF3CF2    0A51          HCC                       H    H    CF3CF2    0A52          CH3CC                    H    H    CF3CF2    0A53          CH2=CH                  H    H    CF3CF2    0A54          CH2=CHCH2              H    H    CF3CF2    0A55          CH3SO2N(CH3)           H    H    CF3CF2    0A56          (CH3)2N                 H    H    CF3CF2    0A57          (CH3)2NSO2             H    H    CF3CF2    0A58          ClCH2                    H    H    CF3CF2    0A59          CH3SCH2                 H    H    CF3CF2    0A60          CH3SOCH2                H    H    CF3CF2    0A61          CH3SO2CH2              H    H    CF3CF2    0A62          [1.2.4]-三唑-1-基甲基      H    H    CF3CF2    0A63          H                         H    H    CF3CF2CF2 0A64          CH3                      H    H    CF3CF2CF2 0A65          CH3CH2                  H    H    CF3CF2CF2 0A66          环丙基                     H    H    CF3CF2CF2 0A67          (CH3)3C                 H    H    CF3CF2CF2 0A68          (CH3)2CH                H    H    CF3CF2CF2 0A69          CH3(CH2)2              H    H    CF3CF2CF2 0A70          CH3OCH2                 H    H    CF3CF2CF2 0A71          CH3O(CH2)2             H    H    CF3CF2CF2 0A72          Ph                         H    H    CF3CF2CF2 0A73          PhO                        H    H    CF3CF2CF2 0化合物序号    R2                      R3  R4      R5       pA74           PhS                       H    H    CF3CF2CF2 0A75           PhSO                      H    H    CF3CF2CF2 0A76           PhSO2                    H    H    CF3CF2CF2 0A77           CH3S                     H    H    CF3CF2CF2 0A78           CH3SO                    H    H    CF3CF2CF2 0A79           CF3                      H    H    CF3CF2CF2 0A80           F2CH                     H    H    CF3CF2CF2 0A81           HCC                       H    H    CF3CF2CF2 0A82           CH3CC                    H    H    CF3CF2CF2 0A83           CH2=CH                  H    H    CF3CF2CF2 0A84           CH2=CHCH2              H    H    CF3CF2CF2 0A85           CH3SO2N(CH3)           H    H    CF3CF2CF2 0A86           (CH3)2N                 H    H    CF3CF2CF2 0A87           (CH3)2NSO2             H    H    CF3CF2CF2 0A88           ClCH2                    H    H    CF3CF2CF2 0A89           CH3SCH2                 H    H    CF3CF2CF2 0A90           CH3SOCH2                H    H    CF3CF2CF2 0A91           CH3SO2CH2              H    H    CF3CF2CF2 0A92           [1.2.4]-三唑-1-基甲基      H    H    CF3CF2CF2 0A93           H                          H    H    CF2Cl        0A94           CH3                      H    H    CF2Cl        0A95           CH3CH2                  H    H    CF2Cl        0A96           环丙基                     H    H    CF2Cl        0A97           (CH3)3C                 H    H    CF2Cl        0A98           (CH3)2CH                H    H    CF2Cl        0A99           CH3(CH2)2              H    H    CF2Cl        0A100          CH3OCH2                 H    H    CF2Cl        0A101          CH3O(CH2)2             H    H    CF2Cl        0A102          Ph                         H    H    CF2Cl        0A103          PhO                        H    H    CF2Cl        0A104          PhS                        H    H    CF2Cl        0A105          PhSO                       H    H    CF2Cl        0A106          PhSO2                     H    H    CF2Cl        0化合物序号    R2                      R3  R4    R5     pA107          CH3S                    H    H    CF2Cl    0A108          CH3SO                   H    H    CF2Cl    0A109          CF3                     H    H    CF2Cl    0A110          F2CH                    H    H    CF2Cl    0A111          HCC                      H    H    CF2Cl    0A112          CH3CC                   H    H    CF2Cl    0A113          CH2=CH                 H    H    CF2Cl    0A114          CH2=CHCH2             H    H    CF2Cl    0A115          CH3SO2N(CH3)          H    H    CF2Cl    0A116          (CH3)2N                H    H    CF2Cl    0A117          (CH3)2NSO2            H    H    CF2Cl    0A118          ClCH2                   H    H    CF2Cl    0A119          CH3SCH2                H    H    CF2Cl    0A120          CH3SOCH2               H    H    CF2Cl    0A121          CH3SO2CH2             H    H    CF2Cl    0A122          [1.2.4]-三唑-1-基甲基     H    H    CF2Cl    0A123          H                         H    H    CHF2     0A124          CH3                      H    H    CHF2    0A125          CH3CH2                 H    H    CHF2     0A126          环丙基                    H    H    CHF2    0A127          (CH3)3C                H    H    CHF2     0A128          (CH3)2CH               H    H    CHF2     0A129          CH3(CH2)2             H    H    CHF2     0A130          CH3OCH2                H    H    CHF2     0A131          CH3O(CH2)2            H    H    CHF2     0A132          Ph                        H    H    CHF2     0A133          PhO                       H    H    CHF2     0A134          PhS                       H    H    CHF2     0A135          PhSO                      H    H    CHF2     0A136          PhSO2                    H    H    CHF2     0A137          CH3S                     H    H    CHF2     0A138          CH3SO                    H    H    CHF2     0A139          CF3                      H    H    CHF2     0化合物序号    R2                      R3  R4  R5     pA140          F2CH                    H    H    CHF2    0A141          HCC                      H    H    CHF2    0A142          CH3CC                   H    H    CHF2    0A143          CH2=CH                 H    H    CHF2    0A144          CH2=CHCH2             H    H    CHF2    0A145          CH3SO2N(CH3)          H    H    CHF2    0A146          (CH3)2N                H    H    CHF2    0A147          (CH3)2NSO2            H    H    CHF2    0A148          ClCH2                   H    H    CHF2    0A149          CH3SCH2                H    H    CHF2    0A150          CH3SOCH2               H    H    CHF2    0A151          CH3SO2CH2             H    H    CHF2    0A152          [1.2.4]-三唑-1-基甲基    H    H    CHF2    0A153          H                        H    H    CCl3    0A154          CH3                     H    H    CCl3    0A155          CH3CH2                 H    H    CCl3    0A156          环丙基                   H    H    CCl3    0A157          (CH3)3C                H    H    CCl3    0A158          (CH3)2CH               H    H    CCl3    0A159          CH3(CH2)2             H    H    CCl3    0A160          CH3OCH2                H    H    CCl3    0A161          CH3O(CH2)2            H    H    CCl3    0A162          Ph                       H    H    CCl3    0A163          PhO                      H    H    CCl3    0A164          PhS                      H    H    CCl3    0A165          PhSO                     H    H    CCl3    0A166          PhSO2                   H    H    CCl3    0A167          CH3S                    H    H    CCl3    0A168          CH3SO                   H    H    CCl3    0A169          CF3                     H    H    CCl3    0A170          F2CH                    H    H    CCl3    0A171          HCC                      H    H    CCl3    0A172          CH3CC                   H    H    CCl3    0化合物序号  R2                      R3  R4   R5      pA173        CH2=CH                 H    H     CCl3    0A174        CH2=CHCH2             H    H     CCl3    0A175        CH3SO2N(CH3)          H    H     CCl3    0A176        (CH3)2N                H    H     CCl3    0A177        (CH3)2NSO2            H    H     CCl3    0A178        ClCH2                   H    H     CCl3    0A179        CH3SCH2                H    H     CCl3    0A180        CH3SOCH2               H    H     CCl3    0A181        CH3SO2CH2            H    H     CCl3    0A182        [1.2.4]-三唑-1-基甲基    H    H     CCl3    0A183        H                        H    CH3  CF3     0A184        CH3                     H    CH3  CF3     0A185        CH3CH2                 H    CH3  CF3     0A186        环丙基                   H    CH3  CF3     0A187        (CH3)3C                H    CH3  CF3     0A188        (CH3)2CH               H    CH3  CF3     0A189        CH3(CH2)2             H    CH3  CF3     0A190        CH3OCH2                H    CH3  CF3     0A191        CH3O(CH2)2           H    CH3  CF3     0A192        Ph                       H    CH3  CF3     0A193        PhO                      H    CH3  CF3     0A194        PhS                      H    CH3  CF3     0A195        PhSO                     H    CH3  CF3     0A196        PhSO2                   H    CH3  CF3     0A197        CH3S                    H    CH3  CF3     0A198        CH3SO                   H    CH3  CF3     0A199        CF3                     H    CH3  CF3     0A200        F2CH                    H    CH3  CF3     0A201        HCC                      H    CH3  CF3     0A202        CH3CC                   H    CH3  CF3     0A203        CH2=CH                 H    CH3  CF3     0A204        CH2=CHCH2             H    CH3  CF3     0A205        CH3SO2N(CH3)         H    CH3  CF3     0化合物序号   R2            R3  R4     R5        pA206        (CH3)2N       H    CH3    CF3        0A207        (CH3)2NSO2  H    CH3    CF3        0A208        ClCH2          H    CH3    CF3        0A209        CH3SCH2       H    CH3    CF3        0A210        CH3SOCH2      H    CH3    CF3        0A211        CH3SO2CH2    H    CH3    CF3        0A212        H               H    CH3    CF3CF2    0A213        CH3            H    CH3    CF3CF2    0A214        CH3CH2        H    CH3    CF3CF2    0A215        环丙基           H    CH3    CF3CF2    0A216        (CH3)3C       H    CH3    CF3CF2    0A217        (CH3)2CH      H    CH3    CF3CF2    0A218        CH3(CH2)2   H    CH3    CF3CF2    0A219        CH3OCH2       H    CH3    CF3CF2    0A220        CH3O(CH2)2  H    CH3    CF3CF2    0A221        Ph              H    CH3    CF3CF2    0A222        PhO             H    CH3    CF3CF2    0A223        PhS             H    CH3    CF3CF2    0A224        PhSO            H    CH3    CF3CF2    0A225        PhSO2          H    CH3    CF3CF2    0A226        CH3S           H    CH3    CF3CF2    0A227        CH3SO          H    CH3    CF3CF2    0A228        CF3            H    CH3    CF3CF2    0A229        F2CH           H    CH3    CF3CF2    0A230        HCC             H    CH3    CF3CF2    0A231        CH3CC          H    CH3    CF3CF2    0A232        CH2=CH        H    CH3    CF3CF2    0A233        CH2=CHCH2    H    CH3    CF3CF2    0A234        CH3SO2N(CH3) H    CH3    CF3CF2    0A235        (CH3)2N       H    CH3    CF3CF2    0A236        (CH3)2NSO2   H    CH3    CF3CF2    0A237        ClCH2          H    CH3    CF3CF2    0A238        CH3SCH2       H    CH3    CF3CF2    0化合物序号    R2           R3   R4      R5        pA239          CH3SOCH2    H    CH3    CF3CF2     0A240          CH3SO2CH2  H    CH3    CF3CF2     0A241          H              H    CH3    CF3CF2CF2 0A242          CH3           H    CH3    CF3CF2CF2 0A243          CH3CH2      H    CH3    CF3CF2CF2 0A244          环丙基         H    CH3    CF3CF2CF2 0A245          (CH3)3C     H    CH3    CF3CF2CF2 0A246          (CH3)2CH    H    CH3    CF3CF2CF2 0A247          CH3(CH2)2  H    CH3    CF3CF2CF2 0A248          CH3OCH2     H    CH3    CF3CF2CF2 0A249          CH3O(CH2)2 H    CH3    CF3CF2CF2 0A250          Ph             H    CH3    CF3CF2CF2 0A251          PhO            H    CH3    CF3CF2CF2 0A252          PhS            H    CH3    CF3CF2CF2 0A253          PhSO           H    CH3    CF3CF2CF2 0A254          PhSO2         H    CH3    CF3CF2CF2 0A255          CH3S          H    CH3    CF3CF2CF2 0A256          CH3SO         H    CH3    CF3CF2CF2 0A257          CF3           H    CH3    CF3CF2CF2 0A258          F2CH          H    CH3    CF3CF2CF2 0A259          HCC            H    CH3    CF3CF2CF2 0A260          CH3CC         H    CH3    CF3CF2CF2 0A261          CH2=CH       H    CH3    CF3CF2CF2 0A262          CH2=CHCH2   H    CH3    CF3CF2CF2 0A263          CH3SO2N(CH3)H    CH3    CF3CF2CF2 0A264          (CH3)2N      H    CH3    CF3CF2CF2 0A265          (CH3)2NSO2  H    CH3    CF3CF2CF2 0A266          ClCH2         H    CH3    CF3CF2CF2 0A267          CH3SCH2      H    CH3    CF3CF2CF2 0A268          CH3SOCH2     H    CH3    CF3CF2CF2 0A269          CH3SO2CH2   H    CH3    CF3CF2CF2 0A270          H               H    CH3    CF2Cl       0A271          CH3            H    CH3    CF2Cl       0化合物序号    R2            R3   R4     R5      pA272          CH3CH2       H    CH3    CF2Cl    0A273          环丙基          H    CH3    CF2Cl    0A274          (CH3)3C      H    CH3    CF2Cl    0A275          (CH3)2CH     H    CH3    CF2Cl    0A276          CH3(CH2)2  H    CH3    CF2Cl    0A277          CH3OCH2      H    CH3    CF2Cl    0A278          CH3O(CH2)2 H    CH3    CF2Cl    0A279          Ph             H    CH3    CF2Cl    0A280          PhO            H    CH3    CF2Cl    0A281          PhS            H    CH3    CF2Cl    0A282          PhSO           H    CH3    CF2Cl    0A283          PhSO2         H    CH3    CF2Cl    0A284          CH3S          H    CH3    CF2Cl    0A285          CH3SO         H    CH3    CF2Cl    0A286          CF3           H    CH3    CF2Cl    0A287          F2CH          H    CH3    CF2Cl    0A288          HCC            H    CH3    CF2Cl    0A289          CH3CC         H    CH3    CF2Cl    0A290          CH2=CH       H    CH3    CF2Cl    0A291          CH2=CHCH2   H    CH3    CF2Cl    0A292          CH3SO2N(CH3)H    CH3    CF2Cl    0A293          (CH3)2N      H    CH3    CF2Cl    0A294          (CH3)2NSO2  H    CH3    CF2Cl    0A295          ClCH2          H    CH3    CF2Cl    0A296          CH3SCH2      H    CH3    CF2Cl    0A297          CH3SOCH2     H    CH3    CF2Cl    0A298          CH3SO2CH2   H    CH3    CF2Cl    0A299          H               H    CH3    CHF2     0A300          CH3           H    CH3    CHF2     0A301          CH3CH2       H    CH3    CHF2     0A302          环丙基          H    CH3    CHF2     0A303          (CH3)3C      H    CH3    CHF2     0A304          (CH3)2CH     H    CH3    CHF2     0化合物序号    R2             R3  R4     R5     pA305          CH3(CH2)2   H    CH3    CHF2    0A306          CH3OCH2      H    CH3    CHF2    0A307          CH3O(CH2)2  H    CH3    CHF2    0A308          Ph              H    CH3    CHF2    0A309          PhO             H    CH3    CHF2    0A310          PhS             H    CH3    CHF2    0A311          PhSO            H    CH3    CHF2    0A312          PhSO2          H    CH3    CHF2    0A313          CH3S           H    CH3    CHF2    0A314          CH3SO          H    CH3    CHF2    0A315          CF3            H    CH3    CHF2    0A316          F2CH           H    CH3    CHF2    0A317          HCC             H    CH3    CHF2    0A318          CH3CC          H    CH3    CHF2    0A319          CH2=CH        H    CH3    CHF2    0A320          CH2=CHCH2    H    CH3    CHF2    0A321          CH3SO2N(CH3) H    CH3    CHF2    0A322          (CH3)2N       H    CH3    CHF2    0A323          (CH3)2NSO2   H    CH3    CHF2    0A324          ClCH2          H    CH3    CHF2    0A325          CH3SCH2       H    CH3    CHF2    0A326          CH3SOCH2      H    CH3    CHF2    0A327          CH3SO2CH2    H    CH3    CHF2    0A328          H                H    CH3    CCl3    0A329          CH3            H    CH3    CCl3    0A330          CH3CH2        H    CH3    CCl3    0A331          (CH3)3C       H    CH3    CCl3    0A332          (CH3)2CH      H    CH3    CCl3    0A333          环丙基           H    CH3    CCl3    0A334          CH3(CH2)2    H    CH3    CCl3    0A335          CH3OCH2       H    CH3    CCl3    0A336          CH3O(CH2)2   H    CH3    CCl3    0A337          Ph               H    CH3    CCl3    0化合物序号    R2             R3  R4     R5     pA338          PhO             H    CH3    CCl3    0A339          PhS             H    CH3    CCl3    0A340          PhSO            H    CH3    CCl3    0A341          PhSO2          H    CH3    CCl3    0A342          CH3S           H    CH3    CCl3    0A343          CH3SO          H    CH3    CCl3    0A344          CF3            H    CH3    CCl3    0A345          F2CH           H    CH3    CCl3    0A346          HCC             H    CH3    CCl3    0A347          CH3CC          H    CH3    CCl3    0A348          CH2=CH        H    CH3    CCl3    0A349          CH2=CHCH2    H    CH3    CCl3    0A350          CH3SO2N(CH3) H    CH3    CCl3    0A351          (CH3)2N       H    CH3    CCl3    0A352          (CH3)2NSO2   H    CH3    CCl3    0A353          ClCH2           H    CH3    CCl3    0A354          CH3SCH2       H    CH3    CCl3    0A355          CH3SOCH2      H    CH3    CCl3    0A356          CH3SO2CH2    H    CH3    CCl3    0A357          H                H    Ph      CF3     0A358          CH3            H    Ph      CF3     0A359          CH3CH2        H    Ph      CF3     0A360          环丙基           H    Ph      CF3     0A361          (CH3)3C       H    Ph      CF3     0A362          (CH3)2CH      H    Ph      CF3     0A363          CH3(CH2)2    H    Ph      CF3     0A364          CH3OCH2       H    Ph      CF3     0A365          CH3O(CH2)2   H    Ph      CF3     0A366          Ph               H    Ph      CF3     0A367          PhO              H    Ph      CF3     0A368          PhS              H    Ph      CF3     0A369          PhSO             H    Ph      CF3     0A370          PhSO2           H    Ph      CF3     0化合物序号    R2             R3  R4   R5        pA371          CH3S           H    Ph    CF3        0A372          CH3SO          H    Ph    CF3        0A373          CF3            H    Ph    CF3        0A374          F2CH           H    Ph    CF3        0A375          HCC             H    Ph    CF3        0A376          CH3CC          H    Ph    CF3        0A377          CH2=CH        H    Ph    CF3        0A378          CH2=CHCH2    H    Ph    CF3        0A379          CH3SO2N(CH3) H    Ph    CF3        0A380          (CH3)2N       H    Ph    CF3        0A381          (CH3)2NSO2   H    Ph    CF3        0A382          ClCH2          H    Ph    CF3        0A383          CH3SCH2       H    Ph    CF3        0A384          CH3SOCH2      H    Ph    CF3        0A385          CH3SO2CH2    H    Ph    CF3        0A386          H                H    Ph    CF3CF2    0A387          CH3            H    Ph    CF3CF2    0A388          CH3CH2        H    Ph    CF3CF2    0A389          环丙基           H    Ph    CF3CF2    0A390          (CH3)3C       H    Ph    CF3CF2    0A391          (CH3)2CH      H    Ph    CF3CF2    0A392          CH3(CH2)2    H    Ph    CF3CF2    0A393          CH3OCH2       H    Ph    CF3CF2    0A394          CH3O(CH2)2   H    Ph    CF3CF2    0A395          Ph               H    Ph    CF3CF2    0A396          PhO              H    Ph    CF3CF2    0A397          PhS              H    Ph    CF3CF2    0A398          PhSO             H    Ph    CF3CF2    0A399          PhSO2           H    Ph    CF3CF2    0A400          CH3S            H    Ph    CF3CF2    0A401          CH3SO           H    Ph    CF3CF2    0A402          CF3             H    Ph    CF3CF2    0A403          F2CH            H    Ph    CF3CF2    0化合物序号    R2            R3  R4    R5         pA404          HCC             H    Ph    CF3CF2     0A405          CH3CC          H    Ph    CF3CF2     0A406          CH2=CH        H    Ph    CF3CF2     0A407          CH2=CHCH2    H    Ph    CF3CF2     0A408          CH3SO2N(CH3) H    Ph    CF3CF2     0A409          (CH3)2N       H    Ph    CF3CF2     0A410          (CH3)2NSO2   H    Ph    CF 3CF2     0A411          ClCH2           H    Ph    CF3CF2     0A412          CH3SCH2       H    Ph    CF3CF2     0A413          CH3SOCH2      H    Ph    CF3CF2     0A414          CH3SO2CH2   H    Ph    CF3CF2     0A415          H               H    Ph    CF3CF2CF2 0A416          CH3            H    Ph    CF3CF2CF2 0A417          CH3CH2        H    Ph    CF3CF2CF2 0A418          环丙基          H    Ph    CF3CF2CF2 0A419          (CH3)3C       H    Ph    CF3CF2CF2 0A420          (CH3)2CH      H    Ph    CF3CF2CF2 0A421          CH3(CH2)2    H    Ph    CF3CF2CF2 0A422          CH3OCH2       H    Ph    CF3CF2CF2 0A423          CH3O(CH2)2   H    Ph    CF3CF2CF2 0A424          Ph              H    Ph    CF3CF2CF2 0A425          PhO             H    Ph    CF3CF2CF2 0A426          PhS             H    Ph    CF3CF2CF2 0A427          PhSO            H    Ph    CF3CF2CF2 0A428          PhSO2          H    Ph    CF3CF2CF2 0A429          CH3S           H    Ph    CF3CF2CF2 0A430          CH3SO          H    Ph    CF3CF2CF2 0A431          CF3            H    Ph    CF3CF2CF2 0A432          F2CH           H    Ph    CF3CF2CF2 0A433          HCC             H    Ph    CF3CF2CF2 0A434          CH3CC          H    Ph    CF3CF2CF2 0A435          CH2=CH        H    Ph    CF3CF2CF2 0A436          CH2=CHCH2    H    Ph    CF3CF2CF2 0化合物序号    R2             R3  R4    R5         pA437          CH3SO2N(CH3)H    Ph    CF3CF2CF2 0A438          (CH3)2N      H    Ph    CF3CF2CF2 0A439          (CH3)2NSO2  H    Ph    CF3CF2CF2 0A440          ClCH2         H    Ph    CF3CF2CF2 0A441          CH3SCH2      H    Ph    CF3CF2CF2 0A442          CH3SOCH2     H    Ph    CF3CF2CF2 0A443          CH3SO2CH2   H    Ph    CF3CF2CF2 0A444          H               H    Ph    CF2Cl       0A445          CH3            H    Ph    CF2Cl       0A446          CH3CH2       H    Ph    CF2Cl       0A447          环丙基          H    Ph    CF2Cl       0A448          (CH3)3C      H    Ph    CF2Cl       0A449          (CH3)2CH     H    Ph    CF2Cl       0A450          CH3(CH2)2   H    Ph    CF2Cl       0A451          CH3OCH2      H    Ph    CF2Cl       0A452          CH3O(CH2)2  H    Ph    CF2Cl       0A453          Ph              H    Ph    CF2Cl       0A454          PhO             H    Ph    CF2Cl       0A455          PhS             H    Ph    CF2Cl       0A456          PhSO            H    Ph    CF2Cl       0A457          PhSO2          H    Ph    CF2Cl       0A458          CH3S           H    Ph    CF2Cl       0A459          CH3SO          H    Ph    CF2Cl       0A460          CF3            H    Ph    CF2Cl       0A461          F2CH           H    Ph    CF2Cl       0A462          HCC             H    Ph    CF2Cl       0A463          CH3CC          H    Ph    CF2Cl       0A464          CH2=CH        H    Ph    CF2Cl       0A465          CH2=CHCH2    H    Ph    CF2Cl       0A466          CH3SO2N(CH3) H    Ph    CF2Cl       0A467          (CH3)2N       H    Ph    CF2Cl       0A468          (CH3)2NSO2   H    Ph    CF2Cl       0A469          ClCH2           H    Ph    CF2Cl       0化合物序号    R2           R3  R4   R5      pA470          CH3SCH2     H    Ph    CF2Cl   0A471          CH3SOCH2    H    Ph    CF2Cl   0A472          CH3SO2CH2  H    Ph    CF2Cl   0A473          H              H    Ph    CHF2    0A474          CH3           H    Ph    CHF2    0A475          CH3CH2      H    Ph    CHF2    0A476          环丙基         H    Ph    CHF2    0A477          (CH3)3C     H    Ph    CHF2    0A478          (CH3)2CH    H    Ph    CHF2    0A479          CH3(CH2)2  H    Ph    CHF2    0A480          CH3OCH2     H    Ph    CHF2    0A481          CH3O(CH2)2 H    Ph    CHF2    0A482          Ph             H    Ph    CHF2    0A483          PhO            H    Ph    CHF2    0A484          PhS            H    Ph    CHF2    0A485          PhSO           H    Ph    CHF2    0A486          PhSO2         H    Ph    CHF2    0A487          CH3S          H    Ph    CHF2    0A488          CH3SO         H    Ph    CHF2    0A489          CF3           H    Ph    CHF2    0A490          F2CH          H    Ph    CHF2    0A491          HCC            H    Ph    CHF2    0A492          CH3CC         H    Ph    CHF2    0A493          CH2=CH       H    Ph    CHF2    0A494          CH2=CHCH2   H    Ph    CHF2    0A495          CH3SO2N(CH3)H    Ph    CHF2    0A496          (CH3)2N      H    Ph    CHF2    0A497          (CH3)2NSO2  H    Ph    CHF2    0A498          ClCH2         H    Ph    CHF2    0A499          CH3SCH2      H    Ph    CHF2    0A500          CH3SOCH2     H    Ph    CHF2    0A501          CH3SO2CH2   H    Ph    CHF2    0A502          H               H    Ph    CCl3    0化合物序号    R2             R3         R4   R5     pA503          CH3            H           Ph    CCl3    0A504          CH3CH2       H           Ph    CCl3    0A505          环丙基          H           Ph    CCl3    0A506          (CH3)3C      H           Ph    CCl3    0A507          (CH3)2CH     H           Ph    CCl3    0A508          CH3(CH2)2   H           Ph    CCl3    0A509          CH3OCH2      H           Ph    CCl3    0A510          CH3O(CH2)2  H           Ph    CCl3    0A511          Ph              H           Ph    CCl3    0A512          PhO             H           Ph    CCl3    0A513          PhS             H           Ph    CCl3    0A514          PhSO            H           Ph    CCl3    0A515          PhSO2          H           Ph    CCl3    0A516          CH3S           H           Ph    CCl3    0A517          CH3SO          H           Ph    CCl3    0A518          CF3            H           Ph    CCl3    0A519          F2CH           H           Ph    CCl3    0A520          HCC             H           Ph    CCl3    0A521          CH3CC          H           Ph    CCl3    0A522          CH2=CH        H           Ph    CCl3    0A523          CH2=CHCH2    H           Ph    CCl3    0A524          CH3SO2N(CH3) H           Ph    CCl3    0A525          (CH3)2N       H           Ph    CCl3    0A526          (CH3)2NSO2   H           Ph    CCl3    0A527          ClCH2          H           Ph    CCl3    0A528          CH3SCH2       H           Ph    CCl3    0A529          CH3SOCH2      H           Ph    CCl3    0A530          CH3SO2CH2    H           Ph    CCl3    0A531          H               CH3         H    CF3     0A532          H               CH3CH2     H    CF3     0A533          H               环丙基        H    CF3     0A534          H               (CH3)3CH   H    CF3     0A535          H               (CH3)2CH   H    CF3     0化合物序号    R2   R3          R4  R5      pA536          H    CH3(CH2)2  H    CF3     0A537          H    CH3OCH2     H    CF3     0A538          H    CH3O(CH2)2 H    CF3     0A539          H    Ph             H    CF3     0A540          H    PhO            H    CF3     0A541          H    PhS            H    CF3     0A542          H    PhSO           H    CF3     0A543          H    PhSO2         H    CF3     0A544          H    CH3S          H    CF3     0A545          H    CH3SO         H    CF3     0A546          H    CF3           H    CF3     0A547          H    F2CH          H    CF3     0A548          H    HCC            H    CF3     0A549          H    CH3CC         H    CF3     0A550          H    CH2=CH       H    CF3     0A551          H    CH2=CHCH2   H    CF3     0A552          H    CH3SO2N(CH3)H    CF3     0A553          H    (CH3)2N      H    CF3     0A554          H    (CH3)2NSO2  H    CF3     0A555          H    CH3SCH2      H    CF3     0A556          H    CH3SOCH2     H    CF3     0A557          H    CH3SO2CH2   H    CF3     0A558          H    CH3           H    CF3CF2 0A559          H    CH3CH2       H    CF3CF2 0A560          H    环丙基          H    CF3CF2 0A561          H    (CH3)3C      H    CF3CF2 0A562          H    (CH3)2CH     H    CF3CF2 0A563          H    CH3(CH2)2   H    CF3CF2 0A564          H    CH3OCH2      H    CF3CF2 0A565          H    CH3O(CH2)2  H    CF3CF2 0A566          H    Ph              H    CF3CF2 0A567          H    PhO             H    CF3CF2 0A568          H    PhS             H    CF3CF2 0化合物序号    R2   R3           R4    R5        pA569          H    PhSO            H    CF3CF2     0A570          H    PhSO2          H    CF3CF2     0A571          H    CH3S           H    CF3CF2     0A572          H    CH3SO          H    CF3CF2     0A573          H    CF3            H    CF3CF2     0A574          H    F2CH           H    CF3CF2     0A575          H    HCC             H    CF3CF2     0A576          H    CH3CC          H    CF3CF2     0A577          H    CH2=CH        H    CF3CF2     0A578          H    CH2=CHCH2    H    CF3CF2     0A579          H    CH3SO2N(CH3) H    CF3CF2     0A580          H    (CH3)2N       H    CF3CF2     0A581          H    (CH3)2NSO2   H    CF3CF2     0A582          H    CH3SCH2       H    CF3CF2     0A583          H    CH3SOCH2      H    CF3CF2     0A584          H    CH3SO2CH2    H    CF3CF2     0A585          H    CH3            H    CF3CF2CF2 0A586          H    CH3CH2        H    CF3CF2CF2 0A587          H    环丙基           H    CF3CF3CF2 0A588          H    (CH3)3C       H    CF3CF2CF2 0A589          H    (CH3)2CH      H    CF3CF2CF2 0A590          H    CH3(CH2)2    H    CF3CF2CF2 0A591          H    CH3OCH2       H    CF3CF2CF2 0A592          H    CH3O(CH2)2   H    CF3CF2CF2 0A593          H    Ph               H    CF3CF2CF2 0A594          H    PhO              H    CF3CF2CF2 0A595          H    PhS              H    CF3CF2CF2 0A596          H    PhSO             H    CF3CF2CF2 0A597          H    PhSO2           H    CF3CF2CF2 0A598          H    CH3S            H    CF3CF2CF2 0A599          H    CH3SO           H    CF3CF2CF2 0A600          H    CF3             H    CF3CF2CF2 0A601          H    F2CH            H    CF3CF2CF2 0化合物序号    R2   R3           R4     R5        pA602          H    HCC             H    CF3CF2CF2 0A603          H    CH3CC          H    CF3CF2CF2 0A604          H    CH2=CH        H    CF3CF2CF2 0A605          H    CH2=CHCH2    H    CF3CF2CF2 0A606          H    CH3SO2N(CH3) H    CF3CF2CF2 0A607          H    (CH3)2N       H    CF3CF2CF2 0A608          H    (CH3)2NSO2   H    CF3CF2CF2 0A609          H    CH3SCH2       H    CF3CF2CF2 0A610          H    CH3SOCH2      H    CF3CF2CF2 0A611          H    CH3SO2CH2    H    CF3CF2CF2 0A612          H    CH3             H    CF2Cl       0A613          H    CH3CH2         H    CF2Cl       0A614          H    环丙基           H    CF2Cl       0A615          H    (CH3)3C       H    CF2Cl       0A616          H    (CH3)2CH      H    CF2Cl       0A617          H    CH3(CH2)2    H    CF2Cl       0A618          H    CH3OCH2       H    CF2Cl       0A619          H    CH3O(CH2)2   H    CF2Cl       0A620          H    Ph               H    CF2Cl       0A621          H    PhO              H    CF2Cl       0A622          H    PhS              H    CF2Cl       0A623          H    PhSO             H    CF2Cl       0A624          H    PhSO2          H    CF2Cl       0A625          H    CH3S           H    CF2Cl       0A626          H    CH3SO          H    CF2Cl       0A627          H    CF3            H    CF2Cl       0A628          H    F2CH           H    CF2Cl       0A629          H    HCC              H    CF2Cl       0A630          H    CH3CC          H    CF2Cl       0A631          H    CH2=CH        H    CF2Cl       0A632          H    CH2=CHCH2    H    CF2Cl       0A633          H    CH3SO2N(CH3) H    CF2Cl       0A634          H    (CH3)2N       H    CF2Cl       0化合物序号    R2    R3          R4   R5     pA635          H    (CH3)2NSO2  H    CF2Cl   0A636          H    CH3SCH2      H    CF2Cl   0A637          H    CH3SOCH2     H    CF2Cl   0A638          H    CH3SO2CH2   H    CF2Cl   0A639          H    CH3           H    CHF2    0A640          H    CH3CH2       H    CHF2    0A641          H    环丙基          H    CHF2    0A642          H    (CH3)3C      H    CHF2    0A643          H    (CH3)2CH     H    CHF2    0A644          H    CH3(CH2)2   H    CHF2    0A645          H    CH3OCH2      H    CHF2    0A646          H    CH3O(CH2)2  H    CHF2    0A647          H    Ph              H    CHF2    0A648          H    PhO             H    CHF2    0A649          H    PhS             H    CHF2    0A650          H    PhSO            H    CHF2    0A651          H    PhSO2          H    CHF2    0A652          H    CH3S           H    CHF2    0A653          H    CH3SO          H    CHF2    0A654          H    CF3            H    CHF2    0A655          H    F2CH           H    CHF2    0A656          H    HCC             H    CHF2    0A657          H    CH3CC          H    CHF2    0A658          H    CH2=CH        H    CHF2    0A659          H    CH2=CHCH2    H    CHF2    0A660          H    CH3SO2N(CH3) H    CHF2    0A661          H    (CH3)2N       H    CHF2    0A662          H    (CH3)2NSO2   H    CHF2    0A663          H    CH3SCH2       H    CHF2    0A664          H    CH3SOCH2      H    CHF2    0A665          H    CH3SO2CH2    H    CHF2    0A666          H    CH3            H    CCl3    0A667          H    CH3CH2        H    CCl3    0化合物序号    R2   R3          R4   R5     pA668          H    环丙基         H    CCl3    0A669          H    (CH3)3C     H    CCl3    0A670          H    (CH3)2CH    H    CCl3    0A671          H    CH3(CH2)2  H    CCl3    0A672          H    CH3OCH2     H    CCl3    0A673          H    CH3O(CH2)2 H    CCl3    0A674          H    Ph             H    CCl3    0A675          H    PhO            H    CCl3    0A676          H    PhS            H    CCl3    0A677          H    PhSO           H    CCl3    0A678          H    PhSO2         H    CCl3    0A679          H    CH3S          H    CCl3    0A680          H    CH3SO         H    CCl3    0A681          H    CF3           H    CCl3    0A682          H    F2CH          H    CCl3    0A683          H    HCC            H    CCl3    0A684          H    CH3CC         H    CCl3    0A685          H    CH2=CH       H    CCl3    0A686          H    CH2=CHCH2   H    CCl3    0A687          H    CH3SO2N(CH3)H    CCl3    0A688          H    (CH3)2N      H    CCl3    0A689          H    (CH3)2NSO2  H    CCl3    0A690          H    CH3SCH2      H    CCl3    0A691          H    CH3SOCH2     H    CCl3    0A692          H    CH3SO2CH2   H    CCl3    0A693          H    CH3           CH3 CF3     0A694          H    CH3CH2       CH3 CF3     0A695          H    环丙基          CH3 CF3     0A696          H    (CH3)3C      CH3 CF3     0A697          H    (CH3)2CH     CH3 CF3     0A698          H    CH3(CH2)2   CH3 CF3     0A699          H    CH3OCH2      CH3 CF3     0A700          H    CH3O(CH2)2  CH3 CF3     0化合物序号    R2   R3            R4     R5        pA701          H    Ph              CH3    CF3        0A702          H    PhO             CH3    CF3        0A703          H    PhS             CH3    CF3        0A704          H    PhSO            CH3    CF3        0A705          H    PhSO2          CH3    CF3        0A706          H    CH3S           CH3    CF3        0A707          H    CH3SO          CH3    CF3        0A708          H    CF3            CH3    CF3        0A709          H    F2CH           CH3    CF3        0A710          H    HCC             CH3    CF3        0A711          H    CH3CC          CH3    CF3        0A712          H    CH2=CH        CH3    CF3        0A713          H    CH2=CHCH2    CH3    CF3        0A714          H    CH3SO2N(CH3) CH3    CF3        0A715          H    (CH3)2N       CH3    CF3        0A716          H    (CH3)2NSO2   CH3    CF3        0A717          H    CH3SCH2       CH3    CF3        0A718          H    CH3SOCH2      CH3    CF3        0A719          H    CH3SO2CH2    CH3    CF3        0A720          H    CH3            CH3    CF3CF2    0A721          H    CH3CH2        CH3    CF3CF2    0A722          H    环丙基          CH3    CF3CF2    0A723          H    (CH3)3C       CH3    CF3CF2    0A724          H    (CH3)2CH      CH3    CF3CF2    0A725          H    CH3(CH2)2    CH3    CF3CF2    0A726          H    CH3OCH2       CH3    CF3CF2    0A727          H    CH3O(CH2)2   CH3    CF3CF2    0A728          H    Ph               CH3    CF3CF2    0A729          H    PhO              CH3    CF3CF2    0A730          H    PhS              CH3    CF3CF2    0A731          H    PhSO             CH3    CF3CF2    0A732          H    PhSO2           CH3    CF3CF2    0A733          H    CH3S            CH3    CF3CF2    0化合物序号    R2    R3            R4       R5        pA734          H     CH3SO          CH3    CF3CF2     0A735          H     CF3            CH3    CF3CF2     0A736          H     F2CH           CH3    CF3CF2     0A737          H     HCC             CH3    CF3CF2     0A738          H     CH3CC          CH3    CF3CF2     0A739          H     CH2=CH        CH3    CF3CF2     0A740          H     CH2=CHCH2   CH3    CF3CF2     0A741          H     CH3SO2N(CH3)CH3    CF3CF2     0A742          H     (CH3)2N      CH3    CF3CF2     0A743          H     (CH3)2NSO2  CH3    CF3CF2     0A744          H     CH3SCH2      CH3    CF3CF2     0A745          H     CH3SOCH2     CH3    CF3CF2     0A746          H     CH3SO2CH2   CH3    CF3CF2     0A747          H     CH3            CH3    CF3CF2CF2 0A748          H     CH3CH2       CH3    CF3CF2CF2 0A749          H     环丙基          CH3    CF3CF2CF2 0A750          H     (CH3)3C      CH3    CF3CF2CF2 0A751          H     (CH3)2CH     CH3    CF3CF2CF2 0A752          H     CH3(CH2)2   CH3    CF3CF2CF2 0A753          H     CH3OCH2      CH3    CF3CF2CF2 0A754          H     CH3O(CH2)2  CH3    CF3CF2CF2 0A755          H     Ph              CH3    CF3CF2CF2 0A756          H     PhO             CH3    CF3CF2CF2 0A757          H     PhS             CH3    CF3CF2CF2 0A758          H     PhSO            CH3    CF3CF2CF2 0A759          H     PhSO2          CH3    CF3CF2CF2 0A760          H     CH3S           CH3    CF3CF2CF2 0A761          H     CH3SO          CH3    CF3CF2CF2 0A762          H     CF3            CH3    CF3CF2CF2 0A763          H     F2CH           CH3    CF3CF2CF2 0A764          H     HCC             CH3    CF3CF2CF2 0A765          H     CH3CC          CH3    CF3CF2CF2 0A766          H     CH2=CH        CH3    CF3CF2CF2 0化合物序号    R2   R3             R4      R5         pA767          H    CH2=CHCH2   CH3    CF3CF2CF2 0A768          H    CH3SO2N(CH3)CH3    CF3CF2CF2 0A769          H    (CH3)2N      CH3    CF3CF2CF2 0A770          H    (CH3)2NSO2  CH3    CF3CF2CF2 0A771          H    CH3SCH2      CH3    CF3CF2CF2 0A772          H    CH3SOCH2     CH3    CF3CF2CF2 0A773          H    CH3SO2CH2   CH3    CF3CF2CF2 0A774          H    CH3            CH3    CF2Cl       0A775          H    CH3CH2       CH3    CF2Cl       0A776          H    环丙基          CH3    CF2Cl       0A777          H    (CH3)3C      CH3    CF2Cl       0A778          H    (CH3)2CH     CH3    CF2Cl       0A779          H    CH3(CH2)2   CH3    CF2Cl       0A780          H    CH3OCH2      CH3    CF2Cl       0A781          H    CH3O(CH2)2  CH3    CF2Cl       0A782          H    Ph              CH3    CF2Cl       0A783          H    PhO             CH3    CF2Cl       0A784          H    PhS             CH3    CF2Cl       0A785          H    PhSO            CH3    CF2Cl       0A786          H    PhSO2          CH3    CF2Cl       0A787          H    CH3S           CH3    CF2Cl       0A788          H    CH3SO          CH3    CF2Cl       0A789          H    CF3            CH3    CF2Cl       0A790          H    F2CH           CH3    CF2Cl       0A791          H    HCC             CH3    CF2Cl       0A792          H    CH3CC          CH3    CF2Cl       0A793          H    CH2=CH        CH3    CF2Cl       0A794          H    CH2=CHCH2    CH3    CF2Cl       0A795          H    CH3SO2N(CH3) CH3    CF2Cl       0A796          H    (CH3)2N       CH3    CF2Cl       0A797          H    (CH3)2NSO2   CH3    CF2Cl       0A798          H    CH3SCH2       CH3    CF2Cl       0A799          H    CH3SOCH2      CH3    CF2Cl       0化合物序号    R2   R3           R4      R5      pA800          H    CH3SO2CH2   CH3    CF2Cl   0A801          H    CH3            CH3    CHF2    0A802          H    CH3CH2        CH3    CHF2    0A803          H    环丙基           CH3    CHF2    0A804          H    (CH3)3C       CH3    CHF2    0A805          H    (CH3)2CH      CH3    CHF2    0A806          H    CH3(CH2)2    CH3    CHF2    0A807          H    CH3OCH2       CH3    CHF2    0A808          H    CH3O(CH2)2  CH3    CHF2    0A809          H    Ph              CH3    CHF2    0A810          H    PhO             CH3    CHF2    0A811          H    PhS             CH3    CHF2    0A812          H    PhSO            CH3    CHF2    0A813          H    PhSO2          CH3    CHF2    0A814          H    CH3S           CH3    CHF2    0A815          H    CH3SO          CH3    CHF2    0A816          H    CF3            CH3    CHF2    0A817          H    F2CH           CH3    CHF2    0A818          H    HCC             CH3    CHF2    0A819          H    CH3CC          CH3    CHF2    0A820          H    CH2=CH        CH3    CHF2    0A821          H    CH2=CHCH2    CH3    CHF2    0A822          H    CH3SO2N(CH3) CH3    CHF2    0A823          H    (CH3)2N       CH3    CHF2    0A824          H    (CH3)2NSO2   CH3    CHF2    0A825          H    CH3SCH2       CH3    CHF2    0A826          H    CH3SOCH2      CH3    CHF2    0A827          H    CH3SO2CH2    CH3    CHF2    0A828          H    CH3            CH3    CCl3    0A829          H    CH3CH2        CH3    CCl3    0A830          H    环丙基           CH3    CCl3    0A831          H    (CH3)3C       CH3    CCl3    0A832          H    (CH3)2CH      CH3    CCl3    0化合物序号    R2   R3            R4     R5     pA833          H    CH3(CH2)2   CH3    CCl3    0A834          H    CH3OCH2      CH3    CCl3    0A835          H    CH3O(CH2)2  CH3    CCl3    0A836          H    Ph              CH3    CCl3    0A837          H    PhO             CH3    CCl3    0A838          H    PhS             CH3    CCl3    0A839          H    PhSO            CH3    CCl3    0A840          H    PhSO2          CH3    CCl3    0A841          H    CH3S           CH3    CCl3    0A842          H    CH3SO          CH3    CCl3    0A843          H    CF3            CH3    CCl3    0A844          H    F2CH           CH3    CCl3    0A845          H    HCC             CH3    CCl3    0A846          H    CH3CC          CH3    CCl3    0A847          H    CH2=CH        CH3    CCl3    0A848          H    CH2=CHCH2    CH3    CCl3    0A849          H    CH3SO2N(CH3) CH3    CCl3    0A850          H    (CH3)2N       CH3    CCl3    0A851          H    (CH3)2NSO2   CH3    CCl3    0A852          H    CH3SCH2       CH3    CCl3    0A853          H    CH3SOCH2      CH3    CCl3    