CN1176907C - 取代的吡啶除草剂 - Google Patents

取代的吡啶除草剂

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CN1176907C
CN1176907C CNB998157864A CN99815786A CN1176907C CN 1176907 C CN1176907 C CN 1176907C CN B998157864 A CNB998157864 A CN B998157864A CN 99815786 A CN99815786 A CN 99815786A CN 1176907 C CN1176907 C CN 1176907C
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alkyl
methyl
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carbonyl
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CN1333751A (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
技术领域
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。
背景技术
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。
发明内容
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 C9981578600051
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,C2C6二烷基氨基,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 C9981578600081
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)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R3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 C9981578600151
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
Figure C9981578600171
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。
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权利要求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:
Figure C9981578600211
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:
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 C9981578600213
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 C9981578600214
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):
路线b):
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
(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 C9981578600241
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)。
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I N-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.;J Org 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.;Heterocycles1986,24,2169),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:
Figure C9981578600281
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:
Figure C9981578600301
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,DE 3902818,GB8706557,DE 4434987,WO 9213821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 Acta 71,596(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 C9981578600302
其中R501为C1-C6卤代烷基,
酰化式V化物:
Figure C9981578600303
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:
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 C9981578600312
随后与式IX化合物进行缩合反应:
Figure C9981578600321
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:
得到式XVIa化合物:
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:
与式XII化合物进行缩合反应:
Figure C9981578600333
并且氯化(例如使用POCl3)所生成的式XIII化合物:
Figure C9981578600334
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 C9981578600335
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:
Figure C9981578600341
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 C9981578600351
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
反应流程4
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 C9981578600402
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。
具体实施方式
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℃。
1HNMR(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,J 8.1Hz,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16.7g3-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2.14g2-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-(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1.4g2-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-1,3-三酮(化合物A12010-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4NHCl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1.77 ppm,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,1.41ppm,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,7.72 d,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pH 2.5,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(J 8.2Hz),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0.55g10%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I 5-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II 5-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-C1):
将3.4g氢化钠(55%油悬浮物,78.0mmol)加到1l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1l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,brs,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,m4H;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-Bll04)
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-磺酰基甲基)-6-三氟甲基吡 啶-3-羰基]-3-羟基环己-2-烯酮(化合物A1090-B1)
将100mg2-[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-NMR(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:
Figure C9981578600581
化合物序号       R2                R3           R4         R5             p
A1               H                  H              H           CF3            0
A2               CH3               H              H           CF3            0
A3               CH3CH2           H              H           CF3            0
A4               (CH3)2CH         H              H           CF3            0
A5               (CH3)3C          H              H           CF3            0
A6               环丙基              H              H           CF3            0
A7               CH3(CH2)2       H              H           CF3            0
化合物序号            R2                          R3         R4          R5              p
A8                    CH3OCH2                    H           H            CF3             0
A9                    CH3O(CH2)2                H           H            CF3             0
A10                   Ph                            H           H            CF3             0
A11                   PhO                           H           H            CF3             0
A12                   PhS                           H           H            CF3             0
A13                   PhSO                          H           H            CF3             0
A14                   PhSO2                        H           H            CF3             0
A15                   CH3S                         H           H            CF3             0
A16                   CH3SO                        H           H            CF3             0
A17                   CF3                          H           H            CF3             0
A18                   F2CH                         H           H            CF3             0
A19                   HCC                           H           H            CF3             0
A20                   CH3CC                        H           H            CF3             0
A21                   CH2=CH                      H           H            CF3             0
A22                   CH2=CHCH2                  H           H            CF3             0
A23                   CH3SO2N(CH3)               H           H            CF3             0
A24                   (CH3)2N                     H           H            CF3             0
A25                   (CH3)2NSO2                 H           H            CF3             0
A26                   ClCH2                        H           H            CF3             0
A27                   CH3SCH2                     H           H            CF3             0
A28                   CH3SOCH2                    H           H            CF3             0
A29                   CH3SO2CH2                 H           H            CF3              0
A30                   [1.2.4]-三唑-1-基甲基         H           H            CF3              0
A31                   CH3                          CF3        H            CH3             0
A32                   CH3                          CH3        H            CF3             0
A33                   H                             H           H            CF3CF2         0
A34                   CH3                          H           H            CF3CF2         0
A35                   CH3CH2                      H           H            CF3CF2         0
A36                   环丙基                         H           H            CF3CF2         0
A37                   (CH3)3C                     H           H            CF3CF2         0
A38                   (CH3)2CH                    H           H            CF3CF2         0
A39                   CH3(CH2)2                  H           H            CF3CF2         0
A40                   CH3OCH2                     H           H            CF3CF2         0
化合物序号           R2                           R3          R4         R5                    p
A41                  CH3O(CH2)2                H             H           CF3CF2               0
A42                  Ph                            H             H           CF3CF2               0
A43                  PhO                           H             H           CF3CF2               0
A44                  PhS                           H             H           CF3CF2               0
A45                  PhSO                          H             H           CF3CF2               0
A46                  PhSO2                        H             H           CF3CF2               0
A47                  CH3S                         H             H           CF3CF2               0
A48                  CH3SO                        H             H           CF3CF2               0
A49                  CF3                          H             H           CF3CF2               0
A50                  F2CH                         H             H           CF3CF2               0
A51                  HCC                           H             H           CF3CF2               0
A52                  CH3CC                        H             H           CF3CF2               0
A53                  CH2=CH                      H             H           CF3CF2               0
A54                  CH2=CHCH2                  H             H           CF3CF2               0
A55                  CH3SO2N(CH3)               H             H           CF3CF2               0
A56                  (CH3)2N                     H             H           CF3CF2               0
A57                  (CH3)2NSO2                 H             H           CF3CF2               0
A58                  ClCH2                        H             H           CF3CF2                0
A59                  CH3SCH2                     H             H           CF3CF2               0
A60                  CH3SOCH2                    H             H           CF3CF2               0
A61                  CH3SO2CH2                  H             H           CF3CF2               0
A62                  [1.2.4]-三唑-1-基甲基          H             H           CF3CF2               0
A63                  H                              H             H           CF3CF2CF2           0
A64                  CH3                          H             H            CF3CF2CF2           0
A65                  CH3CH2                      H             H           CF3CF2CF2           0
A66                  环丙基                         H             H           CF3CF2CF2           0
A67                  (CH3)3C                     H             H           CF3CF2CF2           0
A68                  (CH3)2CH                    H             H           CF3CF2CF2           0
A69                  CH3(CH2)2                  H             H           CF3CF2CF2           0
A70                  CH3OCH2                     H             H           CF3CF2CF2           0
A71                  CH3O(CH2)2                 H             H           CF3CF2CF2           0
A72                  Ph                             H             H           CF3CF2CF2           0
A73                  PhO                            H             H           CF3CF2CF2           0
化合物序           R2                          R3         R4            R5                   p
A74                PhS                          H           H               CF3CF2CF2          0
A75                PhSO                         H           H               CF3CF2CF2          0
A76                PhSO2                       H           H               CF3CF2CF2          0
A77                CH3S                        H           H               CF3CF2CF2          0
A78                CH3SO                       H           H               CF3CF2CF2          0
A79                CF3                         H           H               CF3CF2CF2          0
A80                F2CH                        H           H               CF3CF2CF2          0
A81                HCC                          H           H               CF3CF2CF2          0
A82                CH3CC                       H           H               CF3CF2CF2          0
A83                CH2=CH                     H           H               CF3CF2CF2          0
A84                CH2=CHCH2                 H           H               CF3CF2CF2          0
A85                CH3SO2N(CH3)              H           H               CF3CF2CF2          0
A86                (CH3)2N                    H           H               CF3CF2CF2          0
A87                (CH3)2NSO2                H           H               CF3CF2CF2          0
A88                ClCH2                        H           H               CF3CF2CF2          0
A89                CH3SCH2                    H           H               CF3CF2CF2          0
A90                CH3SOCH2                   H           H               CF3CF2CF2          0
A91                CH3SO2CH2                 H           H               CF3CF2CF2          0
A92                [1.2.4]-三唑-1-基甲基         H           H               CF3CF2CF2          0
A93                H                             H           H               CF2Cl                 0
A94                CH3                          H           H               CF2Cl                 0
A95                CH3CH2                     H           H               CF2Cl                 0
A96                环丙基                        H           H               CF2Cl                 0
A97                (CH3)3C                    H           H               CF2Cl                 0
A98                (CH3)2CH                   H           H               CF2Cl                 0
A99                CH3(CH2)2                 H           H               CF2Cl                 0
A100               CH3OCH2                    H           H               CF2Cl                 0
A101               CH3O(CH2)2                H           H               CF2Cl                 0
A102               Ph                            H           H               CF2Cl                 0
A103               PhO                           H           H               CF2Cl                 0
A104               PhS                           H           H               CF2Cl                 0
A105               PhSO                          H           H               CF2Cl                 0
A106               PhSO2                        H           H               CF2Cl                 0
化合物序号           R2                                R3         R4          R5            p
A107                 CH3S                              H            H            CF2Cl         0
A108                 CH3SO                             H            H            CF2Cl         0
A109                 CF3                               H            H            CF2Cl         0
A110                 F2CH                              H            H            CF2Cl         0
A111                 HCC                                H            H            CF2Cl         0
A112                 CH3CC                             H            H            CF2Cl         0
A113                 CH2=CH                           H            H            CF2Cl         0
A114                 CH2=CHCH2                       H            H            CF2Cl         0
A115                 CH3SO2N(CH3                     H            H            CF2Cl         0
A116                 (CH3)2N                          H            H            CF2Cl         0
A117                 (CH3)2NSO2                      H            H            CF2Cl         0
A118                 ClCH2                             H            H            CF2Cl         0
A119                 CH3SCH2                          H            H            CF2Cl         0
A120                 CH3SOCH2                         H            H            CF2Cl         0
A121                 CH3SO2CH2                      H            H            CF2Cl         0
A122                 [1.2.4]-三唑-1-基甲基              H            H            CF2Cl         0
A123                 H                                  H            H            CHF2          0
A124                 CH3                               H            H            CHF2          0
A125                 CH3CH2                           H            H            CHF2          0
A126                 环丙基                             H            H            CHF2          0
A127                 (CH3)3C                         H            H            CHF2          0
A128                 (CH3)2CH                        H            H            CHF2          0
A129                 CH3(CH2)2                      H            H            CHF2          0
A130                 CH3OCH2                         H            H            CHF2          0
A131                 CH3O(CH2)2                     H            H            CHF2          0
A132                 Ph                                 H            H            CHF2          0
A133                 PhO                                H            H            CHF2          0
A134                 PhS                                H            H            CHF2          0
A135                 PhSO                               H            H            CHF2          0
A136                 PhSO2                             H            H            CHF2          0