0A854          H    CH3SO2CH2   CH3    CCl3    0A855          H    CH3            Ph      CF3     0A856          H    CH3CH2        Ph      CF3     0A857          H    (CH3)2CH      Ph      CF3     0A858          H    (CH3)2CH      Ph      CF3     0A859          H    环丙基           Ph      CF3     0A860          H    CH3(CH2)2    Ph      CF3     0A861          H    CH3OCH2       Ph      CF3     0A862          H    CH3O(CH2)2   Ph      CF3     0A863          H    Ph               Ph      CF3     0A864          H    PhO              Ph      CF3     0A865          H    PhS              Ph      CF3     0化合物序号    R2    R3           R4   R5     pA866          H    PhSO            Ph    CF3     0A867          H    PhSO2          Ph    CF3     0A868          H    CH3S           Ph    CF3     0A869          H    CH3SO          Ph    CF3     0A870          H    CF3            Ph    CF3     0A871          H    F2CH           Ph    CF3     0A872          H    HCC             Ph    CF3     0A873          H    CH3CC          Ph    CF3     0A874          H    CH2=CH        Ph    CF3     0A875          H    CH2=CHCH2    Ph    CF3     0A876          H    CH3SO2N(CH3) Ph    CF3     0A877          H    (CH3)2N       Ph    CF3     0A878          H    (CH3)2NSO2   Ph    CF3     0A879          H    CH3SCH2       Ph    CF3     0A880          H    CH3SOCH2      Ph    CF3     0A881          H    CH3SO2CH2    Ph    CF3     0A882          H    CH3            Ph    CF3CF2 0A883          H    CH3CH2        Ph    CF3CF2 0A884          H    环丙基           Ph    CF3CF2 0A885          H    (CH3)3C       Ph    CF3CF2 0A886          H    (CH3)2CH      Ph    CF3CF2 0A887          H    CH3(CH2)2    Ph    CF3CF2 0A888          H    CH3OCH2       Ph    CF3CF2 0A889          H    CH3O(CH2)2   Ph    CF3CF2 0A890          H    Ph               Ph    CF3CF2 0A891          H    PhO              Ph    CF3CF2 0A892          H    PhS              Ph    CF3CF2 0A893          H    PhSO             Ph    CF3CF2 0A894          H    PhSO2           Ph    CF3CF2 0A895          H    CH3S            Ph    CF3CF2 0A896          H    CH3SO           Ph    CF3CF2 0A897          H    CF3             Ph    CF3CF3 0A898          H    F2CH            Ph    CF3CF2 0化合物序号    R2    R3           R4     R5       pA899          H    HCC             Ph    CF3CF2     0A900          H    CH3CC          Ph    CF3CF2     0A901          H    CH2=CH        Ph    CF3CF2     0A902          H    CH2=CHCH2    Ph    CF3CF2     0A903          H    CH3SO2N(CH3) Ph    CF3CF2     0A904          H    (CH3)2N       Ph    CF3CF2     0A905          H    (CH3)2NSO2   Ph    CF3CF2     0A906          H    CH3SCH2       Ph    CF3CF2     0A907          H    CH3SOCH2      Ph    CF3CF2     0A908          H    CH3SO2CH2    Ph    CF3CF2     0A909          H    CH3            Ph    CF3CF2CF2 0A910          H    CH3CH2        Ph    CF3CF2CF2 0A911          H    环丙基           Ph    CF3CF2CF2 0A912          H    (CH3)3C       Ph    CF3CF2CF2 0A913          H    (CH3)2CH      Ph    CF3CF2CF2 0A914          H    CH3(CH2)2    Ph    CF3CF2CF2 0A915          H    CH3OCH2       Ph    CF3CF2CF2 0A916          H    CH3O(CH2)2   Ph    CF3CF2CF2 0A917          H    Ph              Ph    CF3CF2CF2 0A918          H    PhO             Ph    CF3CF2CF2 0A919          H    PhS             Ph    CF3CF2CF2 0A920          H    PhSO            Ph    CF3CF2CF2 0A921          H    PhSO2          Ph    CF3CF2CF2 0A922          H    CH3S           Ph    CF3CF2CF2 0A923          H    CH3SO          Ph    CF3CF2CF2 0A924          H    CF3            Ph    CF3CF2CF2 0A925          H    F2CH           Ph    CF3CF2CF2 0A926          H    HCC             Ph    CF3CF2CF2 0A927          H    CH3CC          Ph    CF3CF2CF2 0A928          H    CH2=CH        Ph    CF3CF2CF2 0A929          H    CH2=CHCH2    Ph    CF3CF2CF2 0A930          H    CH3SO2N(CH3) Ph    CF3CF2CF2 0A931          H    (CH3)2N       Ph    CF3CF2CF2 0化合物序号    R2    R3           R4    R5         pA932          H    (CH3)2NSO2  Ph    CF3CF2CF2 0A933          H    CH3SCH2      Ph    CF3CF2CF2 0A934          H    CH3SOCH2     Ph    CF3CF2CF2 0A935          H    CH3SO2CH2   Ph    CF3CF2CF2 0A936          H    CH3           Ph    CF2Cl        0A937          H    CH3CH2       Ph    CF2Cl        0A938          H    环丙基          Ph    CF2Cl        0A939          H    (CH3)3C      Ph    CF2Cl        0A940          H    (CH3)2CH     Ph    CF2Cl        0A941          H    CH3(CH2)2   Ph    CF2Cl        0A942          H    CH3OCH2      Ph    CF2Cl        0A943          H    CH3O(CH2)2  Ph    CF2Cl        0A944          H    Ph              Ph    CF2Cl        0A945          H    PhO             Ph    CF2Cl        0A946          H    PhS             Ph    CF2Cl        0A947          H    PhSO            Ph    CF2Cl        0A948          H    PhSO2          Ph    CF2Cl        0A949          H    CH3S           Ph    CF2Cl        0A950          H    CH3SO          Ph    CF2Cl        0A951          H    CF3            Ph    CF2Cl        0A952          H    F2CH           Ph    CF2Cl        0A953          H    HCC             Ph    CF2Cl        0A954          H    CH3CC          Ph    CF2Cl        0A955          H    CH2=CH        Ph    CF2Cl        0A956          H    CH2=CHCH2    Ph    CF2Cl        0A957          H    CH3SO2N(CH3) Ph    CF2Cl        0A958          H    (CH3)2N       Ph    CF2Cl        0A959          H    (CH3)2NSO2   Ph    CF2Cl        0A960          H    CH3SCH2       Ph    CF2Cl        0A961          H    CH3SOCH2      Ph    CF2Cl        0A962          H    CH3SO2CH2    Ph    CF2Cl        0A963          H    CH3            Ph    CHF2         0A964          H    CH3CH2        Ph    CHF2         0化合物序号   R2     R3          R4    R5    pA965         H    (CH3)3C      Ph    CHF2    0A966         H    (CH3)2CH     Ph    CHF2    0A967         H    环丙基          Ph    CHF2    0A968         H    CH3(CH2)2   Ph    CHF2    0A969         H    CH3OCH2      Ph    CHF2    0A970         H    CH3O(CH2)2  Ph    CHF2    0A971         H    Ph              Ph    CHF2    0A972         H    PhO             Ph    CHF2    0A973         H    PhS             Ph    CHF2    0A974         H    PhSO            Ph    CHF2    0A975         H    PhSO2          Ph    CHF2    0A976         H    CH3S           Ph    CHF2    0A977         H    CH3SO          Ph    CHF2    0A978         H    CF3            Ph    CHF2    0A979         H    F2CH           Ph    CHF2    0A980         H    HCC             Ph    CHF2    0A981         H    CH3CC          Ph    CHF2    0A982         H    CH2=CH        Ph    CHF2    0A983         H    CH2=CHCH2    Ph    CHF2    0A984         H    CH3SO2N(CH3) Ph    CHF2    0A985         H    (CH3)2N       Ph    CHF2    0A986         H    (CH3)2NSO2   Ph    CHF2    0A987         H    CH3SCH2       Ph    CHF2    0A988         H    CH3SOCH2      Ph    CHF2    0A989         H    CH3SO2CH2    Ph    CHF2    0A990         H    CH3             Ph    CCl3    0A991         H    CH3CH2        Ph    CCl3    0A992         H    (CH3)3C       Ph    CCl3    0A993         H    (CH3)2CH      Ph    CCl3    0A994         H    环丙基           Ph    CCl3    0A995         H    CH3(CH2)2    Ph    CCl3    0A996         H    CH3OCH2       Ph    CCl3    0A997         H    CH3O(CH2)2   Ph    CCl3    0化合物序号    R2             R3             R4   R5     pA998          H               Ph              Ph    CCl3    0A999          H               PhO             Ph    CCl3    0A1000         H               PhS             Ph    CCl3    0A1001         H               PhSO            Ph    CCl3    0A1002         H               PhSO2          Ph    CCl3    0A1003         H               CH3S           Ph    CCl3    0A1004         H               CH3SO          Ph    CCl3    0A1005         H               CF3            Ph    CCl3    0A1006         H               F2CH           Ph    CCl3    0A1007         H               HCC             Ph    CCl3    0A1008         H               CH3CC          Ph    CCl3    0A1009         H               CH2=CH        Ph    CCl3    0A1010         H               CH2=CHCH2    Ph    CCl3    0A1011         H               CH3SO2N(CH3) Ph    CCl3    0A1012         H               (CH3)2N       Ph    CCl3    0A1013         H               (CH3)2NSO2   Ph    CCl3    0A1014         H               CH3SCH2       Ph    CCl3    0A1015         H               CH3SOCH2      Ph    CCl3    0A1016         H               CH3SO2CH2    Ph    CCl3    0A1017         F                H               H     CF3     0A1018         Cl               H               H     CF3     0A1019         Br               H               H     CF3     0A1020         NC               H               H     CF3     0A1021         CH3SO2O       H               H     CF3     0A1022         CH3O           H               H     CF3     0A1023         CH3CH2O       H               H     CF3     0A1024         CH2CH=CH2O   H               H     CF3     0A1025         HCCCH2O        H               H     CF3     0A1026         PhCH2S         H               H     CF3     0A1027         PhCH2SO2      H               H     CF3     0A1028         ClCH2CH2      H               H     CF3     0A1029         BrCH2          H               H     CF3     0A1030         FCH2           H               H     CF3     0化合物序号   R2                     R3           R4  R5    pA1031        CHF2CH2               H             H    CF3    0A1032        CF3CH2                H             H    CF3    0A1033        [1,3]-咪唑-1-基甲基    H             H    CF3    0A1034        CHCl2CH2              H             H    CF3    0A1035        ClCH=CH                H             H    CF3    0A1036        Cl2C=CH               H             H    CF3    0A1037        CF3CH=CH              H             H    CF3    0A1038        ClCC                    H             H    CF3    0A1039        PhCH2                  H             H    CF3    0A1040        CH3CH2                CH3          H    CF3    0A1041        CH3                    OH            H    CF3    0A1042        CH3                    F             H    CF3    0A1043        CH3                    Cl            H    CF3    0A1044        F                       CH3          H    CF3    0A1045        Cl                      CH3          H    CF3    0A1046        H                       F             H    CF3    0A1047        H                       Cl            H    CF3    0A1048        H                       Br            H    CF3    0A1049        H                       OH            H    CF3    0A1050        H                       OCH3         H    CF3    0A1051        H                       OCHF2        H    CF3    0A1052        H                       OSO2CH3     H    CF3    0A1053        H                       OSO2CF3     H    CF3    0A1054        H                       ClCH2        H    CF3    0A1055        H                       BrCH2        H    CF3    0A1056        H                       FCH2         H    CF3    0A1057        H                       CHF2CH2     H    CF3    0A1058        H                       CF3CH2      H    CF3    0A1059        H                       三唑基甲基    H    CF3    0A1060        H                       CHCl2CH2    H    CF3    0A1061        H                       ClCH=CH      H    CF3    0A1062        H                       Cl2C=CH     H    CF3    0A1063        H                       CF3CH=CH    H    CF3    0化合物序号   R2              R3        R4       R5    pA1064        H                ClCC       H         CF3    0A1065        H                CH3C(O)   H         CF3    0A1066        H                Ph         H         CF3    0A1067        H                SO2CH3   H         CF3    0A1068        H                SO2CF3   H         CF3    0A1069        H                NC         H         CF3    0A1070        H                NO2       H         CF3    0A1071        CH3             H          F         CF3    0A1072        CH3             H          Cl        CF3    0A1073        CH3             H          Br        CF3    0A1074        CH3             H          NC        CF3    0A1075        CH3             H          CH3O     CF3    0A1076        CH3             H          CH3S     CF3    0A1077        CH3             H          CH3SO    CF3    0A1078        CH3             H          CH3SO2  CF3    0A1079        CH3CH2OCH2    H          H         CF3    0A1080        PhOCH2           H          H         CF3    0A1081         
Figure A9981578601021
       H          H         CF3    0A1082        (CH3)2CH2OCH2H          H         CF3    0A1083        BrCH2CH2       H          H         CF3    0A1084        FCH2CH2        H          H         CF3    0A1085               H          H         CF3    0A1086              H          H         CF3    0A1087         
Figure A9981578601024
    H          H         CF3    0A1088         
Figure A9981578601025
    H          H         CF3    0化合物序号    R2                 R3  R4  R5    pA1089         
Figure A9981578601031
      H    H    CF3    0A1090         
Figure A9981578601032
      H    H    CF3    0A1091        环丙基-CH2           H    H    CF3    0A1092        2,2-二氯环丙-1-基    H    H    CF3    0A1093        CH3OC(O)CH=CH       H    H    CF3    0A1094        CH3CH2OC(O)CH=CH   H    H    CF3    0A1095        ClCH2CH=CH          H    H    CF3    0A1096        CH=C=CH             H    H    CF3    0A1097        (CH3)2NCH2        H    H    CF3    0A1098        HOCH2                H    H    CF3    0A1099        CH3C(O)OCH2         H    H    CF3    0A1100        PhC(O)OCH2           H    H    CF3    0A1101        PhCH2CH2            H    H    CF3    0A1102        CH3OC(O)CH2         H    H    CF3    0A1103        NCCH2                H    H    CF3    0A1104        CH3(CH2)7SCH2    H    H    CF3    0A1105        CH3(CH2)7SOCH2   H    H    CF3    0A1106        CH3(CH2)7SO2CH2 H    H    CF3    0A1107         
Figure A9981578601033
          H    H    CF3    0A1108        ClCH2CC               H    H    CF3    0A1109        CHF2CH2CH2         H    H    CF3    0A1110        CHCl2CH2CH2        H    H    CF3    0A1111        CF3SO2O             H    H    CF3    0A1112         
Figure A9981578601034
          H    H    CF3    0A1113         
Figure A9981578601035
          H    H    CF3    0化合物序号   R2                   R3  R4  R5      pA1114      
Figure A9981578601041
         H    H    CF3      0A1115       
Figure A9981578601042
             H    H    CF3      0A1116       
Figure A9981578601043
             H    H    CF3      0A1117       
Figure A9981578601044
             H    H    CF3      0A1118        CH3ON=CHCH2       H    H    CF3      0A1119        O=CHCH2            H    H    CF3      0A1120        CH3CH2OCH2        H    H    CF2Cl    0A1121        PhOCH2              H    H    CF2Cl    0A1122                     H    H    CF2Cl    0A1123        (CH3)2CH2OCH2    H    H    CF2Cl    0A1124        BrCH2                H    H    CF2Cl    0A1125        FCH2                 H    H    CF2Cl    0A1126                    H    H    CF2Cl    0A1127       
Figure A9981578601047
           H    H    CF2Cl    0A1128       
Figure A9981578601048
          H    H    CF2Cl    0A1129                  H    H    CF2Cl    0A1130       
Figure A99815786010410
         H    H    CF2Cl    0A1131                H    H    CF2Cl     0A1132        环丙基-CH2           H    H    CF2Cl     0A1133        2,2-二氯环丙-1-基    H    H    CF2Cl     0化合物序号    R2                 R3  R4  R5      pA1134        CH3OC(O)CH=CH      H    H    CF2Cl    0A1135        CH3CH2OC(O)CH=CH  H    H    CF2Cl    0A1136        ClCH2CH=CH         H    H    CF2Cl    0A1137        CH=C=CH            H    H    CF2Cl    0A1138        (CH3)2NCH2       H    H    CF2Cl    0A1139        HOCH2               H    H    CF2Cl    0A1140        CH3C(O)OCH2        H    H    CF2Cl    0A1141        PhC(O)OCH2          H    H    CF2Cl    0A1142        PhCH2               H    H    CF2Cl    0A1143        CH3OC(O)CH2        H    H    CF2Cl    0A1144        NCCH2               H    H    CF2Cl    0A1145        CH3(CH2)7SCH2   H    H    CF2Cl    0A1146        CH3(CH2)7SOCH2  H    H    CF2Cl    0A1147        CH3(CH2)7SO2CH2H    H    CF2Cl    0A1148      
Figure A9981578601051
           H    H    CF2Cl    0A1149        ClCH2CC             H    H    CF2Cl    0A1150        Br                   H    H    CF2Cl    0A1151        Cl                   H    H    CF2Cl    0A1152        CF3SO2O           H    H    CF2Cl    0A1153      
Figure A9981578601052
           H    H    CF2Cl    0A1154      
Figure A9981578601053
          H    H    CF2Cl    0A1155      
Figure A9981578601054
          H    H    CF2Cl    0A1156       
Figure A9981578601055
            H    H    CF2Cl    0A1157                    H    H    CF2Cl    0A1158                    H    H    CF2Cl    0A1159        CH3ON=CHCH2      H    H    CF2Cl    0化合物序号    R2                   R3  R4  R5     pA1160         O=CHCH2             H    H    CF2Cl   0A1161         CH3CH2OCH2        H    H    CF2H    0A1162         PhOCH2               H    H    CF2H    0A1163                      H    H    CF2H    0A1164         (CH3)2CH2OCH2    H    H    CF2H    0A1165         BrCH2                H    H    CF2H    0A1166         FCH2                 H    H    CF2H    0A1167        
Figure A9981578601062
           H    H    CF2H    0A1168                   H    H    CF2H    0A1169                   H    H    CF2H    0A1170                   H    H    CF2H    0A1171        
Figure A9981578601066
         H    H    CF2H    0A1172        
Figure A9981578601067
        H    H    CF2H    0A1173         环丙基-CH2           H    H    CF2H    0A1174         2,2-二氯环丙-1-基    H    H    CF2H    0A1175         CH3OC(O)CH=CH       H    H    CF2H    0A1176         CH3CH2OC(O)CH=CH   H    H    CF2H    0A1177         ClCH2CH=CH          H    H    CF2H    0A1178         CH=C=CH             H    H    CF2H    0A1179         (CH3)2NCH2        H    H    CF2H    0A1180         HOCH2                H    H    CF2H    0A1181         CH3C(O)OCH2         H    H    CF2H    0A1182         PhC(O)OCH2           H    H    CF2H    0化合物序号    R2                  R3  R4  R5     pA1183         PhCH2               H    H    CF2H    0A1184         CH3OC(O)CH2        H    H    CF2H    0A1185         NCCH2               H    H    CF2H    0A1186         CH3(CH2)7SCH2   H    H    CF2H    0A1187         CH3(CH2)7SOCH2  H    H    CF2H    0A1188         CH3(CH2)7SO2CH2H    H    CF2H    0A1189         
Figure A9981578601071
          H    H    CF2H    0A1190         ClCH2CC              H    H    CF2H    0A1191         Br                    H    H    CF2H    0A1192         Cl                    H    H    CF2H    0A1193         CF3SO2O            H    H    CF2H    0A1194         
Figure A9981578601072
          H    H    CF2H    0A1195         
Figure A9981578601073
          H    H    CF2H    0A1196         
Figure A9981578601074
          H    H    CF2H    0A1197                       H    H    CF2H    0A1198         
Figure A9981578601076
             H    H    CF2H    0A1199         
Figure A9981578601077
             H    H    CF2H    0A1200         CH3ON=CHCH2        H    H    CF2H    0A1201         O=CHCH2             H    H    CF2H    0A1202         CH3CH=CH            H    H    CF3     0A1203         CH3SO2NH            H    H    CF3     0A1204         CH3CH2CH2O        H    CH3 CF3     0A1205         Cl                    CH3 H    CF3     0A1206         F2CHO                H    H    CF3     0A1207         CH3CH2C(O)OCH2     H    H    CF3     0A1208         CH3CH2OC(O)OCH2    H    H    CF3     0化合物序号    R2                   R3  R4  R5    pA1209         CH3OCH2OCH2       H    H    CF3    0A1210         CH3                  H    H    CF3    1A1211         CH3CH2              H    H    CF3    1A1212         环丙基                H    H    CF3    1A1213         CH3(CH2)2           H    H    CF3    1A1214         CH3OCH2             H    H    CF3    1A1215         CF3                  H    H    CF3    1A1216         F2CH                 H    H    CF3    1A1217         ClCH2                H    H    CF3    1A1218         CH3SO2CH2          H    H    CF3    1A1219         CH3                  CF3 H    CH3    1A1220         CH3CH2OCH2         H    H    CF3    1A1221         PhOCH2               H    H    CF3    1A1222         (CH3)2CH2OCH2    H    H    CF3    1A1223         BrCH2                H    H    CF3    1A1224         FCH2                 H    H    CF3    1A1225                    H    H    CF3    1A1226        
Figure A9981578601082
         H    H    CF3    1A1227         环丙基-CH2           H    H    CF3    1A1228         2,2-二氯环丙-1-基     H    H    CF3    1A1229         (CH3)2NCH2         H    H    CF3    1A1230         HOCH2                H    H    CF3    1A1231         CH3C(O)OCH2         H    H    CF3    1A1232         PhC(O)OCH2           H    H    CF3    1A1233         PhCH2                H    H    CF3    1A1234         CH3OC(O)CH2         H    H    CF3    1A1235         NCCH2                H    H    CF3    1A1236         CH3(CH2)7SO2CH2 H    H    CF3    1A1237         Br                     H    H    CF3    1化合物序号    R2                   R3  R4  R5      pA1238         Cl                    H    H    CF3      1A1239         O=CHCH2             H    H    CF3      1A1240         CH3                  H    H    CF2Cl    1A1241         CH3CH2             H    H    CF2Cl    1A1242         环丙基                H    H    CF2Cl    1A1243         CH3(CH2)2         H    H    CF2Cl    1A1244         CH3OCH2            H    H    CF2Cl    1A1245         CF3                  H    H    CF2Cl    1A1246         F2CH                 H    H    CF2Cl    1A1247         ClCH2                H    H    CF2Cl    1A1248         CH3SO2CH2          H    H    CF2Cl    1A1249         CH3                  CF3 H    CF2Cl    1A1250         CH3CH2OCH2        H    H    CF2Cl    1A1251         PhOCH2               H    H    CF2Cl    1A1252         (CH3)2CH2OCH2    H    H    CF2Cl    1A1253         BrCH2                H    H    CF2Cl    1A1254         FCH2                 H    H    CF2Cl    1A1255                   H    H    CF2Cl    1A1256                 H    H    CF2Cl    1A1257         环丙基-CH2           H    H    CF2Cl    1A1258         2,2-二氯环丙-1-基    H    H    CF2Cl    1A1259         (CH3)2NCH2        H    H    CF2Cl    1A1260         HOCH2                H    H    CF2Cl    1A1261         CH3C(O)OCH2         H    H    CF2Cl    1A1262         PhC(O)OCH2           H    H    CF2Cl    1A1263         PhCH2                H    H    CF2Cl    1A1264         CH3OC(O)CH2         H    H    CF2Cl    1A1265         NCCH2                H    H    CF2Cl    1A1266         CH3(CH2)7SO2CH2 H    H    CF2Cl    1化合物序号    R2                    R3  R4  R5     pA1267         Br                     H    H    CF2Cl   1A1268         Cl                     H    H    CF2Cl   1A1269         O=CHCH2              H    H    CF2Cl   1A1270         CH3                   H    H    CF2H    1A1271         CH3CH2              H    H    CF2H    1A1272         环丙基                 H    H    CF2H    1A1273         CH3(CH2)2          H    H    CF2H    1A1274         CH3OCH2              H    H    CF2H    1A1275         CF3                   H    H    CF2H    1A1276         F2CH                  H    H    CF2H    1A1277         ClCH2                 H    H    CF2H    1A1278         CH3SO2CH2          H    H    CF2H    1A1279         CH3                  CF3 H    CF2H    1A1280         CH3CH2OCH2         H    H    CF2H    1A1281         PhOCH2                H    H    CF2H    1A1282         (CH3)2CH2OCH2     H    H    CF2H    1A1283         BrCH2                 H    H    CF2H    1A1284         FCH2                  H    H    CF2H    1A1285                    H    H    CF2H    1A1286        
Figure A9981578601102
         H    H    CF2H    1A1287         环丙基-CH2            H    H    CF2H    1A1288         2,2-二氯环丙-1-基     H    H    CF2H    1A1289         (CH3)2NCH2         H    H    CF2H    1A1290         HOCH2                 H    H    CF2H    1A1291         CH3C(O)OCH2          H    H    CF2H    1A1292         PhC(O)OCH2            H    H    CF2H    1A1293         PhCH2                 H    H    CF2H    1A1294         CH3OC(O)CH2          H    H    CF2H    1A1295         NCCH2                 H    H    CF2H    1化合物序号    R2                  R3  R4             R5      pA1296         CH3(CH2)7SO2CH2H    H               CF2H    1A1297         Br                    H    H               CF2H    1A1298         Cl                    H    H               CF2H    1A1299         O=CHCH2             H    H               CF2H    1A1300         CH3                  H    H               CF3CF2 1A1301         HO                    H    Ph              CF3     0A1302         CH3                  H    CH2=CH        CF3    0A1303         CH3                  H    CH3CH2O       CF3    0A1304         HO                    CH3 H               CF3     0A1305         HO                    H    H               CF3     0A1306         (CH3CH2)2N(O)CO   H    H               CF3     0A1307         CH3                  H    甲苯磺酰基-O    CF3     0A1308         CH3                  H    CH3CC          CF3     0A1309         CH3                  H    HCC             CF3     0A1310         CH3                  H    ClCH2CC        CF3     0A1311         CH3                  H    PhCH2O         CF3     0A1312         CH3                  H    CF3SO2O       CF3     0A1313         CH3                  H    (CH3)2N       CF3     0A1314         CH3                  H    CH3C(O)O       CF3     0A1315         CH3                  H    CH3CH2C(O)O   CF3     0A1316         CH3                  H    PhC(O)O         CF3     0A1317         CH3                  H    3-吡啶基        CF3     0A1318         CH3OCH2OCH2       H    H               CF2Cl   0A1319         CH3OCH2OCH2       H    H               CF2H    0A1320         CH3OCH2OCH2       H    H               CF2CF3 0A1321         CH3OCH2OCH2       H    H               CF3     1A1322         CH3O                 H    CH3            CF3     0下表2中,Q为Q1
Figure A9981578601121
并且Q1代表下列基团B:表2:基团B;基团    R6          R7  R8  R9  R10  WB1      H            H    H    H    OH    CH2B2      CH3         H    H    H    OH    CH2B3      CH3CH2     H    H    H    OH    CH2B4      CH3CH2CH2 H    H    H    OH    CH2B5      (CH3)2CH   H    H    H    OH    CH2B6      (CH3)3C    H    H    H    OH    CH2B7      CH3S        H    H    H    OH    CH2B8      CH3SO       H    H    H    OH    CH2B9      CH3SO2     H    H    H    OH    CH2B10     Ph           H    H    H    OH    CH2B11     CH3O        H    H    H    OH    CH2B12     CH3OC(O)    H    H    H    OH    CH2B13     CH3CH2OC(O)H    H    H    OH    CH2B14     CH2=CHCH2 H    H    H    OH    CH2B15     HCCCH2      H    H    H    OH    CH2B16     CF3         H    H    H    OH    CH2B17     (CH3)2NSO2H    H    H    OH    CH2B18     (CH3)2N    H    H    H    OH    CH2B19     PhO           H    H    H    OH    CH2B20     PhS           H    H    H    OH    CH2B21     PhSO          H    H    H    OH    CH2B22     PhSO2       H    H    H    OH    CH2基团   R6            R7     R8  R9  R10  WB23    CN              H       H    H    OH    CH2B24    CH3           CH3    H    H    OH    CH2B25    CH3CH2       CH3    H    H    OH    CH2B26    CH3CH2CH2   CH3    H    H    OH    CH2B27    (CH3)2CH     CH3    H    H    OH    CH2B28    (CH3)3C      CH3    H    H    OH    CH2B29    CH3S          CH3    H    H    OH    CH2B30    CH3SO         CH3    H    H    OH    CH2B31    CH3SO2       CH3    H    H    OH    CH2B32    Ph             CH3    H    H    OH    CH2B33    CH3O          CH3    H    H    OH    CH2B34    CH3OC(O)      CH3    H    H    OH    CH2B35    CH3CH2OC(O)  CH3    H    H    OH    CH2B36    CH2=CHCH2   CH3    H    H    OH    CH2B37    HCCCH2        CH3    H    H    OH    CH2B38    CF3           CH3    H    H    OH    CH2B39    (CH3)2NSO2  CH3    H    H    OH    CH2B40    (CH3)2N      CH3    H    H    OH    CH2B41    PhO            CH3    H    H    OH    CH2B42    PhS            CH3    H    H    OH    CH2B43    PhSO           CH3    H    H    OH    CH2B44    PhSO2         CH3    H    H    OH    CH2B45    CN             CH3    H    H    OH    CH2B46    CH3           H       CH3 H    OH    CH2B47    CH3CH2       H       CH3 H    OH    CH2B48    CH3CH2CH2   H       CH3 H    OH    CH2B49    (CH3)2CH     H       CH3 H    OH    CH2B50    (CH3)3C      H       CH3 H    OH    CH2B51    CH3S          H       CH3 H    OH    CH2B52    CH3SO         H       CH3 H    OH    CH2B53    CH3SO2       H       CH3 H    OH    CH2B54    Ph             H       CH3 H    OH    CH2B55    CH3O          H       CH3 H    OH    CH2基团    R6             R7    R8    R9  R10  WB56    CH3OC(O)        H       CH3    H    OH    CH2B57    CH3CH2OC(O)    H       CH3    H    OH    CH2B58    CH2=CHCH2     H       CH3    H    OH    CH2B59    HCCCH2          H       CH3    H    OH    CH2B60    CF3             H       CH3    H    OH    CH2B61    (CH3)2NSO2    H       CH3    H    OH    CH2B62    (CH3)2N        H       CH3    H    OH    CH2B63    PhO               H       CH3    H    OH    CH2B64    PhS               H       CH3    H    OH    CH2B65    PhSO              H       CH3    H    OH    CH2B66    PhSO2            H       CH3    H    OH    CH2B67    CN                H       CH3    H    OH    CH2B68    CH3             CH3    CH3    H    OH    CH2B69    CH3CH2         CH3    CH3    H    OH    CH2B70    CH3CH2CH2     CH3    CH3    H    OH    CH2B71    (CH3)2CH       CH3    CH3    H    OH    CH2B72    (CH3)3C        CH3    CH3    H    OH    CH2B73    CH3S            CH3    CH3    H    OH    CH2B74    CH3SO           CH3    CH3    H    OH    CH2B75    CH3SO2         CH3    CH3    H    OH    CH2B76    Ph               CH3    CH3    H    OH    CH2B77    CH3O            CH3    CH3    H    OH    CH2B78    CH3OC(O)        CH3    CH3    H    OH    CH2B79    CH3CH2OC(O)    CH3    CH3    H    OH    CH2B80    CH2=CHCH2     CH3    CH3    H    OH    CH2B81    HCCCH2          CH3    CH3    H    OH    CH2B82    CF3             CH3    CH3    H    OH    CH2B83    (CH3)2NSO2    CH3    CH3    H    OH    CH2B84    (CH3)2N        CH3    CH3    H    OH    CH2B85    PhO               CH3    CH3    H    OH    CH2B86    PhS               CH3    CH3    H    OH    CH2B87    PhSO              CH3    CH3    H    OH    CH2B88    PhSO2            CH3    CH3    H    OH    CH2基团    R6          R7          R8     R9     R10   WB89     CN             CH3        CH3   H       OH    CH2B90     CH3           CH3        CH3   CH3    OH    CH2B91     CH3CH2       CH3        CH3   CH3    OH    CH2B92     CH3CH2CH2   CH3        CH3   CH3    OH    CH2B93     (CH3)2CH     CH3        CH3   CH3    OH    CH2B94     (CH3)3C      CH3        CH3   CH3    OH    CH2B95     CH3S          CH3        CH3   CH3    OH    CH2B96     CH3SO         CH3        CH3   CH3    OH    CH2B97     CH3SO2       CH3        CH3   CH3    OH    CH2B98     Ph             CH3        CH3   CH3    OH    CH2B99     CH3O          CH3        CH3   CH3    OH    CH2B100    CH3OC(O)      CH3        CH3   CH3    OH    CH2B101    CH3CH2OC(O) CH3        CH3   CH3    OH    CH2B102    CH2=CHCH2  CH3        CH3   CH3    OH    CH2B103    HCCCH2       CH3        CH3   CH3    OH    CH2B104    CF3          CH3        CH3   CH3    OH    CH2B105    (CH3)2NSO2 CH3        CH3   CH3    OH    CH2B106    (CH3)2N     CH3        CH3   CH3    OH    CH2B107    PhO           CH3        CH3   CH3    OH    CH2B108    PhS           CH3        CH3   CH3    OH    CH2B109    PhSO          CH3        CH3   CH3    OH    CH2B110    PhSO2        CH3        CH3   CH3    OH    CH2B111    CN             CH3       CH3   CH3    OH    CH2B112    CH3CH2      CH3CH2    H      H       OH    CH2B113    CH3CH2CH2  CH3CH2    H      H       OH    CH2B114    (CH3)2CH    CH3CH2    H      H       OH    CH2B115    (CH3)3C     CH3CH2    H      H       OH    CH2B116    CH3S         CH3CH2    H      H       OH    CH2B117    CH3SO        CH3CH2    H      H       OH    CH2B118    CH3SO2      CH3CH2    H      H       OH    CH2B119    Ph            CH3CH2    H      H       OH    CH2B120    CH3O         CH3CH2    H      H       OH    CH2B121    CH3OC(O)     CH3CH2    H      H       OH    CH2基团    R6             R7        R8  R9  R10   WB122    CH3CH2OC(O)  CH3CH2    H    H    OH    CH2B123    CH2=CHCH2   CH3CH2    H    H    OH    CH2B124    HCCCH2        CH3CH2    H    H    OH    CH2B125    CF3           CH3CH2    H    H    OH    CH2B126    (CH3)2NSO2 CH3CH2    H    H    OH    CH2B127    (CH3)2N     CH3CH2    H    H    OH    CH2B128    PhO            CH3CH2    H    H    OH    CH2B129    PhS            CH3CH2    H    H    OH    CH2B130    PhSO           CH3CH2    H    H    OH    CH2B131    PhSO2         CH3CH2    H    H    OH    CH2B132    CN             CH3CH2    H    H    OH    CH2B133    H              H            H    H    OH    CHCH3B134    CH3           H            H    H    OH    CHCH3B135    CH3CH2       H            H    H    OH    CHCH3B136    CH3CH2CH2   H            H    H    OH    CHCH3B137    (CH3)2CH     H            H    H    OH    CHCH3B138    (CH3)3C      H            H    H    OH    CHCH3B139    CH3S          H            H    H    OH    CHCH3B140    CH3SO         H            H    H    OH    CHCH3B141    CH3SO2       H            H    H    OH    CHCH3B142    Ph             H            H    H    OH    CHCH3B143    CH3O          H            H    H    OH    CHCH3B144    CH3OC(O)      H            H    H    OH    CHCH3B145    CH3CH2OC(O)  H            H    H    OH    CHCH3B146    CH2=CHCH2   H            H    H    OH    CHCH3B147    HCCCH2        H            H    H    OH    CHCH3B148    CF3           H            H    H    OH    CHCH3B149    (CH3)2NSO2 H            H    H    OH    CHCH3B150    (CH3)2N     H            H    H    OH    CHCH3B151    PhO            H            H    H    OH    CHCH3B152    PhS            H            H    H    OH    CHCH3B153    PhSO           H            H    H    OH    CHCH3B154    PhSO2         H            H    H    OH    CHCH3基团    R6            R7    R8  R9  R10   WB155    CN              H      H    H    OH    CHCH3B156    CH3           CH3    H    H    OH    CHCH3B157    CH3CH2       CH3    H    H    OH    CHCH3B158    CH3CH2CH2  CH3    H    H    OH    CHCH3B159    (CH3)2CH     CH3    H    H    OH    CHCH3B160    (CH3)3C      CH3    H    H    OH    CHCH3B161    CH3S          CH3    H    H    OH    CHCH3B162    CH3SO         CH3    H    H    OH    CHCH3B163    CH3SO2       CH3    H    H    OH    CHCH3B164    Ph              CH3    H    H    OH    CHCH3B165    CH3O          CH3    H    H    OH    CHCH3B166    CH3OC(O)      CH3    H    H    OH    CHCH3B167    CH3CH2OC(O)  CH3    H    H    OH    CHCH3B168    CH2=CHCH2   CH3    H    H    OH    CHCH3B169    HCCCH2        CH3    H    H    OH    CHCH3B170    CF3           CH3    H    H    OH    CHCH3B171    (CH3)2NSO2  CH3    H    H    OH    CHCH3B172    (CH3)2N      CH3    H    H    OH    CHCH3B173    PhO             CH3    H    H    OH    CHCH3B174    PhS             CH3    H    H    OH    CHCH3B175    PhSO            CH3    H    H    OH    CHCH3B176    PhSO2         CH3    H    H    OH    CHCH3B177    CN             CH3    H    H    OH    CHCH3B178    CH3           H       CH3 H    OH    CHCH3B179    CH3CH2       H       CH3 H    OH    CHCH3B180    CH3CH2CH2   H       CH3 H    OH    CHCH3B181    (CH3)2CH     H       CH3 H    OH    CHCH3B182    (CH3)3C      H       CH3 H    OH    CHCH3B183    CH3S          H       CH3 H    OH    CHCH3B184    CH3SO         H       CH3 H    OH    CHCH3B185    CH3SO2       H       CH3 H    OH    CHCH3B186    Ph              H       CH3 H    OH    CHCH3B187    CH3O          H       CH3 H    OH    CHCH3基团    R6            R7     R8    R9   R10  WB188    CH3OC(O)      H       CH3    H    OH    CHCH3B189    CH3CH2OC(O)  H       CH3    H    OH    CHCH3B190    CH2=CHCH2   H       CH3    H    OH    CHCH3B191    HCCCH2        H       CH3    H    OH    CHCH3B192    CF3           H       CH3    H    OH    CHCH3B193    (CH3)2NSO2 H       CH3    H    OH    CHCH3B194    (CH3)2N      H       CH3    H    OH    CHCH3B195    PhO            H       CH3    H    OH    CHCH3B196    PhS            H       CH3    H    OH    CHCH3B197    PhSO           H       CH3    H    OH    CHCH3B198    PhSO2         H       CH3    H    OH    CHCH3B199    CN             H       CH3    H    OH    CHCH3B200    CH3           CH3    CH3    H    OH    CHCH3B201    CH3CH2       CH3    CH3    H    OH    CHCH3B202    CH3CH2CH2   CH3    CH3    H    OH    CHCH3B203    (CH3)2CH     CH3    CH3    H    OH    CHCH3B204    (CH3)3C      CH3    CH3    H    OH    CHCH3B205    CH3S          CH3    CH3    H    OH    CHCH3B206    CH3SO         CH3    CH3    H    OH    CHCH3B207    CH3SO2       CH3    CH3    H    OH    CHCH3B208    Ph             CH3    CH3    H    OH    CHCH3B209    CH3O          CH3    CH3    H    OH    CHCH3B210    CH3OC(O)      CH3    CH3    H    OH    CHCH3B211    CH3CH2OC(O)  CH3    CH3    H    OH    CHCH3B212    CH2=CHCH2   CH3    CH3    H    OH    CHCH3B213    HCCCH2        CH3    CH3    H    OH    CHCH3B214    CF3           CH3    CH3    H    OH    CHCH3B215    (CH3)2NSO2  CH3    CH3    H    OH    CHCH3B216    (CH3)2N      CH3    CH3    H    OH    CHCH3B217    PhO            CH3    CH3    H    OH    CHCH3B218    PhS            CH3    CH3    H    OH    CHCH3B219    PhSO           CH3    CH3    H    OH    CHCH3B220    PhSO2         CH3    CH3    H    OH    CHCH3基团    R6            R7        R8     R9     R10   WB221    CN             CH3        CH3    H       OH    CHCH3B222    CH3           CH3        CH3    CH3    OH    CHCH3B223    CH3CH2       CH3        CH3    CH3    OH    CHCH3B224    CH3CH2CH2   CH3        CH3    CH3    OH    CHCH3B225    (CH3)2CH     CH3        CH3    CH3    OH    CHCH3B226    (CH3)3C      CH3        CH3    CH3    OH    CHCH3B227    CH3S          CH3        CH3    CH3    OH    CHCH3B228    CH3SO         CH3        CH3    CH3    OH    CHCH3B229    CH3SO2       CH3        CH3    CH3    OH    CHCH3B230    Ph             CH3        CH3    CH3    OH    CHCH3B231    CH3O          CH3        CH3    CH3    OH    CHCH3B232    CH3OC(O)      CH3        CH3    CH3    OH    CHCH3B233    CH3CH2OC(O)  CH3        CH3    CH3    OH    CHCH3B234    CH2=CHCH2   CH3        CH3    CH3    OH    CHCH3B235    HCCCH2        CH3        CH3    CH3    OH    CHCH3B236    CF3           CH3        CH3    CH3    OH    CHCH3B237    (CH3)2NSO2  CH3        CH3    CH3    OH    CHCH3B238    (CH3)2N      CH3        CH3    CH3    OH    CHCH3B239    PhO            CH3        CH3    CH3    OH    CHCH3B240    PhS            CH3        CH3    CH3    OH    CHCH3B241    PhSO           CH3        CH3    CH3    OH    CHCH3B242    PhSO2         CH3        CH3    CH3    OH    CHCH3B243    CN              CH3        CH3    CH3    OH    CHCH3B244    CH3CH2       CH3CH2    H       H       OH    CHCH3B245    CH3CH2CH2   CH3CH2    H       H       OH    CHCH3B246    (CH3)2CH     CH3CH2    H       H       OH    CHCH3B247    (CH3)3C      CH3CH2    H       H       OH    CHCH3B248    CH3S          CH3CH2    H       H       OH    CHCH3B249    CH3SO         CH3CH2    H       H       OH    CHCH3B250    CH3SO2       CH3CH2    H       H       OH    CHCH3B251    Ph             CH3CH2    H       H       OH    CHCH3B252    CH3O          CH3CH2    H       H       OH    CHCH3B253    CH3OC(O)      CH3CH2    H       H       OH    CHCH3基团    R6               R7      R8  R9  R10   WB254    CH3CH2OC(O)    CH3CH2  H    H    OH    CHCH3B255    CH2=CHCH2     CH3CH2  H    H    OH    CHCH3B256    HCCCH2          CH3CH2  H    H    OH    CHCH3B257    CF3             CH3CH2  H    H    OH    CHCH3B258    (CH3)2NSO2    CH3CH2  H    H    OH    CHCH3B259    (CH3)2N        CH3CH2  H    H    OH    CHCH3B260    PhO              CH3CH2  H    H    OH    CHCH3B261    PhS              CH3CH2  H    H    OH    CHCH3B262    PhSO             CH3CH2  H    H    OH    CHCH3B263    PhSO2           CH3CH2  H    H    OH    CHCH3B264    CN               CH3CH2  H    H    OH    CHCH3B265    H                 H         H    H    OH    C=OB266    CH3             H         H    H    OH    C=OB267    CH3CH2         H         H    H    OH    C=OB268    CH3CH2CH2     H         H    H    OH    C=OB269    (CH3)2CH       H         H    H    OH    C=OB270    (CH3)3C        H         H    H    OH    C=OB271    CH3S            H         H    H    OH    C=OB272    CH3SO           H         H    H    OH    C=OB273    CH3SO2         H         H    H    OH    C=OB274    Ph               H         H    H    OH    C=OB275    CH3O            H         H    H    OH    C=OB276    CH3OC(O)        H         H    H    OH    C=OB277    CH3CH2OC(O)    H         H    H    OH    C=OB278    CH2=CHCH2     H         H    H    OH    C=OB279    HCCCH2          H         H    H    OH    C=OB280    CF3             H         H    H    OH    C=OB281    (CH3)2NSO2    H         H    H    OH    C=OB282    (CH3)2N        H         H    H    OH    C=OB283    PhO               H         H    H    OH    C=OB284    PhS               H         H    H    OH    C=OB285    PhSO              H         H    H    OH    C=OB286    PhSO2           H         H    H    OH    C=O基团    R6           R7     R8  R9   R10   WB287    CN             H       H     H    OH    C=OB288    CH3           CH3    H     H    OH    C=OB289    CH3CH2       CH3    H     H    OH    C=OB290    CH3CH2CH2   CH3    H     H    OH    C=OB291    (CH3)2CH     CH3    H     H    OH    C=OB292    (CH3)3C      CH3    H     H    OH    C=OB293    CH3S          CH3    H     H    OH    C=OB294    CH3SO         CH3    H     H    OH    C=OB295    CH3SO2       CH3    H     H    OH    C=OB296    Ph             CH3    H     H    OH    C=OB297    CH3O          CH3    H     H    OH    C=OB298    CH3OC(O)      CH3    H     H    OH    C=OB299    CH3CH2OC(O)  CH3    H     H    OH    C=OB300    CH2=CHCH2   CH3    H     H    OH    C=OB301    HCCCH2        CH3    H     H    OH    C=OB302    CF3           CH3    H     H    OH    C=OB303    (CH3)2NSO2  CH3    H     H    OH    C=OB304    (CH3)2N      CH3    H     H    OH    C=OB305    PhO            CH3    H     H    OH    C=OB306    PhS            CH3    H     H    OH    C=OB307    PhSO           CH3    H     H    OH    C=OB308    PhSO2         CH3    H     H    OH    C=OB309    CN             CH3    H     H    OH    C=OB310    CH3           H       CH3  H    OH    C=OB311    CH3CH2       H       CH3  H    OH    C=OB312    CH3CH2CH2   H       CH3  H    OH    C=OB313    (CH3)2CH     H       CH3  H    OH    C=OB314    (CH3)3C      H       CH3  H    OH    C=OB315    CH3S          H       CH3  H    OH    C=OB316    CH3SO         H       CH3  H    OH    C=OB317    CH3SO2       H       CH3  H    OH    C=OB318    Ph             H       CH3  H    OH    C=OB319    CH3O          H       CH3  H    OH    C=O基团    R6            R7     R8    R9   R10   WB320    CH3OC(O)      H       CH3    H    OH    C=O8321    CH3CH2OC(O)  H       CH3    H    OH    C=OB322    CH2=CHCH2   H       CH3    H    OH    C=OB323    HCCCH2        H       CH3    H    OH    C=OB324    CF3           H       CH3    H    OH    C=OB325    (CH3)2NSO2  H       CH3    H    OH    C=OB326    (CH3)2N      H       CH3    H    OH    C=OB327    PhO            H       CH3    H    OH    C=OB328    PhS            H       CH3    H    OH    C=OB329    PhSO           H       CH3    H    OH    C=OB330    PhSO2         H       CH3    H    OH    C=OB331    CN             H       CH3    H    OH    C=OB332    CH3           CH3    CH3    H    OH    C=OB333    CH3CH2       CH3    CH3    H    OH    C=OB334    CH3CH2CH2   CH3    CH3    H    OH    C=OB335    (CH3)2CH     CH3    CH3    H    OH    C=OB336    (CH3)3C      CH3    CH3    H    OH    C=OB337    CH3S          CH3    CH3    H    OH    C=OB338    CH3SO         CH3    CH3    H    OH    C=OB339    CH3SO2       CH3    CH3    H    OH    C=OB340    Ph             CH3    CH3    H    OH    C=OB341    CH3O          CH3    CH3    H    OH    C=OB342    CH3OC(O)      CH3    CH3    H    OH    C=OB343    CH3CH2OC(O)  CH3    CH3    H    OH    C=OB344    CH2=CHCH2   CH3    CH3    H    OH    C=OB345    HCCCH2        CH3    CH3    H    OH    C=OB346    CF3           CH3    CH3    H    OH    C=OB347    (CH3)2NSO2  CH3    CH3    H    OH    C=OB348    (CH3)2N      CH3    CH3    H    OH    C=OB349    PhO            CH3    CH3    H    OH    C=OB350    PhS            CH3    CH3    H    OH    C=OB351    PhSO           CH3    CH3    H    OH    C=OB352    PhSO2         CH3    CH3    H    OH    C=O基团    R6           R7        R8     R9     R10   WB353    CN             CH3       CH3    H       OH    C=OB354    CH3           CH3       CH3    CH3    OH    C=OB355    CH3CH2       CH3       CH3    CH3    OH    C=OB356    CH3CH2CH2   CH3       CH3    CH3    OH    C=OB357    (CH3)2CH     CH3       CH3    CH3    OH    C=OB358    (CH3)3C      CH3       CH3    CH3    OH    C=OB359    CH3S          CH3       CH3    CH3    OH    C=OB360    CH3SO         CH3       CH3    CH3    OH    C=OB361    CH3SO2       CH3       CH3    CH3    OH    C=OB362    Ph             CH3       CH3    CH3    OH    C=OB363    CH3O          CH3       CH3    CH3    OH    C=OB364    CH3OC(O)      CH3       CH3    CH3    OH    C=OB365    CH3CH2OC(O)  CH3       CH3    CH3    OH    C=OB366    CH2=CHCH2   CH3       CH3    CH3    OH    C=OB367    HCCCH2        CH3       CH3    CH3    OH    C=OB368    CF3           CH3       CH3    CH3    OH    C=OB369    (CH3)2NSO2  CH3       CH3    CH3    OH    C=OB370    (CH3)2N      CH3       CH3    CH3    OH    C=OB371    PhO            CH3       CH3    CH3    OH    C=OB372    PhS            CH3       CH3    CH3    OH    C=OB373    PhSO           CH3       CH3    CH3    OH    C=OB374    PhSO2         CH3       CH3    CH3    OH    C=OB375    CN             CH3       CH3    CH3    OH    C=OB376    CH3CH2       CH3CH2   H       H       OH    C=OB377    CH3CH2CH2   CH3CH2   H       H       OH    C=OB378    (CH3)2CH     CH3CH2   H       H       OH    C=OB379    (CH3)3C      CH3CH2   H       H       OH    C=OB380    CH3S          CH3CH2   H       H       OH    C=OB381    CH3SO         CH3CH2   H       H       OH    C=OB382    CH3SO2       CH3CH2   H       H       OH    C=OB383    Ph             CH3CH2   H       H       OH    C=OB384    CH3O          CH3CH2   H       H       OH    C=OB385    CH3OC(O)      CH3CH2   H       H       OH    C=O基团    R6               R7      R8  R9   R10   WB386    CH3CH2OC(O)    CH3CH2  H    H    OH    C=OB387    CH2=CHCH2     CH3CH2  H    H    OH    C=OB388    HCCCH2          CH3CH2  H    H    OH    C=OB389    CF3             CH3CH2  H    H    OH    C=OB390    (CH3)2NSO2    CH3CH2  H    H    OH    C=OB391    (CH3)2N        CH3CH2  H    H    OH    C=OB392    PhO              CH3CH2  H    H    OH    C=OB393    PhS              CH3CH2  H    H    OH    C=OB394    PhSO             CH3CH2  H    H    OH    C=OB395    PhSO2           CH3CH2  H    H    OH    C=OB396    CN               CH3CH2  H    H    OH    C=OB397    H                H         H    H    OH    N-CH3B398    CH3             H         H    H    OH    N-CH3B399    CH3CH2         H         H    H    OH    N-CH3B400    CH3CH2CH2     H         H    H    OH    N-CH3B401    (CH3)2CH       H         H    H    OH    N-CH3B402    (CH3)3C        H         H    H    OH    N-CH3B403    CH3S            H         H    H    OH    N-CH3B404    CH3SO           H         H    H    OH    N-CH3B405    CH3SO2         H         H    H    OH    N-CH3B406    Ph               H         H    H    OH    N-CH3B407    CH3O            H         H    H    OH    N-CH3B408    CH3OC(O)        H         H    H    OH    N-CH3B409    CH3CH2OC(O)    H         H    H    OH    N-CH3B410    CH2=CHCH2     H         H    H    OH    N-CH3B411    HCCCH2          H         H    H    OH    N-CH3B412    CF3             H         H    H    OH    N-CH3B413    (CH3)2NSO2    H         H    H    OH    N-CH3B414    (CH3)2N        H         H    H    OH    N-CH3B415    PhO              H         H    H    OH    N-CH3B416    PhS              H         H    H    OH    N-CH3B417    PhSO             H         H    H    OH    N-CH3B418    PhSO2           H         H    H    OH    N-CH3基团    R6           R7     R8  R9  R10   WB419    CN             H       H    H    OH    N-CH3B420    CH3           CH3    H    H    OH    N-CH3B421    CH3CH2       CH3    H    H    OH    N-CH3B422    CH3CH2CH2   CH3    H    H    OH    N-CH3B423    (CH3)2CH     CH3    H    H    OH    N-CH3B424    (CH3)3C      CH3    H    H    OH    N-CH3B425    CH3S          CH3    H    H    OH    N-CH3B426    CH3SO         CH3    H    H    OH    N-CH3B427    CH3SO2       CH3    H    H    OH    N-CH3B428    Ph             CH3    H    H    OH    N-CH3B429    CH3O          CH3    H    H    OH    N-CH3B430    CH3OC(O)      CH3    H    H    OH    N-CH3B431    CH3CH2OC(O)  CH3    H    H    OH    N-CH3B432    CH2=CHCH2   CH3    H    H    OH    N-CH3B433    HCCCH2        CH3    H    H    OH    N-CH3B434    CF3           CH3    H    H    OH    N-CH3B435    (CH3)2NSO2  CH3    H    H    OH    N-CH3B436    (CH3)2N      CH3    H    H    OH    N-CH3B437    PhO            CH3    H    H    OH    N-CH3B438    PhS            CH3    H    H    OH    N-CH3B439    PhSO           CH3    H    H    OH    N-CH3B440    PhSO2         CH3    H    H    OH    N-CH3B441    CN             CH3    H    H    OH    N-CH3B442    CH3           H       CH3 H    OH    N-CH3B443    CH3CH2       H       CH3 H    OH    N-CH3B444    CH3CH2CH2   H       CH3 H    OH    N-CH3B445    (CH3)2CH     H       CH3 H    OH    N-CH3B446    (CH3)3C      H       CH3 H    OH    N-CH3B447    CH3S          H       CH3 H    OH    N-CH3B448    CH3SO         H       CH3 H    OH    N-CH3B449    CH3SO2       H       CH3 H    OH    N-CH3B450    Ph             H       CH3 H    OH    N-CH3B451    CH3O          H       CH3 H    OH    N-CH3基团    R6             R7     R8     R9  R10   WB452    CH3OC(O)        H       CH3    H    OH    N-CH3B453    CH3CH2OC(O)    H       CH3    H    OH    N-CH3B454    CH2=CHCH2     H       CH3    H    OH    N-CH3B455    HCCCH2          H       CH3    H    OH    N-CH3B456    CF3             H       CH3    H    OH    N-CH3B457    (CH3)2NSO2    H       CH3    H    OH    N-CH3B458    (CH3)2N        H       CH3    H    OH    N-CH3B459    PhO              H       CH3    H    OH    N-CH3B460    PhS              H       CH3    H    OH    N-CH3B461    PhSO             H       CH3    H    OH    N-CH3B462    PhSO2           H       CH3    H    OH    N-CH3B463    CN               H       CH3    H    OH    N-CH3B464    CH3             CH3    CH3    H    OH    N-CH3B465    CH3CH2         CH3    CH3    H    OH    N-CH3B466    CH3CH2CH2     CH3    CH3    H    OH    N-CH3B467    (CH3)2CH       CH3    CH3    H    OH    N-CH3B468    (CH3)3C        CH3    CH3    H    OH    N-CH3B469    CH3S            CH3    CH3    H    OH    N-CH3B470    CH3SO           CH3    CH3    H    OH    N-CH3B471    CH3SO2         CH3    CH3    H    OH    N-CH3B472    Ph               CH3    CH3    H    OH    N-CH3B473    CH3O            CH3    CH3    H    OH    N-CH3B474    CH3OC(O)        CH3    CH3    H    OH    N-CH3B475    CH3CH2OC(O)    CH3    CH3    H    OH    N-CH3B476    CH2=CHCH2     CH3    CH3    H    OH    N-CH3B477    HCCCH2          CH3    CH3    H    OH    N-CH3B478    CF3             CH3    CH3    H    OH    N-CH3B479    (CH3)2NSO2    CH3    CH3    H    OH    N-CH3B480    (CH3)2N        CH3    CH3    H    OH    N-CH3B481    PhO              CH3    CH3    H    OH    N-CH3B482    PhS              CH3    CH3    H    OH    N-CH3B483    PhSO             CH3    CH3    H    OH    N-CH3B484    PhSO2           CH3    CH3    H    OH    N-CH3基团    R6           R7        R8   R9     R10   WB485    CN             CH3       CH3  H       OH    N-CH3B486    CH3           CH3       CH3  CH3    OH    N-CH3B487    CH3CH2       CH3       CH3  CH3    OH    N-CH3B488    CH3CH2CH2   CH3       CH3  CH3    OH    N-CH3B489    (CH3)2CH     CH3       CH3  CH3    OH    N-CH3B490    (CH3)3C      CH3       CH3  CH3    OH    N-CH3B491    CH3S          CH3       CH3  CH3    OH    N-CH3B492    CH3SO         CH3       CH3  CH3    OH    N-CH3B493    CH3SO2       CH3       CH3  CH3    OH    N-CH3B494    Ph             CH3       CH3  CH3    OH    N-CH3B495    CH3O          CH3       CH3  CH3    OH    N-CH3B496    CH3OC(O)      CH3       CH3  CH3    OH    N-CH3B497    CH3CH2OC(O)  CH3       CH3  CH3    OH    N-CH3B498    CH2=CHCH2   CH3       CH3  CH3    OH    N-CH3B499    HCCCH2        CH3       CH3  CH3    OH    N-CH3B500    CF3           CH3       CH3  CH3    OH    N-CH3B501    (CH3)2NSO2  CH3       CH3  CH3    OH    N-CH3B502    (CH3)2N      CH3       CH3  CH3    OH    N-CH3B503    PhO            CH3       CH3  CH3    OH    N-CH3B504    PhS            CH3       CH3  CH3    OH    N-CH3B505    PhSO           CH3       CH3  CH3    OH    N-CH3B506    PhSO2         CH3       CH3  CH3    OH    N-CH3B507    CN             CH3       CH3  CH3    OH    N-CH3B508    CH3CH2       CH3CH2   H     H       OH    N-CH3B509    CH3CH2CH2   CH3CH2   H     H       OH    N-CH3B510    (CH3)2CH     CH3CH2   H     H       OH    N-CH3B511    (CH3)3C      CH3CH2   H     H       OH    N-CH3B512    CH3S          CH3CH2   H     H       OH    N-CH3B513    CH3SO         CH3CH2   H     H       OH    N-CH3B514    CH3SO2       CH3CH2   H     H       OH    N-CH3B515    Ph             CH3CH2   H     H       OH    N-CH3B516    CH3O          CH3CH2   H     H       OH    N-CH3B517    CH3OC(O)      CH3CH2   H     H       OH    N-CH3基团    R6               R7      R8  R9  R10   WB518    CH3CH2OC(O)    CH3CH2  H    H    OH    N-CH3B519    CH2=CHCH2      CH3CH2  H    H    OH    N-CH3B520    HCCCH2          CH3CH2  H    H    OH    N-CH3B521    CF3             CH3CH2  H    H    OH    N-CH3B522    (CH3)2NSO2    CH3CH2  H    H    OH    N-CH3B523    (CH3)2N        CH3CH2  H    H    OH    N-CH3B524    PhO              CH3CH2  H    H    OH    N-CH3B525    PhS              CH3CH2  H    H    OH    N-CH3B526    PhSO             CH3CH2  H    H    OH    N-CH3B527    PhSO2           CH3CH2  H    H    OH    N-CH3B528    CN               CH3CH2  H    H    OH    N-CH3B529    H                 H         H    H    OH    OB530    CH3             H         H    H    OH    OB531    CH3CH2         H         H    H    OH    OB532    CH3CH2CH2     H         H    H    OH    OB533    (CH3)2CH       H         H    H    OH    OB534    (CH3)3C        H         H    H    OH    OB535    CH3S            H         H    H    OH    OB536    CH3SO           H         H    H    OH    OB537    CH3SO2         H         H    H    OH    OB538    Ph               H         H    H    OH    OB539    CH3O            H         H    H    OH    OB540    CH3OC(O)        H         H    H    OH    OB541    CH3CH2OC(O)    H         H    H    OH    OB542    CH2=CHCH2      H         H    H    OH    OB543    HCCCH2          H         H    H    OH    OB544    CF3             H         H    H    OH    OB545    (CH3)2NSO2   H         H    H    OH    OB546    (CH3)2N        H         H    H    OH    OB547    PhO              H         H    H    OH    OB548    PhS              H         H    H    OH    OB549    PhSO             H         H    H    OH    OB550    PhSO2           H         H    H    OH    O基团    R6            R7    R8  R9  R10  WB551    CN              H      H    H    OH    OB552    CH3           CH3   H    H    OH    OB553    CH3CH2       CH3   H    H    OH    OB554    CH3CH2CH2   CH3   H    H    OH    OB555    (CH3)2CH     CH3   H    H    OH    OB556    (CH3)3C      CH3   H    H    OH    OB557    CH3S          CH3   H    H    OH    OB558    CH3SO         CH3   H    H    OH    OB559    CH3SO2       CH3   H    H    OH    OB560    Ph             CH3   H    H    OH    OB561    CH3O          CH3   H    H    OH    OB562    CH3OC(O)      CH3   H    H    OH    OB563    CH3CH2OC(O)  CH3   H    H    OH    OB564    CH2=CHCH2    CH3   H    H    OH    OB565    HCCCH2        CH3   H    H    OH    OB566    CF3           CH3   H    H    OH    OB567    (CH3)2NSO2  CH3   H    H    OH    OB568    (CH3)2N      CH3   H    H    OH    OB569    PhO            CH3   H    H    OH    OB570    PhS            CH3   H    H    OH    OB571    PhSO           CH3   H    H    OH    OB572    PhSO2         CH3   H    H    OH    OB573    CN             CH3   H    H    OH    OB574    CH3           H      CH3 H    OH    OB575    CH3CH2       H      CH3 H    OH    OB576    CH3CH2CH2   H      CH3 H    OH    OB577    (CH3)2CH     H      CH3 H    OH    OB578    (CH3)3C      H      CH3 H    OH    OB579    CH3S          H      CH3 H    OH    OB580    CH3SO         H      CH3 H    OH    OB581    CH3SO2       H      CH3 H    OH    OB582    Ph             H      CH3 H    OH    OB583    CH3O          H      CH3 H    OH    O基团    R6             R7    R8    R9  R10  WB584    CH3OC(O)       H      CH3    H    OH    OB585    CH3CH2OC(O)   H      CH3    H    OH    OB586    CH2=CHCH2    H      CH3    H    OH    OB587    HCCCH2         H      CH3    H    OH    OB588    CF3            H      CH3    H    OH    OB589   (CH3)2NSO2   H      CH3    H    OH    OB590   (CH3)2N       H      CH3    H    OH    OB591    PhO             H      CH3    H    OH    OB592    PhS             H      CH3    H    OH    OB593    PhSO            H      CH3    H    OH    OB594    PhSO2          H      CH3    H    OH    OB595    CN              H      CH3    H    OH    OB596    CH3            CH3   CH3    H    OH    OB597    CH3CH2        CH3   CH3    H    OH    OB598    CH3CH2CH2    CH3   CH3    H    OH    OB599    (CH3)2CH      CH3   CH3    H    OH    OB600    (CH3)3C       CH3   CH3    H    OH    OB601    CH3S           CH3   CH3    H    OH    OB602    CH3SO          CH3   CH3    H    OH    OB603    CH3SO2        CH3   CH3    H    OH    OB604    Ph              CH3   CH3    H    OH    OB605    CH3O           CH3   CH3    H    OH    OB606    CH3OC(O)       CH3   CH3    H    OH    OB607    CH3CH2OC(O)   CH3   CH3    H    OH    OB608    CH2=CHCH2    CH3   CH3    H    OH    OB609     HCCCH2         CH3   CH3    H    OH    OB610    CF3             CH3   CH3    H    OH    OB611    (CH3)2NSO2   CH3   CH3    H    OH    OB612    (CH3)2N       CH3   CH3    H    OH    OB613    PhO             CH3   CH3    H    OH    OB614    PhS             CH3   CH3    H    OH    OB615    PhSO            CH3   CH3    H    OH    OB616    PhSO2          CH3   CH3    H    OH    O基团    R6             R7        R8  R9    R10  WB617    CN             CH3        CH3  H      OH    OB618    CH3           CH3       CH3  CH3   OH    OB619    CH3CH2       CH3       CH3  CH3   OH    OB620    CH3CH2CH2   CH3       CH3  CH3   OH    OB621    (CH3)2CH     CH3       CH3  CH3   OH    OB622    (CH3)3C      CH3       CH3  CH3   OH    OB623    CH3S          CH3       CH3  CH3   OH    OB624    CH3SO         CH3       CH3  CH3   OH    OB625    CH3SO2       CH3       CH3  CH3   OH    OB626    Ph             CH3       CH3  CH3   OH    OB627    CH3O          CH3       CH3  CH3   OH    OB628    CH3OC(O)      CH3       CH3  CH3   OH    OB629    CH3CH2OC(O)  CH3       CH3  CH3   OH    OB630    CH2=CHCH2   CH3       CH3  CH3   OH    OB631    HCCCH2        CH3       CH3  CH3   OH    OB632    CF3           CH3       CH3  CH3   OH    OB633    (CH3)2NSO2  CH3       CH3  CH3   OH    OB634    (CH3)2N      CH3       CH3  CH3   OH    OB635    PhO            CH3       CH3  CH3   OH    OB636    PhS            CH3       CH3  CH3   OH    OB637    PhSO           CH3       CH3  CH3   OH    OB638    PhSO2         CH3       CH3  CH3   OH    OB639    CN             CH3       CH3  CH3   OH    OB640    CH3CH2      CH3CH2   H     H      OH    OB641    CH3CH2CH2  CH3CH2   H     H      OH    OB642    (CH3)2CH    CH3CH2   H     H      OH    OB643    (CH3)3C     CH3CH2   H     H      OH    OB644    CH3S         CH3CH2   H     H      OH    OB645    CH3SO        CH3CH2   H     H      OH    OB646    CH3SO2      CH3CH2   H     H      OH    OB647    Ph            CH3CH2   H     H      OH    OB648    CH3O         CH3CH2   H     H      OH    OB649    CH3OC(O)     CH3CH2   H     H      OH    O基团    R6               R7         R8  R9  R10  WB650    CH3CH2OC(O)    CH3CH2    H    H    OH    OB651    CH2=CHCH2     CH3CH2    H    H    OH    OB652    HCCCH2          CH3CH2    H    H    OH    OB653    CF3             CH3CH2    H    H    OH    OB654    (CH3)2NSO2    CH3CH2    H    H    OH    OB655    (CH3)2N        CH3CH2    H    H    OH    OB656    PhO              CH3CH2    H    H    OH    OB657    PhS              CH3CH2    H    H    OH    OB658    PhSO             CH3CH2    H    H    OH    OB659    PhSO2           CH3CH2    H    H    OH    OB660    CN               CH3CH2    H    H    OH    OB661    H                H           H    H    OH    SB662    CH3             H           H    H    OH    SB663    CH3CH2         H           H    H    OH    SB664    CH3CH2CH2     H           H    H    OH    SB665    (CH3)2CH       H           H    H    OH    SB666    (CH3)3C        H           H    H    OH    SB667    CH3S            H           H    H    OH    SB668    CH3SO           H           H    H    OH    SB669    CH3SO2         H           H    H    OH    SB670    Ph               H           H    H    OH    SB671    CH3O            H           H    H    OH    SB672    CH3OC(O)        H           H    H    OH    SB673    CH3CH2OC(O)    H           H    H    OH    SB674    CH2=CHCH2     H           H    H    OH    SB675    HCCCH2          H           H    H    OH    SB676    CF3             H           H    H    OH    SB677    (CH3)2NSO2   H           H    H    OH    SB678    (CH3)2N       H           H    H    OH    SB679    PhO              H           H    H    OH    SB680    PhS              H           H    H    OH    SB681    PhSO             H           H    H    OH    SB682    PhSO2           H           H    H    OH    S基团    R6             R7    R8  R9  R10  WB683    CN              H       H     H    OH    SB684    CH3           CH3    H     H    OH    SB685    CH3CH2       CH3    H     H    OH    SB686    CH3CH2CH2   CH3    H     H    OH    SB687    (CH3)2CH     CH3    H     H    OH    SB688    (CH3)3C      CH3    H     H    OH    SB689    CH3S          CH3    H     H    OH    SB690    CH3SO         CH3    H     H    OH    SB691    CH3SO2       CH3    H     H    OH    SB692    Ph             CH3    H     H    OH    SB693    CH3O          CH3    H     H    OH    SB694    CH3OC(O)      CH3    H     H    OH    SB695    CH3CH2OC(O)  CH3    H     H    OH    SB696    CH2=CHCH2   CH3    H     H    OH    SB697    HCCCH2        CH3    H     H    OH    SB698    CF3           CH3    H     H    OH    SB699    (CH3)2NSO2  CH3    H     H    OH    SB700    (CH3)2N      CH3    H     H    OH    SB701    PhO            CH3    H     H    OH    SB702    PhS            CH3    H     H    OH    SB703    PhSO           CH3    H     H    OH    SB704    PhSO2         CH3    H     H    OH    SB705    CN             CH3    H     H    OH    SB706    CH3           H       CH3  H    OH    SB707    CH3CH2       H       CH3  H    OH    SB708    CH3CH2CH2   H       CH3  H    OH    SB709    (CH3)2CH     H       CH3  H    OH    SB710    (CH3)3C      H       CH3  H    OH    SB711    CH3S          H       CH3  H    OH    SB712    CH3SO         H       CH3  H    OH    SB713    CH3SO2       H       CH3  H    OH    SB714    Ph             H       CH3  H    OH    SB715    CH3O          H       CH3  H    OH    S基团    R6              R7     R8    R9  R10  WB716    CH3OC(O)        H       CH3    H    OH    SB717    CH3CH2OC(O)    H       CH3    H    OH    SB718    CH2=HCH2      H       CH3    H    OH    SB719    HCCCH2          H       CH3    H    OH    SB720    CF3             H       CH3    H    OH    SB721    (CH3)2NSO2    H       CH3    H    OH    SB722    (CH3)2N        H       CH3    H    OH    SB723    PhO              H       CH3    H    OH    SB724    PhS              H       CH3    H    OH    SB725    PhSO             H       CH3    H    OH    SB726    PhSO2           H       CH3    H    OH    SB727    CN               H       CH3    H    OH    SB728    CH3             CH3    CH3    H    OH    SB729    CH3CH2         CH3    CH3    H    OH    SB730    CH3CH2CH2     CH3    CH3    H    OH    SB731    (CH3)2CH       CH3    CH3    H    OH    SB732    (CH3)3C        CH3    CH3    H    OH    SB733    CH3S            CH3    CH3    H    OH    SB734    CH3SO           CH3    CH3    H    OH    SB735    CH3SO2         CH3    CH3    H    OH    SB736    Ph               CH3    CH3    H    OH    SB737    CH3O            CH3    CH3    H    OH    SB738    CH3OC(O)        CH3    CH3    H    OH    SB739    CH3CH2OC(O)    CH3    CH3    H    OH    SB740    CH2=CHCH2     CH3    CH3    H    OH    SB741    HCCCH2          CH3    CH3    H    OH    SB742    CF3             CH3    CH3    H    OH    SB743    (CH3)2NSO2    CH3    CH3    H    OH    SB744    (CH3)2N        CH3    CH3    H    OH    SB745    PhO              CH3    CH3    H    OH    SB746    PhS              CH3    CH3    H    OH    SB747    PhSO             CH3    CH3    H    OH    SB748    PhSO2           CH3    CH3    H    OH    S基团    R6            R7       R8  R9     R10   WB749    CN             CH3      CH3  H       OH    SB750    CH3           CH3      CH3  CH3    OH    SB751    CH3CH2       CH3      CH3  CH3    OH    SB752    CH3CH2CH2   CH3      CH3  CH3    OH    SB753    (CH3)2CH     CH3      CH3  CH3    OH    SB754    (CH3)3C      CH3      CH3  CH3    OH    SB755    CH3S          CH3      CH3  CH3    OH    SB756    CH3SO         CH3      CH3  CH3    OH    SB757    CH3SO2       CH3      CH3  CH3    OH    SB758    Ph             CH3      CH3  CH3    OH    SB759    CH3O          CH3      CH3  CH3    OH    SB760    CH3OC(O)      CH3      CH3  CH3    OH    SB761    CH3CH2OC(O)  CH3      CH3  CH3    OH    SB762    CH2=CHCH2   CH3      CH3  CH3    OH    SB763    HCCCH2        CH3      CH3  CH3    OH    SB764    CF3           CH3      CH3  CH3    OH    SB765    (CH3)2NSO2  CH3      CH3  CH3    OH    SB766    (CH3)2N      CH3      CH3  CH3    OH    SB767    PhO            CH3      CH3  CH3    OH    SB768    PhS            CH3      CH3  CH3    OH    SB769    PhSO           CH3      CH3  CH3    OH    SB770    PhSO2         CH3      CH3  CH3    OH    SB771    CN             CH3      CH3  CH3    OH    SB772    CH3CH2       CH3CH2   H    H       OH    SB773    CH3CH2CH2   CH3CH2   H    H       OH    SB774    (CH3)2CH     CH3CH2   H    H       OH    SB775    (CH3)3C      CH3CH2   H    H       OH    SB776    CH3S          CH3CH2   H    H       OH    SB777    CH3SO         CH3CH2   H    H       OH    SB778    CH3SO2       CH3CH2   H    H       OH    SB779    Ph             CH3CH2   H    H       OH    SB780    CH3O          CH3CH2   H    H       OH    SB781    CH3OC(O)      CH3CH2   H    H       OH    S基团    R6               R7        R8   R9  R10  WB782    CH3CH2OC(O)    CH3CH2    H    H    OH    SB783    CH2=CHCH2     CH3CH2    H    H    OH    SB784    HCCCH2          CH3CH2    H    H    OH    SB785    CF3             CH3CH2    H    H    OH    SB786    (CH3)2NSO2    CH3CH2    H    H    OH    SB787    (CH3)2N        CH3CH2    H    H    OH    SB788    PhO              CH3CH2    H    H    OH    SB789    PhS              CH3CH2    H    H    OH    SB790    PhSO             CH3CH2    H    H    OH    SB791    PhSO2           CH3CH2    H    H    OH    SB792    CN               CH3CH2    H    H    OH    SB793    H                H           H    H    OH    SO2B794    CH3             H           H    H    OH    SO2B795    CH3CH2         H           H    H    OH    SO2B796    CH3CH2CH2     H           H    H    OH    SO2B797    (CH3)2CH       H           H    H    OH    SO2B798    (CH3)3C        H           H    H    OH    SO2B799    CH3S            H           H    H    OH    SO2B800    CH3SO           H           H    H    OH    SO2B801    CH3SO2         H           H    H    OH    SO2B802    Ph               H           H    H    OH    SO2B803    CH3O            H           H    H    OH    SO2B804    CH3OC(O)        H           H    H    OH    SO2B805    CH3CH2OC(O)    H           H    H    OH    SO2B806    CH2=CHCH2     H           H    H    OH    SO2B807    HCCCH2          H           H    H    OH    SO2B808    CF3             H           H    H    OH    SO2B809    (CH3)2NSO2    H           H    H    OH    SO2B810    (CH3)2N        H           H    H    OH    SO2B811    PhO              H           H    H    OH    SO2B812    PhS              H           H    H    OH    SO2B813    PhSO             H           H    H    OH    SO2B814    PhSO2           H           H    H    OH    SO2基团    R6             R7     R8    R9   R10   WB815    CN               H       H      H     OH    SO2B816    CH3             CH3    H      H     OH    SO2B817    CH3CH2         CH3    H      H     OH    SO2B818    CH3CH2CH2     CH3    H      H     OH    SO2B819    (CH3)2CH       CH3    H      H     OH    SO2B820    (CH3)3C        CH3    H      H     OH    SO2B821    CH3S            CH3    H      H     OH    SO2B822    CH3SO           CH3    H      H     OH    SO2B823    CH3SO2         CH3    H      H     OH    SO2B824    Ph               CH3    H      H     OH    SO2B825    CH3O            CH3    H      H     OH    SO2B826    CH3OC(O)        CH3    H      H     OH    SO2B827    CH3CH2OC(O)    CH3    H      H     OH    SO2B828    CH2=CHCH2     CH3    H      H     OH    SO2B829    HCCCH2          CH3    H      H     OH    SO2B830    CF3             CH3    H      H     OH    SO2B831    (CH3)2NSO2    CH3    H      H     OH    SO2B832    (CH3)2N        CH3    H      H     OH    SO2B833    PhO              CH3    H      H     OH    SO2B834    PhS              CH3    H      H     OH    SO2B835    PhSO             CH3    H      H     OH    SO2B836    PhSO2           CH3    H      H     OH    SO2B837    CN               CH3    H      H     OH    SO2B838    CH3             H       CH3   H     OH    SO2B839    CH3CH2         H       CH3   H     OH    SO2B840    CH3CH2CH2     H       CH3   H     OH    SO2B841    (CH3)2CH       H       CH3   H     OH    SO2B842    (CH3)3C        H       CH3   H     OH    SO2B843    CH3S            H       CH3   H     OH    SO2B844    CH3SO           H       CH3   H     OH    SO2B845    CH3SO2         H       CH3   H     OH    SO2B846    Ph               H       CH3   H     OH    SO2B847    CH3O            H       CH3   H     OH    SO2基团    R6              R7     R8    R9  R10   WB848    CH3OC(O)        H       CH3    H    OH    SO2B849    CH3CH2OC(O)    H       CH3    H    OH    SO2B850    CH2=CHCH2     H       CH3    H    OH    SO2B851    HCCCH2          H       CH3    H    OH    SO2B852    CF3             H       CH3    H    OH    SO2B853    (CH3)2NSO2    H       CH3    H    OH    SO2B854    (CH3)2N        H       CH3    H    OH    SO2B855    PhO              H       CH3    H    OH    SO2B856    PhS              H       CH3    H    OH    SO2B857    PhSO             H       CH3    H    OH    SO2B858    PhSO2           H       CH3    H    OH    SO2B859    CN               H       CH3    H    OH    SO2B860    CH3             CH3    CH3    H    OH    SO2B861    CH3CH2         CH3    CH3    H    OH    SO2B862    CH3CH2CH2     CH3    CH3    H    OH    SO2B863    (CH3)2CH       CH3    CH3    H    OH    SO2B864    (CH3)3C        CH3    CH3    H    OH    SO2B865    CH3S            CH3    CH3    H    OH    SO2B866    CH3SO           CH3    CH3    H    OH    SO2B867    CH3SO2         CH3    CH3    H    OH    SO2B868    Ph               CH3    CH3    H    OH    SO2B869    CH3O            CH3    CH3    H    OH    SO2B870    CH3OC(O)        CH3    CH3    H    OH    SO2B871    CH3CH2OC(O)    CH3    CH3    H    OH    SO2B872    CH2=CHCH2     CH3    CH3    H    OH    SO2B873    HCCCH2          CH3    CH3    H    OH    SO2B874    CF3             CH3    CH3    H    OH    SO2B875    (CH3)2NSO2    CH3    CH3    H    OH    SO2B876    (CH3)2N        CH3    CH3    H    OH    SO2B877    PhO              CH3    CH3    H    OH    SO2B878    PhS              CH3    CH3    H    OH    SO2B879    PhSO             CH3    CH3    H    OH    SO2B880    PhSO2           CH3    CH3    H    OH    SO2基团    R6            R7        R8   R9     R10   WB881    CN             CH3       CH3  H       OH    SO2B882    CH3           CH3       CH3  CH3    OH    SO2B883    CH3CH2       CH3       CH3  CH3    OH    SO2B884    CH3CH2CH2   CH3       CH3  CH3    OH    SO2B885    (CH3)2CH     CH3       CH3  CH3    OH    SO2B886    (CH3)3C      CH3       CH3  CH3    OH    SO2B887    CH3S          CH3       CH3  CH3    OH    SO2B888    CH3SO         CH3       CH3  CH3    OH    SO2B889    CH3SO2       CH3       CH3  CH3    OH    SO2B890    Ph             CH3       CH3  CH3    OH    SO2B891    CH3O          CH3       CH3  CH3    OH    SO2B892    CH3OC(O)      CH3       CH3  CH3    OH    SO2B893    CH3CH2OC(O)  CH3       CH3  CH3    OH    SO2B894    CH2=CHCH2   CH3       CH3  CH3    OH    SO2B895    HCCCH2        CH3       CH3  CH3    OH    SO2B896    CF3           CH3       CH3  CH3    OH    SO2B897    (CH3)2NSO2  CH3       CH3  CH3    OH    SO2B898    (CH3)2N      CH3       CH3  CH3    OH    SO2B899    PhO            CH3       CH3  CH3    OH    SO2B900    PhS            CH3       CH3  CH3    OH    SO2B901    PhSO           CH3       CH3  CH3    OH    SO2B902    PhSO2         CH3       CH3  CH3    OH    SO2B903    CN             CH3       CH3  CH3    OH    SO2B904    CH3CH2       CH3CH2   H     H       OH    SO2B905    CH3CH2CH2   CH3CH2   H     H       OH    SO2B906    (CH3)2CH     CH3CH2   H     H       OH    SO2B907    (CH3)3C      CH3CH2   H     H       OH    SO2B908    CH3S          CH3CH2   H     H       OH    SO2B909    CH3SO         CH3CH2   H     H       OH    SO2B910    CH3SO2       CH3CH2   H     H       OH    SO2B911    Ph             CH3CH2   H     H       OH    SO2B912    CH3O          CH3CH2   H     H       OH    SO2B913    CH3OC(O)      CH3CH2   H     H       OH    SO2基团    R6              R7        R8   R9  R10  WB914    CH3CH2OC(O)    CH3CH2  H     H    OH    SO2B915    CH2=CHCH2     CH3CH2  H     H    OH    SO2B916    HCCCH2          CH3CH2  H     H    OH    SO2B917    CF3             CH3CH2  H     H    OH    SO2B918    (CH3)2NSO2    CH3CH2  H     H    OH    SO2B919    (CH3)2N        CH3CH2  H     H    OH    SO2B920    PhO              CH3CH2  H     H    OH    SO2B921    PhS              CH3CH2  H     H    OH    SO2B922    PhSO             CH3CH2  H     H    OH    SO2B923    PhSO2           CH3CH2  H     H    OH    SO2B924    CN               CH3CH2  H     H    OH    SO2B925    H                H         H     H    OH    CHC(O)OCH2CH3B926    CH3             H         H     H    OH    CHC(O)OCH2CH3B927    CH3CH2         H         H     H    OH    CHC(O)OCH2CH3B928    CH3CH2CH2     H         H     H    OH    CHC(O)OCH2CH3B929    (CH3)2CH       H         H     H    OH    CHC(O)OCH2CH3B930    (CH3)3C        H         H     H    OH    CHC(O)OCH2CH3B931    CH3S            H         H     H    OH    CHC(O)OCH2CH3B932    CH3SO           H         H     H    OH    CHC(O)OCH2CH3B933    CH3SO2         H         H     H    OH    CHC(O)OCH2CH3B934    Ph               H         H     H    OH    CHC(O)OCH2CH3B935    CH3O            H         H     H    OH    CHC(O)OCH2CH3B936    CH3OC(O)        H         H     H    OH    CHC(O)OCH2CH3B937    CH3CH2OC(O)    H         H     H    OH    CHC(O)OCH2CH3B938    CH2=CHCH2     H         H     H    OH    CHC(O)OCH2CH3B939    HCCCH2          H         H     H    OH    CHC(O)OCH2CH3B940    CF3             H         H     H    OH    CHC(O)OCH2CH3B941    (CH3)2NSO2    H         H     H    OH    CHC(O)OCH2CH3B942    (CH3)2N        H         H     H    OH    CHC(O)OCH2CH3B943    PhO              H         H     H    OH    CHC(O)OCH2CH3B944    PhS              H         H     H    OH    CHC(O)OCH2CH3B945    PhSO             H         H     H    OH    CHC(O)OCH2CH3B946    PhSO2           H         H     H    OH    CHC(O)OCH2CH3基团    R6           R7     R8    R9  R10     WB947    CN             H       H      H    OH    CHC(O)OCH2CH3B948    CH3           CH3    H      H    OH    CHC(O)OCH2CH3B949    CH3CH2       CH3    H      H    OH    CHC(O)OCH2CH3B950    CH3CH2CH2   CH3    H      H    OH    CHC(O)OCH2CH3B951    (CH3)2CH     CH3    H      H    OH    CHC(O)OCH2CH3B952    (CH3)3C      CH3    H      H    OH    CHC(O)OCH2CH3B953    CH3S          CH3    H      H    OH    CHC(O)OCH2CH3B954    CH3SO         CH3    H      H    OH    CHC(O)OCH2CH3B955    CH3SO2       CH3    H      H    OH    CHC(O)OCH2CH3B956    Ph             CH3    H      H    OH    CHC(O)OCH2CH3B957    CH3O          CH3    H      H    OH    CHC(O)OCH2CH3B958    CH3OC(O)      CH3    H      H    OH    CHC(O)OCH2CH3B959    CH3CH2OC(O)  CH3    H      H    OH    CHC(O)OCH2CH3B960    CH2=CHCH2   CH3    H      H    OH    CHC(O)OCH2CH3B961    HCCCH2        CH3    H      H    OH    CHC(O)OCH2CH3B962    CF3           CH3    H      H    OH    CHC(O)OCH2CH3B963    (CH3)2NSO2  CH3    H      H    OH    CHC(O)OCH2CH3B964    (CH3)2N      CH3    H      H    OH    CHC(O)OCH2CH3B965    PhO            CH3    H      H    OH    CHC(O)OCH2CH3B966    PhS            CH3    H      H    OH    CHC(O)OCH2CH3B967    PhSO           CH3    H      H    OH    CHC(O)OCH2CH3B968    PhSO2         CH3    H      H    OH    CHC(O)OCH2CH3B969    CN             CH3    H      H    OH    CHC(O)OCH2CH3B970    CH3           H       CH3   H    OH    CHC(O)OCH2CH3B971    CH3CH2       H       CH3   H    OH    CHC(O)OCH2CH3B972    CH3CH2CH2   H       CH3   H    OH    CHC(O)OCH2CH3B973    (CH3)2CH     H       CH3   H    OH    CHC(O)OCH2CH3B974    (CH3)3C      H       CH3   H    OH    CHC(O)OCH2CH3B975    CH3S          H       CH3   H    OH    CHC(O)OCH2CH3B976    CH3SO         H       CH3   H    OH    CHC(O)OCH2CH3B977    CH3SO2       H       CH3   H    OH    CHC(O)OCH2CH3B978    Ph             H       CH3   H    OH    CHC(O)OCH2CH3B979    CH3O          H       CH3   H    OH    CHC(O)OCH2CH3基团     R6             R7     R8     R9   R10     WB980     CH3OC(O)        H       CH3    H    OH    CHC(O)OCH2CH3B981     CH3CH2OC(O)    H       CH3    H    OH    CHC(O)OCH2CH3B982     CH2=CHCH2     H       CH3    H    OH    CHC(O)OCH2CH3B983     HCCCH2          H       CH3    H    OH    CHC(O)OCH2CH3B984     CF3             H       CH3    H    OH    CHC(O)OCH2CH3B985     (CH3)2NSO2    H       CH3    H    OH    CHC(O)OCH2CH3B986     (CH3)2N        H       CH3    H    OH    CHC(O)OCH2CH3B987     PhO              H       CH3    H    OH    CHC(O)OCH2CH3B988     PhS              H       CH3    H    OH    CHC(O)OCH2CH3B989     PhSO             H       CH3    H    OH    CHC(O)OCH2CH3B990     PhSO2           H       CH3    H    OH    CHC(O)OCH2CH3B991     CN               H       CH3    H    OH    CHC(O)OCH2CH3B992     CH3             CH3    CH3    H    OH    CHC(O)OCH2CH3B993     CH3CH2         CH3    CH3    H    OH    CHC(O)OCH2CH3B994     CH3CH2CH2     CH3    CH3    H    OH    CHC(O)OCH2CH3B995     (CH3)2CH       CH3    CH3    H    OH    CHC(O)OCH2CH3B996     (CH3)3C        CH3    CH3    H    OH    CHC(O)OCH2CH3B997     CH3S            CH3    CH3    H    OH    CHC(O)OCH2CH3B998     CH3SO           CH3    CH3    H    OH    CHC(O)OCH2CH3B999     CH3SO2         CH3    CH3    H    OH    CHC(O)OCH2CH3B1000    Ph               CH3    CH3    H    OH    CHC(O)OCH2CH3B1001    CH3O            CH3    CH3    H    OH    CHC(O)OCH2CH3B1002    CH3OC(O)        CH3    CH3    H    OH    CHC(O)OCH2CH3B1003    CH3CH2OC(O)    CH3    CH3    H    OH    CHC(O)OCH2CH3B1004    CH2=CHCH2     CH3    CH3    H    OH    CHC(O)OCH2CH3B1005    HCCCH2          CH3    CH3    H    OH    CHC(O)OCH2CH3B1006    CF3             CH3    CH3    H    OH    CHC(O)OCH2CH3B1007    (CH3)2NSO2    CH3    CH3    H    OH    CHC(O)OCH2CH3B1008    (CH3)2N        CH3    CH3    H    OH    CHC(O)OCH2CH3B1009    PhO              CH3    CH3    H    OH    CHC(O)OCH2CH3B1010    PhS              CH3    CH3    H    OH    CHC(O)OCH2CH3B1011    PhSO             CH3    CH3    H    OH    CHC(O)OCH2CH3B1012    PhSO2           CH3    CH3    H    OH    CHC(O)OCH2CH3基团     R6             R7        R8  R9      R10       WB1013    CN              CH3        CH3 H       OH    CHC(O)OCH2CH3B1014    CH3            CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1015    CH3CH2        CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1016    CH3CH2CH2    CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1017    (CH3)2CH      CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1018    (CH3)3C       CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1019    CH3S           CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1020    CH3SO          CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1021    CH3SO2        CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1022    Ph              CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1023    CH3O           CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1024    CH3OC(O)       CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1025    CH3CH2OC(O)   CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1026    CH2=CHCH2    CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1027    HCCCH2         CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1028    CF3            CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1029    (CH3)2NSO2   CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1030    (CH3)2N       CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1031    PhO             CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1032    PhS             CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1033    PhSO            CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1034    PhSO2          CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1035    CN              CH3        CH3 CH3    OH    CHC(O)OCH2CH3B1036    CH3CH2        CH3CH2    H    H       OH    CHC(O)OCH2CH3B1037    CH3CH2CH2    CH3CH2    H    H       OH    CHC(O)OCH2CH3B1038    (CH3)2CH      CH3CH2    H    H       OH    CHC(O)OCH2CH3B1039    (CH3)3C       CH3CH2    H    H       OH    CHC(O)OCH2CH3B1040    CH3S           CH3CH2    H    H       OH    CHC(O)OCH2CH3B1041    CH3SO          CH3CH2    H    H       OH    CHC(O)OCH2CH3B1042    CH3SO2        CH3CH2    H    H       OH    CHC(O)OCH2CH3B1043    Ph              CH3CH2    H    H       OH    CHC(O)OCH2CH3B1044    CH3O           CH3CH2    H    H       OH    CHC(O)OCH2CH3B1045    CH3OC(O)       CH3CH2    H    H       OH    CHC(O)OCH2CH3基团     R6            R7       R8  R9  R10       WB1046    CH3CH2OC(O)  CH3CH2  H    H    OH    CHC(O)OCH2CH3B1047    CH2=CHCH2   CH3CH2  H    H    OH    CHC(O)OCH2CH3B1048    HCCCH2        CH3CH2  H    H    OH    CHC(O)OCH2CH3B1049    CF3           CH3CH2  H    H    OH    CHC(O)OCH2CH3B1050    (CH3)2NSO2 CH3CH2  H    H    OH    CHC(O)OCH2CH3B1051    (CH3)2N      CH3CH2  H    H    OH    CHC(O)OCH2CH3B1052    PhO            CH3CH2  H    H    OH    CHC(O)OCH2CH3B1053    PhS            CH3CH2  H    H    OH    CHC(O)OCH2CH3B1054    PhSO           CH3CH2  H    H    OH    CHC(O)OCH2CH3B1055    PhSO2         CH3CH2  H    H    OH    CHC(O)OCH2CH3B1056    CN             CH3CH2  H    H    OH    CHC(O)OCH2CH3B1057    CH3OC(O)      H         H    H    OH    CHPhB1058    H              H         H    H    OH    CHPhB1059    H              H         H    H    OH    CH(CH2CH3)B1060    H              H         H    H    OH    CH(CH2CH2CH3)B1061    H              H         H    H    OH    CH(CH(CH3)2)B1062    H              H         H    H    OH    CH(C(CH3)3)B1063    H              H         H    H    OH    C(CH3)2B1064    H              H         H    H    OH    CH(CF3)B1065    CH3OC(O)      H         H    H    OH    C(CH3)(CF3)B1066    H              H         H    H    OH    C(CH3)(CF3)B1067    CH3OC(O)      CH3O     H    H    OH    CH2B1068    H              CH3O     H    H    OH    CH2B1069    CH3O          CH3OC(O) H    CH3 OH    CH2B1070    CH3O          H         CH3 H    OH    CH2B1071    Cl             H         H    H    OH    CH2B1072    F              H         H    H    OH    CH2B1073    H              H         H    H    OH    CH(OCH3)2B1074    H              H         H    H    OH    CH2OSO2CH3B1075    CH3           CH3      CH3 CH3 OH    S(O)B1076    ClCH2CH2     H         H    H    OH    CH2B1077    HO(CH2)2     H         H    H    OH    CH2B1078    MsO(CH2)2    H         H    H    OH    CH2基团     R6             R7       R8    R9    R10              WB1079    HOCH(CH3)CH2  H         H      H      OH                CH2B1080    MsOCH(CH3)CH2 H         H      H      OH                CH2B1081    (CH3)2CH      H         CH3   CH3   OH                CH2B1082    HCCCH2         H         CH3   CH3   OH                CH2B1083    H2C=CCH2     H         CH3   CH3   OH                CH2B1084    H2C=C(CH3)   H         H      H      OH                CHCH3B1085    H               H         H      H      OH                CHCONHCH2PhB1086    H               H         H      H      OH            