A137                 CH3S                              H            H            CHF2          0
A138                 CH3SO                             H            H            CHF2          0
A139                 CF3                               H            H            CHF2          0
化合物序号            R2                             R3              R4         R5                 p
A140                  F2CH                            H                H           CHF2               0
A141                  HCC                              H                H           CHF2               0
A142                  CH3CC                           H                H           CHF2               0
A143                  CH2=CH                         H                H           CHF2               0
A144                  CH2=CHCH2                     H                H           CHF2               0
A145                  CH3SO2N(CH3)                  H                H           CHF2               0
A146                  (CH3)2N                        H                H           CHF2               0
A147                  (CH3)2NSO2                    H                H           CHF2               0
A148                  ClCH2                           H                H           CHF2               0
A149                  CH3SCH2                        H                H           CHF2               0
A150                  CH3SOCH2                       H                H           CHF2               0
A151                  CH3SO2CH2                     H                H           CHF2               0
A152                  [1.2.4]-三唑-1-基甲基             H                H           CHF2               0
A153                  H                                 H                H           CCl3               0
A154                  CH3                              H                H           CCl3               0
A155                  CH3CH2                         H                H           CCl3               0
A156                  环丙基                            H                H           CCl3               0
A157                  (CH3)3C                        H                H           CCl3               0
A158                  (CH3)2CH                       H                H           CCl3               0
A159                  CH3(CH2)2                     H                H           CCl3               0
A160                  CH3OCH2                        H                H           CCl3               0
A161                  CH3O(CH2)2                    H                H           CCl3               0
A162                  Ph                                H                H           CCl3               0
A163                  PhO                               H                H           CCl3               0
A164                  PhS                               H                H           CCl3               0
A165                  PhSO                              H                H           CCl3               0
A166                  PhSO2                            H                H           CCl3               0
A167                  CH3S                             H                H           CCl3               0
A168                  CH3SO                            H                H           CCl3               0
A169                  CF3                              H                H           CCl3               0
A170                  F2CH                             H                H           CCl3               0
A171                  HCC                               H                H           CCl3               0
A172                  CH3CC                            H                H           CCl3               0
化合物序号            R2                              R3        R4         R5          p
A173                  CH2=CH                         H          H           CCl3        0
A174                  CH2=CHCH2                     H          H           CCl3        0
A175                  CH3SO2N(CH3)                  H          H           CCl3        0
A176                  (CH3)2N                        H          H           CCl3        0
A177                  (CH3)2NSO2                    H          H           CCl3        0
A178                  ClCH2                            H          H           CCl3        0
A179                  CH3SCH2                         H          H           CCl3        0
A180                  CH3SOCH2                        H          H           CCl3        0
A181                  CH3SO2CH2                      H          H           CCl3        0
A182                  [1.2.4]-三唑-1-基甲基              H          H           CCl3        0
A183                  H                                  H          CH3        CF3         0
A184                  CH3                              H           CH3        CF3         0
A185                  CH3CH2                          H          CH3        CF3         0
A186                  环丙基                             H          CH3        CF3         0
A187                  (CH3)3C                         H          CH3        CF3         0
A188                  (CH3)2CH                        H          CH3        CF3         0
A189                  CH3(CH2)2                      H          CH3        CF3         0
A190                  CH3OCH2                         H          CH3        CF3         0
A191                  CH3O(CH2)2                     H          CH3        CF3         0
A192                  Ph                                 H          CH3        CF3         0
A193                  PhO                                H          CH3        CF3         0
A194                  PhS                                H          CH3        CF3         0
A195                  PhSO                               H          CH3        CF3         0
A196                  PhSO2                             H          CH3        CF3         0
A197                  CH3S                              H          CH3        CF3         0
A198                  CH3SO                             H          CH3        CF3         0
A199                  CF3                               H          CH3        CF3         0
A200                  F2CH                              H          CH3        CF3         0
A201                  HCC                                H          CH3        CF3         0
A202                  CH3CC                             H          CH3        CF3         0
A203                  CH2=CH                           H          CH3        CF3         0
A204                  CH2=CHCH2                       H          CH3        CF3         0
A205                  CH3SO2N(CH3)                    H          CH3        CF3         0
化合物序号           R2               R3         R4            R5               p
A206                (CH3)2N         H            CH3           CF3              0
A207                (CH3)2NSO2     H            CH3           CF3              0
A208                ClCH2            H            CH3           CF3              0
A209                CH3SCH2         H            CH3           CF3              0
A210                CH3SOCH2        H            CH3           CF3              0
A211                CH3SO2CH2      H            CH3           CF3              0
A212                H                  H            CH3           CF3CF2          0
A213                CH3               H            CH3           CF3CF2          0
A214                CH3CH2          H            CH3           CF3CF2          0
A215                环丙基             H            CH3           CF3CF2          0
A216                (CH3)3C         H            CH3           CF3CF2          0
A217                (CH3)2CH        H            CH3           CF3CF2          0
A218                CH3(CH2)2      H            CH3           CF3CF2          0
A219                CH3OCH2         H            CH3           CF3CF2          0
A220                CH3O(CH2)2     H            CH3           CF3CF2          0
A221                Ph                 H            CH3           CF3CF2          0
A222                PhO                H            CH3           CF3CF2          0
A223                PhS                H            CH3           CF3CF2          0
A224                PhSO               H            CH3           CF3CF2          0
A225                PhSO2             H            CH3           CF3CF2          0
A226                CH3S              H            CH3           CF3CF2          0
A227                CH3SO             H            CH3           CF3CF2          0
A228                CF3               H            CH3           CF3CF2          0
A229                F2CH              H            CH3           CF3CF2          0
A230                HCC                H            CH3           CF3CF2          0
A231                CH3CC             H            CH3           CF3CF2          0
A232                CH2=CH           H            CH3           CF3CF2          0
A233                CH2=CHCH2       H            CH3           CF3CF2          0
A234                CH3SO2N(CH3)    H            CH3           CF3CF2          0
A235                (CH3)2N          H            CH3           CF3CF2          0
A236                (CH3)2NSO2      H            CH3           CF3CF2          0
A237                ClCH2             H            CH3            CF3CF2          0
A238                CH3SCH2          H            CH3           CF3CF2          0
化合物序号           R2                    R3        R4           R5                       p
A239                 CH3SOCH2             H          CH3          CF3CF2                  0
A240                 CH3SO2CH2           H          CH3          CF3CF2                  0
A241                 H                       H          CH3          CF3CF2CF2              0
A242                 CH3                   H          CH3          CF3CF2CF2              0
A243                 CH3CH2               H          CH3          CF3CF2CF2              0
A244                 环丙基                  H          CH3          CF3CF2CF2              0
A245                 (CH3)3C              H          CH3          CF3CF2CF2              0
A246                 (CH3)2CH             H          CH3          CF3CF2CF2              0
A247                 CH3(CH2)2           H          CH3          CF3CF2CF2              0
A248                 CH3OCH2              H          CH3          CF3CF2CF2              0
A249                 CH3O(CH2)2          H          CH3          CF3CF2CF2              0
A250                 Ph                      H          CH3          CF3CF2CF2              0
A251                 PhO                     H          CH3          CF3CF2CF2              0
A252                 PhS                     H          CH3          CF3CF2CF2              0
A253                 PhSO                    H          CH3          CF3CF2CF2              0
A254                 PhSO2                  H          CH3          CF3CF2CF2              0
A255                 CH3S                   H          CH3          CF3CF2CF2              0
A256                 CH3SO                  H          CH3          CF3CF2CF2              0
A257                 CF3                    H          CH3          CF3CF2CF2              0
A258                 F2CH                   H          CH3          CF3CF2CF2              0
A259                 HCC                     H          CH3          CF3CF2CF2              0
A260                 CH3CC                  H          CH3          CF3CF2CF2              0
A261                 CH2=CH                H          CH3          CF3CF2CF2              0
A262                 CH2=CHCH2            H          CH3          CF3CF2CF2              0
A263                 CH3SO2N(CH3)         H          CH3          CF3CF2CF2              0
A264                 (CH3)2N               H          CH3          CF3CF2CF2              0
A265                 (CH3)2NSO2           H          CH3          CF3CF2CF2              0
A266                 ClCH2                  H          CH3          CF3CF2CF2               0
A267                 CH3SCH2               H          CH3          CF3CF2CF2              0
A268                 CH3SOCH2              H          CH3          CF3CF2CF2              0
A269                 CH3SO2CH2            H          CH3          CF3CF2CF2              0
A270                 H                        H          CH3          CF2Cl                     0
A271                 CH3                     H          CH3          CF2Cl                     0
化合物序号            R2                    R3            R4               R5            p
A272                  CH3CH2               H              CH3              CF2Cl         0
A273                  环丙基                  H              CH3              CF2Cl         0
A274                  (CH3)3C              H              CH3              CF2Cl         0
A275                  (CH3)2CH             H              CH3              CF2Cl         0
A276                  CH3(CH2)2           H              CH3              CF2Cl         0
A277                  CH3OCH2              H              CH3              CF2Cl         0
A278                  CH3O(CH2)2          H              CH3              CF2Cl         0
A279                  Ph                      H              CH3              CF2Cl         0
A280                  PhO                     H              CH3              CF2Cl         0
A281                  PhS                     H              CH3              CF2Cl         0
A282                  PhSO                    H              CH3              CF2Cl         0
A283                  PhSO2                  H              CH3              CF2Cl         0
A284                  CH3S                   H              CH3              CF2Cl         0
A285                  CH3SO                  H              CH3              CF2Cl         0
A286                  CF3                    H              CH3              CF2Cl         0
A287                  F2CH                   H              CH3              CF2Cl         0
A288                  HCC                     H              CH3              CF2Cl         0
A289                  CH3CC                  H              CH3              CF2Cl         0
A290                  CH2=CH                H              CH3              CF2Cl         0
A291                  CH2=CHCH2            H              CH3              CF2Cl         0
A292                  CH3SO2N(CH3)         H              CH3              CF2Cl         0
A293                  (CH3)2N               H              CH3              CF2Cl         0
A294                  (CH3)2NSO2           H              CH3              CF2Cl         0
A295                  ClCH2                  H              CH3              CF2Cl          0
A296                  CH3SCH2               H              CH3              CF2Cl          0
A297                  CH3SOCH2              H              CH3              CF2Cl          0
A298                  CH3SO2CH2            H              CH3              CF2Cl         0
A299                  H                        H              CH3              CHF2          0
A300                  CH3                    H              CH3              CHF2           0
A301                  CH3CH2                H              CH3              CHF2           0
A302                  环丙基                   H              CH3              CHF2           0
A303                  (CH3)3C               H              CH3              CHF2           0
A304                  (CH3)2CH              H              CH3              CHF2           0
化合物序号          R2                   R3           R4              R5               p
A305                CH3(CH2)2          H             CH3             CHF2             0
A306                CH3OCH2             H             CH3             CHF2             0
A307                CH3O(CH2)2         H             CH3             CHF2             0
A308                Ph                     H             CH3             CHF2             0
A309                PhO                    H             CH3             CHF2             0
A310                PhS                    H             CH3             CHF2             0
A311                PhSO                   H             CH3             CHF2             0
A312                PhSO2                 H             CH3             CHF2             0
A313                CH3S                  H             CH3             CHF2             0
A314                CH3SO                 H             CH3             CHF2             0
A315                CF3                   H             CH3             CHF2             0
A316                F2CH                  H             CH3             CHF2             0
A317                HCC                    H             CH3             CHF2             0
A318                CH3CC                 H             CH3             CHF2             0
A319                CH2=CH               H             CH3             CHF2             0
A320                CH2=CHCH2           H             CH3             CHF2             0
A321                CH3SO2N(CH3)        H             CH3             CHF2             0
A322                (CH3)2N              H             CH3             CHF2             0
A323                (CH3)2NSO2          H             CH3             CHF2             0
A324                ClCH2                 H             CH3             CHF2             0
A325                CH3SCH2              H             CH3             CHF2             0
A326                CH3SOCH2             H             CH3             CHF2             0
A327                CH3SO2CH2           H             CH3             CHF2             0
A328                H                       H             CH3             CCl3             0
A329                CH3                   H             CH3             CCl3             0
A330                CH3CH2               H             CH3             CCl3             0
A331                (CH3)3C              H             CH3             CCl3             0
A332                (CH3)2CH             H             CH3             CCl3             0
A333                环丙基                  H             CH3             CCl3             0
A334                CH3(CH2)2           H             CH3             CCl3             0
A335                CH3OCH2              H             CH3             CCl3             0
A336                CH3O(CH2)2          H             CH3             CCl3             0
A337                Ph                      H             CH3             CCl3             0
化合物序号             R2                  R3              R4          R5         p
A338                   PhO                  H                CH3         CCl3        0
A339                   PhS                  H                CH3         CCl3        0
A340                   PhSO                 H                CH3         CCl3        0
A341                   PhSO2               H                CH3         CCl3        0
A342                   CH3S                H                CH3         CCl3        0
A343                   CH3SO               H                CH3         CCl3        0
A344                   CF3                 H                CH3         CCl3        0
A345                   F2CH                H                CH3         CCl3        0
A346                   HCC                  H                CH3         CCl3        0
A347                   CH3CC               H                CH3         CCl3        0
A348                   CH2=CH             H                CH3         CCl3        0
A349                   CH2=CHCH2         H                CH3         CCl3        0
A350                   CH3SO2N(CH3)      H                CH3         CCl3        0
A351                   (CH3)2N            H                CH3         CCl3        0
A352                   (CH3)2NSO2        H                CH3         CCl3        0
A353                   ClCH2               H                CH3         CCl3        0
A354                   CH3SCH2            H                CH3         CCl3        0
A355                   CH3SOCH2           H                CH3         CCl3        0
A356                   CH3SO2CH2         H                CH3         CCl3        0
A357                   H                     H                Ph           CF3         0
A358                   CH3                  H                Ph           CF3         0
A359                   CH3CH2             H                Ph           CF3         0
A360                   环丙基                H                Ph           CF3         0
A361                   (CH3)3C            H                Ph           CF3         0
A362                   (CH3)2CH           H                Ph           CF3         0
A363                   CH3(CH2)2         H                Ph           CF3         0
A364                   CH3OCH2            H                Ph           CF3         0
A365                   CH3O(CH2)2        H                Ph           CF3         0
A366                   Ph                    H                Ph           CF3         0
A367                   PhO                   H                Ph           CF3         0
A368                   PhS                   H                Ph           CF3         0
A369                   PhSO                  H                Ph           CF3         0
A370                   PhSO2                H                Ph           CF3         0
化合物序号     R2                    R3         R4             R5               p
A371           CH3S                  H            Ph              CF3              0
A372           CH3SO                 H            Ph              CF3              0
A373           CF3                   H            Ph              CF3              0
A374           F2CH                  H            Ph              CF3              0
A375           HCC                    H            Ph              CF3              0
A376           CH3CC                 H            Ph              CF3              0
A377           CH2=CH               H            Ph              CF3              0
A378           CH2=CHCH2           H            Ph              CF3              0
A379           CH3SO2N(CH3)        H            Ph              CF3              0
A380           (CH3)2N              H            Ph              CF3              0
A381           (CH3)2NSO2          H            Ph              CF3              0
A382           ClCH2                  H            Ph              CF3              0
A383           CH3SCH2              H            Ph              CF3              0
A384           CH3SOCH2             H            Ph              CF3              0
A385           CH3SO2CH2           H            Ph              CF3              0
A386           H                       H            Ph              CF3CF2          0
A387           CH3                    H            Ph              CF3CF2          0
A388           CH3CH2               H            Ph              CF3CF2          0
A389           环丙基                  H            Ph              CF3CF2          0
A390           (CH3)3C              H            Ph              CF3CF2          0
A391           (CH3)2CH             H            Ph              CF3CF2          0
A392           CH3(CH2)2           H            Ph              CF3CF2          0
A393           CH3OCH2              H            Ph              CF3CF2          0
A394           CH3O(CH2)2          H            Ph              CF3CF2          0
A395           PH                      H            Ph              CF3CF2          0
A396           PhO                     H            Ph              CF3CF2          0
A397           PhS                     H            Ph              CF3CF2          0
A398           PhSO                    H            Ph              CF3CF2          0
A399           PhSO2                  H            Ph              CF3CF2          0
A400           CH3S                   H            Ph              CF3CF2          0
A401           CH3SO                  H            Ph              CF3CF2          0
A402           CF3                    H            Ph              CF3CF2          0
A403           F2CH                   H            Ph              CF3CF2          0
化合物序号          R2                 R3        R4         R5                 p
A404                HCC                 H          Ph          CF3CF2            0
A405                CH3CC              H          Ph          CF3CF2            0
A406                CH2=CH            H          Ph          CF3CF2            0
A407                CH2=CHCH2        H          Ph          CF3CF2            0
A408                CH3SO2N(CH3)    H          Ph          CF3CF2            0
A409                (CH3)2N           H          Ph          CF3CF2            0
A410                (CH3)2NSO2      H          Ph          CF3CF2            0
A411                ClCH2              H          Ph          CF3CF2            0
A412                CH3SCH2           H          Ph          CF3CF2            0
A413                CH3SOCH2          H          Ph          CF3CF2            0
A414                CH3SO2CH2       H          Ph          CF3CF2            0
A415                H                   H          Ph          CF3CF2CF2        0
A416                CH3                H          Ph          CF3CF2CF2        0
A417                CH3CH2           H          Ph          CF3CF2CF2        0
A418                环丙基              H          Ph          CF3CF2CF2        0
A419                (CH3)3C          H          Ph          CF3CF2CF2        0
A420                (CH3)2CH         H          Ph          CF3CF2CF2        0
A421                CH3(CH2)2       H          Ph          CF3CF2CF2        0
A422                CH3OCH2          H          Ph          CF3CF2CF2        0
A423                CH3O(CH2)2      H          Ph          CF3CF2CF2        0
A424                Ph                  H          Ph          CF3CF2CF2        0
A425                PhO                 H          Ph          CF3CF2CF2        0
A426                PhS                 H          Ph          CF3CF2CF2        0
A427                PhSO                H          Ph          CF3CF2CF2        0
A428                PhSO2              H          Ph          CF3CF2CF2        0
A429                CH3S               H          Ph          CF3CF2CF2        0
A430                CH3SO              H          Ph          CF3CF2CF2        0
A431                CF3                H          Ph          CF3CF2CF2        0
A432                F2CH               H          Ph          CF3CF2CF2        0
A433                HCC                 H          Ph          CF3CF2CF2        0
A434                CH3CC              H          Ph          CF3CF2CF2        0
A435                CH2=CH            H          Ph          CF3CF2CF2        0
A436                CH2=CHCH2        H          Ph          CF3CF2CF2        0
化合物序号           R2                  R3       R4       R5             p
A437                 CH3SO2N(CH3)     H         Ph        CF3CF2CF2    0
A438                 (CH3)2N           H         Ph        CF3CF2CF2    0
A439                 (CH3)2NSO2       H         Ph        CF3CF2CF2    0
A440                 ClCH2              H         Ph        CF3CF2CF2    0
A441                 CH3SCH2           H         Ph        CF3CF2CF2    0
A442                 CH3SOCH2          H         Ph        CF3CF2CF2    0
A443                 CH3SO2CH2        H         Ph        CF3CF2CF2    0
A444                 H                    H         Ph        CF2Cl          0
A445                 CH3                 H         Ph        CF2Cl          0
A446                 CH3CH2            H         Ph        CF2Cl          0
A447                 环丙基               H         Ph        CF2Cl          0
A448                 (CH3)3C           H         Ph        CF2Cl          0
A449                 (CH3)2CH          H         Ph        CF2Cl          0
A450                 CH3(CH2)2        H         Ph        CF2Cl          0
A451                 CH3OCH2           H         Ph        CF2Cl          0
A452                 CH3O(CH2)2       H         Ph        CF2Cl          0
A453                 Ph                   H         Ph        CF2Cl          0
A454                 PhO                  H         Ph        CF2Cl          0
A455                 PhS                  H         Ph        CF2Cl          0
A456                 PhSO                 H         Ph        CF2Cl          0
A457                 PhSO2               H         Ph        CF2Cl          0
A458                 CH3S                H         Ph        CF2Cl          0
A459                 CH3SO               H         Ph        CF2Cl          0
A460                 CF3                 H         Ph        CF2Cl          0
A461                 F2CH                H         Ph        CF2Cl          0
A462                 HCC                  H         Ph        CF2Cl          0
A463                 CH3CC               H         Ph        CF2Cl          0
A464                 CH2=CH             H         Ph        CF2Cl          0
A465                 CH2=CHCH2         H         Ph        CF2Cl          0
A466                 CH3SO2N(CH3)      H         Ph        CF2Cl          0
A467                 (CH3)2N            H         Ph        CF2Cl          0
A468                 (CH3)2NSO2        H         Ph        CF2Cl          0
A469                 ClCH2                H         Ph        CF2Cl          0
化合物序号         R2                  R3          R4       R5           p
A470               CH3SCH2            H            Ph        CF2Cl        0
A471               CH3SOCH2           H            Ph        CF2Cl        0
A472               CH3SO2CH2         H            Ph        CF2Cl        0
A473               H                     H            Ph        CHF2         0
A474               CH3                 H            Ph        CHF2         0
A475               CH3CH2             H            Ph        CHF2         0
A476               环丙基                H            Ph        CHF2         0
A477               (CH3)3C            H            Ph        CHF2         0
A478               (CH3)2C            H            Ph        CHF2         0
A479               CH3(CH2)2         H            Ph        CHF2         0
A480               CH3OCH2            H            Ph        CHF2         0
A481               CH3O(CH2)2        H            Ph        CHF2         0
A482               Ph                    H            Ph        CHF2         0
A483               PhO                   H            Ph        CHF2         0
A484               PhS                   H            Ph        CHF2         0
A485               PhSO                  H            Ph        CHF2         0
A486               PhSO2                H            Ph        CHF2         0
A487               CH3S                 H            Ph        CHF2         0
A488               CH3SO                H            Ph        CHF2         0
A489               CF3                  H            Ph        CHF2         0
A490               F2CH                 H            Ph        CHF2         0
A49                HCC                   H            Ph        CHF2         0
A492               CH3CC                H            Ph        CHF2         0
A493               CH2=CH              H            Ph        CHF2         0
A494               CH2=CHCH2          H            Ph        CHF2         0
A495               CH3SO2N(CH3)       H            Ph        CHF2         0
A496               (CH3)2N             H            Ph        CHF2         0
A497               (CH3)2NSO2         H            Ph        CHF2         0
A498               ClCH2                H            Ph        CHF2         0
A499               CH3SCH2             H            Ph        CHF2         0
A500               CH3SOCH2            H            Ph        CHF2         0
A501               CH3SO2CH2          H            Ph        CHF2         0
A502               H                      H            Ph        CCl3         0
化合物序号       R2               R3                R4             R5           p
A503             CH3              H                  Ph              CCl3         0
A504             CH3CH2          H                  Ph              CCl3         0
A505             环丙基             H                  Ph              CCl3         0
A506             (CH3)3C         H                  Ph              CCl3         0
A507             (CH3)2CH        H                  Ph              CCl3         0
A508             CH3(CH2)2      H                  Ph              CCl3         0
A509             CH3OCH2         H                  Ph              CCl3         0
A510             CH3O(CH2)2     H                  Ph              CCl3         0
A511             Ph                 H                  Ph              CCl3         0
A512             PhO                H                  Ph              CCl3         0
A513             PhS                H                  Ph              CCl3         0
A514             PhSO               H                  Ph              CCl3         0
A515             PhSO2             H                  Ph              CCl3         0
A516             CH3S              H                  Ph              CCl3         0
A517             CH3SO             H                  Ph              CCl3         0
A518             CF3               H                  Ph              CCl3         0
A519             F2CH              H                  Ph              CCl3         0
A520             HCC                H                  Ph              CCl3         0
A521             CH3CC             H                  Ph              CCl3         0
A522             CH2=CH           H                  Ph              CCl3         0
A523             CH2=CHCH2       H                  Ph              CCl3         0
A524             CH3SO2N(CH3)    H                  Ph              CCl3         0
A525             (CH3)2N          H                  Ph              CCl3         0
A526             (CH3)2NSO2      H                  Ph              CCl3         0
A527             ClCH2             H                  Ph              CCl3         0
A528             CH3SCH2          H                  Ph              CCl3         0
A529             CH3SOCH2         H                  Ph              CCl3         0
A530             CH3SO2CH2      H                  Ph              CCl3         0
A531             H                  CH3               H               CF3          0
A532             H                  CH3CH2           H               CF3          0
A533             H                  环丙基              H               CF3          0
A534             H                  (CH3)3CH         H               CF3          0
A535             H                  (CH3)2CH         H               CF3          0
化合物序号       R2        R3                 R4        R5              p
A536             H          CH3(CH2)2        H          CF3             0
A537             H          CH3OCH2           H          CF3             0
A538             H          CH3O(CH2)2       H          CF3             0
A539             H          Ph                   H          CF3             0
A540             H          PhO                  H          CF3             0
A541             H          PhS                  H          CF3             0