Figure A9981578601451
B1087    CH3OC(O)       CH3      H      H      OH                C(CH3)2B1088    H               H         H      H      OH            
Figure A9981578601452
B1089    CH3CH2        H         CH3   CH3   OH                CH2B1090    CH3OC(O)       H         H      H      OH                CF3CH2CH2B1091    CH3CH2S      CH3CH2  CH3   H      OH                CH2B1092    CH3S           Ph        CH3   H      OH                CH2B1093    CH3CH2       CH3CH2  CH3   H      OH                CH2B1094    CH3OC(O)       H         H      H      OH                C(CH3)2B1095    CH3            H         H      H      OH                C(CH3)2B1096    H               H         H      H      OH                NCOCH2SCH3B1097   
Figure A9981578601453
        H         H      H      OH                CH2B1098 1,1-二甲基乙烯基  H         H      H      OH                CH2B1099   
Figure A9981578601454
   H         H      H      OH                CH2B1100    H               H         H      H      -ONH+(CH2CH3)3CH2B1101    H               H         H      H      -ONH+(CH2CH3)3CH(CH3)B1102    H               H         H      H      PhS               CH2B1103    H               H         H      H      PhSO              CH2B1104    H               H         H      H      PhSO2            CH2B1105    CH3           CH3      CH3   CH3   Cl                C=OB1106    H               H         H      H      OH                CHCH2CH(CH3)2基团     R6             R7     R8     R9     R10         WB1107    CH3             CH3    CH3   CH3   CH3C(O)O   C=OB1108    CH3OC(O)CH2    H       H      H      OH          CH2B1109    CH3OC(O)CH2    CH3    H      H      OH          CH2B1110    CH3OC(O)CH2    CH3    CH3   H      OH          CH2B1111    CH3OC(O)CH2    CH3    CH3   CH3   OH          CH2B1112    CH3OC(O)CH2    H       CH3   CH3   OH          CH2B1113    CH3OC(O)CH2    H       H      H      OH          CH(CH3)B1114    CH3OC(O)CH2    CH3    H      H      OH          CH(CH3)B1115    CH3OC(O)CH2    CH3    CH3   H      OH          CH(CH3)B1116    CH3OC(O)CH2    CH3    CH3   CH3   OH          CH(CH3)B1117    CH3OC(O)CH2    H       CH3   CH3   OH          CH(CH3)B1118    CH3OC(O)CH2    H       H      H      OH          C(CH3)2B1119    CH3OC(O)CH2    CH3    H      H      OH          C(CH3)2B1120    CH3OC(O)CH2    CH3    CH3   H      OH          C(CH3)2B1121    CH3OC(O)CH2    CH3    CH3   CH3   OH          C(CH3)2B1122    CH3OC(O)CH2    H       CH3   CH3   OH          C(CH3)2B1123 CH3CH2OC(O)CH2   H       H      H      OH          CH2B1124 CH3CH2OC(O)CH2   CH3    H      H      OH          CH2B1125 CH3CH2OC(O)CH2   CH3    CH3   H      OH          CH2B1126 CH3CH2OC(O)CH2   CH3    CH3   CH3   OH          CH2B1127 CH3CH2OC(O)CH2   H       CH3   CH3   OH          CH2B1128 CH3CH2OC(O)CH2   H       H      H      OH          CH(CH3)B1129 CH3CH2OC(O)CH2   CH3    H      H      OH          CH(CH3)B1130 CH3CH2OC(O)CH2   CH3    CH3   H      OH          CH(CH3)B1131 CH3CH2OC(O)CH2   CH3    CH3   CH3   OH          CH(CH3)B1132 CH3CH2OC(O)CH2   H       CH3   CH3   OH          CH(CH3)B1133 CH3CH2OC(O)CH2   H       H      H      OH          C(CH3)2B1134 CH3CH2OC(O)CH2   CH3    H      H      OH          C(CH3)2B1135 CH3CH2OC(O)CH2   CH3    CH3   H      OH          C(CH3)2B1136 CH3CH2OC(O)CH2   CH3    CH3   CH3   OH          C(CH3)2B1137 CH3CH2OC(O)CH2   H       CH3   CH3   OH          C(CH3)2B1138 
Figure A9981578601461
   CH3    H      H      OH          CH2基团     R6             R7    R8    R9    R10   WB1139    CH3SCH2        H      H      H      OH    CH2B1140    CH3SCH2        CH3   H      H      OH    CH2B1141    CH3SCH2        CH3   CH3   H      OH    CH2B1142    CH3SCH2        CH3   CH3   CH3   OH    CH2B1143    CH3SCH2        H      CH3   CH3   OH    CH2B1144    CH3SOCH2       H      H      H      OH    CH2B1145    CH3SOCH2       CH3   H      H      OH    CH2B1146    CH3SOCH2       CH3   CH3   H      OH    CH2B1147    CH3SOCH2       CH3   CH3   CH3   OH    CH2B1148    CH3SOCH2        H      CH3   CH3   OH    CH2B1149    CH3SO2CH2     H      H      H      OH    CH2B1150    CH3SO2CH2     CH3   H      H      OH    CH2B1151    CH3SO2CH2     CH3   CH3   H      OH    CH2B1152    CH3SO2CH2     CH3   CH3   CH3   OH    CH2B1153    CH3SO2CH2     H      CH3   CH3   OH    CH2B1154    HOCH2           H      H      H      OH    CH2B1155    HOCH2           CH3   H      H      OH    CH2B1156    HOCH2           CH3   CH3   H      OH    CH2B1157    HOCH2           CH3   CH3   CH3   OH    CH2B1158    HOCH2           H      CH3   CH3   OH    CH2B1159    NCCH2           H      H      H      OH    CH2B1160    NCCH2           CH3   H      H      OH    CH2B1161    NCCH2           CH3   CH3   H      OH    CH2B1162    NCCH2           CH3   CH3   CH3   OH    CH2B1163    NCCH2           H      CH3   CH3   OH    CH2B1164    CH3C(O)OCH2    H      H      H      OH    CH2B1165    CH3C(O)OCH2    CH3   H      H      OH    CH2B1166    CH3C(O)OCH2    CH3   CH3   H      OH    CH2B1167    CH3C(O)OCH2    CH3   CH3   CH3   OH    CH2B1168    CH3C(O)OCH2    H      CH3   CH3   OH    CH2B1169    CH3OCH2        H      H      H      OH    CH2B1170    CH3OCH2        CH3   H      H      OH    CH2B1171    CH3OCH2        CH3    CH3   H      OH    CH2基团     R6         R7   R8  R9  R10                  WB1172    CH3OCH2  CH3  CH3  CH3 OH                    CH2B1173    CH3OCH2  H     CH3  CH3 OH                    CH2B1174    PhCH2     H      H     H    OH                    CH2B1175    PhCH2     CH3  H     H    OH                    CH2B1176    PhCH2     CH3  CH3  H    OH                    CH2B1177    PhCH2     CH3  CH3  CH3 OH                    CH2B1178    PhCH2     H     CH3  CH3 OH                    CH2B1179    H          H      H     H    O-K+                  CH2B1180    H          H     H     H    S(CH2)7CH3         CH2B1181    H          H     H     H    S(CH2)7CH3         CH2B1182    H          H     H     H    SO(CH2)7CH3        CH2B1183    H          H     H     H    SO2(CH2)7CH3      CH2B1184    H          H     H     H    NHSO2CH3            CH2B1185    H          H     H     H    NH(CO)S(CH2)7CH3   CH2B1186    H          H     H     H    Cl                    CH2B1187    H          H     H     H    NH2                  CH2B1188    H          H     H     H    OC(O)C(CH3)3        CH2B1189    H          H     H     H    OC(O)CH3             CH2B1190    H          H     H     H    OC(O)Ph               CH2B1191    H          H     H     H    OC(O)-环丙基          CH2B1192    H          H     H     H    OC(O)CH2CH3         CH2B1193    H          H     H     H    OC(O)CH=CH2         CH2B1194    H          H     H     H    OC(O)CH=CHCH3       CH2B1195    H          H     H     H    OC(O)SCH3            CH2B1196    H          H     H     H    OC(O)S(CH2)7CH3    CH2B1197    H          H     H     H    OC(O)OCH2CH3        CH2B1198    H          H     H     H    OC(O)N(CH2CH3)2    CH2B1199    H          H     H     H    S-(4-Cl-苯基)         CH2B1200    H          H     H     H    SO-(4-Cl-苯基)        CH2B1201    H          H     H     H    SO2-(4-Cl-苯基)      CH2B1202    H          H     H     H    S-(4-CF3-苯基)       CH2B1203    H          H     H     H    SO-(4-CF3-苯基)      CH2B1204    H          H     H     H    SO2-(4-CF3-苯基)    CH2基团     R6     R7    R8   R9    R10                 WB1205    H       H       H     H    S-(4-NO2-苯基)        CH2B1206    H       H       H     H    SO-(4-NO2-苯基)       CH2B1207    H       H       H     H    SO2-(4-NO2-苯基)     CH2B1208    H       H       H     H      
Figure A9981578601491
              CH2B1209    H       H       H     H      
Figure A9981578601492
               CH2B1210    H       H       H     H      
Figure A9981578601493
             CH2B1211    H       H       H     H                  CH2B1212    H       H       H     H      
Figure A9981578601495
            CH2B1179    CH3    CH3    H    H    O-K+                    CH2B1180    CH3    CH3    H    H    S(CH2)7CH3          CH2B1181    CH3    CH3    H    H    S(CH2)7CH3          CH2B1182    CH3    CH3    H    H    SO(CH2)7CH3         CH2B1183    CH3    CH3    H    H    SO2(CH2)7CH3       CH2B1184    CH3    CH3    H    H    NHSO2CH3             CH2B1185    CH3    CH3    H    H    NH(CO)S(CH2)7CH3    CH2B1186    CH3    CH3    H    H    Cl                     CH2B1187    CH3    CH3    H    H    NH2                   CH2B1188    CH3    CH3    H    H    OC(O)C(CH3)3         CH2B1189    CH3    CH3    H    H    OC(O)CH3              CH2B1190    CH3    CH3    H    H    OC(O)Ph                CH2B1191    CH3    CH3    H    H    OC(O)-环丙基           CH2B1192    CH3    CH3    H    H    OC(O)CH2CH3          CH2B1193    CH3    CH3    H    H    OC(O)CH=CH2          CH2B1194    CH3    CH3    H    H    OC(O)CH=CHCH3        CH2B1195    CH3    CH3    H    H    OC(O)SCH3             CH2B1196    CH3    CH3    H    H    OC(O)S(CH2)7CH3     CH2B1197    CH3    CH3    H    H    OC(O)OCH2CH3         CH2B1198    CH3    CH3    H    H    OC(O)N(CH2CH3)2     CH2B1199    CH3    CH3    H    H    S-(4-Cl-苯基)          CH2B1200    CH3    CH3    H    H    SO-(4-Cl-苯基)         CH2基团     R6     R7     R8  R9   R10               WB1201    CH3    CH3    H    H    SO2-(4-Cl-苯基)   CH2B1202    CH3    CH3    H    H    S-(4-CF3-苯基)    CH2B1203    CH3    CH3    H    H    SO-(4-CF3-苯基)   CH2B1204    CH3    CH3    H    H    SO2-(4-CF3-苯基) CH2B1205    CH3    CH3    H    H    S-(4-NO2-苯基)    CH2B1206    CH3    CH3    H    H    SO-(4-NO2-苯基    CH2B1207    CH3    CH3    H    H    SO2-(4-NO2-苯基) CH2B1208    CH3    CH3    H    H    
Figure A9981578601501
           CH2B1209    CH3    CH3    H    H    
Figure A9981578601502
            CH2B1210    CH3    CH3    H    H                CH2B1211    CH3    CH3    H    H    
Figure A9981578601504
         CH2B1212    CH3    CH3    H    H               CH2B1213    H       H       H    H    OH                 -CH2CH2-B1214    CH3    H       H    H    OH                 -CH2CH2-B1215    CH3    CH3    H    H    OH                 -CH2CH2-B1216    CH3    CH3    CH3 H    OH                 -CH2CH2-B1217    CH3    CH3    CH3 CH3 OH                 -CH2CH2-下表3中,Q代表Q2
Figure A9981578601506
且Q2代表下列基团C:表3:基团C:基团     R6      R7      R16     R10 p    W基团   R6           R7   R16 R10 p   WC1     H              H      H    OH  1    CH2C2     CH3           H      H    OH  1    CH2C3     CH3CH2       H      H    OH  1    CH2C4     CH3CH2CH2   H      H    OH  1    CH2C5     (CH3)2CH     H      H    OH  1    CH2C6     (CH3)3C      H      H    OH  1    CH2C7     CH3S          H      H    OH  1    CH2C8     CH3SO         H      H    OH  1    CH2C9     CH3SO2       H      H    OH  1    CH2C10    Ph             H      H    OH  1    CH2C11    CH3O          H      H    OH  1    CH2C12    CH3OC(O)      H      H    OH  1    CH2C13    CH3CH2OC(O)  H      H    OH  1    CH2C14    CH2=CHCH2   H      H    OH  1    CH2C15    HCCCH2        H      H    OH  1    CH2C16    CF3           H      H    OH  1    CH2C17    (CH3)2NSO2  H      H    OH  1    CH2C18    (CH3)2N      H      H    OH  1    CH2C19    PhO            H      H    OH  1    CH2C20    PhS            H      H    OH  1    CH2C21    PhSO           H      H    OH  1    CH2C22    PhSO2         H      H    OH  1    CH2C23    CN             H      H    OH  1    CH2C24    CH3           CH3   H    OH  1    CH2C25    CH3CH2       CH3   H    OH  1    CH2C26    CH3CH2CH2   CH3   H    OH  1    CH2C27    (CH3)2CH     CH3   H    OH  1    CH2C28    (CH3)3C      CH3   H    OH  1    CH2C29    CH3S          CH3   H    OH  1    CH2C30    CH3SO         CH3   H    OH  1    CH2C31    CH3SO2       CH3   H    OH  1    CH2C32    Ph             CH3   H    OH  1    CH2基团    R6              R7  R16 R10 p    WC33    CH3O            CH3   H    OH  1    CH2C34    CH3OC(O)        CH3   H    OH  1    CH2C35    CH3CH2OC(O)    CH3   H    OH  1    CH2C36    CH2=CHCH2      CH3   H    OH  1    CH2C37    HCCCH2          CH3   H    OH  1    CH2C38    CF3             CH3   H    OH  1    CH2C39    (CH3)2NSO2    CH3   H    OH  1    CH2C40    (CH3)2N        CH3   H    OH  1    CH2C41    PhO              CH3   H    OH  1    CH2C42    PhS              CH3   H    OH  1    CH2C43    PhSO             CH3   H    OH  1    CH2C44    PhSO2           CH3   H    OH  1    CH2C45    CN               CH3   H    OH  1    CH2C46    H                H      H    OH  4    CH2C47    CH3             H      H    OH  4    CH2C48    CH3CH2         H      H    OH  4    CH2C49    CH3CH2CH2     H      H    OH  4    CH2C50    (CH3)2CH       H      H    OH  4    CH2C51    (CH3)3C        H      H    OH  4    CH2C52    CH3S            H      H    OH  4    CH2C53    CH3SO           H      H    OH  4    CH2C54    CH3SO2         H      H    OH  4    CH2C55    Ph               H      H    OH  4    CH2C56    CH3O            H      H    OH  4    CH2C57    CH3OC(O)        H      H    OH  4    CH2C58    CH3CH2OC(O)    H      H    OH  4    CH2C59    CH2=CHCH2      H      H    OH  4    CH2C60    HCCCH2          H      H    OH  4    CH2C61    CF3             H      H    OH  4    CH2C62    (CH3)2NSO2    H      H    OH  4    CH2C63    (CH3)2N        H      H    OH  4    CH2C64    PhO              H      H    OH  4    CH2C65    PhS              H      H    OH  4    CH2基团   R6           R7     R16 R10 p    WC66    PhSO           H       H    OH  4    CH2C67    PhSO2         H       H    OH  4    CH2C68    CN             H       H    OH  4    CH2C69    CH3           CH3    H    OH  4    CH2C70    CH3CH2       CH3    H    OH  4    CH2C71    CH3CH2CH2   CH3    H    OH  4    CH2C72    (CH3)2CH     CH3    H    OH  4    CH2C73    (CH3)3C      CH3    H    OH  4    CH2C74    CH3S          CH3    H    OH  4    CH2C75    CH3SO         CH3    H    OH  4    CH2C76    CH3SO2       CH3    H    OH  4    CH2C77    Ph             CH3    H    OH  4    CH2C78    CH3O          CH3    H    OH  4    CH2C79    CH3OC(O)      CH3    H    OH  4    CH2C80    CH3CH2OC(O)  CH3    H    OH  4    CH2C81    CH2=CHCH2   CH3    H    OH  4    CH2C82    HCCCH2        CH3    H    OH  4    CH2C83    CF3           CH3    H    OH  4    CH2C84    (CH3)2NSO2  CH3    H    OH  4    CH2C85    (CH3)2N      CH3    H    OH  4    CH2C86    PhO            CH3    H    OH  4    CH2C87    PhS            CH3    H    OH  4    CH2C88    PhSO           CH3    H    OH  4    CH2C89    PhSO2         CH3    H    OH  4    CH2C90    CN             CH3    H    OH  4    CH2C91    H              H       H    OH  3    CH2C92    CH3           H       H    OH  3    CH2C93    CH3CH2       H       H    OH  3    CH2C94    CH3CH2CH2   H       H    OH  3    CH2C95    (CH3)2CH     H       H    OH  3    CH2C96    (CH3)3C      H       H    OH  3    CH2C97    CH3S          H       H    OH  3    CH2C98    CH3SO         H       H    OH  3    CH2基团    R6            R7     R16 R10p    WC99     CH3SO2        H      H    OH  3    CH2C100    Ph              H      H    OH  3    CH2C101    CH3O           H      H    OH  3    CH2C102    CH3OC(O)       H      H    OH  3    CH2C103    CH3CH2OC(O)   H      H    OH  3    CH2C104    CH2=CHCH2    H      H    OH  3    CH2C105    HCCCH2         H      H    OH  3    CH2C106    CF3            H      H    OH  3    CH2C107    (CH3)2NSO2   H      H    OH  3    CH2C108    (CH3)2N       H      H    OH  3    CH2C109    PhO             H      H    OH  3    CH2C110    PhS             H      H    OH  3    CH2C111    PhSO            H      H    OH  3    CH2C112    PhSO2          H      H    OH  3    CH2C113    CN              H      H    OH  3    CH2C114    CH3            CH3   H    OH  3    CH2C115    CH3CH2        CH3   H    OH  3    CH2C116    CH3CH2CH2    CH3   H    OH  3    CH2C117    (CH3)2CH      CH3   H    OH  3    CH2C118    (CH3)3C       CH3   H    OH  3    CH2C119    CH3S           CH3   H    OH  3    CH2C120    CH3SO          CH3   H    OH  3    CH2C121    CH3SO2        CH3   H    OH  3    CH2C122    Ph              CH3   H    OH  3    CH2C123    CH3O           CH3   H    OH  3    CH2C124    CH3OC(O)       CH3   H    OH  3    CH2C125    CH3CH2OC(O)   CH3   H    OH  3    CH2C126    CH2=CHCH2    CH3   H    OH  3    CH2C127    HCCCH2         CH3   H    OH  3    CH2C128    CF3            CH3   H    OH  3    CH2C129    (CH3)2NSO2   CH3   H    OH  3    CH2C130    (CH3)2N       CH3   H    OH  3    CH2C131    PhO             CH3   H    OH  3    CH2基团    R6        R7       R16 R10p    WC132    PhS         CH3      H    OH  3    CH2C133    PhSO        CH3      H    OH  3    CH2C134    PhSO2      CH3      H    OH  3    CH2C135    CN          CH3      H    OH  3    CH2C136    CH3CH2   CH3CH2  H    OH  1    CH2C137    H           H         H    OH  1    CH(CH3)C138    CH3        H         H    OH  1    CH(CH3)C139    CH3        CH3      H    OH  1    CH(CH3)C140    CH2CH3    H         H    OH  1    CH(CH3)C141    CH2CH3   CH3      H    OH  1    CH(CH3)C142   CH3CH2    CH3CH2  H    OH  1    CH(CH3)C143    H           H         CH3 OH  1    CH2C144    CH3        CH3      CH3 OH  1    CH2C145   CH3CH2    CH3CH2  CH3 OH  1    CH2C146    H           H          H    OH  2    CH2C147    CH3        CH3      H    OH  2    CH2C148    CH2CH2   CH3CH2  H    OH  2    CH2C149    H           H         H    OH  5    CH2C150    CH3        CH3      H    OH  5    CH2C151    CH3CH2   CH3CH2  H    OH  5    CH2C152    CH3        H         H    OH  2    CH2下表4中,Q代表Q3
Figure A9981578601551
并且 Q3代表下列基团D:表4:基团D:基团    R6    R7     R8     R12     R10 o基团   R6            R7    R8  R12 R10oD1     H               H      H    H    OH  2D2     CH3            H      H    H    OH  2D3     CH3CH2        H      H    H    OH  2D4     CH3CH2CH2    H      H    H    OH  2D5     (CH3)2CH      H      H    H    OH  2D6     (CH3)3C       H      H    H    OH  2D7     CH3S           H      H    H    OH  2D8     CH3SO          H      H    H    OH  2D9     CH3SO2        H      H    H    OH  2D10    Ph              H      H    H    OH  2D11    CH3O           H      H    H    OH  2D12    CH2=CHCH2    H      H    H    OH  2D13    HCCCH2         H      H    H    OH  2D14    CF3            H      H    H    OH  2D15    PhO             H      H    H    OH  2D16    PhS             H      H    H    OH  2D17    PhSO            H      H    H    OH  2D18    PhSO2          H      H    H    OH  2D19    CH3            CH3   H    H    OH  2D20    CH3CH2        CH3   H    H    OH  2D21    CH3CH2CH2    CH3   H    H    OH  2D22    (CH3)2CH      CH3   H    H    OH  2D23    (CH3)3C       CH3   H    H    OH  2D24    CH3S           CH3   H    H    OH  2D25    CH3SO          CH3   H    H    OH  2D26    CH3SO2        CH3   H    H    OH  2D27    Ph              CH3   H    H    OH  2D28    CH3O           CH3   H    H    OH  2D29    CH2=CHCH2   CH3   H    H    OH  2D30    HCCCH2         CH3   H    H    OH  2D31    CF3            CH3   H    H    OH  2D32    PhO             CH3   H    H    OH  2基团   R6         R7    R8  R12 R10oD33    PhS          CH3   H    H    OH  2D34    PhSO         CH3   H    H    OH  2D35    PhSO2       CH3   H    H    OH  2D36    H            H      H    H    OH  3D37    CH3         H      H    H    OH  3D38    CH3CH2     H      H    H    OH  3D39    CH3CH2CH2 H      H    H    OH  3D40    (CH3)2CH   H      H    H    OH  3D41    (CH3)3C    H      H    H    OH  3D42    CH3S        H      H    H    OH  3D43    CH3SO       H      H    H    OH  3D44    CH3SO2     H      H    H    OH  3D45    Ph           H      H    H    OH  3D46    CH3O        H      H    H    OH  3D47    CH2=CHCH2 H      H    H    OH  3D48    HCCCH2      H      H    H    OH  3D49    CF3         H      H    H    OH  3D50    PhO          H      H    H    OH  3D51    PhS          H      H    H    OH  3D52    PhSO         H      H    H    OH  3D53    PhSO2       H      H    H    OH  3D54    CH3         CH3   H    H    OH  3D55    CH3CH2     CH3   H    H    OH  3D56    CH3CH2CH2 CH3   H    H    OH  3D57    (CH3)2CH   CH3   H    H    OH  3D58    (CH3)3C    CH3   H    H    OH  3D59    CH3S        CH3   H    H    OH  3D60    CH3SO       CH3   H    H    OH  3D61    CH3SO2     CH3   H    H    OH  3D62    Ph           CH3   H    H    OH  3D63    CH3O        CH3   H    H    OH  3D64    CH2=CHCH2 CH3   H    H    OH  3D65    HCCCH2      CH3   H    H    OH  3基团    R6         R7   R8   R12 R10oD66    CF3         CH3   H    H    OH  3D67    PhO          CH3   H    H    OH  3D68    PhS          CH3   H    H    OH  3D69    PhSO         CH3   H    H    OH  3D70    PhSO2       CH3   H    H    OH  3D71    H            H      H    H    OH  4D72    CH3         H      H    H    OH  4D73    CH3CH2     H      H    H    OH  4D74    CH3CH2CH2 H      H    H    OH  4D75    (CH3)2CH   H      H    H    OH  4D76    (CH3)3C    H      H    H    OH  4D77    CH3S        H      H    H    OH  4D78    CH3SO       H      H    H    OH  4D79    CH3SO2     H      H    H    OH  4D80    Ph            H      H    H    OH  4D81    CH3O        H      H    H    OH  4D82    CH2=CHCH2 H      H    H    OH  4D83    HCCCH2      H      H    H    OH  4D84    CF3         H      H    H    OH  4D85    PhO          H      H    H    OH  4D86    PhS          H      H    H    OH  4D87    PhSO         H      H    H    OH  4D88    PhSO2       H      H    H    OH  4D89    CH3         CH3   H    H    OH  4D90    CH3CH2     CH3   H    H    OH  4D91    CH3CH2CH2 CH3   H    H    OH  4D92    (CH3)2CH   CH3   H    H    OH  4D93    (CH3)3C    CH3   H    H    OH  4D94    CH3S        CH3   H    H    OH  4D95    CH3SO       CH3   H    H    OH  4D96    CH3SO2     CH3   H    H    OH  4D97    Ph           CH3   H    H    OH  4D98    CH3O        CH3   H    H    OH  4基团    R6             R7        R8  R12 R10oD99     CH2=CHCH2    CH3       H    H    OH  4D100    HCCCH2         CH3       H    H    OH  4D101    CF3            CH3       H    H    OH  4D102    PhO             CH3       H    H    OH  4D103    PhS             CH3       H    H    OH  4D104    PhSO            CH3       H    H    OH  4D105    PhSO2          CH3       H    H    OH  4D106    H               H          H    CH3 OH  4D107    H               H          H    CH3 OH  3D108    H               H          H    H    OH  1D109    CH3            H          H    H    OH  1D110    CH3OC(O)       CH3       H    H    OH  1D111    CH3CH2OC(O)   CH3       H    H    OH  1D112    CH3O           CH3       H    H    OH  1D113    CH3S           CH3       H    H    OH  1D114    CH3SO          CH3       H    H    OH  1D115    CH3SO2        CH3       H    H    OH  1D116    CH3CH2         H         H    H    OH  1D117    CH3OC(O)       CH3CH2   H    H    OH  1D118    CH3CH2OC(O)   CH3CH2   H    H    OH  1D119    CH3O           CH3CH2   H    H    OH  1D120    CH3S           CH3CH2   H    H    OH  1D121    CH3SO          CH3CH2   H    H    OH  1D122    CH3SO2        CH3CH2   H    H    OH  1D123    CH3CH2S       CH3       H    H    OH  1D124    CH3CH2SO      CH3       H    H    OH  1D125    CH3CH2SO2    CH3       H    H    OH  1D126    CH3CH2S       CH3CH2   H    H    OH  1D127    CH3CH2SO      CH3CH2   H    H    OH  1D128    CH3CH2SO2    CH3CH2   H    H    OH  1D129    H                H          CH3 H    OH  1D130    CH3             H          CH3 H    OH  1D131    CH3OC(O)       CH3        CH3 H    OH  1基团    R6             R7     R8    R12  R10oD132    CH3CH2OC(O)   CH3    CH3    H    OH  1D133    CH3O           CH3    CH3    H    OH  1D134    CH3S           CH3    CH3    H    OH  1D135    CH3SO          CH3    CH3    H    OH  1D136    CH3SO2        CH3    CH3    H    OH  1D137    H                H       H       CH3 OH  1D138    CH3             H       H       CH3 OH  1D139    H                H       CH3    CH3 OH  1D140    CH3CH2OC(O)   CH3    H       H    OH  4下表5中,Q代表Q4
Figure A9981578601601
并且Q4代表下列基团E:表5:基团E:基团    R6          R7         R10  X     Y       W       qE1      H            H           OH    S     CH2    CH2    2E2      CH3         H           OH    S     CH2    CH2    2E3      CH3         CH3        OH    S     CH2    CH2    2E4      CH3OC(O)    H           OH    S     CH2    CH2    2E5      CH3         CH3OC(O)   OH    S     CH2    CH2    2E6      H            H           OH    SO    CH2    CH2    2E7      CH3         H           OH    SO    CH2    CH2    2E8      CH3         CH3        OH    SO    CH2    CH2    2E9      CH3OC(O)    H           OH    SO    CH2    CH2    2E10     CH3         CH3OC(O)   OH    SO    CH2    CH2    2E11     H            H           OH    SO2  CH2    CH2    2基团   R6          R7        R10   X      Y    W      qE12    CH3         H          OH    SO2   CH2 CH2    2E13    CH3         CH3       OH    SO2   CH2 CH2    2E14    CH3OC(O)    H          OH    SO2   CH2 CH2    2E15    CH3         CH3OC(O)  OH    SO2   CH2 CH2    2E16    H            H           OH    CO     O    CH2    2E17    CH3         H           OH    CO     O    CH2    2E18    CH3         CH3        OH    CO     O    CH2    2E19    CH3OC(O)    H           OH    CO     O    CH2    2E20    CH3         CH3OC(O)   OH    CO     O    CH2    2E21    H            H            OH    CO     O    CH2    2E22    CH3         H           OH    CO     O    CH2    2E23    CH3         CH3        OH    CO     O    CH2    2E24    CH3OC(O)    H           OH    CO     O    CH2    2E25    CH3         CH3OC(O)   OH    CO     O    CH2    2E26    H            H            OH    CO     O    CH2    2E27    CH3         H           OH    CO     O    CH2    2E28    CH3         CH3        OH    CO     O    CH2    2E29    CH3OC(O)    H           OH    CO     O    CH2    2E30    CH3         CH3OC(O)   OH    CO     O    CH2    2下表6中,Q代表Q5
Figure A9981578601611
并且Q5代表下列基团F:表6:基团F:基团    R6   R7  R8   R10F1      H     H     H     OHF2      CH3  H     H     OH基团    R6    R7    R8    R10F3      CH3   CH3   H      OHF4      CH3   CH3   CH3   OHF5      H      H      CH3   OHF6      H      CH3   CH3   OH表7:式Ia化合物
Figure A9981578601621
化合物序号    R2            R3  R4  R5    Q1 pA1            H              H    H    CF3    B24 0A2            CH3           H    H    CF3    B24 0A3            CH3CH2       H    H    CF3    B24 0A4            (CH3)2CH     H    H    CF3    B24 0A5            (CH3)3C      H    H    CF3    B24 0A6            环丙基          H    H    CF3    B24 0A7            CH3(CH2)2   H    H    CF3    B24 0A8            CH3OCH2      H    H    CF3    B24 0A9            CH3O(CH2)2  H    H    CF3    B24 0A10            Ph             H    H    CF3    B24 0A11            PhO            H    H    CF3    B24 0A12            PhS            H    H    CF3    B24 0A13            PhSO           H    H    CF3    B24 0A14            PhSO2         H    H    CF3    B24 0A15            CH3S          H    H    CF3    B24 0A16            CH3SO         H    H    CF3    B24 0A17            CF3           H    H    CF3    B24 0A18            F2CH          H    H    CF3    B24 0化合物序号   R2                       R3  R4  R5        Q1 pA19          HCC                        H    H    CF3        B24 0A20          CH3CC                     H    H    CF3        B24 0A21          CH2=CH                   H    H    CF3        B24 0A22          CH2=CHCH2               H    H    CF3        B24 0A23          CH3SO2N(CH3)           H    H    CF3        B24 0A24          (CH3)2N                 H    H    CF3        B24 0A25          (CH3)2NSO2             H    H    CF3        B24 0A26          ClCH2                     H    H    CF3        B24 0A27          CH3SCH2                  H    H    CF3        B24 0A28          CH3SOCH2                 H    H    CF3        B24 0A29          CH3SO2CH2              H    H    CF3        B24 0A30          [1.2.4]-三唑-1-基甲基      H    H    CF3        B24 0A31          CH3                       CF3 H    CH3        B24 0A32          CH3                       CH3 H    CF3        B24 0A33          H                          H    H    CF3CF2    B24 0A34          CH3                       H    H    CF3CF2    B24 0A35          CH3CH2                   H    H    CF3CF2    B24 0A36          环丙基                      H    H    CF3CF2    B24 0A37          (CH3)3C                  H    H    CF3CF2    B24 0A38          (CH3)2CH                 H    H    CF3CF2    B24 0A39          CH3(CH2)2               H    H    CF3CF2    B24 0A40          CH3OCH2                  H    H    CF3CF2    B24 0A41          CH3O(CH2)2              H    H    CF3CF2    B24 0A42          Ph                          H    H    CF3CF2    B24 0A43          PhO                         H    H    CF3CF2    B24 0A44          PhS                         H    H    CF3CF2    B24 0A45          PhSO                        H    H    CF3CF2    B24 0A46          PhSO2                      H    H    CF3CF2    B24 0A47          CH3S                       H    H    CF3CF2    B24 0A48          CH3SO                      H    H    CF3CF2    B24 0A49          CF3                        H    H    CF3CF2    B24 0化合物序号   R2                       R3   R4   R5         Q1 pA50          F2CH                      H    H    CF3CF2     B24 0A51          HCC                        H    H    CF3CF2     B24 0A52          CH3CC                     H    H    CF3CF2     B24 0A53          CH2=CH                   H    H    CF3CF2     B24 0A54          CH2=CHCH2               H    H    CF3CF2     B24 0A55          CH3SO2N(CH3)            H    H    CF3CF2     B24 0A56          (CH3)2N                  H    H    CF3CF2     B24 0A57          (CH3)2NSO2             H    H    CF3CF2     B24 0A58          ClCH2                     H    H    CF3CF2     B24 0A59          CH3SCH2                  H    H    CF3CF2     B24 0A60          CH3SOCH2                 H    H    CF3CF2     B24 0A61          CH3SO2CH2              H    H    CF3CF2     B24 0A62          [1.2.4]-三唑-1-基甲基      H    H    CF3CF2     B24 0A63          H                          H    H    CF3CF2CF2 B24 0A64          CH3                      H    H    CF3CF2CF2  B24 0A65          CH3CH2                  H    H    CF3CF2CF2 B24 0A66          环丙基                     H    H    CF3CF2CF2 B24 0A67          (CH3)3C                  H    H    CF3CF2CF2 B24 0A68          (CH3)2CH                 H    H    CF3CF2CF2 B24 0A69          CH3(CH2)2               H    H    CF3CF2CF2 B24 0A70          CH3OCH2                  H    H    CF3CF2CF2 B24 0A71          CH3O(CH2)2              H    H    CF3CF2CF2 B24 0A72          Ph                         H    H    CF3CF2CF2  B24 0A73          PhO                        H    H    CF3CF2CF2  B24 0A74          PhS                        H    H    CF3CF2CF2  B24 0A75          PhSO                       H    H    CF3CF2CF2  B24 0A76          PhSO2                     H    H    CF3CF2CF2  B24 0A77          CH3S                      H    H    CF3CF2CF2  B24 0A78          CH3SO                     H    H    CF3CF2CF2  B24 0A79          CF3                       H    H    CF3CF2CF2  B24 0A80          F2CH                      H    H    CF3CF2CF2  B24 0化合物序号    R2                      R3 R4   R5        Q1  pA81           HCC                      H    H    CF3CF2CF2 B24 0A82           CH3CC                   H    H    CF3CF2CF2 B24 0A83           CH2=CH                 H    H    CF3CF2CF2 B24 0A84           CH2=CHCH2             H    H    CF3CF2CF2 B24 0A85           CH3SO2N(CH3)          H    H    CF3CF2CF2 B24 0A86           (CH3)2N                H    H    CF3CF2CF2 B24 0A87           (CH3)2NSO2            H    H    CF3CF2CF2 B24 0A88           ClCH2                   H    H    CF3CF2CF2 B24 0A89           CH3SCH2                H    H    CF3CF2CF2 B24 0A90           CH3SOCH2               H    H    CF3CF2CF2 B24 0A91           CH3SO2CH2             H    H    CF3CF2CF2 B24 0A92           [1.2.4]-三唑-1-基甲基     H    H    CF3CF2CF2 B24 0A93           H                         H    H    CF2Cl        B24 0A94           CH3                      H    H    CF2Cl        B24 0A95           CH3CH2                  H    H    CF2Cl        B24 0A96           环丙基                     H    H    CF2Cl        B24 0A97           (CH3)3C                 H    H    CF2Cl        B24 0A98           (CH3)2CH                H    H    CF2Cl        B24 0A99           CH3(CH2)2              H    H    CF2Cl        B24 0A100          CH3OCH2                 H    H    CF2Cl        B24 0A101          CH3O(CH2)2             H    H    CF2Cl        B24 0A102          Ph                         H    H    CF2Cl        B24 0A103          PhO                        H    H    CF2Cl        B24 0A104          PhS                        H    H    CF2Cl        B24 0A105          PhSO                       H    H    CF2Cl        B24 0A106          PhSO2                     H    H    CF2Cl        B24 0A107          CH3S                      H    H    CF2Cl        B24 0A108          CH3SO                     H    H    CF2Cl        B24 0A109          CF3                       H    H    CF2Cl        B24 0A110          F2CH                      H    H    CF2Cl        B24 0A111          HCC                        H    H    CF2Cl        B24 0化合物序号    R2                      R3 R4   R5    Q1  pA112          CH3CC                   H    H    CF2Cl   B24 0A113          CH2=CH                 H    H    CF2Cl   B24 0A114          CH2=CHCH2             H    H    CF2Cl   B24 0A115          CH3SO2N(CH3)          H    H    CF2Cl   B24 0A116          (CH3)2N                H    H    CF2Cl   B24 0A117          (CH3)2NSO2            H    H    CF2Cl   B24 0A118          ClCH2                   H    H    CF2Cl   B24 0A119          CH3SCH2                H    H    CF2Cl   B24 0A120          CH3SOCH2               H    H    CF2Cl   B24 0A121          CH3SO2CH2             H    H    CF2Cl   B24 0A122          [1.2.4]-三唑-1-基甲基     H    H    CF2Cl   B24 0A123          H                         H    H    CHF2    B24 0A124          CH3                      H    H    CHF2    B24 0A125          CH3CH2                  H    H    CHF2    B24 0A126          环丙基                     H    H    CHF2    B24 0A127          (CH3)3C                 H    H    CHF2    B24 0A128          (CH3)2CH                H    H    CHF2    B24 0A129          CH3(CH2)2              H    H    CHF2    B24 0A130          CH3OCH2                 H    H    CHF2    B24 0A131          CH3O(CH2)2             H    H    CHF2    B24 0A132          Ph                         H    H    CHF2    B24 0A133          PhO                        H    H    CHF2    B24 0A134          PhS                        H    H    CHF2    B24 0A135          PhSO                       H    H    CHF2    B24 0A136          PhSO2                     H    H    CHF2    B24 0A137          CH3S                      H    H    CHF2    B24 0A138          CH3SO                     H    H    CHF2    B24 0A139          CF3                       H    H    CHF2    B24 0A140          F2CH                      H    H    CHF2    B24 0A141          HCC                        H    H    CHF2    B24 0A142          CH3CC                     H    H    CHF2    B24 0化合物序号    R2                       R3  R4   R5     Q1 pA143          CH2=CH                   H    H    CHF2    B24 0A144          CH2=CHCH2               H    H    CHF2    B24 0A145          CH3SO2N(CH3)            H    H    CHF2    B24 0A146          (CH3)2N                  H    H    CHF2    B24 0A147          (CH3)2NSO2              H    H    CHF2    B24 0A148          ClCH2                     H    H    CHF2    B24 0A149          CH3SCH2                  H    H    CHF2    B24 0A150          CH3SOCH2                 H    H    CHF2    B24 0A151          CH3SO2CH2              H    H    CHF2    B24 0A152          [1.2.4]-三唑-1-基甲基      H    H    CHF2    B24 0A153          H                          H    H    CCl3    B24 0A154          CH3                       H    H    CCl3    B24 0A155          CH3CH2                   H    H    CCl3    B24 0A156          环丙基                      H    H    CCl3    B24 0A157          (CH3)3C                  H    H    CCl3    B24 0A158          (CH3)2CH                 H    H    CCl3    B24 0A159          CH3(CH2)2               H    H    CCl3    B24 0A160          CH3OCH2                  H    H    CCl3    B24 0A161          CH3O(CH2)2              H    H    CCl3    B24 0A162          Ph                          H    H    CCl3    B24 0A163          PhO                         H    H    CCl3    B24 0A164          PhS                         H    H    CCl3    B24 0A165          PhSO                        H    H    CCl3    B24 0A166          PhSO2                      H    H    CCl3    B24 0A167          CH3S                       H    H    CCl3    B24 0A168          CH3SO                      H    H    CCl3    B24 0A169          CF3                        H    H    CCl3    B24 0A170          F2CH                       H    H    CCl3    B24 0A171          HCC                         H    H    CCl3    B24 0A172          CH3CC                      H    H    CCl3    B24 0A173          CH2=CH                    H    H    CCl3    B24 0化合物序号    R2                       R3  R4     R5    Q1 pA174          CH2=CHCH2              H    H       CCl3   B24 0A175          CH3SO2N(CH3)           H    H       CCl3   B24 0A176          (CH3)2N                 H    H       CCl3   B24 0A177          (CH3)2NSO2             H    H       CCl3   B24 0A178          ClCH2                    H    H       CCl3   B24 0A179          CH3SCH2                 H    H       CCl3   B24 0A180          CH3SOCH2                H    H       CCl3   B24 0A181          CH3SO2CH2              H    H       CCl3   B24 0A182          [1.2.4]-三唑-1-基甲基      H    H       CCl3   B24 0A183          H                          H    CH3    CF3    B24 0A184          CH3                       H    CH3    CF3    B24 0A185          CH3CH2                   H    CH3    CF3    B24 0A186          环丙基                      H    CH3    CF3    B24 0A187          (CH3)3C                  H    CH3    CF3    B24 0A188          (CH3)2CH                 H    CH3    CF3    B24 0A189          CH3(CH2)2               H    CH3    CF3    B24 0A190          CH3OCH2                  H    CH3    CF3    B24 0A191          CH3O(CH2)2              H    CH3    CF3    B24 0A192          Ph                          H    CH3    CF3    B24 0A193          PhO                         H    CH3    CF3    B24 0A194          PhS                         H    CH3    CF3    B24 0A195          PhSO                        H    CH3    CF3    B24 0A196          PhSO2                      H    CH3    CF3    B24 0A197          CH3S                       H    CH3    CF3    B24 0A198          CH3SO                      H    CH3    CF3    B24 0A199          CF3                        H    CH3    CF3    B24 0A200          F2CH                       H    CH3    CF3    B24 0A201          HCC                         H    CH3    CF3    B24 0A202          CH3CC                      H    CH3    CF3    B24 0A203          CH2=CH                    H    CH3    CF3    B24 0A204          CH2=CHCH2                H    CH3    CF3    B24 0化合物序号  R2               R3    R4    R5     Q1 pNo.A205        CH3SO2N(CH3)   H    CH3    CF3     B24 0A206        (CH3)2N         H    CH3    CF3     B24 0A207        (CH3)2NSO2     H    CH3    CF3     B24 0A208        ClCH2            H    CH3    CF3     B24 0A209        CH3SCH2         H    CH3    CF3     B24 0A210        CH3SOCH2        H    CH3    CF3     B24 0A211        CH3SO2CH2     H    CH3    CF3     B24 0A212        H                 H    CH3    CF3CF2 B24 0A213        CH3              H    CH3    CF3CF2 B24 0A214        CH3CH2          H    CH3    CF3CF2 B24 0A215        环丙基             H    CH3    CF3CF2 B24 0A216        (CH3)3C         H    CH3    CF3CF2 B24 0A217        (CH3)2CH        H    CH3    CF3CF2 B24 0A218        CH3(CH2)2      H    CH3    CF3CF2 B24 0A219        CH3OCH2         H    CH3    CF3CF2 B24 0A220        CH3O(CH2)2     H    CH3    CF3CF2 B24 0A221        Ph                 H    CH3    CF3CF2 B24 0A222        PhO                H    CH3    CF3CF2 B24 0A223        PhS                H    CH3    CF3CF2 B24 0A224        PhSO               H    CH3    CF3CF2 B24 0A225        PhSO2             H    CH3    CF3CF2 B24 0A226        CH3S              H    CH3    CF3CF2 B24 0A227        CH3SO             H    CH3    CF3CF2 B24 0A228        CF3               H    CH3    CF3CF2 B24 0A229        F2CH              H    CH3    CF3CF2 B24 0A230        HCC                H    CH3    CF3CF2 B24 0A231        CH3CC             H    CH3    CF3CF2 B24 0A232        CH2=CH           H    CH3    CF3CF2 B24 0A233        CH2=CHCH2       H    CH3    CF3CF2 B24 0A234        CH3SO2N(CH3)    H    CH3    CF3CF2 B24 0A235        (CH3)2N          H    CH3    CF3CF2 B24 0A236        (CH3)2NSO2      H    CH3    CF3CF2 B24 0化合物序号  R2            R3   R4       R5        Q1 pA237        ClCH2          H    CH3    CF3CF2     B24 0A238        CH3SCH2       H    CH3    CF3CF2     B24 0A239        CH3SOCH2      H    CH3    CF3CF2     B24 0A240        CH3SO2CH2   H    CH3    CF3CF2     B24 0A241        H               H    CH3    CF3CF2CF2 B24 0A242        CH3            H    CH3    CF3CF2CF2 B24 0A243        CH3CH2       H    CH3    CF3CF2CF2 B24 0A244        环丙基          H    CH3    CF3CF2CF2 B24 0A245        (CH3)3C      H    CH3    CF3CF2CF2 B24 0A246        (CH3)2CH     H    CH3    CF3CF2CF2 B24 0A247        CH3(CH2)2   H    CH3    CF3CF2CF2 B24 0A248        CH3OCH2      H    CH3    CF3CF2CF2 B24 0A249        CH3O(CH2)2  H    CH3    CF3CF2CF2 B24 0A250        Ph              H    CH3    CF3CF2CF2 B24 0A251        PhO             H    CH3    CF3CF2CF2 B24 0A252        PhS             H    CH3    CF3CF2CF2 B24 0A253        PhSO            H    CH3    CF3CF2CF2 B24 0A254        PhSO2          H    CH3    CF3CF2CF2 B24 0A255        CH3S           H    CH3    CF3CF2CF2 B24 0A256        CH3SO          H    CH3    CF3CF2CF2 B24 0A257        CF3            H    CH3    CF3CF2CF2 B24 0A258        F2CH           H    CH3    CF3CF2CF2 B24 0A259        