A542             H          PhSO                 H          CF3             0
A543             H          PhSO2               H          CF3             0
A544             H          CH3S                H          CF3             0
A545             H          CH3SO               H          CF3             0
A546             H          CF3                 H          CF3             0
A547             H          F2CH                H          CF3             0
A548             H          HCC                  H          CF3             0
A549             H          CH3CC               H          CF3             0
A550             H          CH2=CH             H          CF3             0
A551             H          CH2=CHCH2         H          CF3             0
A552             H          CH3SO2N(CH3)      H          CF3             0
A553             H          (CH3)2N            H          CF3             0
A554             H          (CH3)2NSO2        H          CF3             0
A555             H          CH3SCH2            H          CF3             0
A556             H          CH3SOCH2           H          CF3             0
A557             H          CH3SO2CH2         H          CF3             0
A558             H          CH3                 H          CF3CF2         0
A559             H          CH3CH2             H          CF3CF2         0
A560             H          环丙基                H          CF3CF2         0
A561             H          (CH3)3C            H          CF3CF2         0
A562             H          (CH3)2CH           H          CF3CF2         0
A563             H          CH3(CH2)2         H          CF3CF2         0
A564             H          CH3OCH2            H          CF3CF2         0
A565             H          CH3O(CH2)2        H          CF3CF2         0
A566             H          Ph                    H          CF3CF2         0
A567             H          PhO                   H          CF3CF2         0
A568             H          PhS                   H          CF3CF2         0
化合物序号       R2        R3                R4         R5                  p
A569             H          PhSO               H           CF3CF2             0
A570             H          PhSO2             H           CF3CF2             0
A571             H          CH3S              H           CF3CF2             0
A572             H          CH3SO             H           CF3CF2             0
A573             H          CF3               H           CF3CF2             0
A574             H          F2CH              H           CF3CF2             0
A575             H          HCC                H           CF3CF2             0
A576             H          CH3CC             H           CF3CF2             0
A577             H          CH2=CH           H           CF3CF2             0
A578             H          CH2=CHCH2       H           CF3CF2             0
A579             H          CH3SO2N(CH3)    H           CF3CF2             0
A580             H          (CH3)2N          H           CF3CF2             0
A581             H          (CH3)2NSO2      H           CF3CF2             0
A582             H          CH3SCH2          H           CF3CF2             0
A583             H          CH3SOCH2         H           CF3CF2             0
A584             H          CH3SO2CH2       H           CF3CF2             0
A585             H          CH3                H           CF3CF2CF2         0
A586             H          CH3CH2           H           CF3CF2CF2         0
A587             H          环丙基              H           CF3CF2CF2         0
A588             H          (CH3)3C          H           CF3CF2CF2         0
A589             H          (CH3)2CH         H           CF3CF2CF2         0
A590             H          CH3(CH2)2       H           CF3CF2CF2         0
A591             H          CH3OCH2          H           CF3CF2CF2         0
A592             H          CH3O(CH2)2      H           CF3CF2CF2         0
A593             H          Ph                  H           CF3CF2CF2         0
A594             H          PhO                 H           CF3CF2CF2         0
A595             H          PhS                 H           CF3CF2CF2         0
A596             H          PhSO                H           CF3CF2CF2         0
A597             H          PhSO2              H           CF3CF2CF2         0
A598             H          CH3S               H           CF3CF2CF2         0
A599             H          CH3SO              H           CF3CF2CF2         0
A600             H          CF3                H           CF3CF2CF2         0
A601             H          F2CH               H           CF3CF2CF2         0
化合物序号         R2        R3                 R4        R5                  p
A602               H          HCC                  H          CF3CF2CF2         0
A603               H          CH3CC               H          CF3CF2CF2         0
A604               H          CH2=CH             H          CF3CF2CF2         0
A605               H          CH2=CHCH2         H          CF3CF2CF2         0
A606               H          CH3SO2N(CH3)      H          CF3CF2CF2         0
A607               H          (CH3)2N            H          CF3CF2CF2         0
A608               H          (CH3)2NSO2        H          CF3CF2CF2         0
A609               H          CH3SCH2            H          CF3CF2CF2         0
A610               H          CH3SOCH2           H          CF3CF2CF2         0
A611               H          CH3SO2CH2         H          CF3CF2CF2         0
A612               H          CH3                  H          CF2Cl               0
A613               H          CH3CH2             H          CF2Cl                0
A614               H          环丙基                H          CF2Cl               0
A615               H          (CH3)3C            H          CF2Cl               0
A616               H          (CH3)2CH           H          CF2Cl               0
A617               H          CH3(CH2)2         H          CF2Cl               0
A618               H          CH3OCH2            H          CF2Cl               0
A619               H          CH3O(CH2)2        H          CF2Cl               0
A620               H          Ph                    H          CF2Cl               0
A621               H          PhO                   H          CF2Cl               0
A622               H          PhS                   H          CF2Cl               0
A623               H          PhSO                  H          CF2Cl               0
A624               H          PhSO2                H          CF2Cl               0
A625               H          CH3S                 H          CF2Cl               0
A626               H          CH3SO                H          CF2Cl               0
A627               H          CF3                  H          CF2Cl               0
A628               H          F2CH                 H          CF2Cl               0
A629               H          HCC                   H          CF2Cl               0
A630               H          CH3CC                H          CF2Cl               0
A631               H          CH2=CH              H          CF2Cl               0
A632               H          CH2=CHCH2          H          CF2Cl               0
A633               H          CH3SO2N(CH3)       H          CF2Cl               0
A634               H          (CH3)2N             H          CF2Cl               0
化合物序号          R2          R3              R4        R5           p
A635                H           (CH3)2NSO2     H          CF2Cl        0
A636                H           CH3SCH2         H          CF2Cl        0
A637                H           CH3SOCH2        H          CF2Cl        0
A638                H           CH3SO2CH2      H          CF2Cl        0
A639                H           CH3               H          CHF2         0
A640                H           CH3CH2          H          CHF2         0
A641                H           环丙基             H          CHF2         0
A642                H           (CH3)3C         H          CHF2         0
A643                H           (CH3)2CH        H          CHF2         0
A644                H           CH3(CH2)2      H          CHF2         0
A645                H           CH3OCH2         H          CHF2         0
A646                H           CH3O(CH2)2     H          CHF2         0
A647                H           Ph                 H          CHF2         0
A648                H           PhO                H          CHF2         0
A649                H           PhS                H          CHF2         0
A650                H           PhSO               H          CHF2         0
A651                H           PhSO2             H          CHF2         0
A652                H           CH3S              H          CHF2         0
A653                H           CH3SO             H          CHF2         0
A654                H           CF3               H          CHF2         0
A655                H           F2CH              H          CHF2         0
A656                H           HCC                H          CHF2         0
A657                H           CH3CC             H          CHF2         0
A658                H           CH2=CH           H          CHF2         0
A659                H           CH2=CHCH2       H          CHF2         0
A660                H           CH3SO2N(CH3)    H          CHF2         0
A661                H           (CH3)2N          H          CHF2         0
A662                H           (CH3)2NSO2      H          CHF2         0
A663                H           CH3SCH2          H          CHF2         0
A664                H           CH3SOCH2         H          CHF2         0
A665                H           CH3SO2CH2       H          CHF2         0
A666                H           CH3                H          CCl3         0
A667                H           CH3CH2           H          CCl3         0
化合物序号          R2         R3               R4             R5           p
A668                H           环丙基             H               CCl3         0
A669                H           (CH3)3C         H               CCl3         0
A670                H           (CH3)2CH        H               CCl3         0
A671                H           CH3(CH2)2      H               CCl3         0
A672                H           CH3OCH2         H               CCl3         0
A673                H           CH3O(CH2)2     H               CCl3         0
A674                H           Ph                 H               CCl3         0
A675                H           PhO                H               CCl3         0
A676                H           PhS                H               CCl3         0
A677                H           PhSO               H               CCl3         0
A678                H           PhSO2             H               CCl3         0
A679                H           CH3S              H               CCl3         0
A680                H           CH3SO             H               CCl3         0
A681                H           CF3               H               CCl3         0
A682                H           F2CH              H               CCl3         0
A683                H           HCC                H               CCl3         0
A684                H           CH3CC             H               CCl3         0
A685                H           CH2=CH           H               CCl3         0
A686                H           CH2=CHCH2       H               CCl3         0
A687                H           CH3SO2N(CH3)    H               CCl3         0
A688                H           (CH3)2N          H               CCl3         0
A689                H           (CH3)2NSO2      H               CCl3         0
A690                H           CH3SCH2          H               CCl3         0
A691                H           CH3SOCH2         H               CCl3         0
A692                H           CH3SO2CH2       H               CCl3         0
A693                H           CH3                CH3            CF3          0
A694                H           CH3CH2           CH3            CF3          0
A695                H           环丙基              CH3            CF3          0
A696                H           (CH3)3C          CH3            CF3          0
A697                H           (CH3)2CH         CH3            CF3          0
A698                H           CH3(CH2)2       CH3            CF3          0
A699                H           CH3OCH2          CH3            CF3          0
A700                H           CH3O(CH2)2      CH3            CF3          0
化合物序号           R2           R3                    R4              R5             p
A701                 H             Ph                     CH3             CF3             0
A702                 H             PhO                    CH3             CF3             0
A703                 H             PhS                    CH3             CF3             0
A704                 H             PhSO                   CH3             CF3             0
A705                 H             PhSO2                 CH3             CF3             0
A706                 H             CH3S                  CH3             CF3             0
A707                 H             CH3SO                 CH3             CF3             0
A708                 H             CF3                   CH3             CF3             0
A709                 H             F2CH                  CH3             CF3             0
A710                 H             HCC                    CH3             CF3             0
A711                 H             CH3CC                 CH3             CF3             0
A712                 H             CH2=CH               CH3             CF3             0
A713                 H             CH2=CHCH2           CH3             CF3             0
A714                 H             CH3SO2N(CH3)        CH3             CF3             0
A715                 H             (CH3)2N              CH3             CF3             0
A716                 H             (CH3)2NSO2          CH3             CF3             0
A717                 H             CH3SCH2              CH3             CF3             0
A718                 H             CH3SOCH2             CH3             CF3             0
A719                 H             CH3SO2CH2           CH3             CF3             0
A720                 H             CH3                    CH3             CF3CF2        0
A721                 H             CH3CH2                CH3             CF3CF2        0
A722                 H             环丙基                  CH3             CF3CF2         0
A723                 H             (CH3)3C              CH3             CF3CF2         0
A724                 H             (CH3)2CH             CH3             CF3CF2         0
A725                 H             CH3(CH2)2           CH3             CF3CF2         0
A726                 H             CH3OCH2              CH3             CF3CF2         0
A727                 H             CH3O(CH2)2          CH3             CF3CF2         0
A728                 H             Ph                      CH3             CF3CF2         0
A729                 H             PhO                     CH3             CF3CF2         0
A730                 H             PhS                     CH3             CF3CF2         0
A731                 H             PhSO                    CH3             CF3CF2         0
A732                 H             PhSO2                  CH3             CF3CF2         0
A733                 H             CH3S                   CH3             CF3CF2         0
化合物序号         R2         R3                     R4                R5                     p
A734               H           CH3SO                  CH3               CF3CF2                0
A735               H           CF3                    CH3               CF3CF2                0
A736               H           F2CH                   CH3               CF3CF2                0
A737               H           HCC                     CH3               CF3CF2                0
A738               H           CH3CC                  CH3               CF3CF2                0
A739               H           CH2=CH                CH3               CF3CF2                0
A740               H           CH2=CHCH2            CH3               CF3CF2                0
A741               H           CH3SO2N(CH3)         CH3               CF3CF2                0
A742               H           (CH3)2N               CH3               CF3CF2                0
A743               H           (CH3)2NSO2           CH3               CF3CF2                0
A744               H           CH3SCH2               CH3               CF3CF2                0
A745               H           CH3SOCH2              CH3               CF3CF2                0
A746               H           CH3SO2CH2            CH3               CF3CF2                0
A747               H           CH3                    CH3               CF3CF2CF2            0
A748               H           CH3CH2                CH3               CF3CF2CF2            0
A749               H           环丙基                   CH3               CF3CF2CF2            0
A750               H           (CH3)3C               CH3               CF3CF2CF2            0
A751               H           (CH3)2CH              CH3               CF3CF2CF2            0
A752               H           CH3(CH2)2            CH3               CF3CF2CF2            0
A753               H           CH3OCH2               CH3               CF3CF2CF2            0
A754               H           CH3O(CH2)2           CH3               CF3CF2CF2            0
A755               H           Ph                       CH3               CF3CF2CF2            0
A756               H           PhO                      CH3               CF3CF2CF2            0