HCC             H    CH3    CF3CF2CF2 B24 0A260        CH3CC          H    CH3    CF3CF2CF2 B24 0A261        CH2=CH        H    CH3    CF3CF2CF2 B24 0A262        CH2=CHCH2    H    CH3    CF3CF2CF2 B24 0A263        CH3SO2N(CH3) H    CH3    CF3CF2CF2 B24 0A264        (CH3)2N       H    CH3    CF3CF2CF2 B24 0A265        (CH3)2NSO2   H    CH3    CF3CF2CF2 B24 0A266        ClCH2          H    CH3    CF3CF2CF2 B24 0A267        CH3SCH2       H    CH3    CF3CF2CF2 B24 0A268        CH3SOCH2      H    CH3    CF3CF2CF2 B24 0化合物序号  R2           R3   R4    R5           Q1pA269        CH3SO2CH2  H    CH3    CF3CF2CF2B24 0A270        H              H    CH3    CF2Cl       B24 0A271        CH3          H    CH3    CF2Cl       B24 0A272        CH3CH2      H    CH3    CF2Cl       B24 0A273        环丙基         H    CH3    CF2Cl       B24 0A274        (CH3)3C     H    CH3    CF2Cl       B24 0A275        (CH3)2CH    H    CH3    CF2Cl       B24 0A276        CH3(CH2)2  H    CH3    CF2Cl       B24 0A277        CH3OCH2     H    CH3    CF2Cl       B24 0A278        CH3O(CH2)2 H    CH3    CF2Cl       B24 0A279        Ph             H    CH3    CF2Cl       B24 0A280        PhO            H    CH3    CF2Cl       B24 0A281        PhS            H    CH3    CF2Cl       B24 0A282        PhSO           H    CH3    CF2Cl       B24 0A283        PhSO2         H    CH3    CF2Cl       B24 0A284        CH3S          H    CH3    CF2Cl       B24 0A285        CH3SO         H    CH3    CF2Cl       B24 0A286        CF3           H    CH3    CF2Cl       B24 0A287        F2CH          H    CH3    CF2Cl       B24 0A288        HCC            H    CH3    CF2Cl       B24 0A289        CH3CC         H    CH3    CF2Cl       B24 0A290        CH2=CH       H    CH3    CF2Cl       B24 0A291        CH2=CHCH2   H    CH3    CF2Cl       B24 0A292        CH3SO2N(CH3)H    CH3    CF2Cl       B24 0A293        (CH3)2N      H    CH3    CF2Cl       B24 0A294        (CH3)2NSO2  H    CH3    CF2Cl       B24 0A295        ClCH2         H    CH3    CF2Cl       B24 0A296        CH3SCH2      H    CH3    CF2Cl       B24 0A297        CH3SOCH2     H    CH3    CF2Cl       B24 0A298        CH3SO2CH2   H    CH3    CF2Cl       B24 0A299        H               H    CH3    CHF2        B24 0A300        CH3           H    CH3    CHF2        B24 0化合物序号  R2              R3   R4     R5     Q1 pA301        CH3CH2         H    CH3    CHF2    B24 0A302        环丙基            H    CH3    CHF2    B24 0A303        (CH3)3C        H    CH3    CHF2    B24 0A304        (CH3)2CH       H    CH3    CHF2    B24 0A305        CH3(CH2)2     H    CH3    CHF2    B24 0A306        CH3OCH2        H    CH3    CHF2    B24 0A307        CH3O(CH2)2    H    CH3    CHF2    B24 0A308        Ph                H    CH3    CHF2    B24 0A309        PhO               H    CH3    CHF2    B24 0A310        PhS               H    CH3    CHF2    B24 0A311        PhSO              H    CH3    CHF2    B24 0A312        PhSO2            H    CH3    CHF2    B24 0A313        CH3S             H    CH3    CHF2    B24 0A314        CH3SO            H    CH3    CHF2    B24 0A315        CF3              H    CH3    CHF2    B24 0A316        F2CH             H    CH3    CHF2    B24 0A317        HCC               H    CH3    CHF2    B24 0A318        CH3CC            H    CH3    CHF2    B24 0A319        CH2=CH          H    CH3    CHF2    B24 0A320        CH2=CHCH2      H    CH3    CHF2    B24 0A321        CH3SO2N(CH3)   H    CH3    CHF2    B24 0A322        (CH3)2N         H    CH3    CHF2    B24 0A323        (CH3)2NSO2     H    CH3    CHF2    B24 0A324        ClCH2            H    CH3    CHF2    B24 0A325        CH3SCH2         H    CH3    CHF2    B24 0A326        CH3SOCH2        H    CH3    CHF2    B24 0A327        CH3SO2CH2      H    CH3    CHF2    B24 0A328        H                  H    CH3    CCl3    B24 0A329        CH3              H    CH3    CCl3    B24 0A330        CH3CH2          H    CH3    CCl3    B24 0A331        (CH3)3C         H    CH3    CCl3    B24 0A332        (CH3)2CH        H    CH3    CCl3    B24 0化合物序号  R2            R3   R4     R5      Q1pA333        环丙基          H    CH3    CCl3    B24 0A334        CH3(CH2)2   H    CH3    CCl3    B24 0A335        CH3OCH2      H    CH3    CCl3    B24 0A336        CH3O(CH2)2  H    CH3    CCl3    B24 0A337        Ph              H    CH3    CCl3    B24 0A338        PhO             H    CH3    CCl3    B24 0A339        PhS             H    CH3    CCl3    B24 0A340        PhSO            H    CH3    CCl3    B24 0A341        PhSO2          H    CH3    CCl3    B24 0A342        CH3S           H    CH3    CCl3    B24 0A343        CH3SO          H    CH3    CCl3    B24 0A344        CF3            H    CH3    CCl3    B24 0A345        F2CH           H    CH3    CCl3    B24 0A346        HCC             H    CH3    CCl3    B24 0A347        CH3CC          H    CH3    CCl3    B24 0A348        CH2=CH        H    CH3    CCl3    B24 0A349        CH2=CHCH2    H    CH3    CCl3    B24 0A350        CH3SO2N(CH3) H    CH3    CCl3    B24 0A351        (CH3)2N       H    CH3    CCl3    B24 0A352        (CH3)2NSO2   H    CH3    CCl3    B24 0A353        ClCH2          H    CH3    CCl3    B24 0A354        CH3SCH2       H    CH3    CCl3    B24 0A355        CH3SOCH2      H    CH3    CCl3    B24 0A356        CH3SO2CH2    H    CH3    CCl3    B24 0A357        H                H    Ph      CF3     B24 0A358        CH3            H    Ph      CF3     B24 0A359        CH3CH2        H    Ph      CF3     B24 0A360        环丙基           H    Ph      CF3     B24 0A361        (CH3)3C       H    Ph      CF3     B24 0A362        (CH3)2CH      H    Ph      CF3     B24 0A363        CH3(CH2)2    H    Ph      CF3     B24 0A364        CH3OCH2       H    Ph      CF3     B24 0化合物序号  R2              R3   R4   R5       Q1 pA365        CH3O(CH2)2    H    Ph    CF3       B24 0A366        Ph                H    Ph    CF3       B24 0A367        PhO               H    Ph    CF3       B24 0A368        PhS               H    Ph    CF3       B24 0A369        PhSO              H    Ph    CF3       B24 0A370        PhSO2            H    Ph    CF3       B24 0A371        CH3S             H    Ph    CF3       B24 0A372        CH3SO            H    Ph    CF3       B24 0A373        CF3              H    Ph    CF3       B24 0A374        F2CH             H    Ph    CF3       B24 0A375        HCC               H    Ph    CF3       B24 0A376        CH3CC            H    Ph    CF3       B24 0A377        CH2=CH          H    Ph    CF3       B24 0A378        CH2=CHCH2      H    Ph    CF3       B24 0A379        CH3SO2N(CH3)   H    Ph    CF3       B24 0A380        (CH3)2N         H    Ph    CF3       B24 0A381        (CH3)2NSO2     H    Ph    CF3       B24 0A382        ClCH2            H    Ph    CF3       B24 0A383        CH3SCH2         H    Ph    CF3       B24 0A384        CH3SOCH2        H    Ph    CF3       B24 0A385        CH3SO2CH2      H    Ph    CF3       B24 0A386        H                  H    Ph    CF3CF2   B24 0A387        CH3              H    Ph    CF3CF2   B24 0A388        CH3CH2          H    Ph    CF3CF2   B24 0A389        环丙基             H    Ph    CF3CF2   B24 0A390        (CH3)3C         H    Ph    CF3CF2   B24 0A391        (CH3)2CH        H    Ph    CF3CF2   B24 0A392        CH3(CH2)2      H    Ph    CF3CF2   B24 0A393        CH3OCH2         H    Ph    CF3CF2   B24 0A394        CH3O(CH2)2     H    Ph    CF3CF2   B24 0A395        Ph                 H    Ph    CF3CF2   B24 0A396        PhO                H    Ph    CF3CF2   B24 0化合物序号  R2              R3   R4    R5        Q1 pA397        PhS               H    Ph    CF3CF2     B24 0A398        PhSO              H    Ph    CF3CF2     B24 0A399        PhSO2            H    Ph    CF3CF2     B24 0A400        CH3S             H    Ph    CF3CF2     B24 0A401        CH3SO            H    Ph    CF3CF2     B24 0A402        CF3              H    Ph    CF3CF2     B24 0A403        F2CH             H    Ph    CF3CF2     B24 0A404        HCC               H    Ph    CF3CF2     B24 0A405        CH3CC            H    Ph    CF3CF2     B24 0A406        CH2=CH          H    Ph    CF3CF2     B24 0A407        CH2=CHCH2      H    Ph    CF3CF2     B24 0A408        CH3SO2N(CH3)   H    Ph    CF3CF2     B24 0A409        (CH3)2N         H    Ph    CF3CF2     B24 0A410        (CH3)2NSO2     H    Ph    CF3CF2     B24 0A411        ClCH2            H    Ph    CF3CF2     B24 0A412        CH3SCH2         H    Ph    CF3CF2     B24 0A413        CH3SOCH2        H    Ph    CF3CF2     B24 0A414        CH3SO2CH2      H    Ph    CF3CF2     B24 0A415        H                  H    Ph    CF3CF2CF2 B24 0A416        CH3              H    Ph    CF3CF2CF2 B24 0A417        CH3CH2          H    Ph    CF3CF2CF2 B24 0A418        环丙基             H    Ph    CF3CF2CF2 B24 0A419        (CH3)3C         H    Ph    CF3CF2CF2 B24 0A420        (CH3)2CH        H    Ph    CF3CF2CF2 B24 0A421        CH3(CH2)2      H    Ph    CF3CF2CF2 B24 0A422        CH3OCH2         H    Ph    CF3CF2CF2 B24 0A423        CH3O(CH2)2     H    Ph    CF3CF2CF2 B24 0A424        Ph                 H    Ph    CF3CF2CF2 B24 0A425        PhO                H    Ph    CF3CF2CF2 B24 0A426        PhS                H    Ph    CF3CF2CF2 B24 0A427        PhSO               H    Ph    CF3CF2CF2 B24 0A428        PhSO2             H    Ph    CF3CF2CF2 B24 0化合物序号  R2              R3   R4    R5         Q1 pA429        CH3S             H    Ph    CF3CF2CF2 B24 0A430        CH3SO            H    Ph    CF3CF2CF2 B24 0A431        CF3              H    Ph    CF3CF2CF2 B24 0A432        F2CH             H    Ph    CF3CF2CF2 B24 0A433        HCC               H    Ph    CF3CF2CF2 B24 0A434        CH3CC            H    Ph    CF3CF2CF2 B24 0A435        CH2=CH          H    Ph    CF3CF2CF2 B24 0A436        CH2=CHCH2      H    Ph    CF3CF2CF2 B24 0A437        CH3SO2N(CH3)   H    Ph    CF3CF2CF2 B24 0A438        (CH3)2N         H    Ph    CF3CF2CF2 B24 0A439        (CH3)2NSO2     H    Ph    CF3CF2CF2 B24 0A440        ClCH2            H    Ph    CF3CF2CF2 B24 0A441        CH3SCH2         H    Ph    CF3CF2CF2 B24 0A442        CH3SOCH2        H    Ph    CF3CF2CF2 B24 0A443        CH3SO2CH2      H    Ph    CF3CF2CF2 B24 0A444        H                  H    Ph    CF2Cl       B24 0A445        CH3              H    Ph    CF2Cl       B24 0A446        CH3CH2          H    Ph    CF2Cl       B24 0A447        环丙基             H    Ph    CF2Cl       B24 0A448        (CH3)3C         H    Ph    CF2Cl       B24 0A449        (CH3)2CH        H    Ph    CF2Cl       B24 0A450        CH3(CH2)2      H    Ph    CF2Cl       B24 0A451        CH3OCH2         H    Ph    CF2Cl       B24 0A452        CH3O(CH2)2     H    Ph    CF2Cl       B24 0A453        Ph                 H    Ph    CF2Cl       B24 0A454        PhO                H    Ph    CF2Cl       B24 0A455        PhS                H    Ph    CF2Cl       B24 0A456        PhSO               H    Ph    CF2Cl       B24 0A457        PhSO2             H    Ph    CF2Cl       B24 0A458        CH3S              H    Ph    CF2Cl       B24 0A459        CH3SO             H    Ph    CF2Cl       B24 0A460        CF3               H    Ph    CF2Cl       B24 0化合物序号  R2              R3   R4    R5     Q1 pA461        F2CH             H    Ph    CF2Cl    B24 0A462        HCC               H    Ph    CF2Cl    B24 0A463        CH3CC            H    Ph    CF2Cl    B24 0A464        CH2=CH          H    Ph    CF2Cl    B24 0A465        CH2=CHCH2      H    Ph    CF2Cl    B24 0A466        CH3SO2N(CH3)   H    Ph    CF2Cl    B24 0A467        (CH3)2N         H    Ph    CF2Cl    B24 0A468        (CH3)2NSO2     H    Ph    CF2Cl    B24 0A469        ClCH2            H    Ph    CF2Cl    B24 0A470        CH3SCH2         H    Ph    CF2Cl    B24 0A471        CH3SOCH2        H    Ph    CF2Cl    B24 0A472        CH3SO2CH2      H    Ph    CF2Cl    B24 0A473        H                  H    Ph    CHF2     B24 0A474        CH3              H    Ph    CHF2     B24 0A475        CH3CH2          H    Ph    CHF2     B24 0A476        环丙基             H    Ph    CHF2     B24 0A477        (CH3)3C         H    Ph    CHF2     B24 0A478        (CH3)2CH        H    Ph    CHF2     B24 0A479        CH3(CH2)2      H    Ph    CHF2     B24 0A480        CH3OCH2         H    Ph    CHF2     B24 0A481        CH3O(CH2)2     H    Ph    CHF2     B24 0A482        Ph                 H    Ph    CHF2     B24 0A483        PhO                H    Ph    CHF2     B24 0A484        PhS                H    Ph    CHF2     B24 0A485        PhSO               H    Ph    CHF2     B24 0A486        PhSO2             H    Ph    CHF2     B24 0A487        CH3S              H    Ph    CHF2     B24 0A488        CH3SO             H    Ph    CHF2     B24 0A489        CF3               H    Ph    CHF2     B24 0A490        F2CH              H    Ph    CHF2     B24 0A491        HCC                H    Ph    CHF2     B24 0A492        CH3CC             H    Ph    CHF2     B24 0化合物序号  R2              R3   R4    R5    Q1 pA493        CH2=CH          H    Ph    CHF2    B24 0A494        CH2=CHCH2      H    Ph    CHF2    B24 0A495        CH3SO2N(CH3)   H    Ph    CHF2    B24 0A496        (CH3)2N         H    Ph    CHF2    B24 0A497        (CH3)2NSO2     H    Ph    CHF2    B24 0A498        ClCH2            H    Ph    CHF2    B24 0A499        CH3SCH2         H    Ph    CHF2    B24 0A500        CH3SOCH2        H    Ph    CHF2    B24 0A501        CH3SO2CH2      H    Ph    CHF2    B24 0A502        H                  H    Ph    CCl3    B24 0A503        CH3              H    Ph    CCl3    B24 0A504        CH3CH2          H    Ph    CCl3    B24 0A505        环丙基             H    Ph    CCl3    B24 0A506        (CH3)3C         H    Ph    CCl3    B24 0A507        (CH3)2CH        H    Ph    CCl3    B24 0A508        CH3(CH2)2      H    Ph    CCl3    B24 0A509        CH3OCH2         H    Ph    CCl3    B24 0A510        CH3O(CH2)2     H    Ph    CCl3    B24 0A511        Ph                 H    Ph    CCl3    B24 0A512        PhO                H    Ph    CCl3    B24 0A513        PhS                H    Ph    CCl3    B24 0A514        PhSO               H    Ph    CCl3    B24 0A515        PhSO2             H    Ph    CCl3    B24 0A516        CH3S              H    Ph    CCl3    B24 0A517        CH3SO             H    Ph    CCl3    B24 0A518        CF3               H    Ph    CCl3    B24 0A519        F2CH              H    Ph    CCl3    B24 0A520        HCC                H    Ph    CCl3    B24 0A521        CH3CC             H    Ph    CCl3    B24 0A522        CH2=CH           H    Ph    CCl3    B24 0A523        CH2=CHCH2       H    Ph    CCl3    B24 0A524        CH3SO2N(CH3)    H    Ph    CCl3    B24 0化合物序号  R2            R3           R4   R5    Q1 pA525        (CH3)2N     H              Ph   CCl3   B24 0A526        (CH3)2NSO2 H              Ph   CCl3   B24 0A527        ClCH2        H              Ph   CCl3   B24 0A528        CH3SCH2     H              Ph   CCl3   B24 0A529        CH3SOCH2    H              Ph   CCl3   B24 0A530        CH3SO2CH2  H              Ph   CCl3   B24 0A531        H             CH3           H    CF3    B24 0A532        H             CH3CH2       H    CF3    B24 0A533        H             环丙基          H    CF3    B24 0A534        H             (CH3)3CH     H    CF3    B24 0A535        H             (CH3)2CH     H    CF3    B24 0A536        H             CH3(CH2)2   H    CF3    B24 0A537        H             CH3OCH2      H    CF3    B24 0A538        H             CH3O(CH2)2  H    CF3    B24 0A539        H             Ph              H    CF3    B24 0A540        H             PhO             H    CF3    B24 0A541        H             PhS             H    CF3    B24 0A542        H             PhSO            H    CF3    B24 0A543        H             PhSO2          H    CF3    B24 0A544        H             CH3S           H    CF3    B24 0A545        H             CH3SO          H    CF3    B24 0A546        H             CF3            H    CF3    B24 0A547        H             F2CH            H    CF3    B24 0A548        H             HCC             H    CF3    B24 0A549        H             CH3CC          H    CF3    B24 0A550        H             CH2=CH        H    CF3    B24 0A551        H             CH2=CHCH2    H    CF3    B24 0A552        H             CH3SO2N(CH3) H    CF3    B24 0A553        H             (CH3)2N       H    CF3    B24 0A554        H             (CH3)2NSO2   H    CF3    B24 0A555        H             CH3SCH2       H    CF3    B24 0A556        H             CH3SOCH2      H    CF3    B24 0化合物序号  R2   R3           R4   R5        Q1 pA557        H    CH3SO2CH2   H    CF3        B24 0A558        H    CH3            H    CF3CF2    B24 0A559        H    CH3CH2       H    CF3CF2    B24 0A560        H    环丙基          H    CF3CF2    B24 0A561        H    (CH3)3C      H    CF3CF2    B24 0A562        H    (CH3)2CH     H    CF3CF2    B24 0A563        H    CH3(CH2)2   H    CF3CF2    B24 0A564        H    CH3OCH2      H    CF3CF2    B24 0A565        H    CH3O(CH2)2  H    CF3CF2    B24 0A566        H    Ph              H    CF3CF2    B24 0A567        H    PhO             H    CF3CF2    B24 0A568        H    PhS             H    CF3CF2    B24 0A569        H    PhSO            H    CF3CF2    B24 0A570        H    PhSO2          H    CF3CF2    B24 0A571        H    CH3S           H    CF3CF2    B24 0A572        H    CH3SO          H    CF3CF2    B24 0A573        H    CF3            H    CF3CF2    B24 0A574        H    F2CH           H    CF3CF2    B24 0A575        H    HCC             H    CF3CF2    B24 0A576        H    CH3CC          H    CF3CF2    B24 0A577        H    CH2=CH        H    CF3CF2    B24 0A578        H    CH2=CHCH2    H    CF3CF2    B24 0A579        H    CH3SO2N(CH3) H    CF3CF2    B24 0A580        H    (CH3)2N       H    CF3CF2    B24 0A581        H    (CH3)2NSO2   H    CF3CF2    B24 0A582        H    CH3SCH2       H    CF3CF2    B24 0A583        H    CH3SOCH2      H    CF3CF2    B24 0A584        H    CH3SO2CH2    H    CF3CF2    B24 0A585        H    CH3            H    CF3CF2CF2B24 0A586        H    CH3CH2        H    CF3CF2CF2B24 0A587        H    环丙基           H    CF3CF2CF2B24 0A588        H    (CH3)3C       H    CF3CF2CF2B24 0化合物序号  R2   R3            R4     R5        Q1 pA589        H    (CH3)2CH       H    CF3CF2CF2 B24 0A590        H    CH3(CH2)2     H    CF3CF2CF2 B24 0A591        H    CH3OCH2        H    CF3CF2CF2 B24 0A592        H    CH3O(CH2)2    H    CF3CF2CF2 B24 0A593        H    Ph                H    CF3CF2CF2 B24 0A594        H    PhO               H    CF3CF2CF2 B24 0A595        H    PhS               H    CF3CF2CF2 B24 0A596        H    PhSO              H    CF3CF2CF2 B24 0A597        H    PhSO2            H    CF3CF2CF2 B24 0A598        H    CH3S             H    CF3CF2CF2 B24 0A599        H    CH3SO            H    CF3CF2CF2 B24 0A600        H    CF3              H    CF3CF2CF2 B24 0A601        H    F2CH             H    CF3CF2CF2 B24 0A602        H    HCC               H    CF3CF2CF2 B24 0A603        H    CH3CC            H    CF3CF2CF2 B24 0A604        H    CH2=CH          H    CF3CF2CF2 B24 0A605        H    CH2=CHCH2      H    CF3CF2CF2 B24 0A606        H    CH3SO2N(CH3)   H    CF3CF2CF2 B24 0A607        H    (CH3)2N         H    CF3CF2CF2 B24 0A608        H    (CH3)2NSO2     H    CF3CF2CF2 B24 0A609        H    CH3SCH2         H    CF3CF2CF2 B24 0A610        H    CH3SOCH2        H    CF3CF2CF2 B24 0A611        H    CH3SO2CH2      H    CF3CF2CF2 B24 0A612        H    CH3               H    CF2Cl       B24 0A613        H    CH3CH2           H    CF2Cl       B24 0A614        H    环丙基              H    CF2Cl       B24 0A615        H    (CH3)3C          H    CF2Cl       B24 0A616        H    (CH3)2CH         H    CF2Cl       B24 0A617        H    CH3(CH2)2       H    CF2Cl       B24 0A618        H    CH3OCH2          H    CF2Cl       B24 0A619        H    CH3O(CH2)2      H    CF2Cl       B24 0A620        H    Ph                  H    CF2Cl       B24 0化合物      R2   R3             R4    R5     Q1 pA621        H    PhO               H    CF2Cl    B24 0A622        H    PhS               H    CF2Cl    B24 0A623        H    PhSO              H    CF2Cl    B24 0A624        H    PhSO2            H    CF2Cl    B24 0A625        H    CH3S             H    CF2Cl    B24 0A626        H    CH3SO            H    CF2Cl    B24 0A627        H    CF3              H    CF2Cl    B24 0A628        H    F2CH             H    CF2Cl    B24 0A629        H    HCC               H    CF2Cl    B24 0A630        H    CH3CC            H    CF2Cl    B24 0A631        H    CH2=CH          H    CF2Cl    B24 0A632        H    CH2=CHCH2      H    CF2Cl    B24 0A633        H    CH3SO2N(CH3)   H    CF2Cl    B24 0A634        H    (CH3)2N         H    CF2Cl    B24 0A635        H    (CH3)2NSO2     H    CF2Cl    B24 0A636        H    CH3SCH2         H    CF2Cl    B24 0A637        H    CH3SOCH2        H    CF2Cl    B24 0A638        H    CH3SO2CH2      H    CF2Cl    B24 0A639        H    CH3              H    CHF2     B24 0A640        H    CH3CH2          H    CHF2     B24 0A641        H    环丙基             H    CHF2     B24 0A642        H    (CH3)3C         H    CHF2     B24 0A643        H    (CH3)2CH        H    CHF2     B24 0A644        H    CH3(CH2)2      H    CHF2     B24 0A645        H    CH3OCH2         H    CHF2     B24 0A646        H    CH3O(CH2)2     H    CHF2     B24 0A647        H    Ph                 H    CHF2     B24 0A648        H    PhO                H    CHF2     B24 0A649        H    PhS                H    CHF2     B24 0A650        H    PhSO               H    CHF2     B24 0A651        H    PhSO2             H    CHF2     B24 0A652        H    CH3S              H    CHF2     B24 0化合物序号  R2   R3            R4   R5     Q1 pA653        H    CH3SO           H    CHF2    B24 0A654        H    CF3             H    CHF2    B24 0A655        H    F2CH            H    CHF2    B24 0A656        H    HCC              H    CHF2    B24 0A657        H    CH3CC           H    CHF2    B24 0A658        H    CH2=CH         H    CHF2    B24 0A659        H    CH2=CHCH2     H    CHF2    B24 0A660        H    CH3SO2N(CH3)  H    CHF2    B24 0A661        H    (CH3)2N        H    CHF2    B24 0A662        H    (CH3)2NSO2    H    CHF2    B24 0A663        H    CH3SCH2        H    CHF2    B24 0A664        H    CH3SOCH2       H    CHF2    B24 0A665        H    CH3SO2CH2     H    CHF2    B24 0A666        H    CH3             H    CCl3    B24 0A667        H    CH3CH2         H    CCl3    B24 0A668        H    环丙基            H    CCl3    B24 0A669        H    (CH3)3C        H    CCl3    B24 0A670        H    (CH3)2CH       H    CCl3    B24 0A671        H    CH3(CH2)2     H    CCl3    B24 0A672        H    CH3OCH2        H    CCl3    B24 0A673        H    CH3O(CH2)2    H    CCl3    B24 0A674        H    Ph                H    CCl3    B24 0A675        H    PhO               H    CCl3    B24 0A676        H    PhS               H    CCl3    B24 0A677        H    PhSO              H    CCl3    B24 0A678        H    PhSO2            H    CCl3    B24 0A679        H    CH3S             H    CCl3    B24 0A680        H    CH3SO            H    CCl3    B24 0A681        H    CF3              H    CCl3    B24 0A682        H    F2CH             H    CCl3    B24 0A683        H    HCC               H    CCl3    B24 0A684        H    CH3CC            H    CCl3    B24 0化合物序号  R2   R3            R4     R5    Q1 pA685        H    CH2=CH        H       CCl3   B24 0A686        H    CH2=CHCH2    H       CCl3   B24 0A687        H    CH3SO2N(CH3) H       CCl3   B24 0A688        H    (CH3)2N       H       CCl3   B24 0A689        H    (CH3)2NSO2   H       CCl3   B24 0A690        H    CH3SCH2       H       CCl3   B24 0A691        H    CH3SOCH2      H       CCl3   B24 0A692        H    CH3SO2CH2    H       CCl3   B24 0A693        H    CH3            CH3    CF3    B24 0A694        H    CH3CH2        CH3    CF3    B24 0A695        H    环丙基          CH3    CF3    B24 0A696        H    (CH3)3C       CH3    CF3    B24 0A697        H    (CH3)2CH      CH3    CF3    B24 0A698        H    CH3(CH2)2    CH3    CF3    B24 0A699        H    CH3OCH2       CH3    CF3    B24 0A700        H    CH3O(CH2)2   CH3    CF3    B24 0A701        H    Ph               CH3    CF3    B24 0A702        H    PhO              CH3    CF3    B24 0A703        H    PhS              CH3    CF3    B24 0A704        H    PhSO             CH3    CF3    B24 0A705        H    PhSO2           CH3    CF3    B24 0A706        H    CH3S            CH3    CF3    B24 0A707        H    CH3SO           CH3    CF3    B24 0A708        H    CF3             CH3    CF3    B24 0A709        H    F2CH            CH3    CF3    B24 0A710        H    HCC              CH3    CF3    B24 0A711        H    CH3CC           CH3    CF3    B24 0A712        H    CH2=CH         CH3    CF3    B24 0A713        H    CH2=CHCH2     CH3    CF3    B24 0A714        H    CH3SO2N(CH3)  CH3    CF3    B24 0A715        H    (CH3)2N        CH3    CF3    B24 0A716        H    (CH3)2NSO2    CH3    CF3    B24 0化合物序号  R2   R3              R4     R5         Q1 pA717        H    CH3SCH2         CH3    CF3        B24 0A718        H    CH3SOCH2        CH3    CF3        B24 0A719        H    CH3SO2CH2      CH3    CF3        B24 0A720        H    CH3              CH3    CF3CF2    B24 0A721        H    CH3CH2          CH3    CF3CF2    B24 0A722        H    环丙基             CH3    CF3CF2    B24 0A723        H    (CH3)3C         CH3    CF3CF2    B24 0A724        H    (CH3)2CH        CH3    CF3CF2    B24 0A725        H    CH3(CH2)2      CH3    CF3CF2    B24 0A726        H    CH3OCH2         CH3    CF3CF2    B24 0A727        H    CH3O(CH2)2     CH3    CF3CF2    B24 0A728        H    Ph                 CH3    CF3CF2    B24 0A729        H    PhO                CH3    CF3CF2    B24 0A730        H    PhS                CH3    CF3CF2    B24 0A731        H    PhSO               CH3    CF3CF2    B24 0A732        H    PhSO2             CH3    CF3CF2    B24 0A733        H    CH3S              CH3    CF3CF2    B24 0A734        H    CH3SO             CH3    CF3CF2    B24 0A735        H    CF3               CH3    CF3CF2    B24 0A736        H    F2CH              CH3    CF3CF2    B24 0A737        H    HCC                CH3    CF3CF2    B24 0A738        H    CH3CC             CH3    CF3CF2    B24 0A739        H    CH2=CH           CH3    CF3CF2    B24 0A740        H    CH2=CHCH2       CH3    CF3CF2    B24 0A741        H    CH3SO2N(CH3)    CH3    CF3CF2    B24 0A742        H    (CH3)2N          CH3    CF3CF2    B24 0A743        H    (CH3)2NO2      CH3    CF3CF2    B24 0A744        H    CH3SCH2          CH3    CF3CF2    B24 0A745        H    CH3SOCH2         CH3    CF3CF2    B24 0A746        H    CH3SO2CH2       CH3    CF3CF2    B24 0A747        H    CH3               CH3    CF3CF2CF2B24 0A748        H    CH3CH2           CH3    CF3CF2CF2B24 0化合物序号  R2   R3           R4       R5        Q1 pNo.A749        H    环丙基         CH3    CF3CF2CF2 B24 0A750        H    (CH3)3C     CH3    CF3CF2CF2 B24 0A751        H    (CH3)2CH    CH3    CF3CF2CF2 B24 0A752        H    CH3(CH2)2  CH3    CF3CF2CF2 B24 0A753        H    CH3OCH2     CH3    CF3CF2CF2 B24 0A754        H    CH3O(CH2)2 CH3    CF3CF2CF2 B24 0A755        H    Ph             CH3    CF3CF2CF2 B24 0A756        H    PhO            CH3    CF3CF2CF2 B24 0A757        H    PhS            CH3    CF3CF2CF2 B24 0A758        H    PhSO           CH3    CF3CF2CF2 B24 0A759        H    PhSO2         CH3    CF3CF2CF2 B24 0A760        H    CH3S          CH3    CF3CF2CF2 B24 0A761        H    CH3SO         CH3    CF3CF2CF2 B24 0A762        H    CF3           CH3    CF3CF2CF2 B24 0A763        H    F2CH          CH3    CF3CF2CF2 B24 0A764        H    HCC            CH3    CF3CF2CF2 B24 0A765        H    CH3CC         CH3    CF3CF2CF2 B24 0A766        H    CH2=CH       CH3    CF3CF2CF2 B24 0A767        H    CH2=CHCH2   CH3    CF3CF2CF2 B24 0A768        H    CH3SO2N(CH3)CH3    CF3CF2CF2 B24 0A769        H    (CH3)2N      CH3    CF3CF2CF2 B24 0A770        H    (CH3)2NSO2  CH3    CF3CF2CF2 B24 0A771        H    CH3SCH2      CH3    CF3CF2CF2 B24 0A772        H    CH3SOCH2     CH3    CF3CF2CF2 B24 0A773        H    CH3SO2CH2   CH3    CF3CF2CF2 B24 0A774        H    CH3            CH3    CF2Cl       B24 0A775        H    CH3CH2        CH3    CF2Cl       B24 0A776        H    环丙基          CH3    CF2Cl       B24 0A777        H    (CH3)3C       CH3    CF2Cl       B24 0A778        H    (CH3)2CH      CH3    CF2Cl       B24 0A779        H    CH3(CH2)2    CH3    CF2Cl       B24 0A780        H    CH3OCH2       CH3    CF2Cl       B24 0化合物序号  R2   R3            R4     R5      Q1 pA781        H    CH3O(CH2)2  CH3    CF2Cl    B24 0A782        H    Ph              CH3    CF2Cl    B24 0A783        H    PhO             CH3    CF2Cl    B24 0A784        H    PhS             CH3    CF2Cl    B24 0A785        H    PhSO            CH3    CF2Cl    B24 0A786        H    PhSO2          CH3    CF2Cl    B24 0A787        H    CH3S           CH3    CF2Cl    B24 0A788        H    CH3SO          CH3    CF2Cl    B24 0A789        H    CF3            CH3    CF2Cl    B24 0A790        H    F2CH           CH3    CF2Cl    B24 0A791        H    HCC             CH3    CF2Cl    B24 0A792        H    CH3CC          CH3    CF2Cl    B24 0A793        H    CH2=CH        CH3    CF2Cl    B24 0A794        H    CH2=CHCH2    CH3    CF2Cl    B24 0A795        H    CH3SO2N(CH3) CH3    CF2Cl    B24 0A796        H    (CH3)2N       CH3    CF2Cl    B24 0A797        H    (CH3)2NSO2   CH3    CF2Cl    B24 0A798        H    CH3SCH2       CH3    CF2Cl    B24 0A799        H    CH3SOCH2      CH3    CF2Cl    B24 0A800        H    CH3SO2CH2    CH3    CF2Cl    B24 0A801        H    CH3            CH3    CHF2     B24 0A802        H    CH3CH2        CH3    CHF2     B24 0A803        H    环丙基           CH3    CHF2     B24 0A804        H    (CH3)3C       CH3    CHF2     B24 0A805        H    (CH3)2CH      CH3    CHF2     B24 0A806        H    CH3(CH2)2    CH3    CHF2     B24 0A807        H    CH3OCH2       CH3    CHF2     B24 0A808        H    CH3O(CH2)2   CH3    CHF2     B24 0A809        H    Ph               CH3    CHF2     B24 0A810        H    PhO              CH3    CHF2     B24 0A811        H    PhS              CH3    CHF2     B24 0A812        H    PhSO             CH3    CHF2     B24 0化合物序号 R2   R3              R4     R5      Q1 pA813       H    PhSO2            CH3    CHF2    B24 0A814       H    CH3S             CH3    CHF2    B24 0A815       H    CH3SO            CH3    CHF2    B24 0A816       H    CF3              CH3    CHF2    B24 0A817       H    F2CH             CH3    CHF2    B24 0A818       H    HCC               CH3    CHF2    B24 0A819       H    CH3CC            CH3    CHF2    B24 0A820       H    CH2=CH          CH3    CHF2    B24 0A821       H    CH2=CHCH2      CH3    CHF2    B24 0A822       H    CH3SO2N(CH3)   CH3    CHF2    B24 0A823       H    (CH3)2N         CH3    CHF2    B24 0A824       H    (CH3)2NSO2     CH3    CHF2    B24 0A825       H    CH3SCH2         CH3    CHF2    B24 0A826       H    CH3SOCH2        CH3    CHF2    B24 0A827       H    CH3SO2CH2      CH3    CHF2    B24 0A828       H    CH3              CH3    CCl3    B24 0A829       H    CH3CH2          CH3    CCl3    B24 0A830       H    环丙基             CH3    CCl3    B24 0A831       H    (CH3)3C         CH3    CCl3    B24 0A832       H    (CH3)2CH        CH3    CCl3    B24 0A833       H    CH3(CH2)2      CH3    CCl3    B24 0A834       H    CH3OCH2         CH3    CCl3    B24 0A835       H    CH3O(CH2)2     CH3    CCl3    B24 0A836       H    Ph                 CH3    CCl3    B24 0A837       H    PhO                CH3    CCl3    B24 0A838       H    PhS                CH3    CCl3    B24 0A839       H    PhSO               CH3    CCl3    B24 0A840       H    PhSO2             CH3    CCl3    B24 0A841       H    CH3S              CH3    CCl3    B24 0A842       H    CH3SO             CH3    CCl3    B24 0A843       H    CF3               CH3    CCl3    B24 0A844       H    F2CH              CH3    CCl3    B24 0化合物序号 R2   R3            R4    R5    Q1 pA845       H    HCC             CH3   CCl3   B24 0A846       H    CH3CC          CH3   CCl3   B24 0A847       H    CH2=CH        CH3   CCl3   B24 0A848       H    CH2=CHCH2    CH3   CCl3   B24 0A849       H    CH3SO2N(CH3) CH3   CCl3   B24 0A850       H    (CH3)2N       CH3   CCl3   B24 0A851       H    (CH3)2NSO2   CH3   CCl3   B24 0A852       H    CH3SCH2       CH3   CCl3   B24 0A853       H    CH3SOCH2      CH3   CCl3   B24 0A854       H    CH3SO2CH2    CH3   CCl3   B24 0A855       H    CH3            Ph     CF3    B24 0A856       H    CH3CH2        Ph     CF3    B24 0A857       H    (CH3)2CH      Ph     CF3    B24 0A858       H    (CH3)2CH      Ph     CF3    B24 0A859       H    环丙基           Ph     CF3    B24 0A860       H    CH3(CH2)2    Ph     CF3    B24 0A861       H    CH3OCH2       Ph     CF3    B24 0A862       H    CH3O(CH2)2   Ph     CF3    B24 0A863       H    Ph               Ph     CF3    B24 0A864       H    PhO              Ph     CF3    B24 0A865       H    PhS              Ph     CF3    B24 0A866       H    PhSO             Ph     CF3    B24 0A867       H    PhSO2           Ph     CF3    B24 0A868       H    CH3S            Ph     CF3    B24 0A869       H    CH3SO           Ph     CF3    B24 0A870       H    CF3             Ph     CF3    B24 0A871       H    F2CH            Ph     CF3    B24 0A872       H    HCC              Ph     CF3    B24 0A873       H    CH3CC           Ph     CF3    B24 0A874       H    CH2=CH         Ph     CF3    B24 0A875       H    CH2=CHCH2     Ph     CF3    B24 0A876       H    CH3SO2N(CH3)  Ph     CF3    B24 0化合物序号  R2   R3           R4    R5        Q1 pA877        H    (CH3)2N      Ph    CF3        B24 0A878        H    (CH3)2NSO2  Ph    CF3        B24 0A879        H    CH3SCH2      Ph    CF3        B24 0A880        H    CH3SOCH2     Ph    CF3        B24 0A881        H    CH3SO2CH2   Ph    CF3        B24 0A882        H    CH3           Ph    CF3CF2    B24 0A883        H    CH3CH2       Ph    CF3CF2    B24 0A884        H    环丙基          Ph    CF3CF2    B24 0A885        H    (CH3)3C      Ph    CF3CF2    B24 OA886        H    (CH3)2CH     Ph    CF3CF2    B24 0A887        H    CH3(CH2)2   Ph    CF3CF2    B24 0A888        H    CH3OCH2      Ph    CF3CF2    B24 0A889        H    CH3O(CH2)2  Ph    CF3CF2    B24 0A890        H    Ph              Ph    CF3CF2    B24 0A891        H    PhO             Ph    CF3CF2    B24 0A892        H    PhS             Ph    CF3CF2    B24 0A893        H    PhSO            Ph    CF3CF2    B24 0A894        H    PhSO2          Ph    CF3CF2    B24 0A895        H    CH3S           Ph    CF3CF2    B24 0A896        H    CH3SO          Ph    CF3CF2    B24 0A897        H    CF3            Ph    CF3CF2    B24 0A898        H    F2CH           Ph    CF3CF2    B24 0A899        H    HCC             Ph    CF3CF2    B24 0A900        H    CH3CC          Ph    CF3CF2    B24 0A901        H    CH2=CH        Ph    CF3CF2    B24 0A902        H    CH2=CHCH2    Ph    CF3CF2    B24 0A903        H    CH3SO2N(CH3) Ph    CF3CF2    B24 0A904        H    (CH3)2N       Ph    CF3CF2    B24 0A905        H    (CH3)2NSO2   Ph    CF3CF2    B24 0A906        H    CH3SCH2       Ph    CF3CF2    B24 0A907        H    CH3SOCH2      Ph    CF3CF2    B24 0A908        H    CH3SO2CH2    Ph    CF3CF2    B24 0化合物序号  R2   R3            R4    R5         Q1 pA909        H    CH3            Ph    CF3CF2CF2 B24 0A910        H    CH3CH2        Ph    CF3CF2CF2 B24 0A911        H    环丙基          Ph    CF3CF2CF2 B24 0A912        H    (CH3)3C       Ph    CF3CF2CF2 B24 0A913        H    (CH3)2CH      Ph    CF3CF2CF2 B24 0A914        H    CH3(CH2)2    Ph    CF3CF2CF2 B24 0A915        H    CH3OCH2       Ph    CF3CF2CF2 B24 0A916        H    CH3O(CH2)2   Ph    CF3CF2CF2 B24 0A917        H    Ph              Ph    CF3CF2CF2 B24 0A918        H    PhO             Ph    CF3CF2CF2 B24 0A919        H    PhS             Ph    CF3CF2CF2 B24 0A920        H    PhSO            Ph    CF3CF2CF2 B24 0A921        H    PhSO2          Ph    CF3CF2CF2 B24 0A922        H    CH3S           Ph    CF3CF2CF2 B24 0A923        H    CH3SO          Ph    CF3CF2CF2 B24 0A924        H    CF3            Ph    CF3CF2CF2 B24 0A925        H    F2CH           Ph    CF3CF2CF2 B24 0A926        H    HCC             Ph    CF3CF2CF2 B24 0A927        H    CH3CC          Ph    CF3CF2CF2 B24 0A928        H    CH2=CH        Ph    CF3CF2CF2 B24 0A929        H    CH2=CHCH2    Ph    CF3CF2CF2 B24 0A930        H    CH3SO2N(CH3) Ph    CF3CF2CF2 B24 0A931        H    (CH3)2N       Ph    CF3CF2CF2 B24 0A932        H    (CH3)2NSO2   Ph    CF3CF2CF2 B24 0A933        H    CH3SCH2       Ph    CF3CF2CF2 B24 0A934        H    CH3SOCH2      Ph    CF3CF2CF2 B24 0A935        H    CH3SO2CH2    Ph    CF3CF2CF2 B24 0A936        H    CH3            Ph    CF2Cl        B24 0A937        H    CH3CH2        Ph    CF2Cl        B24 0A938        H    环丙基           Ph    CF2Cl        B24 0A939        H    (CH3)3C       Ph    CF2Cl        B24 0A940        H    (CH3)2CH      Ph    CF2Cl        B24 0化合物序号    R2   R3             R4    R5     Q1 pA941          H    CH3(CH2)2    Ph    CF2Cl    B24 0A942          H    CH3OCH2       Ph    CF2Cl    B24 0A943          H    CH3O(CH2)2   Ph    CF2Cl    B24 0A944          H    Ph               Ph    CF2Cl    B24 0A945          H    PhO              Ph    CF2Cl    B24 0A946          H    PhS              Ph    CF2Cl    B24 0A947          H    PhSO             Ph    CF2Cl    B24 0A948          H    PhSO2           Ph    CF2Cl    B24 0A949          H    CH3S            Ph    CF2Cl    B24 0A950          H    CH3SO           Ph    CF2Cl    B24 0A951          H    CF3             Ph    CF2Cl    B24 0A952          H    F2CH            Ph    CF2Cl    B24 0A953          H    HCC              Ph    CF2Cl    B24 0A954          H    CH3CC           Ph    CF2Cl    B24 0A955          H    CH2=CH         Ph    CF2Cl    B24 0A956          H    CH2=CHCH2     Ph    CF2Cl    B24 0A957          H    CH3SO2N(CH3)  Ph    CF2Cl    B24 0A958          H    (CH3)2N        Ph    CF2Cl    B24 0A959          H    (CH3)2NSO2    Ph    CF2Cl    B24 0A960          H    CH3SCH2        Ph    CF2Cl    B24 0A961          H    CH3SOCH2       Ph    CF2Cl    B24 0A962          H    CH3SO2CH2     Ph    CF2Cl    B24 0A963          H    CH3             Ph    CHF2     B24 0A964          H    CH3CH2         Ph    CHF2     B24 0A965          H    (CH3)3C        Ph    CHF2     B24 0A966          H    (CH3)2CH       Ph    CHF2     B24 0A967          H    环丙基            Ph    CHF2     B24 0A968          H    CH3(CH2)2     Ph    CHF2     B24 0A969          H    CH3OCH2        Ph    CHF2     B24 0A970          H    CH3O(CH2)2    Ph    CHF2     B24 0A971          H    Ph                Ph    CHF2     B24 0A972          H    PhO               Ph    CHF2     B24 0化合物序号   R2   R3              R4    R5    Q1  pA973         H    PhS               Ph    CHF2    B24  0A974         H    PhSO              Ph    CHF2    B24  0A975         H    PhSO2            Ph    CHF2    B24  0A976         H    CH3S             Ph    CHF2    B24  0A977         H    CH3SO            Ph    CHF2    B24  0A978         H    CF3              Ph    CHF2    B24  0A979         H    F2CH             Ph    CHF2    B24  0A980         H    HCC               Ph    CHF2    B24  0A981         H    CH3CC            Ph    CHF2    B24  0A982         H    CH2=CH          Ph    CHF2    B24  0A983         H    CH2=CHCH2      Ph    CHF2    B24  0A984         H    CH3SO2N(CH3)   Ph    CHF2    B24  0A985         H    (CH3)2N         Ph    CHF2    B24  0A986         H    (CH3)2NSO2     Ph    CHF2    B24  0A987         H    CH3SCH2         Ph    CHF2    B24  0A988         H    CH3SOCH2        Ph    CHF2    B24  0A989         H    CH3SO2CH2      Ph    CHF2    B24  0A990         H    CH3              Ph    CCl3    B24  0A991         H    CH3CH2          Ph    CCl3    B24  0A992         H    (CH3)3C         Ph    CCl3    B24  0A993         H    (CH3)2CH        Ph    CCl3    B24  0A994         H    环丙基             Ph    CCl3    B24  0A995         H    CH3(CH2)2      Ph    CCl3    B24  0A996         H    CH3OCH2         Ph    CCl3    B24  0A997         H    CH3O(CH2)2     Ph    CCl3    B24  0A998         H    Ph                 Ph    CCl3    B24  0A999         H    PhO                Ph    CCl3    B24  0A1000        H    PhS                Ph    CCl3    B24  0A1001        H    PhSO               Ph    CCl3    B24  0A1002        H    PhSO2             Ph    CCl3    B24  0A1003        H    CH3S              Ph    CCl3    B24  0A1004        H    CH3SO             Ph    CCl3    B24  0化合物序号    R2                     R3            R4    R5     Q1 pA1005         H                       CF3           Ph    CCl3    B24  0A1006         H                       F2CH          Ph    CCl3    B24  0A1007         H                       HCC            Ph    CCl3    B24  0A1008         H                       CH3CC         Ph    CCl3    B24  0A1009         H                       CH2=CH       Ph    CCl3    B24  0A1010         H                       CH2=CHCH2   Ph    CCl3    B24  0A1011         H                       CH3SO2N(CH3)Ph    CCl3    B24  0A1012         H                       (CH3)2N      Ph    CCl3    B24  0A1013         H                       (CH3)2NSO2  Ph    CCl3    B24  0A1014         H                       CH3SCH2      Ph    CCl3    B24  0A1015         H                       CH3SOCH2     Ph    CCl3    B24  0A1016         H                       CH3SO2CH2   Ph    CCl3    B24  0A1017         F                       H               H     CF3     B24  0A1018         CI                      H               H     CF3     B24  0A1019         Br                      H               H     CF3     B24  0A1020         NC                      H               H     CF3     B24  0A1021         CH3SO2O               H               H     CF3     B24  0A1022         CH3O                   H               H     CF3     B24  0A1023         CH3CH2O               H               H     CF3     B24  0A1024         CH2CH=CH2O           H               H     CF3     B24  0A1025         HCCCH2O                H               H     CF3     B24  0A1026         PhCH2S                 H               H     CF3     B24  0A1027         PhCH2SO2              H               H     CF3     B24  0A1028         CICH2CH2              H               H     CF3     B24  0A1029         BrCH2                  H               H     CF3     B24  0A1030         FCH2                   H               H     CF3     B24  0A1031         CHF2CH2               H               H     CF3     B24  0A1032         CF3CH2                H               H     CF3     B24  0A1033         [l,3]-咪唑-l-基甲基    H               H     CF3     B24  0A1034         CHCl2CH2              H               H     CF3     B24  0A1035         ClCH=CH                H               H     CF3     B24  0化合物序号    R2         R3         R4  R5    Q1  pA1036         Cl2C=CH   H           H    CF3    B24  0A1037         CF3CH=CH  H           H    CF3    B24  0A1038         ClCC        H           H    CF3    B24  0A1039         PhCH2      H           H    CF3    B24  0A1040         CH3CH2    CH3       H    CF3    B24  0A1041         CH3        OH          H    CF3    B24  0A1042         CH3        F           H    CF3    B24  0A1043         CH3        Cl          H    CF3    B24  0A1044         F           CH3        H    CF3    B24  0A1045         Cl          CH3        H    CF3    B24  0A1046         H           F           H    CF3    B24  0A1047         H           Cl          H    CF3     B24  0A1048         H           Br          H    CF3    B24  0A1049         H           OH          H    CF3    B24  0A1050         H           OCH3       H    CF3    B24  0A1051         H           OCHF2      H    CF3    B24  0A1052         H           OSO2CH3   H    CF3    B24  0A1053         H           OSO2CF3   H    CF3    B24  0A1054         H           ClCH2      H    CF3    B24  0A1055         H           BrCH2      H    CF3    B24  0A1056         H           FCH2       H    CF3    B24  0A1057         H           CHF2CH2   H    CF3    B24  0A1058         H           CF3CH2    H    CF3    B24  0A1059         H           三唑基甲基  H    CF3    B24  0A1060         H           CHCl2CH2  H    CF3    B24  0A1061         H           ClCH=CH    H    CF3    B24  0A1062         H           Cl2C=CH   H    CF3    B24  0A1063         H           CF3CH=CH  H    CF3    B24  0A1064         H           ClCC        H    CF3    B24  0A1065         H           CH3C(O     H    CF3    B24  0A1066         H           Ph          H    CF3    B24  0A1067         H           SO2CH3   H    CF3    B24  0化合物序号   R2               R3       R4      R5     Q1  pA1068        H                 SO2CF3  H        CF3     B24  0A1069        H                 NC        H        CF3     B24  0A1070        H                 NO2      H        CF3     B24  0A1071        CH3              H         F        CF3     B24  0A1072        CH3              H         Cl       CF3     B24  0A1073        CH3              H         Br       CF3     B24  0A1074        CH3              H         NC       CF3     B24  0A1075        CH3              H         CH3O    CF3     B24  0A1076        CH3              H         CH3S    CF3     B24  0A1077        CH3              H         CH3SO   CF3     B24  0A1078        CH3              H         CH3SO2 CF3     B24  0A1079        CH3CH2OCH2    H         H        CF3     B24  0A1080        PhOCH2           H         H        CF3     B24  0A1081                 H         H        CF3     B24  0A1082        (CH3)2CH2OCH2H         H        CF3     B24  0A1083        BrCH2CH2        H         H        CF3     B24  0A1084        FCH2CH2         H         H        CF3     B24  0A1085        
Figure A9981578601962
       H         H       CF3          0A1086        
Figure A9981578601963
      H         H       CF3     B24  0A1087               H         H       CF3     B24  0A1088               H         H       CF3     B24  0A1089        
Figure A9981578601966
     H         H       CF3     B24  0A1090        
Figure A9981578601967
     H         H       CF3     B24  0化合物序号     R2                    R3     R4   R5     Q1  pNO.A1091          丙基-CH2               H      H     CF3     B24  0A1092          2,2-二氯环丙-1-基      H      H     CF3     B24  0A1093          CH3OC(O)CH=CH         H      H     CF3     B24  0A1094          CH3CH2OC(O)CH=CH     H      H     CF3     B24  0A1095          ClCH2CH=CH            H      H     CF3          0A1096          CH=C=CH               H      H     CF3     B24  0A1097          (CH3)2NCH2          H      H     CF3     B24  0A1098          HOCH2                  H      H     CF3     B24  0A1099          CH3C(O)OCH2           H      H     CF3     B24  0A1100          PhC(O)OCH2             H      H     CF3     B24  0A1101          PhCH2CH2              H      H     CF3     B24  0A1102          CH3OC(O)CH2           H      H     CF3     B24  0A1103          NCCH2                  H      H     CF3     B24  0A1104          CH3(CH2)7SCH2      H      H     CF3     B24  0A1105          CH3(CH2)7SOCH2     H      H     CF3     B24  0A1106          CH3(CH2)7SO2CH2   H      H     CF3     B24  0A1107          
Figure A9981578601971
            H      H     CF3     B24  0A1108          ClCH2CC                H      H     CF3     B24  0A1109          CHF2CH2CH2          H      H     CF3     B24  0A1110          CHCl2CH2CH2         H      H     CF3     B24  0A1111          CF3SO2O              H      H     CF3     B24  0A1112                       H      H     CF3     B24  0A1113                       H      H     CF3     B24  0A1114         
Figure A9981578601974
             H      H     CF3     B24  0A1115         
Figure A9981578601975
                H      H     CF3     B24  0化合物序号    R2                    R3     R4    R5      Q1  pA1116        
Figure A9981578601981
               H       H      CF3      B24  0A1117        
Figure A9981578601982
               H       H      CF3      B24  0A1118         CH3ON=CHCH2         H       H      CF3      B24  0A1119         O=CHCH2              H       H      CF3      B24  0A1120         CH3CH2OCH2          H       H      CF2Cl    B24  0A1121         PhOCH2                H       H      CF2Cl    B24  0A1122        
Figure A9981578601983
              H       H      CF2Cl    B24  0A1123         (CH3)2CH2OCH2     H       H      CF2Cl    B24  0A1124         BrCH2                 H       H      CF2Cl    B24  0A1125         FCH2                  H       H      CF2Cl    B24  0A112          
Figure A9981578601984
           H       H      CF2Cl    B24  0A1127                    H       H      CF2Cl    B24  0A1128         
Figure A9981578601986
          H       H      CF2Cl    B24  0A1129                    H       H      CF2Cl    B24  0A1130         
Figure A9981578601988
        H       H      CF2Cl    B24  0A1131                  H       H      CF2Cl    B24  0A1132         环丙基-CH2            H       H      CF2Cl    B24  0A1133         2,2-二氯环丙-1-基     H       H      CF2Cl    B24  0A1134         CH3OC(O)CH=CH        H       H      CF2Cl    B24  0A1135         CH3CH2OC(O)CH=CH    H       H      CF2Cl    B24  0化合物序号  R2                R3      R4     R5        Q1  pA1136       ClCH2CH=CH         H       H      CF2Cl      B24  0A1137       CH=C=CH            H       H      CF2Cl      B24  0A1138       (CH3)2NCH2       H       H      CF2Cl      B24  0A1139       HOCH2               H       H      CF2Cl      B24  0A1140       CH3C(O)OCH2       H       H      CF2Cl      B24  0A1141       PhC(O)OCH2          H       H      CF2Cl      B24  0A1142       PhCH2               H       H      CF2Cl      B24  0A1143       CH3OC(O)CH2        H       H      CF2Cl      B24  0A1144       NCCH2               H       H      CF2Cl      B24  0A1145       CH3(CH2)7SCH2   H       H      CF2Cl      B24  0A1146       CH3(CH2)7SOCH2  H       H      CF2Cl      B24  0A1147       CH3(CH2)7SO2CH2H       H      CF2Cl      B24  0A1148                 H       H      CF2Cl      B24  0A1149       ClCH2CC             H       H      CF2Cl      B24  0A1150       Br                   H       H      CF2Cl      B24  0A1151       Cl                   H       H      CF2Cl      B24  0A1152       CF3SO2O           H       H      CF2Cl      B24  0A1153                 H       H      CF2Cl      B24  0A1154                 H       H      CF2Cl      B24  0A1155                 H       H      CF2Cl      B24  0A1156       
Figure A9981578601995
            H       H      CF2Cl      B24  0A1157                    H       H      CF2Cl      B24  0A1158       
Figure A9981578601997
            H       H      CF2Cl      B24  0A1159       CH3ON=CHCH2       H       H      CF2Cl      B24  0A1160       O=CHCH2            H       H      CF2Cl      B24  0化合物序号    R2                   R3     R4     R5       Q1  pA1161         CH3CH2OCH2         H       H      CF2H      B24  0A1162         PhOCH2               H       H      CF2H      B24  0A1163                      H       H      CF2H      B24  0A1164         (CH3)2CH2OCH2    H       H      CF2H      B24  0A1165         BrCH2                H       H      CF2H      B24  0A1166         FCH2                 H       H      CF2H      B24  0A1167                    H       H      CF2H      B24  0A1168         
Figure A9981578602003
         H       H      CF2H      B24  0A1169                   H       H      CF2H      B24  0A1170         
Figure A9981578602005
         H       H      CF2H      B24  0A1171                  H       H      CF2H      B24  0A1172         
Figure A9981578602007
       H       H      CF2H      B24  0A1173         环丙基-CH2           H       H      CF2H      B24  0A1174         2,2-二氯环丙-1-基    H       H      CF2H      B24  0A1175         CH3OC(O)CH=CH       H       H      CF2H      B24  0A1176         CH3CH2OC(O)CH=CH   H       H      CF2H      B24  0A1177         ClCH2CH=CH          H       H      CF2H      B24  0A1178         CH=C=CH             H       H      CF2H      B24  0A1179         (CH3)2NCH2        H       H      CF2H      B24  0A1180         HOCH2                H       H      CF2H      B24  0A1181         CH3C(O)OCH2         H       H      CF2H      B24  0A1182         PhC(O)OCH2           H       H      CF2H      B24  0化合物序号  R2                 R3      R4      R5         Q1  pA1183       PhCH2               H        H       CF2H        B24  0A1184       CH3OC(O)CH2        H        H       CF2H        B24  0A1185       NCCH2               H        H       CF2H        B24  0A1186       CH3(CH2)7SCH2   H        H       CF2H        B24  0A1187       CH3(CH2)7SOCH2  H        H       CF2H        B24  0A1188       CH3(CH2)7SO2CH2H        H       CF2H        B24  0A1189                 H        H       CF2H        B24  0A1190       ClCH2CC             H        H       CF2H        B24  0A1191       Br                   H        H       CF2H        B24  0A1192       Cl                   H        H       CF2H        B24  0A1193       CF3SO2O           H        H       CF2H        B24  0A1194                 H        H       CF2H        B24  0A1195                 H        H       CF2H        B24  0A1196       
Figure A9981578602014
         H        H       CF2H        B24  0A1197       
Figure A9981578602015
           H        H       CF2H        B24  0A1198       
Figure A9981578602016
           H        H       CF2H        B24  0A1199       
Figure A9981578602017
           H        H       CF2H        B24  0A1200       CH3ON=CHCH2      H        H       CF2H        B24  0A1201       O=CHCH2           H        H       CF2H        B24  0A1202       CH3CH=CH          H        H       CF3         B24  0A1203       CH3SO2NH          H        H       CF3         B24  0A1204       CH3CH2CH2O      H        CH3    CF3         B24  0A1205       Cl                  CH3     H       CF3         B24  0A1206       F2CHO              H        H       CF3         B24  0A1207       CH3CH2C(O)OCH2  H        H       CF3         B24  0化合物序号    R2           R3  R4  R5    Q1 pA1208    CH3CH2OC(O)OCH2H    H    CF3    B24 0A1209    CH3OCH2OCH2    H    H    CF3    B24 0A1210    CH3               H    H    CF3    B24 1A1211    CH3CH2           H    H    CF3    B24 1A1212    环丙基             H    H    CF3    B24 1A1213    CH3(CH2)2      H    H    CF3    B24 1A1214    CH3OCH2          H    H    CF3    B24 1A1215    CF3               H    H    CF3    B24 1A1216    F2CH              H    H    CF3    B24 1A1217    ClCH2             H    H    CF3    B24 1A1218    CH3SO2CH2      H    H    CF3    B24 1A1219    CH3              CF3  H    CH3    B24 1A1220    CH3CH2OCH2     H    H    CF3    B24 1A1221    PhOCH2            H    H    CF3    B24 1A1222    (CH3)2CH2OCH2 H    H    CF3    B24 1A1223    BrCH2             H    H    CF3    B24 1A1224    FCH2              H    H    CF3    B24 1A1225    
Figure A9981578602021
      H    H    CF3    B24 1A1226         H    H    CF3    B24 1A1227    环丙基-CH2        H    H    CF3    B24 1A1228    2,2-二氯环丙-1-基 H    H    CF3    B24 1A1229    (CH3)2NCH2     H    H    CF3    B24 1A1230    HOCH2             H    H    CF3    B24 1A1231    CH3C(O)OCH2      H    H    CF3    B24 1A1232    PhC(O)OCH2        H    H    CF3    B24 1A1233    PhCH2             H    H    CF3    B24 1A1234    CH3OC(O)CH2      H    H    CF3    B24 1A1235    NCCH2             H    H    CF3    B24 1化合物序号    R2            R3   R4   R5     Q1 pA1236    CH3(CH2)7SO2CH2H    H    CF3      B24 1A1237    Br                   H    H    CF3      B24 1A1238    Cl                   H    H    CF3      B24 1A1239    O=CHCH2            H    H    CF3      B24 1A1240    CH3                 H    H    CF2Cl    B24 1A1241    CH3CH2             H    H    CF2Cl    B24 1A1242    环丙基               H    H    CF2Cl    B24 1A1243    CH3(CH2)2        H    H    CF2Cl    B24 1A1244    CH3OCH2            H    H    CF2Cl    B24 1A1245    CF3                 H    H    CF2Cl    B24 1A1246    F2CH                H    H    CF2Cl    B24 1A1247    ClCH2               H    H    CF2Cl    B24 1A1248    CH3SO2CH2        H    H    CF2Cl    B24 1A1249    CH3                CF3  H    CF2Cl    B24 1A1250    CH3CH2OCH2       H    H    CF2Cl    B24 1A1251    PhOCH2              H    H    CF2Cl    B24 1A1252    (CH3)2CH2OCH2   H    H    CF2Cl    B24 1A1253    BrCH2               H    H    CF2Cl    B24 1A1254    FCH2                H    H    CF2Cl    B24 1A1255             H    H    CF2Cl    B24 1A1256   
Figure A9981578602032
        H    H    CF2Cl    B24 1A1257    环丙基-CH2          H    H    CF2Cl    B24 1A1258    2,2-二氯环丙-1-基   H    H    CF2Cl    B24 1A1259    (CH3)2NCH2       H    H    CF2Cl    B24 1A1260    HOCH2               H    H    CF2Cl    B24 1A1261    CH3C(O)OCH2        H    H    CF2Cl    B24 1A1262    PhC(O)OCH2          H    H    CF2Cl    B24 1A1263    PhCH2               H    H    CF2Cl    B24 1化合物序号    R2            R3   R4   R5    Q1 pA1264    CH3OC(O)CH2        H    H    CF2Cl   B24 1A1265    NCCH2               H    H    CF2Cl   B24 1A1266    CH3(CH2)7SO2CH2H    H    CF2Cl   B24 1A1267    Br                   H    H    CF2Cl   B24 1A1268    Cl                   H    H    CF2Cl   B24 1A1269    O=CHCH2            H    H    CF2Cl   B24 1A1270    CH3                 H    H    CF2H    B24 1A1271    CH3CH2            H    H    CF2H    B24 1A1272    环丙基               H    H    CF2H    B24 1A1273    CH3(CH2)2        H    H    CF2H    B24 1A1274    CH3OCH2            H    H    CF2H    B24 1A1275    CF3                 H    H    CF2H    B24 1A1276    F2CH                H    H    CF2H    B24 1A1277    ClCH2               H    H    CF2H    B24 1A1278    CH3SO2CH2         H    H    CF2H    B24 1A1279    CH3                 CF3 H    CF2H    B24 1A1280    CH3CH2OCH2        H    H    CF2H    B24 1A1281    PhOCH2              H    H    CF2H    B24 1A1282    (CH3)2CH2OCH2   H    H    CF2H    B24 1A1283    BrCH2               H    H    CF2H    B24 1A1284    FCH2                H    H    CF2H    B24 1A1285    
Figure A9981578602041
        H    H    CF2H    B24 1A1286   
Figure A9981578602042
       H    H    CF2H    B24 1A1287    环丙基-CH2          H    H    CF2H    B24 1A1288    2,2-二氯环丙-1-基   H    H    CF2H    B24 1A1289    (CH3)2NCH2       H    H    CF2H    B24 1A1290    HOCH2               H    H    CF2H    B24 1A1291    CH3C(O)OCH2        H    H    CF2H    B24 1化合物序号    R2          R3   R4            R5    Q1 pA1292    PhC(O)OCH2          H    H            CF2H    B24 1A1293    PhCH2               H    H            CF2H    B24 1A1294    CH3OC(O)CH2        H    H            CF2H    B24 1A1295    NCCH2               H    H            CF2H    B24 1A1296    CH3(CH2)7SO2CH2H    H            CF2H    B24 1A1297    Br                   H    H            CF2H    B24 1A1298    Cl                   H    H            CF2H    B24 1A1299    O=CHCH2            H    H            CF2H    B24 1A1300    CH3                 H    H            CF3CF2 B24 1A1301    HO                   H    Ph           CF3     B24 0A1302    CH3                 H    CH2=CH     CF3     B24 0A1303    CH3                 H    CH3CH2O    CF3     B24 0A1304    HO                   CH3 H            CF3     B24 0A1305    HO                   H    H            CF3     B24 0A1306    (CH3CH2)2N(O)CO  H    H            CF3     B24 0A1307    CH3                 H    甲苯磺酰基-O CF3     B24 0A1308    CH3                 H    CH3CC       CF3     B24 0A1309    CH3                 H    HCC          CF3     B24 0A1310    CH3                 H    ClCH2CC     CF3     B24 0A1311    CH3                 H    PhCH2O      CF3      B24 0A1312    CH3                 H    CF3SO2O    CF3     B24 0A1313    CH3                 H    (CH3)2N    CF3     B24 0A1314    CH3                 H    CH3C(O)O    CF3     B24 0A1315    CH3                 H    CH3CH2C(O) CF3     B24 0OA1316    CH3                 H    PhC(O)O      CF3     B24 0A1317    CH3                 H    3-吡啶基     CF3     B24 0A1318    CH3OCH2OCH2       H    H            CF2Cl   B24 0A1319    CH3OCH2OCH2       H    H            CF2H    B24 0A1320    CH3OCH2OCH2       H    H            CF2CF3 B24 0A1321    CH3OCH2OCH2       H    H            CF3     B24 1A1322    CH3O                H    CH3         CF3     B24 0
就各表中的结构式而言(例如表7,化合物A1088,取代基R2),与吡啶环的键合部位位于结构式的右手一侧。端价键为甲基。表8:式Ib化合物(P为0或1):
Figure A9981578602071
Q1   Q1   Q1   Q1   Q1  Q1  Q1   Q1   Q1   Q1   Q1   Q1B1    B2     B3    B4    B5    B6    B7    B8    B9    B10   B11   B12B13   B14    B15   B16   B17   B18   B19   B20   B21   B22   B23    -B25   B26    B27   B28   B29   B30   B31   B32   B33   B34   B35   B36B37   B38    B39   B40   B41   B42   B43   B44   B45   B46   B47   B48B49   B50    B51   B52   B53   B54   B55   B56   B57   B58   B59   B60B61   B62    B63   B64   B65   B66   B67   B68   B69   B70   B71   B72B73   B74    B75   B76   B77   B78   B79   B80   B81   B82   B83   B84B85   B86    B87   B88   B89   B90   B91   B92   B93   B94   B95   B96B97   B98    B99   B100  B101  B102  B103  B104  B105  B106  B107  B108B109  B110   B111  B112  B113  B114  B115  B116  B117  B118  B119  B120B121  B122   B123  B124  B125  B126  B127  B128  B129  B130  B131  B132B133  B134   B135  B136  B137  B138  B139  B140  B141  B142  B143  B144B145  B146   B147  B148  B149  B150  B151  B152  B153  B154  B155  B156B157  B158   B159  B160  B161  B162  B163  B164  B165  B166  B167  B168B169  B170   B171  B172  B173  B174  B175  B176  B177  B178  B179  B180B181  B182   B183  B184  B185  B186  B187  B188  B189  B190  B191  B192B193  B194   B195  B196  B197  B198  B199  B200  B201  B202  B203  B204B205  B206   B207  B208  B209  B210  B211  B212  B213  B214  B215  B216B217  B218   B219  B220  B221  B222  B223  B224  B225  B226  B227  B228B229  B230   B231  B232  B233  B234  B235  B236  B237  B238  B239  B240B241  B242   B243  B244  B245  B246  B247  B248  B249  B250  B251  B252B253  B254   B255  B256  B257  B258  B259  B260  B261  B262  B263  B264B265  B266   B267  B268  B269  B270  B271  B272  B273  B274  B275  B276B277  B278   B279  B280  B281  B282  B283  B284  B285  B286  B287  B288B289  B290   B291  B292  B293  B294  B295  B296  B297  B298  B299  B300Q1    Q1  Q1  Q1   Q1   Q1  Q1   Q1   Q1   Q1   Q1  Q1B301  B302  B303  B304  B305  B306  B307  B308  B309  B310  B311  B312B313  B314  B315  B316  B317  B318  B319  B320  B321  B322  B323  B324B325  B326  B327  B328  B329  B330  B331  B332  B333  B334  B335  B336B337  B338  B339  B340  B341  B342  B343  B344  B345  B346  B347  B348B349  B350  B351  B352  B353  B354  B355  B356  B357  B358  B359  B360B361  B362  B363  B364  B365  B366  B367  B368  B369  B370  B371  B372B373  B374  B375  B376  B377  B378  B379  B380  B381  B382  B383  B384B385  B386  B387  B388  B389  B390  B391  B392  B393  B394  B395  B396B397  B398  B399  B400  B401  B402  B403  B404  B405  B406  B407  B408B409  B410  B411  B412  B413  B414  B415  B416  B417  B418  B419  B420B421  B422  B423  B424  B425  B426  B427  B428  B429  B430  B431  B432B433  B434  B435  B436  B437  B438  B439  B440  B441  B442  B443  B444B445  B446  B447  B448  B449  B450  B451  B452  B453  B454  B455  B456B457  B458  B459  B460  B461  B462  B463  B464  B465  B466  B467  B468B469  B470  B471  B472  B473  B474  B475  B476  B477  B478  B479  B480B481  B482  B483  B484  B485  B486  B487  B488  B489  B490  B491  B492B493  B494  B495  B496  B497  B498  B499  B500  B501  B502  B503  B504B505  B506  B507  B508  B509  B510  B511  B512  B513  B514  B515  B516B517  B518  B519  B520  B521  B522  B523  B524  B525  B526  B527  B528B529  B530  B531  B532  B533  B534  B535  B536  B537  B538  B539  B540B541  B542  B543  B544  B545  B546  B547  B548  B549  B550  B551  B552B553  B554  B555  B556  B557  B558  B559  B560  B561  B562  B563  B564B565  B566  B567  B568  B569  B570  B571  B572  B573  B574  B575  B576B577  B578  B579  B580  B581  B582  B583  B584  B585  B586  B587  B588B589  B590  B591  B592  B593  B594  B595  B596  B597  B598  B599  B600B601  B602  B603  B604  B605  B606  B607  B608  B609  B610  B611  B612B613  B614  B615  B616  B617  B618  B619  B620  B621  B622  B623  B624B625  B626  B627  B628  B629  B630  B631  B632  B633  B634  B635  B636B637  B638  B639  B640  B641  B642  B643  B644  B645  B646  B647  B648B649  B650  B651  B652  B653  B654  B655  B656  B657  B658  B659  B660B661  B662  B663  B664  B665  B666  B667  B668  B669  B670  B671  B672B773  B774  B775  B776  B777  B778  B779  B780  B781  B782  B783  B784B785  B786  B787  B788  B789  B790  B791  B792  B793  B794  B795  B796Q1   Q1   Q1   Q1   Q1   Q1   Q1  Q1  Q1  Q1   Q1   Q1B797  B798  B799  B800  B801  B802  B803  B804  B805  B806  B807  B808B809  B810  B811  B812  B813  B814  B815  B816  B817  B818  B819  B820B821  B822  B823  B824  B825  B826  B827  B828  B829  B830  B831  B832B833  B834  B835  B836  B837  B838  B839  B840  B841  B842  B843  B844B845  B846  B847  B848  B849  B850  B851  B852  B853  B854  B855  B856B857  B858  B859  B860  B861  B862  B863  B864  B865  B866  B867  B868B869  B870  B871  B872  B873  B874  B875  B876  B877  B878  B879  B880B881  B882  B883  B884  B885  B886  B887  B888  B889  B890  B891  B892B893  B894  B895  B896  B897  B898  B899  B900  B901  B902  B903  B904B905  B906  B907  B908  B909  B910  B911  B912  B913  B914  B915  B916B917  B918  B919  B920  B921  B922  B923  B924  B925  B926  B927  B928B929  B930  B931  B932  B933  B934  B935  B936  B937  B938  B939  B940B941  B942  B943  B944  B945  B946  B947  B948  B949  B950  B951  B952B953  B954  B955  B956  B957  B958  B959  B960  B961  B962  B963  B964B965  B966  B967  B968  B969  B970  B971  B972  B973  B974  B975  B976B977  B978  B979  B980  B981  B982  B983  B984  B985  B986  B987  B988B989  B990  B991  B992  B993  B994  B995  B996  B997  B998  B999  B1000B1001 B1002 B1003 B1004 B1005 B1006 B1007 B1008 B1009 B1010 B1011 B1012B1013 B1014 B1015 B1016 B1017 B1018 B1019 B1020 B1021 B1022 B1023 B1024B1025 B1026 B1027 B1028 B1029 B1030 B1031 B1032 B1033 B1034 B1035 B1036B1037 B1038 B1039 B1040 B1041 B1042 B1043 B1044 B1045 B1046 B1047 B1048B1049 B1050 B1051 B1052 B1053 B1054 B1055 B1056 B1057 B1058 B1059 B1060B1061 B1062 B1063 B1064 B1065 B1066 B1067 B1068 B1069 B1070 B1071 B1072B1073 B1074 B1075 B1076 B1077 B1078 B1079 B1080 B1081 B1082 B1083 B1084B1085 B1086 B1087 B1088 B1089 B1090 B1091 B1092 B1093 B1094 B1095 B1096B1097 B1098 B1099 B1100 B1101 B1102 B1103 B1104 B1105 B1106 B1107 B1108B1109 B1110 B1111 B1112 B1113 B1114 B1115 B1116 B1117 B1118 B1119 B1120B1121 B1122 B1123 B1124 B1125 B1126 B1127 B1128 B1129 B1130 B1131 B1132B1133 B1134 B1135 B1136 B1137 B1138 B1139 B1140 B1141 B1142 B1143 B1144B1145 B1146 B1147 B1148 B1149 B1150 B1151 B1152 B1153 B1154 B1155 B1156B1157 B1158 B1159 B1160 B1161 B1162 B1163 B1164 B1165 B1166 B1167 B1168B1169 B1170 B1171 B1172 B1173 B1174 B1175 B1176 B1177 B1178 B1179 B1180B1181 B1182 B1183 B1184 B1185 B1186 B1187 B1188 B1189 B1190 B1191 B1192Q1   Q1   Q1   Q1   Q1   Q1   Q1   Q1   Q1  Q1  Q1  Q1B1193 B1194 B1195 B1196 B1197 B1198 B1199 B1200 B1201 B1202 B1203 B1204B1205 B1206 B1207 B1208 B1209 B1210 B1211 B1212 B1213 B1214 B1215 B1216B1217表9:式Ic化合物(P为0或1):
Figure A9981578602101
Q1   Q1  Q1   Q1   Q1   Q1   Q1  Q1   Q1  Q1   Q1   Q1B1    B2    B3    B4    B5    B6    B7    B8    B9    B10   B11   B12B13   B14   B15   B16   B17   B18   B19   B20   B21   B22   B23    -B25   B26   B27   B28   B29   B30   B31   B32   B33   B34   B35   B36B37   B38   B39   B40   B41   B42   B43   B44   B45   B46   B47   B48B49   B50   B51   B52   B53   B54   B55   B56   B57   B58   B59   B60B61   B62   B63   B64   B65   B66   B67   B68   B69   B70   B71   B72B73   B74   B75   B76   B77   B78   B79   B80   B81   B82   B83   B84B85   B86   B87   B88   B89   B90   B91   B92   B93   B94   B95   B96B97   B98   B99   B100  B101  B102  B103  B104  B105  B106  B107  B108B109  B110  B111  B112  B113  B114  B115  B116  B117  B118  B119  B120B121  B122  B123  B124  B125  B126  B127  B128  B129  B130  B131  B132B133  B134  B135  B136  B137  B138  B139  B140  B141  B142  B143  B144B145  B146  B147  B148  B149  B150  B151  B152  B153  B154  B155  B156B157  B158  B159  B160  B161  B162  B163  B164  B165  B166  B167  B168B169  B170  B171  B172  B173  B174  B175  B176  B177  B178  B179  B180B181  B182  B183  B184  B185  B186  B187  B188  B189  B190  B191  B192B193  B194  B195  B196  B197  B198  B199  B200  B201  B202  B203  B204B205  B206  B207  B208  B209  B210  B211  B212  B213  B214  B215  B216B217  B218  B219  B220  B221  B222  B223  B224  B225  B226  B227  B228B229  B230  B231  B232  B233  B234  B235  B236  B237  B238  B239  B240B241  B242  B243  B244  B245  B246  B247  B248  B249  B250  B251  B252Q1   Q1   Q1   Q1   Q1  Q1   Q1  Q1   Q1  Q1  Q1   Q1B253  B254  B255  B256  B257  B258  B259  B260  B261  B262  B263  B264B265  B266  B267  B268  B269  B270  B271  B272  B273  B274  B275  B276B277  B278  B279  B280  B281  B282  B283  B284  B285  B286  B287  B288B289  B290  B291  B292  B293  B294  B295  B296  B297  B298  B299  B300B301  B302  B303  B304  B305  B306  B307  B308  B309  B310  B311  B312B313  B314  B315  B316  B317  B318  B319  B320  B321  B322  B323  B324B325  B326  B327  B328  B329  B330  B331  B332  B333  B334  B335  B336B337  B338  B339  B340  B341  B342  B343  B344  B345  B346  B347  B348B349  B350  B351  B352  B353  B354  B355  B356  B357  B358  B359  B360B361  B362  B363  B364  B365  B366  B367  B368  B369  B370  B371  B372B373  B374  B375  B376  B377  B378  B379  B380  B381  B382  B383  B384B385  B386  B387  B388  B389  B390  B391  B392  B393  B394  B395  B396B397  B398  B399  B400  B401  B402  B403  B404  B405  B406  B407  B408B409  B410  B411  B412  B413  B414  B415  B416  B417  B418  B419  B420B421  B422  B423  B424  B425  B426  B427  B428  B429  B430  B431  B432B433  B434  B435  B436  B437  B438  B439  B440  B441  B442  B443  B444B445  B446  B447  B448  B449  B450  B451  B452  B453  B454  B455  B456B457  B458  B459  B460  B461  B462  B463  B464  B465  B466  B467  B468B469  B470  B471  B472  B473  B474  B475  B476  B477  B478  B479  B480B481  B482  B483  B484  B485  B486  B487  B488  B489  B490  B491  B492B493  B494  B495  B496  B497  B498  B499  B500  B501  B502  B503  B504B505  B506  B507  B508  B509  B510  B511  B512  B513  B514  B515  B516B517  B518  B519  B520  B521  B522  B523  B524  B525  B526  B527  B528B529  B530  B531  B532  B533  B534  B535  B536  B537  B538  B539  B540B541  B542  B543  B544  B545  B546  B547  B548  B549  B550  B551  B552B553  B554  B555  B556  B557  B558  B559  B560  B561  B562  B563  B564B565  B566  B567  B568  B569  B570  B571  B572  B573  B574  B575  B576B577  B578  B579  B580  B581  B582  B583  B584  B585  B586  B587  B588B589  B590  B591  B592  B593  B594  B595  B596  B597  B598  B599  B600B601  B602  B603  B604  B605  B606  B607  B608  B609  B610  B611  B612B613  B614  B615  B616  B617  B618  B619  B620  B621  B622  B623  B624B625  B626  B627  B628  B629  B630  B631  B632  B633  B634  B635  B636B637  B638  B639  B640  B641  B642  B643  B644  B645  B646  B647  B648Q1   Q1   Q1   Q1  Q1   Q1  Q1   Q1  Q1   Q1  Q1   Q1B649  B650  B651  B652  B653  B654  B655  B656  B657  B658  B659  B660B661  B662  B663  B664  B665  B666  B667  B668  B669  B670  B671  B672B773  B774  B775  B776  B777  B778  B779  B780  B781  B782  B783  B784B785  B786  B787  B788  B789  B790  B791  B792  B793  B794  B795  B796B797  B798  B799  B800  B801  B802  B803  B804  B805  B806  B807  B808B809  B810  B811  B812  B813  B814  B815  B816  B817  B818  B819  B820B821  B822  B823  B824  B825  B826  B827  B828  B829  B830  B831  B832B833  B834  B835  B836  B837  B838  B839  B840  B841  B842  B843  B844B845  B846  B847  B848  B849  B850  B851  B852  B853  B854  B855  B856B857  B858  B859  B860  B861  B862  B863  B864  B865  B866  B867  B868B869  B870  B871  B872  B873  B874  B875  B876  B877  B878  B879  B880B881  B882  B883  B884  B885  B886  B887  B888  B889  B890  B891  B892B893  B894  B895  B896  B897  B898  B899  B900  B901  B902  B903  B904B905  B906  B907  B908  B909  B910  B911  B912  B913  B914  B915  B916B917  B918  B919  B920  B921  B922  B923  B924  B925  B926  B927  B928B929  B930  B931  B932  B933  B934  B935  B936  B937  B938  B939  B940B941  B942  B943  B944  B945  B946  B947  B948  B949  B950  B951  B952B953  B954  B955  B956  B957  B958  B959  B960  B961  B962  B963  B964B965  B966  B967  B968  B969  B970  B971  B972  B973  B974  B975  B976B977  B978  B979  B980  B981  B982  B983  B984  B985  B986  B987  B988B989  B990  B991  B992  B993  B994  B995  B996  B997  B998  B999 B1000B1001 B1002 B1003 B1004 B1005 B1006 B1007 B1008 B1009 B1010 B1011 B1012B1013 B1014 B1015 B1016 B1017 B1018 B1019 B1020 B1021 B1022 B1023 B1024B1025 B1026 B1027 B1028 B1029 B1030 B1031 B1032 B1033 B1034 B1035 B1036B1037 B1038 B1039 B1040 B1041 B1042 B1043 B1044 B1045 B1046 B1047 B1048B1049 B1050 B1051 B1052 B1053 B1054 B1055 B1056 B1057 B1058 B1059 B1060B1061 B1062 B1063 B1064 B1065 B1066 B1067 B1068 B1069 B1070 B1071 B1072B1073 B1074 B1075 B1076 B1077 B1078 B1079 B1080 B1081 B1082 B1083 B1084B1085 B1086 B1087 B1088 B1089 B1090 B1091 B1092 B1093 B1094 B1095 B1096B1097 B1098 B1099 B1100 B1101 B1102 B1103 B1104 B1105 B1106 B1107 B1108B1109 B1110 B1111 B1112 B1113 B1114 B1115 B1116 B1117 B1118 B1119 B1120B1121 B1122 B1123 B1124 B1125 B1126 B1127 B1128 B1129 B1130 B1131 B1132B1133 B1134 B1135 B1136 B1137 B1138 B1139 B1140 B1141 B1142 B1143 B1144Q1   Q1   Q1   Q1  Q1   Q1  Q1   Q1  Q1   Q1  Q1   Q1B1145 B1146 B1147 B1148 B1149 B1150 B1151 B1152 B1153 B1154 B1155 B1156B1157 B1158 B1159 B1160 B1161 B1162 B1163 B1164 B1165 B1166 B1167 B1168B1169 B1170 B1171 B1172 B1173 B1174 B1175 B1176 B1177 B1178 B1179 B1180B1181 B1182 B1183 B1184 B1185 B1186 B1187 B1188 B1189 B1190 B1191 B1192B1193 B1194 B1195 B1196 B1197 B1198 B1199 B1200 B1201 B1202 B1203 B1204B1205 B1206 B1207 B1208 B1209 B1210 B1211 B1212 B1213 B1214 B1215 B1216B1217表10:式Id化合物(P为0或1):
Figure A9981578602131
Q1   Q1   Q1  Q1   Q1  Q1   Q1   Q1  Q1   Q1  Q1   Q1B1    B2    B3    B4    B5    B6    B7    B8    B9    B10   B11   B12B13   B14   B15   B16   B17   B18   B19   B20   B21   B22   B23    -B25   B26   B27   B28   B29   B30   B31   B32   B33   B34   B35   B36B37   B38   B39   B40   B41   B42   B43   B44   B45   B46   B47   B48B49   B50   B51   B52   B53   B54   B55   B56   B57   B58   B59   B60B61   B62   B63   B64   B65   B66   B67   B68   B69   B70   B71   B72B73   B74   B75   B76   B77   B78   B79   B80   B81   B82   B83   B84B85   B86   B87   B88   B89   B90   B91   B92   B93   B94   B95   B96B97   B98   B99   B100  B101  B102  B103  B104  B105  B106  B107  B108B109  B110  B111  B112  B113  B114  B115  B116  B117  B118  B119  B120B121  B122  B123  B124  B125  B126  B127  B128  B129  B130  B131  B132B133  B134  B135  B136  B137  B138  B139  B140  B141  B142  B143  B144B145  B146  B147  B148  B149  B150  B151  B152  B153  B154  B155  B156B157  B158  B159  B160  B161  B162  B163  B164  B165  B166  B167  B168B169  B170  B171  B172  B173  B174  B175  B176  B177  B178  B179  B180B181  B182  B183  B184  B185  B186  B187  B188  B189  B190  B191  B192B193  B194  B195  B196  B197  B198  B199  B200  B201  B202  B203  B204Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1  Q1   Q1   Q1B205  B206  B207  B208  B209  B210  B211  B212  B213  B214  B215  B216B217  B218  B219  B220  B221  B222  B223  B224  B225  B226  B227  B228B229  B230  B231  B232  B233  B234  B235  B236  B237  B238  B239  B240B241  B242  B243  B244  B245  B246  B247  B248  B249  B250  B251  B252B253  B254  B255  B256  B257  B258  B259  B260  B261  B262  B263  B264B265  B266  B267  B268  B269  B270  B271  B272  B273  B274  B275  B276B277  B278  B279  B280  B281  B282  B283  B284  B285  B286  B287  B288B289  B290  B291  B292  B293  B294  B295  B296  B297  B298  B299  B300B301  B302  B303  B304  B305  B306  B307  B308  B309  B310  B311  B312B313  B314  B315  B316  B317  B318  B319  B320  B321  B322  B323  B324B325  B326  B327  B328  B329  B330  B331  B332  B333  B334  B335  B336B337  B338  B339  B340  B341  B342  B343  B344  B345  B346  B347  B348B349  B350  B351  B352  B353  B354  B355  B356  B357  B358  B359  B360B361  B362  B363  B364  B365  B366  B367  B368  B369  B370  B371  B372B373  B374  B375  B376  B377  B378  B379  B380  B381  B382  B383  B384B385  B386  B387  B388  B389  B390  B391  B392  B393  B394  B395  B396B397  B398  B399  B400  B401  B402  B403  B404  B405  B406  B407  B408B409  B410  B411  B412  B413  B414  B415  B416  B417  B418  B419  B420B421  B422  B423  B424  B425  B426  B427  B428  B429  B430  B431  B432B433  B434  B435  B436  B437  B438  B439  B440  B441  B442  B443  B444B445  B446  B447  B448  B449  B450  B451  B452  B453  B454  B455  B456B457  B458  B459  B460  B461  B462  B463  B464  B465  B466  B467  B468B469  B470  B471  B472  B473  B474  B475  B476  B477  B478  B479  B480B481  B482  B483  B484  B485  B486  B487  B488  B489  B490  B491  B492B493  B494  B495  B496  B497  B498  B499  B500  B501  B502  B503  B504B505  B506  B507  B508  B509  B510  B511  B512  B513  B514  B515  B516B517  B518  B519  B520  B521  B522  B523  B524  B525  B526  B527  B528B529  B530  B531  B532  B533  B534  B535  B536  B537  B538  B539  B540B541  B542  B543  B544  B545  B546  B547  B548  B549  B550  B551  B552B553  B554  B555  B556  B557  B558  B559  B560  B561  B562  B563  B564B565  B566  B567  B568  B569  B570  B571  B572  B573  B574  B575  B576B577  B578  B579  B580  B581  B582  B583  B584  B585  B586  B587  B588B589  B590  B591  B592  B593  B594  B595  B596  B597  B598  B599  B600Q1     Q1    Q1     Q1     Q1     Q1     Q1     Q1     Q1    Q1    Q1     Q1B601    B602    B603    B604    B605    B606    B607    B608    B609    B610    B611    B612B613    B614    B615    B616    B617    B618    B619    B620    B621    B622    B623    B624B625    B626    B627    B628    B629    B630    B631    B632    B633    B634    B635    B636B637    B638    B639    B640    B641    B642    B643    B644    B645    B646    B647    B648B649    B650    B651    B652    B653    B654    B655    B656    B657    B658    B659    B660B661    B662    B663    B664    B665    B666    B667    B668    B669    B670    B671    B672B773    B774    B775    B776    B777    B778    B779    B780    B781    B782    B783    B784B785    B786    B787    B788    B789    B790    B791    B792    B793    B794    B795    B796B797    B798    B799    B800    B801    B802    B803    B804    B805    B806    B807    B808B809    B810    B811    B812    B813    B814    B815    B816    B817    B818    B819    B820B821    B822    B823    B824    B825    B826    B827    B828    B829    B830    B831    B832B833    B834    B835    B836    B837    B838    B839    B840    B841    B842    B843    B844B845    B846    B847    B848    B849    B850    B851    B852    B853    B854    B855    B856B857    B858    B859    B860    B861    B862    B863    B864    B865    B866    B867    B868B869    B870    B871    B872    B873    B874    B875    B876    B877    B878    B879    B880B881    B882    B883    B884    B885    B886    B887    B888    B889    B890    B891    B892B893    B894    B895    B896    B897    B898    B899    B900    B901    B902    B903    B904B905    B906    B907    B908    B909    B910    B911    B912    B913    B914    B915    B916B917    B918    B919    B920    B921    B922    B923    B924    B925    B926    B927    B928B929    B930    B931    B932    B933    B934    B935    B936    B937    B938    B939    B940B941    B942    B943    B944    B945    B946    B947    B948    B949    B950    B951    B952B953    B954    B955    B956    B957    B958    B959    B960    B961    B962    B963    B964B965    B966    B967    B968    B969    B970    B971    B972    B973    B974    B975    B976B977    B978    B979    B980    B981    B982    B983    B984    B985    B986    B987    B988B989    B990    B991    B992    B993    B994    B995    B996    B997    B998    B999    B1000B1001   B1002   B1003   B1004   B1005   B1006   B1007   B1008   B1009   B1010   B1011   B1012B1013   B1014   B1015   B1016   B1017   B1018   B1019   B1020   B1021   B1022   B1023   B1024B1025   B1026   B1027   B1028   B1029   B1030   B1031   B1032   B1033   B1034   B1035   B1036B1037   B1038   B1039   B1040   B1041   B1042   B1043   B1044   B1045   B1046   B1047   B1048B1049   B1050   B1051   B1052   B1053   B1054   B1055   B1056   B1057   B1058   B1059   B1060B1061   B1062   B1063   B1064   B1065   B1066   B1067   B1068   B1069   B1070   B1071   B1072B1073   B1074   B1075   B1076   B1077   B1078   B1079   B1080   B1081   B1082   B1083   B1084B1085   B1086   B1087   B1088   B1089   B1090   B1091   B1092   B1093   B1094   B1095   B1096 Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B1097 B1098 B1099 B1100 B1101 B1102 B1103 B1104 B1105 B1106 B1107 B1108B1109 B1110 B1111 B1112 B1113 B1114 B1115 B1116 B1117 B1118 B1119 B1120B1121 B1122 B1123 B1124 B1125 B1126 B1127 B1128 B1129 B1130 B1131 B1132B1133 B1134 B1135 B1136 B1137 B1138 B1139 B1140 B1141 B1142 B1143 B1144B1145 B1146 B1147 B1148 B1149 B1150 B1151 B1152 B1153 B1154 B1155 B1156B1157 B1158 B1159 B1160 B1161 B1162 B1163 B1164 B1165 B1166 B1167 B1168B1169 B1170 B1171 B1172 B1173 B1174 B1175 B1176 B1177 B1178 B1179 B1180B1181 B1182 B1183 B1184 B1185 B1186 B1187 B1188 B1189 B1190 B1191 B1192B1193 B1194 B1195 B1196 B1197 B1198 B1199 B1200 B1201 B1202 B1203 B1204B1205 B1206 B1207 B1208 B1209 B1210 B1211 B1212 B1213 B1214 B1215 B1216B1217表11:式Ie化合物(P为0或1):
Figure A9981578602161