A757               H           PhS                      CH3               CF3CF2CF2            0
A758               H           PhSO                     CH3               CF3CF2CF2            0
A759               H           PhSO2                   CH3               CF3CF2CF2            0
A760               H           CH3S                    CH3               CF3CF2CF2            0
A761               H           CH3SO                   CH3               CF3CF2CF2            0
A762               H           CF3                     CH3               CF3CF2CF2            0
A763               H           F2CH                    CH3               CF3CF2CF2            0
A764               H           HCC                      CH3               CF3CF2CF2            0
A765               H           CH3CC                   CH3               CF3CF2CF2            0
A766               H           CH2=CH                 CH3               CF3CF2CF2            0
化合物序号        R2       R3                R4              R5               p
A767              H         CH2=CHCH2       CH3             CF3CF2CF2     0
A768              H         CH3SO2N(CH3)    CH3             CF3CF2CF2     0
A769              H         (CH3)2N          CH3             CF3CF2CF2     0
A770              H         (CH3)2NSO2      CH3             CF3CF2CF2     0
A771              H         CH3SCH2          CH3             CF3CF2CF2     0
A772              H         CH3SOCH2         CH3             CF3CF2CF2     0
A773              H         CH3SO2CH2       CH3             CF3CF2CF2     0
A774              H         CH3                CH3             CF2Cl           0
A775              H         CH3CH2           CH3             CF2Cl            0
A776              H         环丙基              CH3             CF2Cl            0
A777              H         (CH3)3C          CH3             CF2Cl            0
A778              H         (CH3)2CH         CH3             CF2Cl            0
A779              H         CH3(CH2)2       CH3             CF2Cl            0
A780              H         CH3OCH2          CH3             CF2Cl            0
A781              H         CH3O(CH2)2      CH3             CF2Cl            0
A782              H         Ph                  CH3             CF2Cl            0
A783              H         PhO                 CH3             CF2Cl            0
A784              H         PhS                 CH3             CF2Cl            0
A785              H         PhSO                CH3             CF2Cl            0
A786              H         PhSO2              CH3             CF2Cl            0
A787              H         CH3S               CH3             CF2Cl            0
A788              H         CH3SO              CH3             CF2Cl            0
A789              H         CF3                CH3             CF2Cl            0
A790              H         F2CH               CH3             CF2Cl            0
A791              H         HCC                 CH3             CF2Cl            0
A792              H         CH3CC              CH3             CF2Cl            0
A793              H         CH2=CH            CH3             CF2Cl            0
A794              H         CH2=CHCH2        CH3             CF2Cl            0
A795              H         CH3SO2N(CH3)     CH3             CF2Cl            0
A796              H         (CH3)2N           CH3             CF2Cl            0
A797              H         (CH3)2NSO2       CH3             CF2Cl            0
A798              H         CH3SCH2           CH3             CF2Cl            0
A799              H         CH3SOCH2          CH3             CF2Cl            0
化合物序号       R2            R3                   R4          R5         p
A800             H              CH3SO2CH2         CH3         CF2Cl       0
A801             H              CH3                  CH3         CHF2        0
A802             H              CH3CH2             CH3         CHF2        0
A803             H              环丙基                CH3         CHF2        0
A804             H              (CH3)3C            CH3         CHF2        0
A805             H              (CH3)2CH           CH3         CHF2        0
A806             H              CH3(CH2)2         CH3         CHF2        0
A807             H              CH3OCH2            CH3         CHF2        0
A808             H              CH3O(CH2)2        CH3         CHF2        0
A809             H              Ph                    CH3         CHF2        0
A810             H              PhO                   CH3         CHF2        0
A811             H              PhS                   CH3         CHF2        0
A812             H              PhSO                  CH3         CHF2        0
A813             H              PhSO2                CH3         CHF2        0
A814             H              CH3S                 CH3         CHF2        0
A815             H              CH3SO                CH3         CHF2        0
A816             H              CF3                  CH3         CHF2        0
A817             H              F2CH                 CH3         CHF2        0
A818             H              HCC                   CH3         CHF2        0
A819             H              CH3CC                CH3         CHF2        0
A820             H              CH2=CH              CH3         CHF2        0
A821             H              CH2=CHCH2          CH3         CHF2        0
A822             H              CH3SO2N(CH3)       CH3         CHF2        0
A823             H              (CH3)2N             CH3         CHF2        0
A824             H              (CH3)2NSO2         CH3         CHF2        0
A825             H              CH3SCH2             CH3         CHF2        0
A826             H              CH3SOCH2            CH3         CHF2        0
A827             H              CH3SO2CH2          CH3         CHF2        0
A828             H              CH3                  CH3         CCl3        0
A829             H              CH3CH2              CH3         CCl3        0
A830             H              环丙基                 CH3         CCl3        0
A831             H              (CH3)3C             CH3         CCl3        0
A832             H              (CH3)2CH            CH3         CCl3        0
化合物序号          R2         R3              R4         R5         p
A833                H           CH3(CH2)2     CH3        CCl3       0
A834                H           CH3OCH2        CH3        CCl3       0
A835                H           CH3O(CH2)2    CH3        CCl3       0
A836                H           Ph                CH3        CCl3       0
A837                H           PhO               CH3        CCl3       0
A838                H           PhS               CH3        CCl3       0
A839                H           PhSO              CH3        CCl3       0
A840                H           PhSO2            CH3        CCl3       0
A841                H           CH3S             CH3        CCl3       0
A842                H           CH3SO            CH3        CCl3       0
A843                H           CF3              CH3        CCl3       0
A844                H           F2CH             CH3        CCl3       0
A845                H           HCC               CH3        CCl3       0
A846                H           CH3CC            CH3        CCl3       0
A847                H           CH2=CH          CH3        CCl3       0
A848                H           CH2=CHCH2      CH3        CCl3       0
A849                H           CH3SO2N(CH3)   CH3        CCl3       0
A850                H           (CH3)2N         CH3        CCl3       0
A851                H           (CH3)2NSO2     CH3        CCl3       0
A852                H           CH3SCH2         CH3        CCl3       0
A853                H           CH3SOCH2        CH3        CCl3       0
A854                H           CH3SO2CH2      CH3        CCl3       0
A855                H           CH3               Ph          CF3        0
A856                H           CH3CH2          Ph           CF3        0
A857                H           (CH3)2CH        Ph           CF3        0
A858                H           (CH3)2CH        Ph           CF3        0
A859                H           环丙基             Ph           CF3        0
A860                H           CH3(CH2)2      Ph           CF3        0
A861                H           CH3OCH2         Ph           CF3        0
A862                H           CH3O(CH2)2     Ph           CF3        0
A863                H           Ph                 Ph           CF3        0
A864                H           PhO                Ph           CF3        0
A865                H           PhS                Ph           CF3        0
化合物序号          R2         R3                  R4         R5              p
A866                H           PhSO                  Ph          CF3             0
A867                H           PhSO2                Ph          CF3             0
A868                H           CH3S                 Ph          CF3             0
A869                H           CH3SO                Ph          CF3             0
A870                H           CF3                  Ph          CF3             0
A871                H           F2CH                 Ph          CF3             0
A872                H           HCC                   Ph          CF3             0
A873                H           CH3CC                Ph          CF3             0
A874                H           CH2=CH              Ph          CF3             0
A875                H           CH2=CHCH2          Ph          CF3             0
A876                H           CH3SO2N(CH3)       Ph          CF3             0
A877                H           (CH3)2N             Ph          CF3             0
A878                H           (CH3)2NSO2         Ph          CF3             0
A879                H           CH3SCH2             Ph          CF3             0
A880                H           CH3SOCH2            Ph          CF3             0
A881                H           CH3SO2CH2          Ph          CF3             0
A882                H           CH3                   Ph          CF3CF2        0
A883                H           CH3CH2              Ph          CF3CF2         0
A884                H           环丙基                 Ph          CF3CF2         0
A885                H           (CH3)3C             Ph          CF3CF2         0
A886                H           (CH3)2CH            Ph          CF3CF2         0
A887                H           CH3(CH2)2          Ph          CF3CF2         0
A888                H           CH3OCH2             Ph          CF3CF2         0
A889                H           CH3O(CH2)2         Ph          CF3CF2         0
A890                H           Ph                     Ph          CF3CF2         0
A891                H           PhO                    Ph          CF3CF2         0
A892                H           PhS                    Ph          CF3CF2         0
A893                H           PhSO                   Ph          CF3CF2         0
A894                H           PhSO2                Ph          CF3CF2          0
A895                H           CH3S                 Ph          CF3CF2          0
A896                H           CH3SO                Ph          CF3CF2          0
A897                H           CF3                  Ph          CF3CF2          0
A898                H           F2CH                 Ph          CF3CF2          0
化合物序号       R2           R3                   R4         R5                 p
A899             H             HCC                    Ph          CF3CF2            0
A900             H             CH3CC                 Ph          CF3CF2            0
A901             H             CH2=CH               Ph          CF3CF2            0
A902             H             CH2=CHCH2          Ph          CF3CF2             0
A903             H             CH3SO2N(CH3)       Ph          CF3CF2             0
A904             H             (CH3)2N             Ph          CF3CF2             0
A905             H             (CH3)2NSO2         Ph          CF3CF2             0
A906             H             CH3SCH2             Ph          CF3CF2             0
A907             H             CH3SOCH2            Ph          CF3CF2             0
A908             H             CH3SO2CH2          Ph          CF3CF2             0
A909             H             CH3                  Ph          CF3CF2CF2         0
A910             H             CH3CH2              Ph          CF3CF2CF2         0
A911             H             环丙基                 Ph          CF3CF2CF2         0
A912             H             (CH3)3C             Ph          CF3CF2CF2         0
A913             H             (CH3)2CH            Ph          CF3CF2CF2         0
A914             H             CH3(CH2)2          Ph          CF3CF2CF2         0
A915             H             CH3OCH2             Ph          CF3CF2CF2         0
A916             H             CH3O(CH2)2         Ph          CF3CF2CF2         0
A917             H             Ph                     Ph          CF3CF2CF2         0
A918             H             PhO                    Ph          CF3CF2CF2         0
A919             H             PhS                    Ph          CF3CF2CF2         0
A920             H             PhSO                   Ph          CF3CF2CF2         0
A921             H             PhSO2                 Ph          CF3CF2CF2         0
A922             H             CH3S                  Ph          CF3CF2CF2         0
A923             H             CH3SO                 Ph          CF3CF2CF2         0
A924             H             CF3                   Ph          CF3CF2CF2         0
A925             H             F2CH                  Ph          CF3CF2CF2         0
A926             H             HCC                    Ph          CF3CF2CF2         0
A927             H             CH3CC                 Ph          CF3CF2CF2         0
A928             H             CH2=CH               Ph          CF3CF2CF2         0
A929             H             CH2=CHCH2           Ph          CF3CF2CF2        0
A930             H             CH3SO2N(CH3)        Ph          CF3CF2CF2        0
A931             H             (CH3)2N              Ph          CF3CF2CF2        0
化合物序号           R2        R3                  R4         R5           p
A932                 H          (CH3)2NSO2        Ph          CF3CF2CF2  0
A933                 H          CH3SCH2            Ph          CF3CF2CF2  0
A934                 H          CH3SOCH2           Ph          CF3CF2CF2  0
A935                 H          CH3SO2CH2         Ph          CF3CF2CF2  0
A936                 H          CH3                  Ph          CF2Cl        0
A937                 H          CH3CH2             Ph          CF2Cl         0
A938                 H          环丙基                Ph          CF2Cl         0
A939                 H          (CH3)3C            Ph          CF2Cl         0
A940                 H          (CH3)2CH           Ph          CF2Cl         0
A941                 H          CH3(CH2)2         Ph          CF2Cl         0
A942                 H          CH3OCH2            Ph          CF2Cl         0
A943                 H          CH3O(CH2)2        Ph          CF2Cl         0
A944                 H          Ph                    Ph          CF2Cl         0
A945                 H          PhO                   Ph          CF2Cl         0
A946                 H          PhS                   Ph          CF2Cl         0
A947                 H          PhSO                  Ph          CF2Cl         0
A948                 H          PhSO2                Ph          CF2Cl         0
A949                 H          CH3S                 Ph          CF2Cl         0
A950                 H          CH3SO                Ph          CF2Cl         0
A951                 H          CF3                  Ph          CF2Cl         0
A952                 H          F2CH                 Ph          CF2Cl         0
A953                 H          HCC                   Ph          CF2Cl         0
A954                 H          CH3CC                Ph          CF2Cl         0
A955                 H          CH2=CH              Ph          CF2Cl         0
A956                 H          CH2=CHCH2          Ph          CF2Cl         0
A957                 H          CH3SO2N(CH3)       Ph          CF2Cl         0
A958                 H          (CH3)2N             Ph          CF2Cl         0
A959                 H          (CH3)2NSO2         Ph          CF2Cl         0
A960                 H          CH3SCH2             Ph          CF2Cl         0
A961                 H          CH3SOCH2            Ph          CF2Cl         0
A962                 H          CH3SO2CH2          Ph          CF2Cl         0
A963                 H          CH3                   Ph          CHF2         0
A964                 H          CH3CH2              Ph          CHF2          0
化合物序号       R2         R3                 R4           R5         p
A965             H           (CH3)3C           Ph            CHF2       0
A966             H           (CH3)2CH          Ph            CHF2       0
A967             H           环丙基               Ph            CHF2       0
A968             H           CH3(CH2)2        Ph            CHF2       0
A969             H           CH3OCH2           Ph            CHF2       0
A970             H           CH3O(CH2)2       Ph            CHF2       0
A971             H           Ph                   Ph            CHF2       0
A972             H           PhO                  Ph            CHF2       0
A973             H           PhS                  Ph            CHF2       0
A974             H           PhSO                 Ph            CHF2       0
A975             H           PhSO2               Ph            CHF2       0
A976             H           CH3S                Ph            CHF2       0