Q1    Q1  Q1   Q1  Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1B1    B2    B3    B4    B5    B6    B7    B8    B9    B10   B11   B12B13   B14   B15   B16   B17   B18   B19   B20   B21   B22   B23    -B25   B26   B27   B28   B29   B30   B31   B32   B33   B34   B35   B36B37   B38   B39   B40   B41   B42   B43   B44   B45   B46   B47   B48B49   B50   B51   B52   B53   B54   B55   B56   B57   B58   B59   B60B61   B62   B63   B64   B65   B66   B67   B68   B69   B70   B71   B72B73   B74   B75   B76   B77   B78   B79   B80   B81   B82   B83   B84B85   B86   B87   B88   B89   B90   B91   B92   B93   B94   B95   B96B97   B98   B99   B100  B101  B102  B103  B104  B105  B106  B107  B108B109  B110  B111  B112  B113  B114  B115  B116  B117  B118  B119  B120B121  B122  B123  B124  B125  B126  B127  B128  B129  B130  B131  B132B133  B134  B135  B136  B137  B138  B139  B140  B141  B142  B143  B144B145  B146  B147  B148  B149  B150  B151  B152  B153  B154  B155  B156Q1   Q1   Q1   Q1   Q1   Q1  Q1  Q1   Q1  Q1   Q1  Q1B157  B158  B159  B160  B161  B162  B163  B164  B165  B166  B167  B168B169  B170  B171  B172  B173  B174  B175  B176  B177  B178  B179  B180B181  B182  B183  B184  B185  B186  B187  B188  B189  B190  B191  B192B193  B194  B195  B196  B197  B198  B199  B200  B201  B202  B203  B204B205  B206  B207  B208  B209  B210  B211  B212  B213  B214  B215  B216B217  B218  B219  B220  B221  B222  B223  B224  B225  B226  B227  B228B229  B230  B231  B232  B233  B234  B235  B236  B237  B238  B239  B240B241  B242  B243  B244  B245  B246  B247  B248  B249  B250  B251  B252B253  B254  B255  B256  B257  B258  B259  B260  B261  B262  B263  B264B265  B266  B267  B268  B269  B270  B271  B272  B273  B274  B275  B276B277  B278  B279  B280  B281  B282  B283  B284  B285  B286  B287  B288B289  B290  B291  B292  B293  B294  B295  B296  B297  B298  B299  B300B301  B302  B303  B304  B305  B306  B307  B308  B309  B310  B311  B312B313  B314  B315  B316  B317  B318  B319  B320  B321  B322  B323  B324B325  B326  B327  B328  B329  B330  B331  B332  B333  B334  B335  B336B337  B338  B339  B340  B341  B342  B343  B344  B345  B346  B347  B348B349  B350  B351  B352  B353  B354  B355  B356  B357  B358  B359  B360B361  B362  B363  B364  B365  B366  B367  B368  B369  B370  B371  B372B373  B374  B375  B376  B377  B378  B379  B380  B381  B382  B383  B384B385  B386  B387  B388  B389  B390  B391  B392  B393  B394  B395  B396B397  B398  B399  B400  B401  B402  B403  B404  B405  B406  B407  B408B409  B410  B411  B412  B413  B414  B415  B416  B417  B418  B419  B420B421  B422  B423  B424  B425  B426  B427  B428  B429  B430  B431  B432B433  B434  B435  B436  B437  B438  B439  B440  B441  B442  B443  B444B445  B446  B447  B448  B449  B450  B451  B452  B453  B454  B455  B456B457  B458  B459  B460  B461  B462  B463  B464  B465  B466  B467  B468B469  B470  B471  B472  B473  B474  B475  B476  B477  B478  B479  B480B481  B482  B483  B484  B485  B486  B487  B488  B489  B490  B491  B492B493  B494  B495  B496  B497  B498  B499  B500  B501  B502  B503  B504B505  B506  B507  B508  B509  B510  B511  B512  B513  B514  B515  B516B517  B518  B519  B520  B521  B522  B523  B524  B525  B526  B527  B528B529  B530  B531  B532  B533  B534  B535  B536  B537  B538  B539  B540B541  B542  B543  B544  B545  B546  B547  B548  B549  B550  B551  B552Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B553  B554  B555  B556  B557  B558  B559  B560  B561  B562  B563  B564B565  B566  B567  B568  B569  B570  B571  B572  B573  B574  B575  B576B577  B578  B579  B580  B581  B582  B583  B584  B585  B586  B587  B588B589  B590  B591  B592  B593  B594  B595  B596  B597  B598  B599  B600B601  B602  B603  B604  B605  B606  B607  B608  B609  B610  B611  B612B613  B614  B615  B616  B617  B618  B619  B620  B621  B622  B623  B624B625  B626  B627  B628  B629  B630  B631  B632  B633  B634  B635  B636B637  B638  B639  B640  B641  B642  B643  B644  B645  B646  B647  B648B649  B650  B651  B652  B653  B654  B655  B656  B657  B658  B659  B660B661  B662  B663  B664  B665  B666  B667  B668  B669  B670  B671  B672B773  B774  B775  B776  B777  B778  B779  B780  B781  B782  B783  B784B785  B786  B787  B788  B789  B790  B791  B792  B793  B794  B795  B796B797  B798  B799  B800  B801  B802  B803  B804  B805  B806  B807  B808B809  B810  B811  B812  B813  B814  B815  B816  B817  B818  B819  B820B821  B822  B823  B824  B825  B826  B827  B828  B829  B830  B831  B832B833  B834  B835  B836  B837  B838  B839  B840  B841  B842  B843  B844B845  B846  B847  B848  B849  B850  B851  B852  B853  B854  B855  B856B857  B858  B859  B860  B861  B862  B863  B864  B865  B866  B867  B868B869  B870  B871  B872  B873  B874  B875  B876  B877  B878  B879  B880B881  B882  B883  B884  B885  B886  B887  B888  B889  B890  B891  B892B893  B894  B895  B896  B897  B898  B899  B900  B901  B902  B903  B904B905  B906  B907  B908  B909  B910  B911  B912  B913  B914  B915  B916B917  B918  B919  B920  B921  B922  B923  B924  B925  B926  B927  B928B929  B930  B931  B932  B933  B934  B935  B936  B937  B938  B939  B940B941  B942  B943  B944  B945  B946  B947  B948  B949  B950  B951  B952B953  B954  B955  B956  B957  B958  B959  B960  B961  B962  B963  B964B965  B966  B967  B968  B969  B970  B971  B972  B973  B974  B975  B976B977  B978  B979  B980  B981  B982  B983  B984  B985  B986  B987  B988B989  B990  B991  B992  B993  B994  B995  B996  B997  B998  B999  B1000B1001 B1002 B1003 B1004 B1005 B1006 B1007 B1008 B1009 B1010 B1011 B1012B1013 B1014 B1015 B1016 B1017 B1018 B1019 B1020 B1021 B1022 B1023 B1024B1025 B1026 B1027 B1028 B1029 B1030 B1031 B1032 B1033 B1034 B1035 B1036B1037 B1038 B1039 B1040 B1041 B1042 B1043 B1044 B1045 B1046 B1047 B1048Q1   Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1  Q1   Q1B1049 B1050 B1051 B1052 B1053 B1054 B1055 B1056 B1057 B1058 B1059 B1060B1061 B1062 B1063 B1064 B1065 B1066 B1067 B1068 B1069 B1070 B1071 B1072B1073 B1074 B1075 B1076 B1077 B1078 B1079 B1080 B1081 B1082 B1083 B1084B1085 B1086 B1087 B1088 B1089 B1090 B1091 B1092 B1093 B1094 B1095 B1096B1097 B1098 B1099 B1100 B1101 B1102 B1103 B1104 B1105 B1106 B1107 B1108B1109 B1110 B1111 B1112 B1113 B1114 B1115 B1116 B1117 B1118 B1119 B1120B1121 B1122 B1123 B1124 B1125 B1126 B1127 B1128 B1129 B1130 B1131 B1132B1133 B1134 B1135 B1136 B1137 B1138 B1139 B1140 B1141 B1142 B1143 B1144B1145 B1146 B1147 B1148 B1149 B1150 B1151 B1152 B1153 B1154 B1155 B1156B1157 B1158 B1159 B1160 B1161 B1162 B1163 B1164 B1165 B1166 B1167 B1168B1169 B1170 B1171 B1172 B1173 B1174 B1175 B1176 B1177 B1178 B1179 B1180B1181 B1182 B1183 B1184 B1185 B1186 B1187 B1188 B1189 B1190 B1191 B1192B1193 B1194 B1195 B1196 B1197 B1198 B1199 B1200 B1201 B1202 B1203 B1204B1205 B1206 B1207 B1208 B1209 B1210 B1211 B1212 B1213 B1214 B1215 B1216B1217表12:式If化合物
Figure A9981578602191
Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B1    B2    B3    B4    B5    B6    B7    B8    B9    B10   B11   B12B13   B14   B15   B16   B17   B18   B19   B20   B21   B22   B23    -B25   B26   B27   B28   B29   B30   B31   B32   B33   B34   B35   B36B37   B38   B39   B40   B41   B42   B43   B44   B45   B46   B47   B48B49   B50   B51   B52   B53   B54   B55   B56   B57   B58   B59   B60B61   B62   B63   B64   B65   B66   B67   B68   B69   B70   B71   B72B73   B74   B75   B76   B77   B78   B79   B80   B81   B82   B83   B84B85   B86   B87   B88   B89   B90   B91   B92   B93   B94   B95   B96B97   B98   B99   B100  B101  B102  B103  B104  B105  B106  B107  B108Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B109  B110  B111  B112  B113  B114  B115  B116  B117  B118  B119  B120B121  B122  B123  B124  B125  B126  B127  B128  B129  B130  B131  B132B133  B134  B135  B136  B137  B138  B139  B140  B141  B142  B143  B144B145  B146  B147  B148  B149  B150  B151  B152  B153  B154  B155  B156B157  B158  B159  B160  B161  B162  B163  B164  B165  B166  B167  B168B169  B170  B171  B172  B173  B174  B175  B176  B177  B178  B179  B180B181  B182  B183  B184  B185  B186  B187  B188  B189  B190  B191  B192B193  B194  B195  B196  B197  B198  B199  B200  B201  B202  B203  B204B205  B206  B207  B208  B209  B210  B211  B212  B213  B214  B215  B216B217  B218  B219  B220  B221  B222  B223  B224  B225  B226  B227  B228B229  B230  B231  B232  B233  B234  B235  B236  B237  B238  B239  B240B241  B242  B243  B244  B245  B246  B247  B248  B249  B250  B251  B252B253  B254  B255  B256  B257  B258  B259  B260  B261  B262  B263  B264B265  B266  B267  B268  B269  B270  B271  B272  B273  B274  B275  B276B277  B278  B279  B280  B281  B282  B283  B284  B285  B286  B287  B288B289  B290  B291  B292  B293  B294  B295  B296  B297  B298  B299  B300B301  B302  B303  B304  B305  B306  B307  B308  B309  B310  B311  B312B313  B314  B315  B316  B317  B318  B319  B320  B321  B322  B323  B324B325  B326  B327  B328  B329  B330  B331  B332  B333  B334  B335  B336B337  B338  B339  B340  B341  B342  B343  B344  B345  B346  B347  B348B349  B350  B351  B352  B353  B354  B355  B356  B357  B358  B359  B360B361  B362  B363  B364  B365  B366  B367  B368  B369  B370  B371  B372B373  B374  B375  B376  B377  B378  B379  B380  B381  B382  B383  B384B385  B386  B387  B388  B389  B390  B391  B392  B393  B394  B395  B396B397  B398  B399  B400  B401  B402  B403  B404  B405  B406  B407  B408B409  B410  B411  B412  B413  B414  B415  B416  B417  B418  B419  B420B421  B422  B423  B424  B425  B426  B427  B428  B429  B430  B431  B432B433  B434  B435  B436  B437  B438  B439  B440  B441  B442  B443  B444B445  B446  B447  B448  B449  B450  B451  B452  B453  B454  B455  B456B457  B458  B459  B460  B461  B462  B463  B464  B465  B466  B467  B468B469  B470  B471  B472  B473  B474  B475  B476  B477  B478  B479  B480B481  B482  B483  B484  B485  B486  B487  B488  B489  B490  B491  B492B493  B494  B495  B496  B497  B498  B499  B500  B501  B502  B503  B504Q1    Q1    Q1   Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B505   B506   B507  B508   B509  B510  B511  B512  B513  B514  B515  B516B517   B518   B519  B520   B521  B522  B523  B524  B525  B526  B527  B528B529   B530   B531  B532   B533  B534  B535  B536  B537  B538  B539  B540B541   B542   B543  B544   B545  B546  B547  B548  B549  B550  B551  B552B553   B554   B555  B556   B557  B558  B559  B560  B561  B562  B563  B564B565   B566   B567  B568   B569  B570  B571  B572  B573  B574  B575  B576B577   B578   B579  B580   B581  B582  B583  B584  B585  B586  B587  B588B589   B590   B591  B592   B593  B594  B595  B596  B597  B598  B599  B600B601   B602   B603  B604   B605  B606  B607  B608  B609  B610  B611  B612B613   B614   B615  B616   B617  B618  B619  B620  B621  B622  B623  B624B625   B626   B627  B628   B629  B630  B631  B632  B633  B634  B635  B636B637   B638   B639  B640   B641  B642  B643  B644  B645  B646  B647  B648B649   B650   B651  B652   B653  B654  B655  B656  B657  B658  B659  B660B661   B662   B663  B664   B665  B666  B667  B668  B669  B670  B671  B672B773   B774   B775  B776   B777  B778  B779  B780  B781  B782  B783  B784B785   B786   B787  B788   B789  B790  B791  B792  B793  B794  B795  B796B797   B798   B799  B800   B801  B802  B803  B804  B805  B806  B807  B808B809   B810   B811  B812   B813  B814  B815  B816  B817  B818  B819  B820B821   B822   B823  B824   B825  B826  B827  B828  B829  B830  B831  B832B833   B834   B835  B836   B837  B838  B839  B840  B841  B842  B843  B844B845   B846   B847  B848   B849  B850  B851  B852  B853  B854  B855  B856B857   B858   B859  B860   B861  B862  B863  B864  B865  B866  B867  B868B869   B870   B871  B872   B873  B874  B875  B876  B877  B878  B879  B880B881   B882   B883  B884   B885  B886  B887  B888  B889  B890  B891  B892B893   B894   B895  B896   B897  B898  B899  B900  B901  B902  B903  B904B905   B906   B907  B908   B909  B910  B911  B912  B913  B914  B915  B916B917   B918   B919  B920   B921  B922  B923  B924  B925  B926  B927  B928B929   B930   B931  B932   B933  B934  B935  B936  B937  B938  B939  B940B941   B942   B943  B944   B945  B946  B947  B948  B949  B950  B951  B952B953   B954   B955  B956   B957  B958  B959  B960  B961  B962  B963  B964B965   B966   B967  B968   B969  B970  B971  B972  B973  B974  B975  B976B977   B978   B979  B980   B981  B982  B983  B984  B985  B986  B987  B988B989   B990   B991  B992   B993  B994  B995  B996  B997  B998  B999  B1000Q1   Q1   Q1  Q1    Q1    Q1   Q1   Q1    Q1   Q1  Q1    Q1B1001 B1002 B1003 B1004  B1005  B1006 B1007  B1008  B1009 B1010  B1011  B1012B1013 B1014 B1015 B1016  B1017  B1018 B1019  B1020  B1021 B1022  B1023  B1024B1025 B1026 B1027 B1028  B1029  B1030 B1031  B1032  B1033 B1034  B1035  B1036B1037 B1038 B1039 B1040  B1041  B1042 B1043  B1044  B1045 B1046  B1047  B1048B1049 B1050 B1051 B1052  B1053  B1054 B1055  B1056  B1057 B1058  B1059  B1060B1061 B1062 B1063 B1064  B1065  B1066 B1067  B1068  B1069 B1070  B1071  B1072B1073 B1074 B1075 B1076  B1077  B1078 B1079  B1080  B1081 B1082  B1083  B1084B1085 B1086 B1087 B1088  B1089  B1090 B1091  B1092  B1093 B1094  B1095  B1096B1097 B1098 B1099 B1100  B1101  B1102 B1103  B1104  B1105 B1106  B1107  B1108B1109 B1110 B1111 B1112  B1113  B1114 B1115  B1116  B1117 B1118  B1119  B1120B1121 B1122 B1123 B1124  B1125  B1126 B1127  B1128  B1129 B1130  B1131  B1132B1133 B1134 B1135 B1136  B1137  B1138 B1139  B1140  B1141 B1142  B1143  B1144B1145 B1146 B1147 B1148  B1149  B1150 B1151  B1152  B1153 B1154  B1155  B1156B1157 B1158 B1159 B1160  B1161  B1162 B1163  B1164  B1165 B1166  B1167  B1168B1169 B1170 B1171 B1172  B1173  B1174 B1175  B1176  B1177 B1178  B1179  B1180B1181 B1182 B1183 B1184  B1185  B1186 B1187  B1188  B1189 B1190  B1191  B1192B1193 B1194 B1195 B1196  B1197  B1198 B1199  B1200  B1201 B1202  B1203  B1204B1205 B1206 B1207 B1208  B1209  B1210 B1211  B1212  B1213 B1214  B1215  B1216B1217表13:式Ig化合物(P为0或1):
Figure A9981578602221
Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B1    B2    B3    B4    B5    B6    B7    B8    B9    B10   B11   B12B13   B14   B15   B16   B17   B18   B19   B20   B21   B22   B23    -B25   B26   B27   B28   B29   B30   B31   B32   B33   B34   B35   B36B37   B38   B39   B40   B41   B42   B43   B44   B45   B46   B47   B48B49   B50   B51   B52   B53   B54   B55   B56   B57   B58   B59   B60B61   B62   B63   B64   B65   B66   B67   B68   B69   B70   B71   B72Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1B73   B74   B75   B76   B77   B78   B79   B80   B81   B82   B83   B84B85   B86   B87   B88   B89   B90   B91   B92   B93   B94   B95   B96B97   B98   B99   B100  B101  B102  B103  B104  B105  B106  B107  B108B109  B110  B111  B112  B113  B114  B115  B116  B117  B118  B119  B120B121  B122  B123  B124  B125  B126  B127  B128  B129  B130  B131  B132B133  B134  B135  B136  B137  B138  B139  B140  B141  B142  B143  B144B145  B146  B147  B148  B149  B150  B151  B152  B153  B154  B155  B156B157  B158  B159  B160  B161  B162  B163  B164  B165  B166  B167  B168B169  B170  B171  B172  B173  B174  B175  B176  B177  B178  B179  B180B181  B182  B183  B184  B185  B186  B187  B188  B189  B190  B191  B192B193  B194  B195  B196  B197  B198  B199  B200  B201  B202  B203  B204B205  B206  B207  B208  B209  B210  B211  B212  B213  B214  B215  B216B217  B218  B219  B220  B221  B222  B223  B224  B225  B226  B227  B228B229  B230  B231  B232  B233  B234  B235  B236  B237  B238  B239  B240B241  B242  B243  B244  B245  B246  B247  B248  B249  B250  B251  B252B253  B254  B255  B256  B257  B258  B259  B260  B261  B262  B263  B264B265  B266  B267  B268  B269  B270  B271  B272  B273  B274  B275  B276B277  B278  B279  B280  B281  B282  B283  B284  B285  B286  B287  B288B289  B290  B291  B292  B293  B294  B295  B296  B297  B298  B299  B300B301  B302  B303  B304  B305  B306  B307  B308  B309  B310  B311  B312B313  B314  B315  B316  B317  B318  B319  B320  B321  B322  B323  B324B325  B326  B327  B328  B329  B330  B331  B332  B333  B334  B335  B336B337  B338  B339  B340  B341  B342  B343  B344  B345  B346  B347  B348B349  B350  B351  B352  B353  B354  B355  B356  B357  B358  B359  B360B361  B362  B363  B364  B365  B366  B367  B368  B369  B370  B371  B372B373  B374  B375  B376  B377  B378  B379  B380  B381  B382  B383  B384B385  B386  B387  B388  B389  B390  B391  B392  B393  B394  B395  B396B397  B398  B399  B400  B401  B402  B403  B404  B405  B406  B407  B408B409  B410  B411  B412  B413  B414  B415  B416  B417  B418  B419  B420B421  B422  B423  B424  B425  B426  B427  B428  B429  B430  B431  B432B433  B434  B435  B436  B437  B438  B439  B440  B441  B442  B443  B444B445  B446  B447  B448  B449  B450  B451  B452  B453  B454  B455  B456B457  B458  B459  B460  B461  B462  B463  B464  B465  B466  B467  B468Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B469  B470  B471  B472  B473  B474  B475  B476  B477  B478  B479  B480B481  B482  B483  B484  B485  B486  B487  B488  B489  B490  B491  B492B493  B494  B495  B496  B497  B498  B499  B500  B501  B502  B503  B504B505  B506  B507  B508  B509  B510  B511  B512  B513  B514  B515  B516B517  B518  B519  B520  B521  B522  B523  B524  B525  B526  B527  B528B529  B530  B531  B532  B533  B534  B535  B536  B537  B538  B539  B540B541  B542  B543  B544  B545  B546  B547  B548  B549  B550  B551  B552B553  B554  B555  B556  B557  B558  B559  B560  B561  B562  B563  B564B565  B566  B567  B568  B569  B570  B571  B572  B573  B574  B575  B576B577  B578  B579  B580  B581  B582  B583  B584  B585  B586  B587  B588B589  B590  B591  B592  B593  B594  B595  B596  B597  B598  B599  B600B601  B602  B603  B604  B605  B606  B607  B608  B609  B610  B611  B612B613  B614  B615  B616  B617  B618  B619  B620  B621  B622  B623  B624B625  B626  B627  B628  B629  B630  B631  B632  B633  B634  B635  B636B637  B638  B639  B640  B641  B642  B643  B644  B645  B646  B647  B648B649  B650  B651  B652  B653  B654  B655  B656  B657  B658  B659  B660B661  B662  B663  B664  B665  B666  B667  B668  B669  B670  B671  B672B773  B774  B775  B776  B777  B778  B779  B780  B781  B782  B783  B784B785  B786  B787  B788  B789  B790  B791  B792  B793  B794  B795  B796B797  B798  B799  B800  B801  B802  B803  B804  B805  B806  B807  B808B809  B810  B811  B812  B813  B814  B815  B816  B817  B818  B819  B820B821  B822  B823  B824  B825  B826  B827  B828  B829  B830  B831  B832B833  B834  B835  B836  B837  B838  B839  B840  B841  B842  B843  B844B845  B846  B847  B848  B849  B850  B851  B852  B853  B854  B855  B856B857  B858  B859  B860  B861  B862  B863  B864  B865  B866  B867  B868B869  B870  B871  B872  B873  B874  B875  B876  B877  B878  B879  B880B881  B882  B883  B884  B885  B886  B887  B888  B889  B890  B891  B892B893  B894  B895  B896  B897  B898  B899  B900  B901  B902  B903  B904B905  B906  B907  B908  B909  B910  B911  B912  B913  B914  B915  B916B917  B918  B919  B920  B921  B922  B923  B924  B925  B926  B927  B928B929  B930  B931  B932  B933  B934  B935  B936  B937  B938  B939  B940B941  B942  B943  B944  B945  B946  B947  B948  B949  B950  B951  B952B953  B954  B955  B956  B957  B958  B959  B960  B961  B962  B963  B964Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B965  B966  B967  B968  B969  B970  B971  B972  B973  B974  B975  B976B977  B978  B979  B980  B981  B982  B983  B984  B985  B986  B987  B988B989  B990  B991  B992  B993  B994  B995  B996  B997  B998  B999  B1000B1001 B1002 B1003 B1004 B1005 B1006 B1007 B1008 B1009 B1010 B1011 B1012B1013 B1014 B1015 B1016 B1017 B1018 B1019 B1020 B1021 B1022 B1023 B1024B1025 B1026 B1027 B1028 B1029 B1030 B1031 B1032 B1033 B1034 B1035 B1036B1037 B1038 B1039 B1040 B1041 B1042 B1043 B1044 B1045 B1046 B1047 B1048B1049 B1050 B1051 B1052 B1053 B1054 B1055 B1056 B1057 B1058 B1059 B1060B1061 B1062 B1063 B1064 B1065 B1066 B1067 B1068 B1069 B1070 B1071 B1072B1073 B1074 B1075 B1076 B1077 B1078 B1079 B1080 B1081 B1082 B1083 B1084B1085 B1086 B1087 B1088 B1089 B1090 B1091 B1092 B1093 B1094 B1095 B1096B1097 B1098 B1099 B1100 B1101 B1102 B1103 B1104 B1105 B1106 B1107 B1108B1109 B1110 B1111 B1112 B1113 B1114 B1115 B1116 B1117 B1118 B1119 B1120B1121 B1122 B1123 B1124 B1125 B1126 B1127 B1128 B1129 B1130 B1131 B1132B1133 B1134 B1135 B1136 B1137 B1138 B1139 B1140 B1141 B1142 B1143 B1144B1145 B1146 B1147 B1148 B1149 B1150 B1151 B1152 B1153 B1154 B1155 B1156B1157 B1158 B1159 B1160 B1161 B1162 B1163 B1164 B1165 B1166 B1167 B1168B1169 B1170 B1171 B1172 B1173 B1174 B1175 B1176 B1177 B1178 B1179 B1180B1181 B1182 B1183 B1184 B1185 B1186 B1187 B1188 B1189 B1190 B1191 B1192B1193 B1194 B1195 B1196 B1197 B1198 B1199 B1200 B1201 B1202 B1203 B1204B1205 B1206 B1207 B1208 B1209 B1210 B1211 B1212 B1213 B1214 B1215 B1216B1217表14:式Ih化合物(P为0或1):
Figure A9981578602251
Q1   Q1   Q1   Q1   Q1   Q1  Q1   Q1   Q1   Q1  Q1    Q1B1    B2    B3     B4    B5    B6    B7    B8    B9    B10   B11    B12B13   B14   B15   B16   B17   B18   B19   B20   B21    B22   B23     -Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B25   B26   B27   B28   B29   B30   B31   B32   B33   B34   B35   B36B37   B38   B39   B40   B41   B42   B43   B44   B45   B46   B47   B48B49   B50   B51   B52   B53   B54   B55   B56   B57   B58   B59   B60B61   B62   B63   B64   B65   B66   B67   B68   B69   B70   B71   B72B73   B74   B75   B76   B77   B78   B79   B80   B81   B82   B83   B84B85   B86   B87   B88   B89   B90   B91   B92   B93   B94   B95   B96B97   B98   B99   B100  B101  B102  B103  B104  B105  B106  B107  B108B109  B110  B111  B112  B113  B114  B115  B116  B117  B118  B119  B120B121  B122  B123  B124  B125  B126  B127  B128  B129  B130  B131  B132B133  B134  B135  B136  B137  B138  B139  B140  B141  B142  B143  B144B145  B146  B147  B148  B149  B150  B151  B152  B153  B154  B155  B156B157  B158  B159  B160  B161  B162  B163  B164  B165  B166  B167  B168B169  B170  B171  B172  B173  B174  B175  B176  B177  B178  B179  B180B181  B182  B183  B184  B185  B186  B187  B188  B189  B190  B191  B192B193  B194  B195  B196  B197  B198  B199  B200  B201  B202  B203  B204B205  B206  B207  B208  B209  B210  B211  B212  B213  B214  B215  B216B217  B218  B219  B220  B221  B222  B223  B224  B225  B226  B227  B228B229  B230  B231  B232  B233  B234  B235  B236  B237  B238  B239  B240B241  B242  B243  B244  B245  B246  B247  B248  B249  B250  B251  B252B253  B254  B255  B256  B257  B258  B259  B260  B261  B262  B263  B264B265  B266  B267  B268  B269  B270  B271  B272  B273  B274  B275  B276B277  B278  B279  B280  B281  B282  B283  B284  B285  B286  B287  B288B289  B290  B291  B292  B293  B294  B295  B296  B297  B298  B299  B300B301  B302  B303  B304  B305  B306  B307  B308  B309  B310  B311  B312B313  B314  B315  B316  B317  B318  B319  B320  B321  B322  B323  B324B325  B326  B327  B328  B329  B330  B331  B332  B333  B334  B335  B336B337  B338  B339  B340  B341  B342  B343  B344  B345  B346  B347  B348B349  B350  B351  B352  B353  B354  B355  B356  B357  B358  B359  B360B361  B362  B363  B364  B365  B366  B367  B368  B369  B370  B371  B372B373  B374  B375  B376  B377  B378  B379  B380  B381  B382  B383  B384B385  B386  B387  B388  B389  B390  B391  B392  B393  B394  B395  B396B397  B398  B399  B400  B401  B402  B403  B404  B405  B406  B407  B408B409  B410  B411  B412  B413  B414  B415  B416  B417  B418  B419  B420Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1   Q1  Q1   Q1B421  B422  B423  B424  B425  B426  B427  B428  B429  B430  B431  B432B433  B434  B435  B436  B437  B438  B439  B440  B441  B442  B443  B444B445  B446  B447  B448  B449  B450  B451  B452  B453  B454  B455  B456B457  B458  B459  B460  B461  B462  B463  B464  B465  B466  B467  B468B469  B470  B471  B472  B473  B474  B475  B476  B477  B478  B479  B480B481  B482  B483  B484  B485  B486  B487  B488  B489  B490  B491  B492B493  B494  B495  B496  B497  B498  B499  B500  B501  B502  B503  B504B505  B506  B507  B508  B509  B510  B511  B512  B513  B514  B515  B516B517  B518  B519  B520  B521  B522  B523  B524  B525  B526  B527  B528B529  B530  B531  B532  B533  B534  B535  B536  B537  B538  B539  B540B541  B542  B543  B544  B545  B546  B547  B548  B549  B550  B551  B552B553  B554  B555  B556  B557  B558  B559  B560  B561  B562  B563  B564B565  B566  B567  B568  B569  B570  B571  B572  B573  B574  B575  B576B577  B578  B579  B580  B581  B582  B583  B584  B585  B586  B587  B588B589  B590  B591  B592  B593  B594  B595  B596  B597  B598  B599  B600B601  B602  B603  B604  B605  B606  B607  B608  B609  B610  B611  B612B613  B614  B615  B616  B617  B618  B619  B620  B621  B622  B623  B624B625  B626  B627  B628  B629  B630  B631  B632  B633  B634  B635  B636B637  B638  B639  B640  B641  B642  B643  B644  B645  B646  B647  B648B649  B650  B651  B652  B653  B654  B655  B656  B657  B658  B659  B660B661  B662  B663  B664  B665  B666  B667  B668  B669  B670  B671  B672B773  B774  B775  B776  B777  B778  B779  B780  B781  B782  B783  B784B785  B786  B787  B788  B789  B790  B791  B792  B793  B794  B795  B796B797  B798  B799  B800  B801  B802  B803  B804  B805  B806  B807  B808B809  B810  B811  B812  B813  B814  B815  B816  B817  B818  B819  B820B821  B822  B823  B824  B825  B826  B827  B828  B829  B830  B831  B832B833  B834  B835  B836  B837  B838  B839  B840  B841  B842  B843  B844B845  B846  B847  B848  B849  B850  B851  B852  B853  B854  B855  B856B857  B858  B859  B860  B861  B862  B863  B864  B865  B866  B867  B868B869  B870  B871  B872  B873  B874  B875  B876  B877  B878  B879  B880B881  B882  B883  B884  B885  B886  B887  B888  B889  B890  B891  B892B893  B894  B895  B896  B897  B898  B899  B900  B901  B902  B903  B904B905  B906  B907  B908  B909  B910  B911  B912  B913  B914  B915  B916Q1    Q1  Q1   Q1  Q1   Q1   Q1   Q1   Q1   Q1   Q1   Q1B917   B918  B919  B920  B921  B922  B923  B924  B925  B926  B927  B928B929   B930  B931  B932  B933  B934  B935  B936  B937  B938  B939  B940B941   B942  B943  B944  B945  B946  B947  B948  B949  B950  B951  B952B953   B954  B955  B956  B957  B958  B959  B960  B961  B962  B963  B964B965   B966  B967  B968  B969  B970  B971  B972  B973  B974  B975  B976B977   B978  B979  B980  B981  B982  B983  B984  B985  B986  B987  B988B989   B990  B991  B992  B993  B994  B995  B996  B997  B998  B999  B1000B1001  B1002 B1003 B1004 B1005 B1006 B1007 B1008 B1009 B1010 B1011 B1012B1013  B1014 B1015 B1016 B1017 B1018 B1019 B1020 B1021 B1022 B1023 B1024B1025  B1026 B1027 B1028 B1029 B1030 B1031 B1032 B1033 B1034 B1035 B1036B1037  B1038 B1039 B1040 B1041 B1042 B1043 B1044 B1045 B1046 B1047 B1048B1049  B1050 B1051 B1052 B1053 B1054 B1055 B1056 B1057 B1058 B1059 B1060B1061  B1062 B1063 B1064 B1065 B1066 B1067 B1068 B1069 B1070 B1071 B1072B1073  B1074 B1075 B1076 B1077 B1078 B1079 B1080 B1081 B1082 B1083 B1084B1085  B1086 B1087 B1088 B1089 B1090 B1091 B1092 B1093 B1094 B1095 B1096B1097  B1098 B1099 B1100 B1101 B1102 B1103 B1104 B1105 B1106 B1107 B1108B1109  B1110 B1111 B1112 B1113 B1114 B1115 B1116 B1117 B1118 B1119 B1120B1121  B1122 B1123 B1124 B1125 B1126 B1127 B1128 B1129 B1130 B1131 B1132B1133  B1134 B1135 B1136 B1137 B1138 B1139 B1140 B1141 B1142 B1143 B1144B1145  B1146 B1147 B1148 B1149 B1150 B1151 B1152 B1153 B1154 B1155 B1156B1157  B1158 B1159 B1160 B1161 B1162 B1163 B1164 B1165 B1166 B1167 B1168B1169  B1170 B1171 B1172 B1173 B1174 B1175 B1176 B1177 B1178 B1179 B1180B1181  B1182 B1183 B1184 B1185 B1186 B1187 B1188 B1189 B1190 B1191 B1192B1193  B1194 B1195 B1196 B1197 B1198 B1199 B1200 B1201 B1202 B1203 B1204B1205  B1206 B1207 B1208 B1209 B1210 B1211 B1212 B1213 B1214 B1215 B1216B1217表15:式Ik化合物(P为0或1)Q1   Q1   Q1  Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B1    B2    B3    B4    B5    B6    B7    B8    B9    B10   B11   B12B13   B14   B15   B16   B17   B18   B19   B20   B21   B22   B23    -B25   B26   B27   B28   B29   B30   B31   B32   B33   B34   B35   B36B37   B38   B39   B40   B41   B42   B43   B44   B45   B46   B47   B48B49   B50   B51   B52   B53   B54   B55   B56   B57   B58   B59   B60B61   B62   B63   B64   B65   B66   B67   B68   B69   B70   B71   B72B73   B74   B75   B76   B77   B78   B79   B80   B81   B82   B83   B84B85   B86   B87   B88   B89   B90   B91   B92   B93   B94   B95   B96B97   B98   B99   B100  B101  B102  B103  B104  B105  B106  B107  B108B109  B110  B111  B112  B113  B114  B115  B116  B117  B118  B119  B120B121  B122  B123  B124  B125  B126  B127  B128  B129  B130  B131  B132B133  B134  B135  B136  B137  B138  B139  B140  B141  B142  B143  B144B145  B146  B147  B148  B149  B150  B151  B152  B153  B154  B155  B156B157  B158  B159  B160  B161  B162  B163  B164  B165  B166  B167  B168B169  B170  B171  B172  B173  B174  B175  B176  B177  B178  B179  B180B181  B182  B183  B184  B185  B186  B187  B188  B189  B190  B191  B192B193  B194  B195  B196  B197  B198  B199  B200  B201  B202  B203  B204B205  B206  B207  B208  B209  B210  B211  B212  B213  B214  B215  B216B217  B218  B219  B220  B221  B222  B223  B224  B225  B226  B227  B228B229  B230  B231  B232  B233  B234  B235  B236  B237  B238  B239  B240B241  B242  B243  B244  B245  B246  B247  B248  B249  B250  B251  B252B253  B254  B255  B256  B257  B258  B259  B260  B261  B262  B263  B264B265  B266  B267  B268  B269  B270  B271  B272  B273  B274  B275  B276B277  B278  B279  B280  B281  B282  B283  B284  B285  B286  B287  B288B289  B290  B291  B292  B293  B294  B295  B296  B297  B298  B299  B300B301  B302  B303  B304  B305  B306  B307  B308  B309  B310  B311  B312B313  B314  B315  B316  B317  B318  B319  B320  B321  B322  B323  B324B325  B326  B327  B328  B329  B330  B331  B332  B333  B334  B335  B336B337  B338  B339  B340  B341  B342  B343  B344  B345  B346  B347  B348B349  B350  B351  B352  B353  B354  B355  B356  B357  B358  B359  B360B361  B362  B363  B364  B365  B366  B367  B368  B369  B370  B371  B372B373  B374  B375  B376  B377  B378  B379  B380  B381  B382  B383  B384B385  B386  B387  B388  B389  B390  B391  B392  B393  B394  B395  B396Q1   Q1   Q1  Q1   Q1    Q1   Q1    Q1   Q1   Q1   Q1   Q1B397  B398  B399  B400  B401   B402   B403   B404  B405  B406   B407  B408B409  B410  B411  B412  B413   B414   B415   B416  B417  B418   B419  B420B421  B422  B423  B424  B425   B426   B427   B428  B429  B430   B431  B432B433  B434  B435  B436  B437   B438   B439   B440  B441  B442   B443  B444B445  B446  B447  B448  B449   B450   B451   B452  B453  B454   B455  B456B457  B458  B459  B460  B461   B462   B463   B464  B465  B466   B467  B468B469  B470  B471  B472  B473   B474   B475   B476  B477  B478   B479  B480B481  B482  B483  B484  B485   B486   B487   B488  B489  B490   B491  B492B493  B494  B495  B496  B497   B498   B499   B500  B501  B502   B503  B504B505  B506  B507  B508  B509   B510   B511   B512  B513  B514   B515  B516B517  B518  B519  B520  B521   B522   B523   B524  B525  B526   B527  B528B529  B530  B531  B532  B533   B534   B535   B536  B537  B538   B539  B540B541  B542  B543  B544  B545   B546   B547   B548  B549  B550   B551  B552B553  B554  B555  B556  B557   B558   B559   B560  B561  B562   B563  B564B565  B566  B567  B568  B569   B570   B571   B572  B573  B574   B575  B576B577  B578  B579  B580  B581   B582   B583   B584  B585  B586   B587  B588B589  B590  B591  B592  B593   B594   B595   B596  B597  B598   B599  B600B601  B602  B603  B604  B605   B606   B607   B608  B609  B610   B611  B612B613  B614  B615  B616  B617   B618   B619   B620  B621  B622   B623  B624B625  B626  B627  B628  B629   B630   B631   B632  B633  B634   B635  B636B637  B638  B639  B640  B641   B642   B643   B644  B645  B646   B647  B648B649  B650  B651  B652  B653   B654   B655   B656  B657  B658   B659  B660B661  B662  B663  B664  B665   B666   B667   B668  B669  B670   B671  B672B773  B774  B775  B776  B777   B778   B779   B780  B781  B782   B783  B784B785  B786  B787  B788  B789   B790   B791   B792  B793  B794   B795  B796B797  B798  B799  B800  B801   B802   B803   B804  B805  B806   B807  B808B809  B810  B811  B812  B813   B814   B815   B816  B817  B818   B819  B820B821  B822  B823  B824  B825   B826   B827   B828  B829  B830   B831  B832B833  B834  B835  B836  B837   B838   B839   B840  B841  B842   B843  B844B845  B846  B847  B848  B849   B850   B851   B852  B853  B854   B855  B856B857  B858  B859  B860  B861   B862   B863   B864  B865  B866   B867  B868B869  B870  B871  B872  B873   B874   B875   B876  B877  B878   B879  B880B881  B882  B883  B884  B885   B886   B887   B888  B889  B890   B891  B892Q1   Q1   Q1  Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B893  B894  B895  B896  B897  B898  B899  B900  B901  B902  B903  B904B905  B906  B907  B908  B909  B910  B911  B912  B913  B914  B915  B916B917  B918  B919  B920  B921  B922  B923  B924  B925  B926  B927  B928B929  B930  B931  B932  B933  B934  B935  B936  B937  B938  B939  B940B941  B942  B943  B944  B945  B946  B947  B948  B949  B950  B951  B952B953  B954  B955  B956  B957  B958  B959  B960  B961  B962  B963  B964B965  B966  B967  B968  B969  B970  B971  B972  B973  B974  B975  B976B977  B978  B979  B980  B981  B982  B983  B984  B985  B986  B987  B988B989  B990  B991  B992  B993  B994  B995  B996  B997  B998  B999  B1000B1001 B1002 B1003 B1004 B1005 B1006 B1007 B1008 B1009 B1010 B1011 B1012B1013 B1014 B1015 B1016 B1017 B1018 B1019 B1020 B1021 B1022 B1023 B1024B1025 B1026 B1027 B1028 B1029 B1030 B1031 B1032 B1033 B1034 B1035 B1036B1037 B1038 B1039 B1040 B1041 B1042 B1043 B1044 B1045 B1046 B1047 B1048B1049 B1050 B1051 B1052 B1053 B1054 B1055 B1056 B1057 B1058 B1059 B1060B1061 B1062 B1063 B1064 B1065 B1066 B1067 B1068 B1069 B1070 B1071 B1072B1073 B1074 B1075 B1076 B1077 B1078 B1079 B1080 B1081 B1082 B1083 B1084B1085 B1086 B1087 B1088 B1089 B1090 B1091 B1092 B1093 B1094 B1095 B1096B1097 B1098 B1099 B1100 B1101 B1102 B1103 B1104 B1105 B1106 B1107 B1108B1109 B1110 B1111 B1112 B1113 B1114 B1115 B1116 B1117 B1118 B1119 B1120B1121 B1122 B1123 B1124 B1125 B1126 B1127 B1128 B1129 B1130 B1131 B1132B1133 B1134 B1135 B1136 B1137 B1138 B1139 B1140 B1141 B1142 B1143 B1144B1145 B1146 B1147 B1148 B1149 B1150 B1151 B1152 B1153 B1154 B1155 B1156B1157 B1158 B1159 B1160 B1161 B1162 B1163 B1164 B1165 B1166 B1167 B1168B1169 B1170 B1171 B1172 B1173 B1174 B1175 B1176 B1177 B1178 B1179 B1180B1181 B1182 B1183 B1184 B1185 B1186 B1187 B1188 B1189 B1190 B1191 B1192B1193 B1194 B1195 B1196 B1197 B1198 B1199 B1200 B1201 B1202 B1203 B1204B1205 B1206 B1207 B1208 B1209 B1210 B1211 B1212 B1213 B1214 B1215 B1216B1217表16:式Im化合物(P为0或1):Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B1    B2    B3    B4    B5    B6    B7    B8    B9    B10   B11   B12B13   B14   B15   B16   B17   B18   B19   B20   B21   B22   B23    -B25   B26   B27   B28   B29   B30   B31   B32   B33   B34   B35   B36B37   B38   B39   B40   B41   B42   B43   B44   B45   B46   B47   B48B49   B50   B51   B52   B53   B54   B55   B56   B57   B58   B59   B60B61   B62   B63   B64   B65   B66   B67   B68   B69   B70   B71   B72B73   B74   B75   B76   B77   B78   B79   B80   B81   B82   B83   B84B85   B86   B87   B88   B89   B90   B91   B92   B93   B94   B95   B96B97   B98   B99   B100  B101  B102  B103  B104  B105  B106  B107  B108B109  B110  B111  B112  B113  B114  B115  B116  B117  B118  B119  B120B121  B122  B123  B124  B125  B126  B127  B128  B129  B130  B131  B132B133  B134  B135  B136  B137  B138  B139  B140  B141  B142  B143  B144B145  B146  B147  B148  B149  B150  B151  B152  B153  B154  B155  B156B157  B158  B159  B160  B161  B162  B163  B164  B165  B166  B167  B168B169  B170  B171  B172  B173  B174  B175  B176  B177  B178  B179  B180B181  B182  B183  B184  B185  B186  B187  B188  B189  B190  B191  B192B193  B194  B195  B196  B197  B198  B199  B200  B201  B202  B203  B204B205  B206  B207  B208  B209  B210  B211  B212  B213  B214  B215  B216B217  B218  B219  B220  B221  B222  B223  B224  B225  B226  B227  B228B229  B230  B231  B232  B233  B234  B235  B236  B237  B238  B239  B240B241  B242  B243  B244  B245  B246  B247  B248  B249  B250  B251  B252B253  B254  B255  B256  B257  B258  B259  B260  B261  B262  B263  B264B265  B266  B267  B268  B269  B270  B271  B272  B273  B274  B275  B276B277  B278  B279  B280  B281  B282  B283  B284  B285  B286  B287  B288B289  B290  B291  B292  B293  B294  B295  B296  B297  B298  B299  B300B301  B302  B303  B304  B305  B306  B307  B308  B309  B310  B311  B312B313  B314  B315  B316  B317  B318  B319  B320  B321  B322  B323  B324Q1   Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1  Q1   Q1B325  B326  B327  B328  B329  B330  B331  B332  B333  B334  B335  B336B337  B338  B339  B340  B341  B342  B343  B344  B345  B346  B347  B348B349  B350  B351  B352  B353  B354  B355  B356  B357  B358  B359  B360B361  B362  B363  B364  B365  B366  B367  B368  B369  B370  B371  B372B373  B374  B375  B376  B377  B378  B379  B380  B381  B382  B383  B384B385  B386  B387  B388  B389  B390  B391  B392  B393  B394  B395  B396B397  B398  B399  B400  B401  B402  B403  B404  B405  B406  B407  B408B409  B410  B411  B412  B413  B414  B415  B416  B417  B418  B419  B420B421  B422  B423  B424  B425  B426  B427  B428  B429  B430  B431  B432B433  B434  B435  B436  B437  B438  B439  B440  B441  B442  B443  B444B445  B446  B447  B448  B449  B450  B451  B452  B453  B454  B455  B456B457  B458  B459  B460  B461  B462  B463  B464  B465  B466  B467  B468B469  B470  B471  B472  B473  B474  B475  B476  B477  B478  B479  B480B481  B482  B483  B484  B485  B486  B487  B488  B489  B490  B491  B492B493  B494  B495  B496  B497  B498  B499  B500  B501  B502  B503  B504B505  B506  B507  B508  B509  B510  B511  B512  B513  B514  B515  B516B517  B518  B519  B520  B521  B522  B523  B524  B525  B526  B527  B528B529  B530  B531  B532  B533  B534  B535  B536  B537  B538  B539  B540B541  B542  B543  B544  B545  B546  B547  B548  B549  B550  B551  B552B553  B554  B555  B556  B557  B558  B559  B560  B561  B562  B563  B564B565  B566  B567  B568  B569  B570  B571  B572  B573  B574  B575  B576B577  B578  B579  B580  B581  B582  B583  B584  B585  B586  B587  B588B589  B590  B591  B592  B593  B594  B595  B596  B597  B598  B599  B600B601  B602  B603  B604  B605  B606  B607  B608  B609  B610  B611  B612B613  B614  B615  B616  B617  B618  B619  B620  B621  B622  B623  B624B625  B626  B627  B628  B629  B630  B631  B632  B633  B634  B635  B636B637  B638  B639  B640  B641  B642  B643  B644  B645  B646  B647  B648B649  B650  B651  B652  B653  B654  B655  B656  B657  B658  B659  B660B661  B662  B663  B664  B665  B666  B667  B668  B669  B670  B671  B672B773  B774  B775  B776  B777  B778  B779  B780  B781  B782  B783  B784B785  B786  B787  B788  B789  B790  B791  B792  B793  B794  B795  B796B797  B798  B799  B800  B801  B802  B803  B804  B805  B806  B807  B808B809  B810  B811  B812  B813  B814  B815  B816  B817  B818  B819  B820Q1   Q1   Q1   Q1  Q1   Q1  Q1   Q1   Q1   Q1  Q1   Q1B821  B822  B823  B824  B825  B826  B827  B828  B829  B830  B831  B832B833  B834  B835  B836  B837  B838  B839  B840  B841  B842  B843  B844B845  B846  B847  B848  B849  B850  B851  B852  B853  B854  B855  B856B857  B858  B859  B860  B861  B862  B863  B864  B865  B866  B867  B868B869  B870  B871  B872  B873  B874  B875  B876  B877  B878  B879  B880B881  B882  B883  B884  B885  B886  B887  B888  B889  B890  B891  B892B893  B894  B895  B896  B897  B898  B899  B900  B901  B902  B903  B904B905  B906  B907  B908  B909  B910  B911  B912  B913  B914  B915  B916B917  B918  B919  B920  B921  B922  B923  B924  B925  B926  B927  B928B929  B930  B931  B932  B933  B934  B935  B936  B937  B938  B939  B940B941  B942  B943  B944  B945  B946  B947  B948  B949  B950  B951  B952B953  B954  B955  B956  B957  B958  B959  B960  B961  B962  B963  B964B965  B966  B967  B968  B969  B970  B971  B972  B973  B974  B975  B976B977  B978  B979  B980  B981  B982  B983  B984  B985  B986  B987  B988B989  B990  B991  B992  B993  B994  B995  B996  B997  B998  B999 B1000B1001 B1002 B1003 B1004 B1005 B1006 B1007 B1008 B1009 B1010 B1011 B1012B1013 B1014 B1015 B1016 B1017 B1018 B1019 B1020 B1021 B1022 B1023 B1024B1025 B1026 B1027 B1028 B1029 B1030 B1031 B1032 B1033 B1034 B1035 B1036B1037 B1038 B1039 B1040 B1041 B1042 B1043 B1044 B1045 B1046 B1047 B1048B1049 B1050 B1051 B1052 B1053 B1054 B1055 B1056 B1057 B1058 B1059 B1060B1061 B1062 B1063 B1064 B1065 B1066 B1067 B1068 B1069 B1070 B1071 B1072B1073 B1074 B1075 B1076 B1077 B1078 B1079 B1080 B1081 B1082 B1083 B1084B1085 B1086 B1087 B1088 B1089 B1090 B1091 B1092 B1093 B1094 B1095 B1096B1097 B1098 B1099 B1100 B1101 B1102 B1103 B1104 B1105 B1106 B1107 B1108B1109 B1110 B1111 B1112 B1113 B1114 B1115 B1116 B1117 B1118 B1119 B1120B1121 B1122 B1123 B1124 B1125 B1126 B1127 B1128 B1129 B1130 B1131 B1132B1133 B1134 B1135 B1136 B1137 B1138 B1139 B1140 B1141 B1142 B1143 B1144B1145 B1146 B1147 B1148 B1149 B1150 B1151 B1152 B1153 B1154 B1155 B1156B1157 B1158 B1159 B1160 B1161 B1162 B1163 B1164 B1165 B1166 B1167 B1168B1169 B1170 B1171 B1172 B1173 B1174 B1175 B1176 B1177 B1178 B1179 B1180B1181 B1182 B1183 B1184 B1185 B1186 B1187 B1188 B1189 B1190 B1191 B1192B1193 B1194 B1195 B1196 B1197 B1198 B1199 B1200 B1201 B1202 B1203 B1204B1205 B1206 B1207 B1208 B1209 B1210 B1211 B1212 B1213 B1214 B1215 B1216Q1   Q1   Q1   Q1  Q1   Q1   Q1   Q1   Q1  Q1   Q1  Q1B1217表17:式In化合物(P为0或1):Q1      Q1     Q1      Q1    Q1     Q1     Q1     Q1     Q1     Q1    Q1     Q1B1       B2      B3       B4      B5      B6       B7      B8      B9      B10     B11      B12B13      B14     B15      B16     B17     B18      B19     B20     B21     B22     B23       -B25      B26     B27      B28     B29     B30      B31     B32     B33     B34     B35      B36B37      B38     B39      B40     B41     B42      B43     B44     B45     B46     B47      B48B49      B50     B51      B52     B53     B54      B55     B56     B57     B58     B59      B60B61      B62     B63      B64     B65     B66      B67     B68     B69     B70     B71      B72B73      B74     B75      B76     B77     B78      B79     B80     B81     B82     B83      B84B85      B86     B87      B88     B89     B90      B91     B92     B93     B94     B95      B96B97      B98     B99      B100    B101    B102     B103    B104    B105    B106    B107     B108B109     B110    B111     B112    B113    B114     B115    B116    B117    B118    B119     B120B121     B122    B123     B124    B125    B126     B127    B128    B129    B130    B131     B132B133     B134    B135     B136    B137    B138     B139    B140    B141    B142    B143     B144B145     B146    B147     B148    B149    B150     B151    B152    B153    B154    B155     B156B157     B158    B159     B160    B161    B162     B163    B164    B165    B166    B167     B168B169     B170    B171     B172    B173    B174     B175    B176    B177    B178    B179     B180B181     B182    B183     B184    B185    B186     B187    B188    B189    B190    B191     B192B193     B194    B195     B196    B197    B198     B199    B200    B201    B202    B203     B204B205     B206    B207     B208    B209    B210     B211    B212    B213    B214    B215     B216B217     B218    B219     B220    B221    B222     B223    B224    B225    B226    B227     B228B229     B230    B231     B232    B233    B234     B235    B236    B237    B238    B239     B240B241     B242    B243     B244    B245    B246     B247    B248    B249    B250    B251     B252B253     B254    B255     B256    B257    B258     B259    B260    B261    B262    B263     B264Q1   Q1   Q1   Q1  Q1   Q1   Q1   Q1  Q1   Q1   Q1   Q1B265  B266  B267  B268  B269  B270  B271  B272  B273  B274  B275  B276B277  B278  B279  B280  B281  B282  B283  B284  B285  B286  B287  B288B289  B290  B291  B292  B293  B294  B295  B296  B297  B298  B299  B300B301  B302  B303  B304  B305  B306  B307  B308  B309  B310  B311  B312B313  B314  B315  B316  B317  B318  B319  B320  B321  B322  B323  B324B325  B326  B327  B328  B329  B330  B331  B332  B333  B334  B335  B336B337  B338  B339  B340  B341  B342  B343  B344  B345  B346  B347  B348B349  B350  B351  B352  B353  B354  B355  B356  B357  B358  B359  B360B361  B362  B363  B364  B365  B366  B367  B368  B369  B370  B371  B372B373  B374  B375  B376  B377  B378  B379  B380  B381  B382  B383  B384B385  B386  B387  B388  B389  B390  B391  B392  B393  B394  B395  B396B397  B398  B399  B400  B401  B402  B403  B404  B405  B406  B407  B408B409  B410  B411  B412  B413  B414  B415  B416  B417  B418  B419  B420B421  B422  B423  B424  B425  B426  B427  B428  B429  B430  B431  B432B433  B434  B435  B436  B437  B438  B439  B440  B441  B442  B443  B444B445  B446  B447  B448  B449  B450  B451  B452  B453  B454  B455  B456B457  B458  B459  B460  B461  B462  B463  B464  B465  B466  B467  B468B469  B470  B471  B472  B473  B474  B475  B476  B477  B478  B479  B480B481  B482  B483  B484  B485  B486  B487  B488  B489  B490  B491  B492B493  B494  B495  B496  B497  B498  B499  B500  B501  B502  B503  B504B505  B506  B507  B508  B509  B510  B511  B512  B513  B514  B515  B516B517  B518  B519  B520  B521  B522  B523  B524  B525  B526  B527  B528B529  B530  B531  B532  B533  B534  B535  B536  B537  B538  B539  B540B541  B542  B543  B544  B545  B546  B547  B548  B549  B550  B551  B552B553  B554  B555  B556  B557  B558  B559  B560  B561  B562  B563  B564B565  B566  B567  B568  B569  B570  B571  B572  B573  B574  B575  B576B577  B578  B579  B580  B581  B582  B583  B584  B585  B586  B587  B588B589  B590  B591  B592  B593  B594  B595  B596  B597  B598  B599  B600B601  B602  B603  B604  B605  B606  B607  B608  B609  B610  B611  B612B613  B614  B615  B616  B617  B618  B619  B620  B621  B622  B623  B624B625  B626  B627  B628  B629  B630  B631  B632  B633  B634  B635  B636B637  B638  B639  B640  B641  B642  B643  B644  B645  B646  B647  B648B649  B650  B651  B652  B653  B654  B655  B656  B657  B658  B659  B660Q1   Q1  Q1   Q1   Q1  Q1   Q1   Q1   Q1   Q1  Q1   Q1B661  B662  B663  B664  B665  B666  B667  B668  B669  B670  B671  B672B773  B774  B775  B776  B777  B778  B779  B780  B781  B782  B783  B784B785  B786  B787  B788  B789  B790  B791  B792  B793  B794  B795  B796B797  B798  B799  B800  B801  B802  B803  B804  B805  B806  B807  B808B809  B810  B811  B812  B813  B814  B815  B816  B817  B818  B819  B820B821  B822  B823  B824  B825  B826  B827  B828  B829  B830  B831  B832B833  B834  B835  B836  B837  B838  B839  B840  B841  B842  B843  B844B845  B846  B847  B848  B849  B850  B851  B852  B853  B854  B855  B856B857  B858  B859  B860  B861  B862  B863  B864  B865  B866  B867  B868B869  B870  B871  B872  B873  B874  B875  B876  B877  B878  B879  B880B881  B882  B883  B884  B885  B886  B887  B888  B889  B890  B891  B892B893  B894  B895  B896  B897  B898  B899  B900  B901  B902  B903  B904B905  B906  B907  B908  B909  B910  B911  B912  B913  B914  B915  B916B917  B918  B919  B920  B921  B922  B923  B924  B925  B926  B927  B928B929  B930  B931  B932  B933  B934  B935  B936  B937  B938  B939  B940B941  B942  B943  B944  B945  B946  B947  B948  B949  B950  B951  B952B953  B954  B955  B956  B957  B958  B959  B960  B961  B962  B963  B964B965  B966  B967  B968  B969  B970  B971  B972  B973  B974  B975  B976B977  B978  B979  B980  B981  B982  B983  B984  B985  B986  B987  B988B989  B990  B991  B992  B993  B994  B995  B996  B997  B998  B999  B1000B1001 B1002 B1003 B1004 B1005 B1006 B1007 B1008 B1009 B1010 B1011 B1012B1013 B1014 B1015 B1016 B1017 B1018 B1019 B1020 B1021 B1022 B1023 B1024B1025 B1026 B1027 B1028 B1029 B1030 B1031 B1032 B1033 B1034 B1035 B1036B1037 B1038 B1039 B1040 B1041 B1042 B1043 B1044 B1045 B1046 B1047 B1048B1049 B1050 B1051 B1052 B1053 B1054 B1055 B1056 B1057 B1058 B1059 B1060B1061 B1062 B1063 B1064 B1065 B1066 B1067 B1068 B1069 B1070 B1071 B1072B1073 B1074 B1075 B1076 B1077 B1078 B1079 B1080 B1081 B1082 B1083 B1084B1085 B1086 B1087 B1088 B1089 B1090 B1091 B1092 B1093 B1094 B1095 B1096B1097 B1098 B1099 B1100 B1101 B1102 B1103 B1104 B1105 B1106 B1107 B1108B1109 B1110 B1111 B1112 B1113 B1114 B1115 B1116 B1117 B1118 B1119 B1120B1121 B1122 B1123 B1124 B1125 B1126 B1127 B1128 B1129 B1130 B1131 B1132B1133 B1134 B1135 B1136 B1137 B1138 B1139 B1140 B1141 B1142 B1143 B1144B1145 B1146 B1147 B1148 B1149 B1150 B1151 B1152 B1153 B1154 B1155 B1156Q1   Q1   Q1   Q1   Q1  Q1   Q1   Q1   Q1  Q1   Q1  Q1B1157 B1158 B1159 B1160 B1161 B1162 B1163 B1164 B1165 B1166 B1167 B1168B1169 B1170 B1171 B1172 B1173 B1174 B1175 B1176 B1177 B1178 B1179 B1180B1181 B1182 B1183 B1184 B1185 B1186 B1187 B1188 B1189 B1190 B1191 B1192B1193 B1194 B1195 B1196 B1197 B1198 B1199 B1200 B1201 B1202 B1203 B1204B1205 B1206 B1207 B1208 B1209 B1210 B1211 B1212 B1213 B1214 B1215 B1216B1217表18:式I0化合物(P为0或1):Q2  Q2   Q2   Q2  Q2 Q2  Q2  Q2 Q2  Q2  Q2  Q2C1   C2    C3    C4   C5   C6   C7   C8   C9    C10  C11  C12C13  C14   C15   C16  C17  C18  C19  C20  C21   C22  C23  C24C25  C26   C27   C28  C29  C30  C31  C32  C33   C34  C35  C36C37  C38   C39   C40  C41  C42  C43  C44  C45   C46  C47  C48C49  C50   C51   C52  C53  C54  C55  C56  C57   C58  C59  C60C61  C62   C63   C64  C65  C66  C67  C68  C69   C70  C71  C72C73  C74   C75   C76  C77  C78  C79  C80  C81   C82  C83  C84C85  C86   C87   C88  C89  C90  C91  C92  C93   C94  C95  C96C97  C98   C99   C100 C101 C102 C103 C104 C105  C106 C107 C108C109 C110  C111  C112 C113 C114 C115 C116 C117  C118 C119 C120C121 C122  C123  C124 C125 C126 C127 C128 C129  C130 C131 C132C133 C134  C135  C136 C137 C138 C139 C140 C141  C142 C143 C144C145 C146  C147  C148 C149 C150 C151表19:式1q化合物(P为0或1):
Figure A9981578602391
Q2   Q2  Q2 Q2  Q2  Q2  Q2  Q2  Q2  Q2  Q2  Q2C1    C2   C3   C4    C5    C6  C7    C8   C9   C10  C11  C12C13   C14  C15  C16   C17  C18  C19   C20  C21  C22  C23  C24C25   C26  C27  C28   C29  C30  C31   C32  C33  C34  C35  C36C37   C38  C39  C40   C41  C42  C43   C44  C45  C46  C47  C48C49   C50  C51  C52   C53  C54  C55   C56  C57  C58  C59  C60C61   C62  C63  C64   C65  C66  C67   C68  C69  C70  C71  C72C73   C74  C75  C76   C77  C78  C79   C80  C81  C82  C83  C84C85   C86  C87  C88   C89  C90  C91   C92  C93  C94  C95  C96C97   C98  C99  C100  C101 C102 C103  C104 C105 C106 C107 C108C109  C110 C111 C112  C113 C114 C115  C116 C117 C118 C119 C120C121  C122 C123 C124  C125 C126 C127  C128 C129 C130 C131 C132C133  C134 C135 C136  C137 C138 C139  C140 C141 C142 C143 C144C145  C146 C147 C148  C149 C150 C151表20:式Ir化合物(P为0或1):Q3  Q3  Q3 Q3  Q3  Q3  Q3  Q3  Q3 Q3  Q3 Q3D1   D2   D3   D4   D5   D6   D7   D8   D9   D10  D11  D12D13  D14  D15  D16  D17  D18  D19  D20  D21  D22  D23  D24D25  D26  D27  D28  D29  D30  D31  D32  D33  D34  D35  D36D37  D38  D39  D40  D41  D42  D43  D44  D45  D46  D47  D48Q3  Q3  Q3  Q3  Q3  Q3  Q3  Q3  Q3  Q3  Q3  Q3D49  D50  D51  D52  D53  D54  D55  D56  D57  D58  D59  D60D61  D62  D63  D64  D65  D66  D67  D68  D69  D70  D71  D72D73  D74  D75  D76  D77  D78  D79  D80  D81  D82  D83  D84D85  D86  D87  D88  D89  D90  D91  D92  D93  D94  D95  D96D97  D98  D99  D100 D101 D102 D103 D104 D105 D106 D107 D108D109 D110 D111 D112 D113 D114 D115 D116 D117 D118 D119 D120D121 D122 D123 D124 D125 D126 D127 D128 D129 D130 D131 D132D133 D134 D135 D136 D137 D138 D139 D140表21:式Is化合物(P为0或1):
Figure A9981578602401
Q3  Q3  Q3  Q3 Q3 Q3 Q3  Q3  Q3  Q3  Q3  Q3D1   D2   D3   D4   D5   D6   D7   D8   D9   D10  D11  D12D13  D14  D15  D16  D17  D18  D19  D20  D21  D22  D23  D24D25  D26  D27  D28  D29  D30  D31  D32  D33  D34  D35  D36D37  D38  D39  D40  D41  D42  D43  D44  D45  D46  D47  D48D49  D50  D51  D52  D53  D54  D55  D56  D57  D58  D59  D60D61  D62  D63  D64  D65  D66  D67  D68  D69  D70  D71  D72D73  D74  D75  D76  D77  D78  D79  D80  D81  D82  D83  D84D85  D86  D87  D88  D89  D90  D91  D92  D93  D94  D95  D96D97  D98  D99  D100 D101 D102 D103 D104 D105 D106 D107 D108D109 D110 D111 D112 D113 D114 D115 D116 D117 D118 D119 D120D121 D122 D123 D124 D125 D126 D127 D128 D129 D130 D131 D132D133 D134 D135 D136 D137 D138 D139 D140
Figure A9981578602411
Q4 Q4 Q4 Q4Q4 Q4 Q4 Q4Q4 Q4 Q4Q4 Q4 Q4Q4E1  E2  E3  E4  E5  E6  E7  E8  E9  E10 E11 E12 E13 E14 E15E16 E17 E18 E19 E20 E21 E22 E23 E24 E25 E26 E27 E28 E29 E30表23:式Iu化合物(P为0或1):
Figure A9981578602412
Q4Q4 Q4 Q4 Q4 Q4Q4 Q4 Q4 Q4Q4 Q4 Q4Q4 Q4E1  E2  E3  E4  E5  E6  E7  E8  E9  E10 E11 E12 E13 E14 E15E16 E17 E18 E19 E20 E21 E22 E23 E24 E25 E26 E27 E28 E29 E30表24:式Iv化合物(P为0或1):Q5 Q5 Q5Q5 Q5Q5F1  F2  F3  F4  F5  F6表25:式Iw化合物(P为0或1):
Figure A9981578602421
Q5 Q5 Q5 Q5 Q5 Q5F1   F2  F3  F4  F5  F6表26.中间体的物理数据熔点℃化合物 物理数据   化合物       物理数据A17    99-100     A1025         结晶A7     105-106    A1206         94-95A9     73-74      A1022         油A6     148-150    A1203         结晶A26    143-144    A21          无定形A34    170-171    A1023        110-111A1026  结晶       A1085        188-191A1304  结晶       A1088        157-158A1301  结晶       A1092        结晶A1018  110-111    A1095        136-138A1     195-197    A1096        194-196A2     150-151    A124         135-136A15    164-166    A31          209-210A27    107-108    H-B1057      166-167A29    173-174    H-B1058      结晶A32    145-146    H-B1061      结晶A30    178-181    H-B1063      结晶A4     143-144    H-B1065      油A3     148-149    H-B1066      150-152A10    166-167    H-B1067      122-123A8     123-124    H-B1069      117-118化合物  物理数据        化合物    物理数据A5      81-82           H-B1070    结晶A154    108-110         H-C1       116-118A64     134-135         H-C24      172-175A94     134-135         A1205      结晶A531    结晶            H-D113     油A1045   结晶            H-F5       油A1322   结晶            H-E16      145-148A184    146-147         A1088      157-158A358    155-156         A1103      152-153表27.上表中所示式I化合物的物理数据熔点℃化合物序号    m.p.         物理状态    化合物序号      m.p.        物理状态A2-B1        90-92            结晶        A34-B1      53-54         结晶A2-B1082       -              树脂        A9-B1         -           油状物A2-B1083       -              树脂        A184-B1     98-99         结晶A2-B90         -              树脂        A184-B24   101-102        结晶A2-B68      120-121           结晶        A7-B24        -           油状物A2-B24       75-76            结晶        A3-B24        -           油状物A7-B1          -              油状物      A34-B24     51-52         结晶A2-B73         -              树脂        A2-B1091      -           油状物A2-B75         -              无定形      A2-B1 092     -           油状物A2-B95      106-107           结晶        A8-B24      52-53         结晶A2-B93       95-96            结晶        A18-B24       -           油状物A8-B1        97-98            结晶        A2-B552       -           树脂A2-B925        -              油状物      A2-C1 52      -           油状物A3-B1        42-44            结晶        A2-B69        -           树脂A94-B1       57-58            结晶        A2-D36        -           树脂A2-B1057       -              无定形      A2-B618       -           树脂A2-B1063       -              油状物      A2-B49        -           树脂A2-B1061       -              油状物      A2-D71        -           树脂A2-B133      58-60            结晶        A2-B1093      -           树脂化合物序号    m.p.        物理状态    化合物序号     m.p.      物理状态A2-B1058     89-91        结晶         A2-B26         -        油状物A64-B24      80-82        结晶         A2-B33         -        树脂A64-B1       49-51        结晶         A2-B34         -        腊状物A2-B1089                  油状物       A2-B35         -        腊状物A2-B31       151-153      结晶         A2-B1087       -        粘性物A2-B1090     139-140      结晶         A2-B1094       -        粘性物A154-B1       94-95       结晶         A2-B1088    108-109     结晶A2-B46(顺式)  61-62       结晶         A531-B24       -        粘性物A2-B46(反式)  83-84       结晶         A2-B1099     94-96      结晶A2-B91          -         树脂         A2-B1095       -        粘性物A2-B2           -         树脂         A2-B1097       -        油状物A2-B29        87-88       结晶         A2-B1098     92-93      结晶A2-B1066        -         粘性物       A2-C147        -        树脂A2-B25          -         油状物       A2-B70         -        树脂A2-B1067        -         树脂         A2-B49         -        树脂A2-B1069        -         油状物       A2-C1          -        油状物A2-B1068        -         粘性物       A2-B1096       -        树脂A2-B1070        -         粘性物       A2-B1085    176-177     结晶A2-B5           -         树脂         A1022-B24      -        油状物A2-C149         -         树脂         A2-C47      107-110     结晶A2-C146         -         油状物       A2-B1100    128-130     结晶A2-B112         -         树脂         A8-B2        70-71      结晶A2-D140         -         油状物       A8-B1064       -        树脂A2-B354      139-140      结晶         A2-B45         -        树脂A2-E16          -         固体         A2-B10         -        粘性物A6-B1        123-124      结晶         A8-B133      68-69      结晶A6-B24          -         油状物       A8-B1101    113-114     结晶A1322-B24       -         油状物       A8-B1106       -        油状物A2-B1101     124-125      结晶         A2-D111(反式)  -        油状物A2-B156         -         油状物       A2-D111(顺式)  -        树脂A2-B144         -         树脂         A8-D111(反式)  -        油状物A2-B145         -         树脂         A8-D109      62-62      无定形A2-B134         -         树脂         A8-B35         -        油状物化合物序号             m.p.     物理状态    化合物序号        m.p.       物理状态A1210-B354             220      结晶         A1023-B2          -         树脂A2-C2                   -       油状物       A1023-B354      95-97       结晶A358-B1                 -       油状物       A15-B354          -         树脂A2-D36                  -       树脂         A8-B354           -         油状物A1208-B354              -       油状物       A8-B1067          -         油状物A2-D113(lsom.A)         -       油状物       A8-C146           -         油状物A2-D113(lsom.B)         -       油状物       A8-C1             -         油状物A2-D114(lsom.A)      159-160    结晶         A94-B34        108-110      结晶A2-D115                 -       无定形       A94-B35         82-84       结晶A1025-B354              -       粘性物       A1210-B354        -         无定形A2-B1102             124-125    结晶         A2-B1105         119        结晶A2-B1104             165-167    结晶         A1099-B1107       -         无定形A1210-B1             117-119    结晶         A2-B1123          -         树脂A8-B34                  -       油状物       A8-B1123          -         树脂A8-B1103                -       油状物       A2-B1138          -         树脂A8-B1063              90-92     结晶         A124-B1         60-65       结晶A8-B29                  -       油状物       A1170-B1        106-107     结晶A2-C24                  -       油状物       A124-B34           -        油状物A8-B552                 -       油状物       A124-B35           -        油状物A8-B156                 -       树脂         A94-B2           53-57      结晶A1210-B1105          145-146    玻璃状       A2-B1174           -        结晶无定形物A1206-B354              -       无定形       A2-B1213        133-134     结晶A8-B134                 -       油状物       A3-B1213           -        油状物A8-D36                  -       油状物       A4-B1213           -        油状物A8-B1213              71-72     结晶         A2-B1214           -        树脂A8-F5                   -       树脂         A2-F5              -        树脂A1029-B1105          94.5-95    结晶         A2-D109            -        油状物生物实施例实施例B1:植物发芽前的除草作用(芽前作用)
将单子叶和双子叶试验植物播种在置于塑料盆内的标准土壤中。播种后,随即喷施试验物质的水悬液(按照WO97/34485所述方法由25%浓度的可湿性粉剂(实施例F3,b)制备)或乳液(用25%浓度乳油(实施例F1,c)制备),施用量为2 kg活性组份/公顷或250g活性组分/公顷(500升水/公顷)。然后使试验植物在温室中于最佳条件下生长。三周测试期后,分9个等级评价试验结果(1=全部损伤,9=没有作用)。1-4级(特别是1-3级)表示具有好至很好的除草作用。表B1a:芽前作用:化合物      g/ha   莎草    番薯  狗尾草  白芥  茄   繁缕A2-B1       2000    2        2    1        2    2    1A2-B1082    2000    2        2    2        2    1    2A2-B1083    2000    2        3    3        4    2    3A2-B90      2000    1        1    1        1    1    1A2-B68      2000    1        2    1        2    1    2A2-B24      2000    1        1    1        2    1    1A2-B73      2000    3        4    2        2    2    2A2-B75      2000    2        3    2        2    1    2A2-B95      2000    2        4    2        2    1    2A2-B93      2000    2        4    2        2    1    2A3-B1       2000    2        2    4        2    3    2A94-B1      2000    1        2    2        1    1    2A2-B1063    2000    1        2    1        2    1    2A2-B1061    2000    3        3    2        2    1    2A2-B133     2000    1        2    2        2    1    2A64-B24     2000    4        4    2        2    1    2A2-B1089    2000    1        2    2        2    1    2A2-B31      2000    2        3    4        2    1    2A2-B46(cis) 2000    1        2    1        2    1    2化合物          g/ha  莎草 番薯 狗尾草白芥 茄   繁缕A2-B46(反式)    2000    1    2    1    2    1    2A2-B91          2000    1    2    1    2    1    2A2-B2           2000    1    1    1    1    1    2A2-B25          2000    2    3    2    2    1    2A2-B1067        2000    2    3    2    2    3    3A2-B1068        2000    2    2    2    2    1    2A2-B1070        2000    2    3    3    2    2    2A2-C146         2000    1    2    2    2    1    2A2-B354         2000    1    1    1    1    1    2A34-B1          2000    1    2    2    2    2    3A9-B1           2000    2    1    2    1    1    2A184-B1         2000    2    4    2    2    1    2A184-B24        2000    1    3    2    2    1    2A3-B24          2000    1    3    2    2    1    2A8-B24          2000    1    2    2    2    1    3A18-B24         2000    1    1    1    1    1    2A2-B552         2000    1    2    2    2    1    2A2-C152         2000    1    1    2    2    1    2A2-B69          2000    1    4    2    2    1    1A2-D36          2000    1    2    2    2    1    1A2-B618         2000    1    1    1    2    1    1A2-B33          2000    1    3    2    2    1    3A2-B34          2000    1    3    2    2    1    2A2-B35          2000    2    4    2    2    2    2A2-B1095        2000    3    4    2    2    1    2A2-C147         2000    2    4    2    2    2    2A2-B49          2000    2    4    2    2    1    2A2-C1           2000    2    3    1    2    1    2A2-B1100        2000    1    3    1    2    1    2A8-B2           2000    1    3    2    2    1    2A8-B1064        2000    2    4    3    2    1    3A8-B1101        2000    2    4    2    2    1    1A2-B156         2000    1    2    1    2    1    2化合物           g/ha   莎草 番薯 狗尾草 白芥  茄  繁缕A2-B144          2000     3    4     2    2    2    4A2-B134          2000     1    2     1    2    1    1A1210-B354       2000     2    3     2    1    1    2A2-C2            2000     2    3     1    1    1    1A2-D36           2000     1    2     1    2    3    1A2-D113(lsom.A)  2000     4    4     2    1    3    3A2-D115          2000     3    3     2    2    2    3A8-B34           2000     2    3     2    2    2    2A8-B1103         2000     1    3     2    1    1    2A2-C24           2000     1    2     1    1    1    2表B1b:芽前作用:化合物       g/h   稷   马唐  稗  苘麻 苋    藜A8-B1        250    2    2    2    1    1    1A1022-B24    250    2    4    4    3    4    1A2-B145      250    2    2    4    2    3    1A1208-B354   250    1    1    1    1    1    1A8-B1063     250    2    3    3    2    4    1A8-B552      250    2    3    4    1    4    1A8-B156      250    3    3    3    3    4    2A1210-B1105  250    2    3    2    1    4    1
在式I化合物按照WO97/34485的实施例F2及F4-F8所述方法加工配制的情形下,试验得到同样的结果。实施例B2:芽后除草作用
在温室中,使单子叶和双子叶试验植物在塑料盆中的标准土壤中生长,在4-6叶期,喷施式I试验物质的水悬液(按照WO97/34485中所述方法由25%浓度的可湿性粉剂(实施例F3,b)制备)或喷施式I试验物质的乳液(按照WO97/34485中所述方法由25%浓度乳油(实施例F1,c)制备),相当于2kg活性组份/公顷或250g活性组分/公顷(500升水/公顷)施用量。随后将受试植株在温室中于最佳条件下培育。18天试验期后,按照9级制对试验进行评价(1=全部损伤,9=没有作用)。1-4级(特别是1-3级)表示具有良好至很好的除草作用。在本试验中,式I的化合物表现出强有效的除草作用。表B2a:芽后作用化合物          g/ha  番薯 黑麦草狗尾草 白芥 茄  繁缕A2-B1           2000    1    2    1     1    1    2A2-B1082        2000    1    2    2     1    1    2A2-B1083        2000    1    4    2     1    1    2A2-B90          2000    1    2    2     1    2    2A2-B68          2000    1    2    2     1    1    2A2-B24          2000    1    2    2     1    2    2A2-B73          2000    1    3    2     1    1    2A2-B75          2000    2    2    3     1    2    2A2-B95          2000    1    2    2     1    2    2A2-B93          2000    1    2    2     1    2    2A3-B1           2000    1    3    2     1    1    2A94-B1          2000    1    2    2     1    1    1A2-B1063        2000    2    2    4     1    2    2A2-B1061        2000    2    2    2     1    2    2A2-B133         2000    1    2    2     1    2    2A2-B1058        2000    1    2    4     1    2    2A64-B24         2000    2    2    4     1    2    2A64-B1          2000    2    3    4     1    1    2A2-B1089        2000    1    2    2     1    1    2A2-B31          2000    2    2    2     1    2    2A2-B1090        2000    2    4    4     2    2    2A2-B46(顺式)    2000    1    2    3     1    2    2A2-B46(反式)    2000    1    2    2     1    1    2A2-B91          2000    1    2    2     1    2    2A2-B2           2000    1    2    2     1    2    2化合物      g/ha  番薯 黑麦草 狗尾草 白芥 茄  繁缕A2-B29      2000    2     3    2     1    2    2A2-B1066    2000    1     3    2     1    2    2A2-B25      2000    1     2    2     2    1    2A2-B1068    2000    1     2    4     1    1    2A2-B1070    2000    2     4    2     2    2    2A2-B5       2000    1     2    2     1    2    2A2-C149     2000    1     3    2     1    2    2A2-C146     2000    1     2    2     1    2    2A2-B112     2000    2     3    2     1    2    2A2-B354     2000    2     2    2     2    2    2A2-E16      2000    2     3    2     2    2    2A6-B24      2000    1     3    2     1    1    2A34-B1      2000    1     2    2     1    1    2A9-B1       2000    2     4    2     2    2    2A184-B1     2000    1     3    2     1    2    2A184-B24    2000    1     2    2     1    2    2A7-B24      2000    1     2    2     1    2    2A3-B24      2000    2     2    2     1    2    2A34-B24     2000    1     2    2     1    2    2A8-B24      2000    2     2    2     1    2    2A18-B24     2000    1     2    2     1    2    2A2-C152     2000    2     2    3     1    2    2A2-B69      2000    1     2    2     1    2    2A2-D36      2000    2     2    2     1    2    2A2-B618     2000    2     2    2     1    2    2A2-B49      2000    2     2    2     1    2    2A2-B1093    2000    2     2    2     1    2    2A2-B33      2000    2     4    2     1    2    2A2-B34      2000    1     3    2     1    1    2A2-B35      2000    1     3    2     1    1    2A2-B1087    2000    1     4    3     1    2    2A531-B24    2000    2     2    2     1    2    2A2-B1095    2000    1     2    4     1    2    2化合物           g/ha 番薯 黑麦草 狗尾草白芥 茄   繁缕A2-C147          2000    1    2     2    1    2    2A2-B70           2000    3    4     3    1    2    2A2-B49           2000    2    2     2    1    2    2A2-C1            2000    3    2     2    1    2    2A2-B1100         2000    2    2     3    1    1    2A8-B2            2000    2    2     2    2    2    3A8-B1064         2000    2    4     2    1    1    2A8-B133          2000    2    4     2    1    2    2A8-B1101         2000    2    3     2    1    2    2A2-B1101         2000    2    2     2    1    1    3A2-B156          2000    1    2     2    1    2    2A2-B134          2000    2    2     1    1    1    2A1210-B354       2000    2    2     2    1    1    2A2-C2            2000    2    1     1    1    1    1A2-D36           2000    2    1     1    1    1    1A2-D113(Isom.A)  2000    2    1     1    1    1    2A2-D113(Isom.B)  2000    2    2     2    2    1    2A2-D114          2000    2    1     1    1    1    1A2-D115          2000    1    2     1    1    1    1A8-B34           2000    2    2     2    2    2    2A8-B1103         2000    1    4     1    1    1    1A2-C24           2000    1    1     1    1    1    1表B2b:芽后作用:化合物               稷  马唐  稗  苘麻 苍耳 Ipopur.藜
           g/haA8-B1          250    4    3    3    3    3    3    2A2-B1091       250    4    4    2    3    4    3    3A2-B1094       250    2    3    2    3    3    3    2A2-B145        250    2    2    2    3    3    3    1A1208-B354     250    3    4    2    1    2    2    2A1210-B1       250    2    2    2    2    2    2    1A8-B552        250    2    3    3    2    2    2    2A8-B156        250    2    3    3    1    2    2    1A1210-B1105    250    1    2    3    2    2    2    1A8-B134        250    3    3    3    2    3    3    2A8-D36         250    3    3    2    2    3    3    2A2-D111(顺式)  250    2    2    4    2    1    2    2A2-D111(反式)  250    3    3    3    3    1    3    2A8-D111        250    3    3    3    3    1    2    3A8-D109        250    3    3    3    3    1    2    3A8-F5          250    4    3    4    3    3    3    3A2-F5          250    3    3    3    3    3    4    3
在式I化合物按照WO97/34485的实施例F2及F4-F8所述方法加工配制的情形下,试验得到同样的结果。

Claims (17)

1.式I化合物或其农药上可耐受的盐M+或式I化合物的立体异构体或互变异构体:
Figure A9981578600021
其中p为0或1;R5为C1-C6卤代烷基;R2为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,被C1-C2烷氧基羰基或苯基取代的乙烯基,或者为C2-C6炔基,C2-C6卤代炔基,被三甲基甲硅烷基、羟基、C1-C2烷氧基、C1-C2烷氧基羰基或苯基取代的乙炔基,或者为C3-C6二烯基,C3-C6环烷基,被卤素取代的C3-C6环烷基,或者为C1-C6烷氧基,C3-C6链烯氧基,C3-C6炔氧基,C1-C6卤代烷氧基,C3-C6卤代链烯氧基,氰基-C1-C4烷氧基,C1-C4烷氧基-C1-C4烷氧基,C1-C4烷硫基-C1-C4烷氧基,C1-C4烷基亚磺酰基-C1-C4烷氧基,C1-C4烷基磺酰基-C1-C4烷氧基,C1-C4烷氧基羰基-C1-C4烷氧基,C1-C6烷硫基,C1-C6烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷硫基,C1-C6卤代烷基亚磺酰基,C1-C6卤代烷基磺酰基,C1-C4烷氧基羰基-C1-C4烷硫基,C1-C4烷氧基羰基-C1-C4烷基亚磺酰基,C1-C4烷氧基羰基-C1-C4烷基磺酰基,苄基-S(O)n1-,C1-C6烷基氨基,C2-C6二烷基氨基,C1-C6烷基氨基磺酰基,二-(C1-C6烷基氨基)磺酰基,苄氧基,苄基,苯基,苯氧基,苯硫基,苯基亚磺酰基或苯磺酰基,这些含苯基的基团本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,或者R2为OS(O)n2-R21,N(R23)-S(O)n3-R22,氰基,氨基甲酰基,C1-C4烷氧基羰基,甲酰基,卤素,氰硫基,氨基,羟基-C1-C4烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷基-S(O)n4-C1-C4烷基,氰基-C1-C4烷基,C1-C6烷基羰氧基-C1-C4烷基,C1-C4烷氧基羰基-C1-C4烷基,C1-C4烷氧基羰氧基-C1-C4烷基,C1-C4氰硫基-C1-C4烷基,苯甲酰氧基-C1-C4烷基,C2-C6环氧乙烷基,C1-C4烷基氨基-C1-C4烷基,二-(C1-C4烷基)氨基-C1-C4烷基,C1-C12烷基硫代羰基-C1-C4烷基或甲酰基-C1-C4烷基,或者R2为可以是芳香性或部分饱和并且可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或稠合二环环系,所述环系经由C1-C4亚烷基、-CH=CH-、-C≡C-、-CH2O-、-CH2N(C1-C4烷基)-、-CH2SO-、或-CH2SO2基团与吡啶环键连,且每一环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,巯基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C2-C5烷氧基烷硫基,C3-C5乙酰基烷硫基,C3-C6烷氧基羰基烷硫基,C2-C4氰基烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,二-(C1-C4烷基)氨基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素;R3为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C3-C6环烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷硫基,C1-C6烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷硫基,C1-C6卤代烷基亚磺酰基,C1-C6卤代烷基磺酰基,C1-C6烷基氨基,C2-C5二烷基氨基,C1-C6烷基氨基磺酰基,C2-C6二烷基氨基磺酰基,苯基,苯硫基,苯基亚磺酰基,苯磺酰基或苯氧基,其中的苯基部分本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,或者R3为-N(R23)-S(O)n-R22,氰基,卤素,氨基,C1-C4烷氧基-C1-C4烷基或C1-C4烷基-S(O)n-C1-C4烷基;R4为氢,C1-C6烷基,羟基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6卤代链烯氧基,C3-C6炔氧基,C1-C4烷基羰氧基,C1-C4烷基磺酰氧基,甲苯磺酰氧基,C1-C4烷硫基,C1-C4烷基亚磺酰基,C1-C4烷基磺酰基,C1-C4烷基氨基,C1-C4二烷基氨基,C1-C4烷氧基羰基,C1-C4卤代烷基,甲酰基,氰基,卤素,苯基或苯氧基,其中的苯基部分本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代;或者R4为可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或R3-稠合二环环系,其中所述环系,除非稠合,均直接或经由C1-C4亚烷基、-CH=CH-、-C≡C-、-CH2O-、-CH2N(C1-C4烷基)-、-CH2S-、-CH2SO-、或-CH2SO2-基团与吡啶环键连,且所述环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C1-C4烷氧基-C1-C2烷硫基,C1-C4烷基羰基-C1-C2烷硫基,C1-C4烷氧基羰基-C1-C2烷硫基,氰基-C1-C4烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,二-(C1-C4烷基)氨基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素;R21为C1-C4烷基或C1-C4卤代烷基;R22为C1-C4烷基,C1-C4卤代烷基或二-(C1-C4烷基)氨基;R23、R24、R25彼此独立地为氢或C1-C4烷基;n,n1,n2,n3和n4彼此独立地为0,1或2;Q为Q1
Figure A9981578600041
其中R6、R7、R8和R9彼此独立地为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6炔基,C1-C6烷氧基羰基,C1-C6烷基羰基,C1-C6烷基-S(O)n17,C1-C6烷基-NHS(O)2,C1-C6烷基氨基,二-(C1-C6烷基)氨基,羟基,C1-C6烷氧基,C3-C6链烯氧基,C3-C6炔氧基,羟基-C1-C6烷基,C1-C4烷基磺酰氧基-C1-C6烷基,甲苯磺酰氧基-C1-C6烷基,C1-C6烷氧基-C1-C6烷基,C1-C6烷基-S(O)n4-C1-C6烷基,氰基-C1-C6烷基,C1-C6烷氧基-C1-C6烷氧基,苄氧基-C1-C6烷基,C1-C6烷氧基羰基-C1-C6烷基,C1-C6烷氧基羰氧基-C1-C6烷基,氰硫基-C1-C6烷基,环氧乙烷基,C1-C6烷基氨基-C1-C6烷基,二(C1-C6烷基)氨基-C1-C6烷基,甲酰基-C1-C6烷基,C1-C6烷基肟基,卤素,氰基,硝基,苯基或被下列基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、氨基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n18、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n5、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)n19N(C1-C4烷基)2、卤素、硝基、COOH或氰基;或者相邻的R6与R7或R8与R9一起表示-(CH2)m-,C(O)O(CH2)n20-或-S(O)n21(CH2)n22-;n5,n17,n18,n19和n21彼此独立地为0,1或2;n20为2或3;n22为2,3或4;m为2,3,4,5,或6;W为氧,S(O)n6,-CR11R12-,-CR63R64CR65R66,-C(O)-或-NR13;R63、R64、R65和R66彼此独立地为氢或C1-C6烷基,或者R65与R7或R9一起形成直接键;n6为0,1或2;R11为氢,C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷硫基-C1-C4烷基,C1-C4烷硫基-C3-C6环烷基,C1-C4烷基羰氧基-C1-C4烷基,C1-C4烷基磺酰氧基-C1-C4烷基,甲苯磺酰氧基-C1-C4烷基,二-(C1-C3烷氧基烷基)甲基,二-(C1-C3烷硫基烷基)甲基,(C1-C3烷氧基烷基)-(C1-C3烷硫基烷基)甲基,C3-C5氧杂环烷基,C3-C5硫杂环烷基,C3-C4二氧杂环烷基,C3-C4二硫杂环烷基,C3-C4氧硫杂环烷基,甲酰基,C1-C4烷氧基羰基,氨基甲酰基,C1-C4烷基氨基羰基,二-(C1-C4烷基)氨基羰基,苯基氨基羰基,苄基氨基羰基或其本身又可以被下述基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、氨基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n21、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n7、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)n20N(C1-C4烷基)、卤素、硝基、COOH或氰基;n7,n20和n21彼此独立地为0,1或2;或者R12与R6或R9一起代表基团-(CH2)o-;o为1,2,3,4或5;R12为氢,C1-C4烷基或C1-C4卤代烷基;或者R12与R11一起代表基团-(CH2)m1;m1为2,3,4,5,或6;R10为羟基,O-M+,卤素,氰基,SCN,OCN,C1-C12烷氧基,C1-C4烷氧基羰基-C1-C4烷氧基,C1-C12烷硫基,C1-C12烷基亚磺酰基,C1-C12烷基磺酰基,C1-C12卤代烷硫基,C1-C12卤代烷基亚磺酰基,C1-C12卤代烷基磺酰基,C1-C6烷氧基-C1-C6烷硫基,C1-C6烷氧基-C1-C6烷基亚磺酰基,C1-C6烷氧基-C1-C6烷基磺酰基,C2-C12链烯硫基,C2-C12链烯基亚磺酰基,C2-C12链烯基磺酰基,C2-C12炔硫基,C2-C12炔基亚磺酰基,C2-C12炔基磺酰基,C2-C12卤代链烯硫基,C2-C12卤代链烯基亚磺酰基,C2-C12卤代链烯基磺酰基,C1-C4烷氧基羰基-C1-C4烷硫基,C1-C4烷氧基羰基-C1-C4烷基亚磺酰基,C1-C4烷氧基羰基-C1-C4烷基磺酰基,(C1-C4烷氧基)2P(O)O,C1-C4烷基-(C1-C4烷氧基)P(O)O,H(C1-C4烷氧基)P(O)O,R14R15N,R14R15NNH,R16R17NC(O)O-,R16R17NC(O)NH-,C1-C12烷基-S(O)2NR18,C1-C4卤代烷基-S(O)2NR19,C1-C12烷基-S(O)2O,C1-C4卤代烷基-S(O)2O,C1-C18烷基羰氧基,其中的烷基基团可以被卤素、C1-C6烷氧基、C1-C6烷硫基或氰基取代,或者为C2-C18链烯基羰氧基,C2-C18炔基羰氧基,C3-C6环烷基羰氧基,C1-C12烷氧基羰氧基,C1-C12烷硫基羰氧基,C1-C12烷基硫代氨基甲酰基,C1-C6烷基-NH(CS)N(C1-C6烷基)-NH-,二-C1-C6烷基-N(CS)N(C1-C6烷基)-NH-,苄氧基,苄硫基,苄基亚磺酰基,苄基磺酰基,苯氧基,苯硫基,苯基亚磺酰基,苯基磺酰基,苯磺酰基氨基,苯磺酰氧基或苯甲酰氧基,其中的苯基基团部分本身又可被下述基团取代:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷硫基、C1-C4烷基亚磺酰基、C1-C4烷基磺酰基、C1-C4烷基-S(O)2O、C1-C4卤代烷硫基、C1-C4卤代烷基亚磺酰基、C1-C4卤代烷基磺酰基、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)2N(C1-C4烷基)、卤素、硝基或氰基;或者R10为基团Ar1-硫基,Ar2-亚磺酰基,Ar3-磺酰基,-OCO-Ar4或NH-Ar5,其中Ar1、Ar2、Ar3、Ar4和Ar5彼此独立地为可以是芳香性或部分饱和的并且可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或稠合二环环系,且对于每一环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,巯基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C2-C5烷氧基烷硫基,C3-C5乙酰基烷硫基,C3-C6烷氧基羰基烷硫基,C2-C4氰基烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,二-(C1-C4烷基)氨基,卤素,氰基,硝基,苯基和苄硫基,其中的苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮上的取代基不能为卤素;R14、R15、R16、R17和R18彼此独立地为氢或C1-C6烷基;n8,n9,n10,n11,n12,n13和n14彼此独立地为0,1或2;R13为氢,C1-C4烷基,C1-C4烷硫基-C1-C4羰基,C1-C4烷基亚磺酰基-C1-C4羰基,C1-C4烷基磺酰基-C1-C4羰基,C1-C4烷氧基羰基,C1-C4烷基羰基,苯基羰基,或者为其本身还可以被下述基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n15、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n16、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)2N(C1-C4烷基)、卤素、硝基或氰基;以及n15和n16彼此独立地为0,1或2。
2.根据权利要求1的化合物或其农药上可耐受的盐M+或式I化合物的立体异构体或互变异构体,其中:p为0;R5为C1-C6卤代烷基;R2为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C3-C6环烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷硫基,C1-C6烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷硫基,C1-C6卤代烷基亚磺酰基,C1-C6卤代烷基磺酰基,苄基-S(O)n1-,C1-C6烷基氨基,C2-C6二烷基氨基,C1-C6烷基氨基磺酰基,C2-C6-二烷基氨基磺酰基,苯基,苯氧基,苯硫基,苯基亚磺酰基或苯磺酰基,其中的苯基部分本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,或者为OS(O)n2-R21,N(R23)-S(O)n3-R22,氰基,卤素,氨基,C1-C4烷氧基-C1-C4烷基,C1-C4烷基-S(O)n4-C1-C4烷基,氰基-C1-C4烷基或C1-C4烷氧基-C1-C4烷氧基;R3为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C3-C6环烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷硫基,C1-C6烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷硫基,C1-C6卤代烷基亚磺酰基,C1-C6卤代烷基磺酰基,C1-C6烷基氨基,C2-C6二烷基氨基,C1-C6烷基氨基磺酰基,C2-C6二烷基氨基磺酰基,苯基,苯硫基,苯基亚磺酰基,苯磺酰基或苯氧基,其中的苯基部分本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,或者为-N(R23)-S(O)n-R22,氰基,卤素,氨基,C1-C4烷氧基-C1-C4烷基或C1-C4烷基-S(O)n-C1-C4烷基;R4为氢,C1-C6烷基,C1-C4烷氧基,C1-C4卤代烷氧基,C1-C4烷基羰氧基,C1-C4烷硫基,C1-C4烷基亚磺酰基,C1-C4烷基磺酰基,C1-C4卤代烷基,甲酰基,氰基,卤素,苯基或苯氧基,其中的苯基部分本身又可以被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代;或者R4为可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或R3-稠合二环环系,其中所述环系经由C1-C4亚烷基与吡啶环键连,且所述环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C1-C4烷氧基-C1-C2烷硫基,C1-C4烷基羰基-C1-C2烷硫基,C1-C4烷氧基羰基-C1-C2烷硫基,氰基-C1-C4烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,C2-C4二烷基氨基磺酰基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素;R21和R22彼此独立地为C1-C4烷基或C1-C4卤代烷基;R23、R24和R25彼此独立地为氢或C1-C4烷基;n,n1,n2,n3和n4彼此独立地为0,1或2;Q为Q1 其中R6、R7、R8和R9彼此独立地为氢,C1-C6烷基,C1-C6卤代烷基,C2-C6链烯基,C2-C6炔基,C1-C6烷氧基羰基,C1-C6烷基-S(O)n17,C1-C6烷基-NHS(O)2,C1-C6烷基氨基,二-(C1-C6烷基)氨基,羟基,C1-C6烷氧基,C3-C6链烯氧基,C3-C6炔氧基,羟基-C1-C6烷基,C1-C4烷基磺酰氧基-C1-C6烷基,甲苯磺酰氧基-C1-C6烷基,卤素,氰基,硝基,苯基或被下列基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、氨基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n18、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n5、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)n19N(C1-C4烷基)、卤素、硝基、COOH或氰基;或者相邻的R6与R7或R8与R9一起表示-(CH2)m-;n5,n17,n18和n19彼此独立地为0,1或2;m为2,3,4,5,或6;W为氧,S(O)n6,-CR11R12-,-C(O)-或-NR13-;n6为0,1或2;R11为氢,C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷硫基-C1-C4烷基,C1-C4烷基羰氧基-C1-C4烷基,C1-C4烷基磺酰氧基-C1-C4烷基,甲苯磺酰氧基-C1-C4烷基,二-(C1-C3烷氧基烷基)甲基,二-(C1-C3烷硫基烷基)甲基,(C1-C3烷氧基烷基)-(C1-C3烷硫基烷基)甲基,C3-C5氧杂环烷基,C3-C5硫杂环烷基,C3-C4二氧杂环烷基,C3-C4二硫杂环烷基,C3-C4氧硫杂环烷基,甲酰基,C1-C4烷氧基羰基或其本身又可以被下述基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、氨基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n21、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n7、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)n20N(C1-C4烷基)、卤素、硝基、COOH或氰基;n7,n20和n21彼此独立地为0,1或2;或者R12与R9一起代表基团-(CH2)o-;o为1,2,3,4或5;R12为氢,C1-C4烷基或C1-C4卤代烷基;或者R12与R11一起代表基团-(CH2)m1;m1为2,3,4,5,或6;R10为羟基,O-M+,卤素,C1-C12烷氧基,C1-C12烷基羰氧基,C2-C4链烯基羰氧基,C3-C6环烷基羰氧基,C1-C12烷氧基羰氧基,C1-C12烷基羰氧基,R23R24N-C(O)O,C1-C12烷基S(O)n8-,C1-C4卤代烷基-S(O)n9-,C2-C12-链烯基S(O)n10-,C2-C12卤代链烯基S(O)n11-,C2-C12炔基S(O)n12-;苄氧基,苯氧基,苯硫基,苯基亚磺酰基或苯磺酰基,其中的苯基基团部分本身又可被下述基团取代:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n13、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n14、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)2N(C1-C4烷基)、卤素、硝基或氰基,或者为C1-C4烷基-S(O)2O,苯基-S(O)2O,(C1-C4烷氧基)2P(O)O,C1-C4烷基(C1-C4烷氧基)P(O)O,或H(C1-C4烷氧基)P(O)O;n8,n9,n10,n11,n12,n13和n14彼此独立地为0,1或2;R13为氢,C1-C4烷基,C1-C4烷氧基羰基或其本身又可以被下述基团取代的苯基:C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基羰基、C1-C4烷氧基羰基、C1-C4烷基氨基、二-C1-C4烷基氨基、C1-C4烷基-S(O)n15、C1-C4烷基-S(O)2O、C1-C4卤代烷基-S(O)n16、C1-C4卤代烷基-S(O)2O、C1-C4烷基-S(O)2NH、C1-C4烷基-S(O)2N(C1-C4烷基)、卤素、硝基或氰基;n15和n16彼此独立地为0,1或2。
3.根据权利要求1的化合物,其中R10为羟基或O-M+
4.根据权利要求1的化合物,其中W为氧,-CR11R12-或-C(O)-。
5.根据权利要求1的化合物,其中W为氧,并且R6、R7、R8和R9彼此独立地为氢或C1-C3烷基。
6.根据权利要求1的化合物,其中W为-C(O)-,并且R6、R7、R8和R9彼此独立地为C1-C3烷基。
7.根据权利要求1的化合物,其中R2为氢和R3为甲基。
8.根据权利要求1的化合物,其中R2为甲基,乙基,正丙基,异丙基,乙烯基,甲氧基甲基,甲氧基羰氧基甲基,乙氧基羰氧基甲基,乙酰氧基甲基,丙酰氧基甲基,氯甲基,溴甲基,氟甲基,二氟甲基,三氟甲基或氰基甲基。
9.根据权利要求1的化合物,其中R4为氢或甲基。
10.根据权利要求1的化合物,其中R5为三氟甲基,二氟氯甲基,五氟乙基,七氟丙基或二氟甲基。
11.根据权利要求1的化合物,其中R3为氢,并且R2为C1-C4烷基,C1-C3卤代烷基,环丙基,C2-C3链烯基,C2-C3卤代链烯基,C2-C3炔基,丙二烯基,C1-C2烷氧基-C1-C2烷基,C1-C2烷硫基-C1-C2烷基,氰基-C1-C2烷基,C1-C2烷氧基羰基-C1-C2烷基,C1-C4烷基羰氧基-C1-C2烷基,C1-C3烷氧基,C1-C3卤代烷氧基,烯丙氧基,炔丙氧基,C1-C3烷硫基,C1-C3烷基亚磺酰基或氰基。
12.式IIIa化合物:
Figure A9981578600131
其中R501为C1-C6卤代烷基;R301为氢;R401为氢或C1-C6烷基;并且R201为C1-C6烷基,C1-C6卤代烷基-C1-C4烷基,C2-C6链烯基,C2-C6卤代链烯基,或C1-C2烷氧基羰基-或苯基-取代的乙烯基,C2-C6炔基或C2-C6卤代炔基;或者为三甲基甲硅烷基-、羟基-、C1-C2烷氧基-、C1-C2烷氧基羰基-或苯基-取代的乙炔基,或C3-C6二烯基;或者为C3-C6环烷基,卤代C3-C6环烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷基-S(O)n4-C1-C4烷基,氰基-C1-C4烷基,C1-C4烷氧基羰基-C1-C4烷基,C1-C4氰硫基,环氧乙烷基,C1-C4烷基氨基-C1-C4烷基,C1-C4二烷基氨基-C1-C4烷基,羟基-C1-C4烷基,C1-C12烷硫基羰基-C1-C4烷基或甲酰基-C1-C4烷基,或者R201为可以是芳香性或部分饱和的并且可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或稠合二环环系,所述环系经由C1-C4亚烷基、-CH=CH-、-C≡C-、-CH2O-、-CH2N(C1-C4烷基)-、-CH2S-、-CH2SO-或-CH2SO2-基团与吡啶环键连,且每一环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,巯基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C2-C5烷氧基烷硫基,C3-C5乙酰基烷硫基,C3-C6烷氧基羰基烷硫基,C2-C4氰基烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,二-(C1-C4烷基)氨基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素;以及X为卤素或氰基。
13.式XVIa化合物:其中R501为C1-C6卤代烷基;R301为氢;R401为氢或C1-C6烷基;并且R201为C1-C6烷基,C1-C6卤代烷基-C1-C4烷基,C2-C6链烯基,C2-C6卤代链烯基,或C1-C2烷氧基羰基-或苯基-取代的乙烯基,C2-C6炔基或C2-C6卤代炔基;或者为三甲基甲硅烷基-、羟基-、C1-C2烷氧基-、C1-C2烷氧基羰基-或苯基-取代的乙炔基,或C3-C6二烯基;或者为C3-C6环烷基,卤代C3-C6环烷基,C1-C4烷氧基-C1-C4烷基,C1-C4烷基-S(O)n4-C1-C4烷基,氰基-C1-C4烷基,C1-C4烷氧基羰基-C1-C4烷基,C1-C4氰硫基,环氧乙烷基,C1-C4烷基氨基-C1-C4烷基,C1-C4二烷基氨基-C1-C4烷基,羟基-C1-C4烷基,C1-C12烷硫基羰基-C1-C4烷基或甲酰基-C1-C4烷基,或者R201为可以是芳香性或部分饱和的并且可以含有1-4个选自氮、氧和硫的杂原子的5-10元单环或稠合二环环系,所述环系经由C1-C4亚烷基、-CH=CH-、-C≡C-、-CH2O-、-CH2N(C1-C4烷基)-、-CH2S-、-CH2SO-或-CH2SO2基团与吡啶环键连,且每一环系不能含有多于2个的氧原子和多于2个的硫原子,并且所述环系本身还可以被下列基团单-、二-或三取代:C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,C1-C6烷氧基,C1-C6卤代烷氧基,C3-C6链烯氧基,C3-C6炔氧基,巯基,C1-C6烷硫基,C1-C6卤代烷硫基,C3-C6链烯硫基,C3-C6卤代链烯硫基,C3-C6炔硫基,C2-C5烷氧基烷硫基,C3-C5乙酰基烷硫基,C3-C6烷氧基羰基烷硫基,C2-C4氰基烷硫基,C1-C6烷基亚磺酰基,C1-C6卤代烷基亚磺酰基,C1-C6烷基磺酰基,C1-C6卤代烷基磺酰基,氨基磺酰基,C1-C2烷基氨基磺酰基,二-(C1-C2烷基)氨基磺酰基,二-(C1-C4烷基)氨基,卤素,氰基,硝基,苯基和苄硫基,其中苯基和苄硫基本身又可以在苯环上被C1-C3烷基、C1-C3卤代烷基、C1-C3烷氧基、C1-C3卤代烷氧基、卤素、氰基或硝基取代,而且杂环中氮原子上的取代基不能为卤素;并且X为卤素或氰基,但条件是当R501为三氟甲基、同时R301和R401均为氢时,则R201不为C1-C6烷基。
14.除草与抑制植物生长的组合物,其包括除草活性量的式I化合物和惰性载体。
15.防治不需要植物的方法,该方法包括对所述植物或其所在环境施用除草活性量的式I活性成分或包含这种活性成分的组合物。
16.抑制植物生长的方法,该方法包括对所述植物或其所在环境施用除草活性量的式I活性成分或包含这种活性成分的组合物。
17.权利要求14的组合物在防治不需要植物生长方面的应用。
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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102256945A (zh) * 2008-12-18 2011-11-23 巴斯夫欧洲公司 具有除草作用的杂环二酮衍生物
CN104447519A (zh) * 2014-12-21 2015-03-25 成都安斯利生物医药有限公司 一种制备3-取代-2-溴-6-三氟甲基吡啶的方法
CN104496913A (zh) * 2014-12-22 2015-04-08 成都安斯利生物医药有限公司 一种制备5-取代-2,4-二甲硫基嘧啶的方法

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GT200100103A (es) 2000-06-09 2002-02-21 Nuevos herbicidas
DE10043075A1 (de) * 2000-09-01 2002-03-14 Aventis Cropscience Gmbh Heterocyclyl-substituierte Benzoylcyclohexandione, Verfahren zu ihrer Herstellung und ihre Verwendung als Herbizide
EP1659125B1 (en) 2000-10-02 2010-06-02 Emory University Triptolide analogs for the treatment of autoimmune and inflammatory disorders
WO2003020704A1 (en) * 2001-08-28 2003-03-13 Syngenta Participations Ag Sulfonylamino derivatives useful as herbicides
DE10148290A1 (de) * 2001-09-29 2003-04-17 Bayer Cropscience Gmbh Heterocyclische Amide, Verfahren zu ihrer Herstellung, sie enthaltende Mittel und ihre Verwendung
MXPA04005264A (es) * 2001-12-03 2004-10-11 Syngenta Participations Ag Composicion herbicida.
DE10208955A1 (de) 2002-02-28 2003-09-11 Bayer Ag Verfahren zur Herstellung von 2-Halogenalkylnicotinsäuren
DE10219036A1 (de) * 2002-04-29 2003-11-06 Bayer Cropscience Ag Substituierte Pyridylketone
EP1513829A2 (en) * 2002-06-14 2005-03-16 Syngenta Participations AG Nicotinoyl derivatives as herbicidal compounds
US6944901B2 (en) * 2002-09-27 2005-09-20 Colgate-Palmolive Company Brush section for a powered toothbrush
PL1601653T3 (pl) * 2003-03-07 2009-07-31 Syngenta Participations Ag Sposób wytwarzania podstawionych estrów kwasu nikotynowego
US7214825B2 (en) * 2003-10-17 2007-05-08 Honeywell International Inc. O-(3-chloropropenyl) hydroxylamine free base
US7501544B2 (en) * 2004-04-30 2009-03-10 Syngenta Crop Protection, Inc. Process for the production of cyclic diketones
UA92585C2 (ru) * 2004-04-30 2010-11-25 Сингента Партисипейшнс Аг Способ получения циклических дикетонов и промежуточные соединения
US20090137558A1 (en) * 2004-12-03 2009-05-28 Peakdale Molecular Limited Pyridine based compounds useful as intermediates for pharmaceutical or agricultural end-products
TW201002202A (en) * 2008-06-27 2010-01-16 Du Pont Fungicidal pyridines
US8334236B2 (en) 2009-02-03 2012-12-18 Kumiai Chemical Industry Co., Ltd. Ring-fused 2-pyridone derivatives and herbicides
AR076601A1 (es) 2009-05-21 2011-06-22 Chlorion Pharma Inc Pirimidinas como agentes terapeuticos
WO2011064188A1 (en) * 2009-11-27 2011-06-03 Basf Se Insecticidal methods using nitrogen-containing heteroaromatic compounds
CA2854100A1 (en) 2011-11-18 2013-05-23 Basf Se Substituted 1,2,5-oxadiazole compounds and their use as herbicides iii
AU2012343771B2 (en) * 2011-11-30 2015-11-26 Syngenta Limited 2-(substituted-phenyl)-cyclopentane-1,3-dione compounds, and derivatives thereof
BR112014026787A2 (pt) 2012-04-27 2017-06-27 Basf Se compostos de n-(tetrazol-5-il) e n-(triazol-5 il)hetarilcarboxamida substituída e uso dos mesmos como herbicidas.
JP6256469B2 (ja) * 2012-08-03 2018-01-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング スピロ[2.5]オクタン−5,7−ジオンの調製プロセス
WO2014184014A1 (en) 2013-05-15 2014-11-20 Basf Se N-(1,2,5-oxadiazol-3-yl)carboxamide compounds and their use as herbicides
EP2803661A1 (en) 2013-05-16 2014-11-19 Lonza Ltd Method for preparation of 6-trifluoromethylpyridine-3-carboxylic acid derivatives
EP2818461A1 (en) 2013-06-26 2014-12-31 Lonza Ltd Method for preparation of 6-trifluoromethylpyridine-3-carboxylic acid derivatives from 4,4,4-trifluoro-3-oxobutanoyl chloride
EP2821398A1 (en) 2013-07-03 2015-01-07 Lonza Ltd Method for preparation of 6-trifluoromethylpyridine-3-carboxylic acid derivatives from 4,4,4-trifluoro-3-aminobutanoates
EP2821399A1 (en) 2013-07-04 2015-01-07 Lonza Ltd Method for preparation of 6-trifluoromethylpyridine-3-carboxylic acid derivatives from 4,4,4-trifluoro-3-oxobutanoyl chloride
DK2997014T3 (en) 2013-07-19 2017-01-09 Lonza Ag PROCESS FOR THE PREPARATION OF 6-trifluoromethylpyridine-3-carboxylic acid derivatives FROM TRIFLUORACETYLEDDIKESYRE
TW201625511A (zh) 2014-06-26 2016-07-16 隆沙有限公司 由1,1,1-三氟丙酮製備4-烷氧基-1,1,1-三氟丁-3-烯-2-酮之方法
IL277071B1 (en) 2018-03-08 2024-03-01 Incyte Corp Aminopyrizine diol compounds as PI3K–y inhibitors
EA202190111A1 (ru) * 2018-06-25 2021-04-23 Байер Акциенгезельшафт Замещенные гетероарилоксипиридины и их соли, а также их применение в качестве гербицидных действующих веществ
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
CN117642069A (zh) * 2021-07-12 2024-03-01 福提费斯特有限公司 非编码氨基酸的新型衍生物及其作为除草剂的用途

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0245230A1 (en) * 1986-05-09 1987-11-11 Monsanto Company Substituted 2,6-substituted pyridine compounds
IT1219633B (it) 1987-06-05 1990-05-24 Sandoz Ag Benzoil-2h-piran-3,5-4h,6h-diodi sostituiti,loro preparazione e loro impiego come erbicidi
EP0316491A1 (en) 1987-11-19 1989-05-24 Stauffer Agricultural Chemicals Company, Inc. Herbicidal 2-pyridyl and 2-pyrimidine carbonyl 1,3-cyclohexanediones
HUT50312A (en) 1988-02-01 1990-01-29 Sandoz Ag Herbicide composition containing new dion-compounds and process for producing these compounds
IL91083A (en) 1988-07-25 1993-04-04 Ciba Geigy Cyclohexanedione derivatives, their preparation and their use as herbicides
JPH0352862A (ja) * 1989-07-20 1991-03-07 Nippon Soda Co Ltd 置換ピリジン誘導体、その製造法及び除草剤
JPH0429973A (ja) * 1990-05-24 1992-01-31 Nippon Soda Co Ltd 2,6―ジ置換ニコチン酸誘導体、その製造方法及び除草剤
EP0590045A1 (en) * 1991-06-12 1994-04-06 E.I. Du Pont De Nemours And Company Substituted pyridine herbicides
MX9706382A (es) * 1995-02-24 1997-11-29 Basf Ag Derivados de benzoilo.
EP0850218A1 (en) * 1995-07-10 1998-07-01 E.I. Du Pont De Nemours And Company Herbicidal sulfonamides
GB2305174A (en) * 1995-09-15 1997-04-02 Zeneca Ltd Chemical process
WO1997034485A1 (en) 1996-03-15 1997-09-25 Novartis Ag Herbicidal synergistic composition and method of weed control
CA2257196A1 (en) * 1996-06-06 1997-12-11 Morris Padgett Rorer Herbicidal pyridinyl and pyrazolylphenyl ketones
ATE296803T1 (de) * 1998-09-15 2005-06-15 Syngenta Participations Ag Als herbicide verwendbare pyridin-ketone

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102256945A (zh) * 2008-12-18 2011-11-23 巴斯夫欧洲公司 具有除草作用的杂环二酮衍生物
CN104447519A (zh) * 2014-12-21 2015-03-25 成都安斯利生物医药有限公司 一种制备3-取代-2-溴-6-三氟甲基吡啶的方法
CN104447519B (zh) * 2014-12-21 2019-01-22 成都安斯利生物医药有限公司 一种制备3-取代-2-溴-6-三氟甲基吡啶的方法
CN104496913A (zh) * 2014-12-22 2015-04-08 成都安斯利生物医药有限公司 一种制备5-取代-2,4-二甲硫基嘧啶的方法
CN104496913B (zh) * 2014-12-22 2018-08-21 成都安斯利生物医药有限公司 一种制备5-取代-2,4-二甲硫基嘧啶的方法

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CA2354387A1 (en) 2000-07-06
DE69923869T2 (de) 2005-07-14
ZA200105002B (en) 2002-02-19
ES2238871T3 (es) 2005-09-01
BR9916843B1 (pt) 2011-01-25
WO2000039094A1 (en) 2000-07-06
BR9916843A (pt) 2001-12-04
JP2002533443A (ja) 2002-10-08
CA2354387C (en) 2010-03-23
ATE289592T1 (de) 2005-03-15
CN1176907C (zh) 2004-11-24
DE69923869D1 (de) 2005-03-31
AU756636B2 (en) 2003-01-16
EP1140845B1 (en) 2005-02-23
AR023071A1 (es) 2002-09-04
US20030040437A1 (en) 2003-02-27
AU2101500A (en) 2000-07-31
EP1140845A1 (en) 2001-10-10

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