A977             H           CH3SO               Ph            CHF2       0
A978             H           CF3                 Ph            CHF2       0
A979             H           F2CH                Ph            CHF2       0
A980             H           HCC                  Ph            CHF2       0
A981             H           CH3CC               Ph            CHF2       0
A982             H           CH2=CH             Ph            CHF2       0
A983             H           CH2=CHCH2         Ph            CHF2       0
A984             H           CH3SO2N(CH3)      Ph            CHF2       0
A985             H           (CH3)2N            Ph            CHF2       0
A986             H           (CH3)2NSO2        Ph            CHF2       0
A987             H           CH3SCH2            Ph            CHF2       0
A988             H           CH3SOCH2           Ph            CHF2       0
A989             H           CH3SO2CH2         Ph            CHF2       0
A990             H           CH3                 Ph            CCl3       0
A991             H           CH3CH2             Ph            CCl3       0
A992             H           (CH3)3C            Ph            CCl3       0
A993             H           (CH3)2CH           Ph            CCl3       0
A994             H           环丙基                Ph            CCl3       0
A995             H           CH3(CH2)2         Ph            CCl3       0
A996             H           CH3OCH2            Ph            CCl3       0
A997             H           CH3O(CH2)2        Ph            CCl3       0
化合物序号         R2                R3             R4        R5         p
A998               H                  Ph               Ph         CCl3       0
A999               H                  PhO              Ph         CCl3       0
A1000              H                  PhS              Ph         CCl3       0
A1001              H                  PhSO             Ph         CCl3       0
A1002              H                  PhSO2           Ph         CCl3       0
A1003              H                  CH3S            Ph         CCl3       0
A1004              H                  CH3SO           Ph         CCl3       0
A1005              H                  CF3             Ph         CCl3       0
A1006              H                  F2CH            Ph         CCl3       0
A1007              H                  HCC              Ph         CCl3       0
A1008              H                  CH3CC           Ph         CCl3       0
A1009              H                  CH2=CH         Ph         CCl3       0
A1010              H                  CH2=CHCH2     Ph         CCl3       0
A1011              H                  CH3SO2N(CH3)  Ph         CCl3       0
A1012              H                  (CH3)2N        Ph         CCl3       0
A1013              H                  (CH3)2NSO2    Ph         CCl3       0
A1014              H                  CH3SCH2        Ph         CCl3       0
A1015              H                  CH3SOCH2       Ph         CCl3       0
A1016              H                  CH3SO2CH2     Ph         CCl3       0
A1017              F                  H                 H          CF3        0
A1018              Cl                 H                 H          CF3        0
A1019              Br                 H                 H          CF3        0
A1020              NC                 H                 H          CF3        0
A1021              CH3SO2O          H                 H          CF3        0
A1022              CH3O              H                 H          CF3        0
A1023              CH3CH2O          H                 H          CF3        0
A1024              CH2CH=CH2O      H                 H          CF3        0
A1025              HCCCH2O           H                 H          CF3        0
A1026              PhCH2S            H                 H          CF3        0
A1027              PhCH2SO2         H                 H          CF3        0
A1028              ClCH2CH2         H                 H          CF3        0
A1029              BrCH2             H                 H          CF3        0
A1030              FCH2              H                 H          CF3        0
化合物序号     R2                         R3                  R4         R5         p
A1031          CHF2CH2                   H                    H           CF3        0
A1032          CF3CH2                    H                    H           CF3        0
A1033          [1,3]-咪唑-1-基甲基         H                    H           CF3        0
A1034          CHCl2CH2                  H                    H           CF3        0
A1035          ClCH=CH                     H                    H           CF3        0
A1036          Cl2C=CH                    H                    H           CF3        0
A1037          CF3CH=CH                   H                    H           CF3        0
A1038          ClCC                         H                    H           CF3        0
A1039          PhCH2                       H                    H           CF3        0
A1040          CH3CH2                     CH3                H           CF3        0
A1041          CH3                         OH                   H           CF3        0
A1042          CH3                         F                    H           CF3        0
A1043          CH3                         Cl                   H           CF3        0
A1044          F                            CH3                 H           CF3        0
A1045          Cl                           CH3                 H           CF3        0
A1046          H                            F                    H           CF3        0
A1047          H                            Cl                   H           CF3        0
A1048          H                            Br                   H           CF3        0
A1049          H                            OH                   H           CF3        0
A1050          H                            OCH3                H           CF3        0
A1051          H                            OCHF2               H           CF3        0
A1052          H                            OSO2CH3            H           CF3        0
A1053          H                            OSO2CF3            H           CF3        0
A1054          H                            ClCH2               H           CF3        0
A1055          H                            BrCH2               H           CF3        0
A1056          H                            FCH2                H           CF3        0
A1057          H                            CHF2CH2            H           CF3        0
A1058          H                            CF3CH2             H           CF3        0
A1059          H                            三唑基甲基           H           CF3         0
A1060          H                            CHCl2CH2          H           CF3         0
A1061          H                            ClCH=CH             H           CF3         0
A1062          H                            Cl2C=CH            H           CF3         0
A1063          H                            CF3CH=CH           H           CF3         0
化合物序号       R2                R3              R4             R5             p
A1064            H                  ClCC             H                CF3            0
A1065            H                  CH3C(O)         H                CF3            0
A1066            H                  Ph               H                CF3            0
A1067            H                  SO2CH3         H               CF3            O
A1068            H                  SO2CF3         H               CF3            0
A1069            H                  NC               H                CF3            0
A1070            H                  NO2             H                CF3            0
A1071            CH3               H                F                CF3            0
A1072            CH3               H                Cl               CF3            0
A1073            CH3               H                Br               CF3            0
A1074            CH3               H                NC               CF3            0
A1075            CH3               H                CH3O            CF3            0
A1076            CH3               H                CH3S            CF3            0
A1077            CH3               H                CH3SO           CF3            0
A1078            CH3               H                CH3SO2         CF3            0
A1079            CH3CH2OCH2     H                H                 CF3            0
A1080            PhOCH2            H                H                CF3            0
A1081                      H               H                 CF3            0
A1082            (CH3)2CH2OCH2 H               H                 CF3            0
A1083            BrCH2CH2         H               H                 CF3            0
A1084            FCH2CH2          H               H                 CF3            0
A1085            
Figure C9981578600912
        H               H                 CF3            0
A1086            
Figure C9981578600913
       H               H                 CF3            0
A1087            
Figure C9981578600914
      H               H                 CF3            0
A1088            
Figure C9981578600915
      H               H                 CF3            0
化合物序号            R2                       R3       R4         R5          p
A1089                 
Figure C9981578600921
           H         H           CF3         0
A1090                            H         H           CF3         0
A1091                 环丙基-CH2               H         H           CF3         0
A1092                 2,2-二氯环丙-1-基         H         H           CF3         0
A1093                 CH3OC(O)CH=CH           H         H           CF3         0
A1094                 CH3CH2OC(O)CH=CH       H         H           CF3         0
A1095                 ClCH2CH=CH              H         H           CF3         0
A1096                 CH=C=CH                 H         H           CF3         0
A1097                 (CH3)2NCH2            H         H           CF3         0
A1098                 HOCH2                    H         H           CF3         0
A1099                 CH3C(O)OCH2             H         H           CF3         0
A1100                 PhC(O)OCH2               H         H           CF3         0
A1101                 PhCH2CH2                H         H           CF3         0
A1102                 CH3OC(O)CH2             H         H           CF3         0
A1103                 NCCH2                    H         H           CF3         0
A1104                 CH3(CH2)7SCH2        H         H           CF3         0
A1105                 CH3(CH2)7SOCH2       H         H           CF3         0
A1106                 CH3(CH2)7SO2CH2     H         H           CF3         0
A1107                                H         H           CF3         0
A1108                 ClCH2CC                  H         H           CF3         0
A1109                 CHF2CH2CH2             H         H           CF3         0
A1110                 CHCl2CH2CH2            H         H           CF3         0
A1111                 CF3SO2O                 H         H           CF3         0
A1112                 
Figure C9981578600924
              H         H           CF3         0
A1113                 
Figure C9981578600925
             H         H           CF3         0
化合物序号   R2                   R3          R4        R5           p
A1114        
Figure C9981578600931
        H            H          CF3           0
A1115                     H            H          CF3           0
A1116                     H            H          CF3           0
A1117                     H            H          CF3           0
A1118        CH3ON=CHCH2        H            H          CF3           0
A1119        O=CHCH2             H            H          CF3           0
A1120        CH3CH2OCH2        H            H          CF2Cl         0
A1121        PhOCH2               H            H          CF2Cl         0
A1122                    H            H          CF2Cl         0
A1123        (CH3)2CH2OCH2    H            H          CF2Cl         0
A1124        BrCH2                H            H          CF2Cl         0
A1125        FCH2                 H            H          CF2Cl         0
A1126        
Figure C9981578600936
          H            H          CF2Cl         0
A1127                  H            H          CF2Cl         0
A1128                  H            H          CF2Cl         0
A1129                 H            H          CF2Cl         0
A1130        
Figure C99815786009310
       H            H          CF2Cl         0
A1131               H            H          CF2Cl         0
A1132        环丙基-CH2           H            H          CF2Cl         0
A1133        2,2-二氯环丙-1-基     H            H          CF2Cl         0
化合物序号        R2                     R3        R4         R5         p
A1134             CH3OC(O)CH=CH         H          H           CF2Cl       0
A1135             CH3CH2OC(O)CH=CH     H          H           CF2Cl       0
A1136             ClCH2CH=CH            H          H           CF2Cl       0
A1137             CH=C=CH               H          H           CF2Cl       0
A1138             (CH3)2NCH2          H          H           CF2Cl       0
A1139             HOCH2                  H          H           CF2Cl       0
A1140             CH3C(O)OCH2           H          H           CF2Cl       0
A1141             PhC(O)OCH2             H          H           CF2Cl       0
A1142             PhCH2                  H          H           CF2Cl       0
A1143             CH3OC(O)CH2           H          H           CF2Cl       0
A1144             NCCH2                  H          H           CF2Cl       0
A1145             CH3(CH2)7SCH2      H          H           CF2Cl       0
A1146             CH3(CH2)7SOCH2     H          H           CF2Cl       0
A1147             CH3(CH2)7SO2CH2   H          H           CF2Cl       0
A1148             
Figure C9981578600941
            H          H           CF2Cl       0
A1149             ClCH2CC                H          H           CF2Cl       0
A1150             Br                      H          H           CF2Cl       0
A1151             Cl                      H          H           CF2Cl       0
A1152             CF3SO2O              H          H           CF2Cl       0
A1153                         H          H           CF2Cl       0
A1154                         H          H           CF2Cl       0
A1155             
Figure C9981578600944
           H          H           CF2Cl       0
A1156             
Figure C9981578600945
               H          H           CF2Cl       0
A1157                             H          H           CF2Cl       0
A1158             
Figure C9981578600947
               H          H           CF2Cl       0
A1159             CH3ON=CHCH2          H          H           CF2Cl       0
化合物序号      R2                          R3        R4         R5            p
A1160           O=CHCH2                    H          H           CF2Cl          0
A1161           CH3CH2OCH2               H          H           CF2H           0
A1162           PhOCH2                      H          H           CF2H           0
A1163                               H          H           CF2H           0
A1164           (CH3)2CH2OCH2           H          H           CF2H           0
A1165           BrCH2                       H          H           CF2H           0
A1166           FCH2                        H          H           CF2H           0
A1167           
Figure C9981578600952
                H          H           CF2H           0
A1168           
Figure C9981578600953
                H          H           CF2H           0
A1169           
Figure C9981578600954
               H          H           CF2H           0
A1170                           H          H           CF2H           0
A1171           
Figure C9981578600956
           H          H           CF2H           0
A1172                         H          H           CF2H           0
A1173           环丙基-CH2                  H          H           CF2H           0
A1174           2,2-二氯环丙-1-基            H          H           CF2H           0
A1175           CH3OC(O)CH=CH              H          H           CF2H           0
A1176           CH3CH2OC(O)CH=CH          H          H           CF2H           0
A1177           ClCH2CH=CH                 H          H           CF2H           0
A1178           CH=C=CH                    H          H           CF2H           0
A1179           (CH3)2NCH2               H          H           CF2H           0
A1180           HOCH2                       H          H           CF2H           0
A1181           CH3C(O)OCH2                H          H           CF2H           0
A1182           PhC(O)OCH2                  H          H           CF2H           0
化合物序号         R2                    R3       R4       R5           p
A1183              PhCH2                 H          H         CF2H         0
A1184              CH3OC(O)CH2          H          H         CF2H         0
A1185              NCCH2                 H          H         CF2H         0
A1186              CH3(CH2)7SCH2     H          H         CF2H         0
A1187              CH3(CH2)7SOCH2    H          H         CF2H         0
A1188              CH3(CH2)7SO2CH2  H          H         CF2H         0
A1189              
Figure C9981578600961
           H          H         CF2H         0
A1190              ClCH2CC               H          H         CF2H         0
A1191              Br                     H          H         CF2H         0
A1192              Cl                     H          H         CF2H         0
A1193              CF3SO2O             H          H         CF2H         0
A1194              
Figure C9981578600962
           H          H         CF2H         0
A1195              
Figure C9981578600963
          H          H         CF2H         0
A1196                         H          H         CF2H         0
A1197              
Figure C9981578600965
              H          H         CF2H         0
A1198                             H          H         CF2H         0
A1199              
Figure C9981578600967
              H          H         CF2H         0
A1200              CH3ON=CHCH2         H          H         CF2H         0
A1201              O=CHCH2              H          H         CF2H         0
A1202              CH3CH=CH             H          H         CF3          0
A1203              CH3SO2NH             H          H         CF3          0
A1204              CH3CH2CH2O          H          CH3      CF3          0
A1205              Cl                      CH3       H         CF3          0
A1206              F2CHO                  H          H         CF3          0
A1207              CH3CH2C(O)OCH2      H          H         CF3          0
A1208              CH3CH2OC(O)OCH2     H          H         CF3          0
化合物序号        R2                       R3            R4         R5           p
A1209             CH3OCH2OCH2            H              H           CF3          0
A1210             CH3                      H              H           CF3          1
A1211             CH3CH2                  H              H           CF3          1
A1212             环丙基                     H              H           CF3          1
A1213             CH3(CH2)2             H              H           CF3          1
A1214             CH3OCH2                 H              H           CF3          1
A1215             CF3                      H              H           CF3          1
A1216             F2CH                     H              H           CF3          1
A1217             ClCH2                    H              H           CF3          1
A1218             CH3SO2CH2             H              H           CF3          1
A1219             CH3                      CF3           H           CH3          1
A1220             CH3CH2OCH2            H              H           CF3          1
A1221             PhOCH2                   H              H           CF3          1
A1222             (CH3)2CH2OCH2        H              H           CF3          1
A1223             BrCH2                    H              H           CF3          1
A1224             FCH2                     H              H           CF3          1
A1225             
Figure C9981578600971
            H              H           CF3          1
A1226             
Figure C9981578600972
          H              H           CF3          1
A1227             环丙基-CH2               H              H           CF3          1
A1228             2,2-二氯环丙-1-基         H              H           CF3          1
A1229             (CH3)2NCH2            H              H           CF3          1
A1230             HOCH2                    H              H           CF3          1
A1231             CH3C(O)OCH2             H              H           CF3          1
A1232             PhC(O)OCH2               H              H           CF3          1
A1233             PhCH2                    H              H           CF3          1
A1234             CH3OC(O)CH2             H              H           CF3          1
A1235             NCCH2                    H              H           CF3          1
A1236             CH3(CH2)7SO2CH2     H              H           CF3          1
A1237             Br                         H              H           CF3          1
化合物序号         R2                          R3        R4       R5             p
A1238              Cl                           H          H         CF3            1
A1239              O=CHCH2                    H          H         CF3            1
A1240              CH3                         H          H         CF2Cl          1
A1241              CH3CH2                     H          H         CF2Cl          1
A1242              环丙基                        H          H         CF2Cl          1
A1243              CH3(CH2)2                H          H         CF2Cl          1
A1244              CH3OCH2                    H          H         CF2Cl          1
A1245              CF3                         H          H         CF2Cl          1
A1246              F2CH                        H          H         CF2Cl          1
A1247              ClCH2                       H          H         CF2Cl          1
A1248              CH3SO2CH2                H          H         CF2Cl          1
A1249              CH3                         CF3       H         CF2Cl          1
A1250              CH3CH2OCH2               H          H         CF2Cl          1
A1251              PhOCH2                      H          H         CF2Cl          1
A1252              (CH3)2CH2OCH2           H          H         CF2Cl          1
A1253              BrCH2                       H          H         CF2Cl          1
A1254              FCH2                        H          H         CF2Cl          1
A1255                              H          H         CF2Cl          1
A1256                            H          H         CF2Cl          1
A1257              环丙基-CH2                  H          H         CF2Cl          1
A1258              2,2-二氯环丙-1-基            H          H         CF2Cl          1
A1259              (CH3)2NCH2               H          H         CF2Cl          1
A1260              HOCH2                       H          H         CF2Cl          1
A1261              CH3C(O)OCH2                H          H         CF2Cl          1
A1262              PhC(O)OCH2                  H          H         CF2Cl          1
A1263              PhCH2                       H          H         CF2Cl          1
A1264              CH3OC(O)CH2                H          H         CF2Cl          1
A1265              NCCH2                       H          H         CF2Cl          1
A1266              CH3(CH2)7SO2CH2        H          H         CF2Cl          1
化合物序号         R2                          R3         R4        R5         p
A1267              Br                           H           H          CF2Cl       1
A1268              Cl                           H           H          CF2Cl       1
A1269              O=CHCH2                    H           H          CF2Cl       1
A1270              CH3                         H           H          CF2H        1
A1271              CH3CH2                     H           H          CF2H        1
A1272              环丙基                        H           H          CF2H        1
A1273              CH3(CH2)2                 H           H          CF2H        1
A1274              CH3OCH2                    H           H          CF2H        1
A1275              CF3                         H           H          CF2H        1
A1276              F2CH                        H           H          CF2H        1
A1277              ClCH2                       H           H          CF2H        1
A1278              CH3SO2CH2                H           H          CF2H        1
A1279              CH3                         CF3        H          CF2H        1
A1280              CH3CH2OCH2               H           H          CF2H        1
A1281              PhOCH2                      H           H          CF2H        1
A1282              (CH3)2CH2OCH2           H           H          CF2H        1
A1283              BrCH2                       H           H          CF2H        1
A1284              FCH2                        H           H          CF2H        1
A1285              
Figure C9981578600991
                H           H         CF2H        1
A1286                            H           H         CF2H        1
A1287              环丙基-CH2                  H           H         CF2H        1
A1288              2,2-二氯环丙-1-基            H           H         CF2H        1
A1289              (CH3)2NCH2               H           H         CF2H        1
A1290              HOCH2                       H           H         CF2H        1
A1291              CH3C(O)OCH2                H           H         CF2H        1
A1292              PhC(O)OCH2                  H           H         CF2H        1
A1293              PhCH2                       H           H         CF2H        1
A1294              CH3OC(O)CH2                H           H         CF2H        1
A1295              NCCH2                       H           H         CF2H        1
化合物序号        R2                      R3           R4                  R5            p
A1296             CH3(CH2)7SO2CH2    H             H                    CF2H          1
A1297             Br                        H             H                    CF2H          1
A1298             Cl                        H             H                    CF2H          1
A1299             O=CHCH2                 H             H                    CF2H          1
A1300             CH3                      H             H                    CF3CF2      1
A1301             HO                        H             Ph                   CF3           0
A1302             CH3                      H             CH2=CH            CF3           0
A1303             CH3                      H             CH3CH2O           CF3          0
A1304             HO                        CH3          H                    CF3          0
A1305             HO                        H             H                    CF3          0
A1306             (CH3CH2)2N(O)CO       H             H                    CF3          0
A1307             CH3                      H             甲苯磺酰基-O         CF3          0
A1308             CH3                      H             CH3CC               CF3          0
A1309             CH3                      H             HCC                  CF3          0
A1310             CH3                      H             ClCH2CC             CF3          0
A1311             CH3                      H             PhCH2O              CF3          0
A1312             CH3                      H             CF3SO2O            CF3          0
A1313             CH3                      H             (CH3)2N            CF3          0
A1314             CH3                      H             CH3C(O)O            CF3          0
A1315             CH3                      H             CH3CH2C(O)O        CF3          0
A1316             CH3                      H             PhC(O)O              CF3           0
A1317             CH3                      H             3-吡啶基             CF3           0
A1318             CH3OCH2OCH2           H             H                    CF2Cl         0
A1319             CH3OCH2OCH2           H             H                    CF2H          0
A1320             CH3OCH2OCH2           H             H                    CF2CF3       0
A1321             CH3OCH2OCH2           H             H                    CF3           1
A1322             CH3O                     H             CH3                CF3           0
下表2中,Q为Q1
Figure C9981578601011
并且Q1代表下列基团B:
表2:基团B:
基团            R6               R7          R8       R9         R10         W
B1              H                  H            H         H           OH           CH2
B2              CH3               H            H         H           OH           CH2
B3              CH3CH2          H            H         H           OH           CH2
B4              CH3CH2CH2      H            H         H           OH           CH2
B5              (CH3)2CH        H            H         H           OH           CH2
B6              (CH3)3C         H            H         H           OH           CH2
B7              CH3S             H            H         H           OH           CH2
B8              CH3SO            H            H         H           OH           CH2
B9              CH3SO2          H            H         H           OH           CH2
B10             Ph                H            H         H           OH           CH2
B11             CH3O             H            H         H           OH           CH2
B12             CH3OC(O)         H            H         H           OH           CH2
B13             CH3CH2OC(O)     H            H         H           OH           CH2
B14             CH2=CHCH2      H            H         H           OH           CH2
B15             HCCCH2           H            H         H           OH           CH2
B16             CF3              H            H         H           OH           CH2
B17             (CH3)2NSO2    H            H         H           OH           CH2
B18             (CH3)2N        H            H         H           OH           CH2
B19             PhO               H            H         H           OH           CH2
B20             PhS               H            H         H           OH           CH2
B21             PhSO              H            H         H           OH           CH2
B22             PhSO2            H            H         H           OH           CH2
基团             R6                    R7         R8         R9         R10         W
B23              CN                     H            H           H           OH           CH2
B24              CH3                  CH3         H           H           OH           CH2
B25              CH3CH2              CH3         H           H           OH           CH2
B26              CH3CH2CH2          CH3         H           H           OH           CH2
B27              (CH3)2CH            CH3         H           H           OH           CH2
B28              (CH3)3C             CH3         H           H           OH           CH2
B29              CH3S                 CH3         H           H           OH           CH2
B30              CH3SO                CH3         H           H           OH           CH2
B31              CH3SO2              CH3         H           H           OH           CH2
B32              Ph                    CH3         H           H           OH           CH2
B33              CH3O                 CH3         H           H           OH           CH2
B34              CH3OC(O)             CH3         H           H           OH           CH2
B35              CH3CH2OC(O)         CH3         H           H           OH           CH2
B36              CH2=CHCH2          CH3         H           H           OH           CH2
B37              HCCCH2               CH3         H           H           OH           CH2
B38              CF3                  CH3         H           H           OH           CH2
B39              (CH3)2NSO2        CH3         H           H           OH           CH2
B40              (CH3)2N            CH3         H           H           OH           CH2
B41              PhO                   CH3         H           H           OH           CH2
B42              PhS                   CH3         H           H           OH           CH2
B43              PhSO                  CH3         H           H           OH           CH2
B44              PhSO2                CH3         H           H           OH           CH2
B45              CN                    CH3         H           H           OH           CH2
B46              CH3                  H            CH3        H           OH           CH2
B47              CH3CH2              H            CH3        H           OH           CH2
B48              CH3CH2CH2          H            CH3        H           OH           CH2
B49              (CH3)2CH            H            CH3        H           OH           CH2
B50              (CH3)3C             H            CH3        H           OH           CH2
B51              CH3S                 H            CH3        H           OH           CH2
B52              CH3SO                H            CH3        H           OH           CH2
B53              CH3SO2              H            CH3        H           OH           CH2
B54              Ph                    H            CH3        H           OH           CH2
B55              CH3O                 H            CH3        H           OH           CH2
基团               R6                 R7           R8           R9       R10        W
B56                CH3OC(O)           H             CH3          H          OH          CH2
B57                CH3CH2OC(O)       H             CH3          H          OH          CH2
B58                CH2=CHCH2        H             CH3          H          OH          CH2
B59                HCCCH2             H             CH3          H          OH          CH2
B60                CF3                H             CH3          H          OH          CH2
B61                (CH3)2NSO2      H             CH3          H          OH          CH2
B62                (CH3)2N          H             CH3          H          OH          CH2
B63                PhO                 H             CH3          H          OH          CH2
B64                PhS                 H             CH3          H          OH          CH2
B65                PhSO                H             CH3          H          OH          CH2
B66                PhSO2              H             CH3          H          OH          CH2
B67                CN                  H             CH3          H          OH          CH2
B68                CH3               CH3          CH3          H          OH          CH2
B69                CH3CH2           CH3          CH3          H          OH          CH2
B70                CH3CH2CH2       CH3          CH3          H          OH          CH2
B71                (CH3)2CH         CH3          CH3          H          OH          CH2
B72                (CH3)3C          CH3          CH3          H          OH          CH2
B73                CH3S              CH3          CH3          H          OH          CH2
B74                CH3SO             CH3          CH3          H          OH          CH2
B 75              CH3SO2           CH3          CH3          H          OH          CH2
B76                Ph                 CH3          CH3          H          OH          CH2
B77                CH3O              CH3          CH3          H          OH          CH2
B78                CH3OC(O)          CH3          CH3          H          OH          CH2
B79                CH3CH2OC(O)      CH3          CH3          H          OH          CH2
B80                CH2=CHCH2       CH3          CH3          H          OH          CH2
B81                HCCCH2            CH3          CH3          H          OH          CH2
B82                CF3               CH3          CH3          H          OH          CH2
B83                (CH3)2NSO2     CH3          CH3          H          OH          CH2
B84                (CH3)2N         CH3          CH3          H          OH          CH2
B85                PhO                CH3          CH3          H          OH          CH2
B86                PhS                CH3          CH3          H          OH          CH2
B87                PhSO               CH3          CH3          H          OH          CH2
B88                PhSO2             CH3          CH3          H          OH          CH2
基团              R6                    R7              R8             R9          R10       W
B89               CN                     CH3              CH3           H             OH        CH2
B90               CH3                   CH3              CH3           CH3          OH        CH2
B91               CH3CH2               CH3              CH3           CH3          OH        CH2
B92               CH3CH2CH2          CH3              CH3           CH3           OH        CH2
B93               (CH3)2CH            CH3              CH3           CH3           OH        CH2
B94               (CH3)3C             CH3              CH3           CH3           OH        CH2
B95               CH3S                 CH3              CH3           CH3           OH        CH2
B96               CH3SO                CH3              CH3           CH3           OH        CH2
B97               CH3SO2              CH3              CH3           CH3           OH        CH2
B98               Ph                    CH3              CH3           CH3           OH        CH2
B99               CH3O                 CH3              CH3           CH3           OH        CH2
B100              CH3OC(O)             CH3              CH3           CH3           OH        CH2
B101              CH3CH2OC(O)         CH3              CH3           CH3           OH        CH2
B102              CH2=CHCH2          CH3              CH3           CH3           OH        CH2
B103              HCCCH2               CH3              CH3           CH3           OH        CH2
B104              CF3                  CH3              CH3           CH3           OH        CH2
B105              (CH3)2NSO2         CH3              CH3           CH3           OH        CH2
B106              (CH3)2N             CH3              CH3           CH3           OH        CH2
B107              PhO                   CH3              CH3           CH3           OH        CH2
B108              PhS                   CH3              CH3           CH3           OH        CH2
B109              PhSO                  CH3              CH3           CH3           OH        CH2
B110              PhSO2                CH3              CH3           CH3           OH        CH2
B111              CN                    CH3              CH3           CH3           OH        CH2
B112              CH3CH2             CH3CH2          H              H               OH        CH2
B113              CH3CH2CH2         CH3CH2          H              H               OH        CH2
B114              (CH3)2CH           CH3CH2          H              H               OH        CH2
B115              (CH3)3C            CH3CH2          H              H               OH        CH2
B116              CH3S                CH3CH2          H              H               OH        CH2
B117              CH3SO               CH3CH2          H              H               OH        CH2
B118              CH3SO2             CH3CH2          H              H               OH        CH2
B119              Ph                   CH3CH2          H              H                OH        CH2
B120              CH3O                CH3CH2          H              H               OH        CH2
B121              CH3OC(O)            CH3CH2          H              H               OH        CH2
基团         R6                   R7           R8          R9       R10       W
B122         CH3CH2OC(O)         CH3CH2      H            H         OH         CH2
B123         CH2=CHCH2          CH3CH2      H            H         OH         CH2
B124         HCCCH2               CH3CH2      H            H         OH         CH2
B125         CF3                  CH3CH2      H            H         OH         CH2
B126         (CH3)2NSO2        CH3CH2      H            H         OH         CH2
B127         (CH3)2N            CH3CH2      H            H         OH         CH2
B128         PhO                   CH3CH2      H            H         OH         CH2
B129         PhS                   CH3CH2      H            H         OH         CH2
B130         PhSO                  CH3CH2      H            H         OH         CH2
B131         PhSO2                CH3CH2      H            H         OH         CH2
B132         CN                    CH3CH2      H            H         OH         CH2
B133         H                     H             H            H         OH         CHCH3
B134         CH3                  H             H            H         OH         CHCH3
B135         CH3CH2              H             H            H         OH         CHCH3
B136         CH3CH2CH2          H             H            H         OH         CHCH3
B137         (CH3)2CH            H             H            H         OH         CHCH3
B138         (CH3)3C             H             H            H         OH         CHCH3
B139         CH3S                 H             H            H         OH         CHCH3
B140         CH3SO                H             H            H         OH         CHCH3
B141         CH3SO2              H             H            H         OH         CHCH3
B142         Ph                    H             H            H         OH         CHCH3
B143         CH3O                 H             H            H         OH         CHCH3
B144         CH3OC(O)             H             H            H         OH         CHCH3
B145         CH3CH2OC(O)         H             H            H         OH         CHCH3
B146         CH2=CHCH2          H             H            H         OH         CHCH3
B147         HCCCH2               H             H            H         OH         CHCH3
B148         CF3                  H             H            H         OH         CHCH3
B149         (CH3)2NSO2        H             H            H         OH         CHCH3
B150         (CH3)2N            H             H            H         OH         CHCH3
B151         PhO                   H             H            H         OH         CHCH3
B152         PhS                   H             H            H         OH         CHCH3
B153         PhSO                  H             H            H         OH         CHCH3
B154         PhSO2                H             H            H         OH         CHCH3
基团           R6                    R7          R8        R9      R10     W
B155           CN                     H             H          H        OH       CHCH3
B156           CH3                   CH3         H          H        OH       CHCH3
B157           CH3CH2               CH3         H          H        OH       CHCH3
B158           CH3CH2CH2           CH3         H          H        OH       CHCH3
B159           (CH3)2CH             CH3         H          H        OH       CHCH3
B160           (CH3)3C              CH3         H          H        OH       CHCH3
B161           CH3S                  CH3         H          H        OH       CHCH3
B162           CH3SO                 CH3         H          H        OH       CHCH3
B163           CH3SO2               CH3         H          H        OH       CHCH3
B164           Ph                     CH3         H          H        OH       CHCH3
B165           CH3O                  CH3         H          H        OH       CHCH3
B166           CH3OC(O)              CH3         H          H        OH       CHCH3
B167           CH3CH2OC(O)          CH3         H          H        OH       CHCH3
B168           CH2=CHCH2           CH3         H          H        OH       CHCH3
B169           HCCCH2                CH3         H          H        OH       CHCH3
B170           CF3                   CH3         H          H        OH       CHCH3
B171           (CH3)2NSO2          CH3         H          H        OH       CHCH3
B172           (CH3)2N              CH3         H          H        OH       CHCH3
B173           PhO                    CH3         H          H        OH       CHCH3
B174           PhS                    CH3         H          H        OH       CHCH3
B175           PhSO                   CH3         H          H        OH       CHCH3
B176           PhSO2                 CH3         H          H        OH       CHCH3
B177           CN                     CH3         H          H        OH       CHCH3
B178           CH3                   H            CH3       H        OH       CHCH3
B179           CH3CH2              H            CH3       H        OH       CHCH3
B180           CH3CH2CH2          H            CH3       H        OH       CHCH3
B181           (CH3)2CH            H            CH3       H        OH       CHCH3
B182           (CH3)3C             H            CH3       H        OH       CHCH3
B183           CH3S                 H            CH3       H        OH       CHCH3
B184           CH3SO                H            CH3       H        OH       CHCH3
B185           CH3SO2              H            CH3       H        OH       CHCH3
B186           Ph                     H            CH3       H        0H       CHCH3
B187           CH3O                  H            CH3       H        OH       CHCH3
基团            R6                   R7           R8          R9         R10       W
B188            CH3OC(O)             H             CH3         H           OH         CHCH3
B189            CH3CH2OC(O)         H             CH3         H           OH         CHCH3
B190            CH2=CHCH2          H             CH3         H           OH         CHCH3
B191            HCCCH2               H             CH3         H           OH         CHCH3
B192            CF3                  H             CH3         H           OH         CHCH3
B193            (CH3)2NSO2         H             CH3         H           OH         CHCH3
B194            (CH3)2N             H             CH3         H           OH         CHCH3
B195            PhO                    H             CH3         H           OH         CHCH3
B196            PhS                    H             CH3         H           OH         CHCH3
B197            PhSO                   H             CH3         H           OH         CHCH3
B198            PhSO2                 H             CH3         H           OH         CHCH3
B199            CN                     H             CH3         H           OH         CHCH3
B200            CH3                  CH3          CH3         H           OH         CHCH3
B201            CH3CH2              CH3          CH3         H           OH         CHCH3
B202            CH3CH2CH2          CH3          CH3         H           OH         CHCH3
B203            (CH3)2CH            CH3          CH3         H           OH         CHCH3
B204            (CH3)3C             CH3          CH3         H           OH         CHCH3
B205            CH3S                 CH3          CH3         H           OH         CHCH3
B206            CH3SO                CH3          CH3         H           OH         CHCH3
B207            CH3SO2              CH3          CH3         H           OH         CHCH3
B208            Ph                    CH3          CH3         H           OH         CHCH3
B209            CH3O                 CH3          CH3         H           OH         CHCH3
B210            CH3OC(O)             CH3          CH3         H           OH         CHCH3
B211            CH3CH2OC(O)         CH3          CH3         H           OH         CHCH3
B212            CH2=CHCH2          CH3          CH3         H           OH         CHCH3
B213            HCCCH2               CH3          CH3         H           OH         CHCH3
B214            CF3                  CH3          CH3         H           OH         CHCH3
B215            (CH3)2NSO2        CH3          CH3         H           OH         CHCH3
B216            (CH3)2N            CH3          CH3         H           OH         CHCH3
B217            PhO                   CH3          CH3         H           OH         CHCH3
B218            PhS                   CH3          CH3         H           OH         CHCH3
B219            PhSO                  CH3          CH3         H           OH         CHCH3
B220            PhSO2                CH3          CH3         H           OH         CHCH3
基团             R6                  R7             R8         R9          R10        W
B221             CN                   CH3            CH3        H             OH          CHCH3
B222             CH3                 CH3            CH3        CH3         OH          CHCH3
B223             CH3CH2             CH3            CH3        CH3         OH          CHCH3
B224             CH3CH2CH2         CH3            CH3        CH3         OH          CHCH3
B225             (CH3)2CH           CH3            CH3        CH3         OH          CHCH3
B226             (CH3)3C            CH3            CH3        CH3         OH          CHCH3
B227             CH3S                CH3            CH3        CH3         OH          CHCH3
B228             CH3SO               CH3            CH3        CH3         OH          CHCH3
B229             CH3SO2             CH3            CH3        CH3         OH          CHCH3
B230             Ph                   CH3            CH3        CH3         OH          CHCH3
B231             CH3O                CH3            CH3        CH3         OH          CHCH3
B232             CH3OC(O)            CH3            CH3        CH3         OH          CHCH3
B233             CH3CH2OC(O)        CH3            CH3        CH3         OH          CHCH3
B234             CH2=CHCH2         CH3            CH3        CH3         OH          CHCH3
B235             HCCCH2              CH3            CH3        CH3         OH          CHCH3
B236             CF3                 CH3            CH3        CH3         OH          CHCH3
B237             (CH3)2NSO2        CH3            CH3        CH3         OH          CHCH3
B238             (CH3)2N            CH3            CH3        CH3         OH          CHCH3
B239             PhO                   CH3            CH3        CH3         OH          CHCH3
B240             PhS                   CH3            CH3        CH3         OH          CHCH3
B241             PhSO                  CH3            CH3        CH3         OH          CHCH3
B242             PhSO2                CH3            CH3        CH3         OH          CHCH3
B243             CN                    CH3            CH3        CH3         OH          CHCH3
B244             CH3CH2             CH3CH2        H           H            OH          CHCH3
B245             CH3CH2CH2         CH3CH2        H           H            OH          CHCH3
B246             (CH3)2CH           CH3CH2        H           H            OH          CHCH3
B247             (CH3)3C            CH3CH2        H           H            OH          CHCH3
B248             CH3S                CH3CH2        H           H            OH          CHCH3
B249             CH3SO               CH3CH2        H           H            OH          CHCH3
B250             CH3SO2             CH3CH2        H           H            OH          CHCH3
B251             Ph                    CH3CH2        H           H            OH          CHCH3
B252             CH3O                CH3CH2        H           H            OH          CHCH3
B253             CH3OC(O)            CH3CH2        H           H            OH          CHCH3
基团          R6                   R7           R8      R9        R10      W
B254          CH3CH2OC(O)         CH3CH2      H        H          OH        CHCH3
B255          CH2=CHCH2          CH3CH2      H        H          OH        CHCH3
B256          HCCCH2               CH3CH2      H        H          OH        CHCH3
B257          CF3                  CH3CH2      H        H          OH        CHCH3
B258          (CH3)2NSO2        CH3CH2      H        H          OH        CHCH3
B259          (CH3)2N            CH3CH2      H        H          OH        CHCH3
B260          PhO                   CH3CH2      H        H          OH        CHCH3
B261          PhS                   CH3CH2      H        H          OH        CHCH3
B262          PhSO                  CH3CH2      H        H          OH        CHCH3
B263          PhSO2                CH3CH2      H        H          OH        CHCH3
B264          CN                    CH3CH2      H        H          OH        CHCH3
B265          H                     H             H        H           OH        C=O
B266          CH3                  H             H        H           OH        C=O
B267          CH3CH2              H             H        H          OH        C=O
B268          CH3CH2CH2          H             H        H          OH        C=O
B269          (CH3)2CH            H             H        H          OH        C=O
B270          (CH3)3C             H             H        H          OH        C=O
B271          CH3S                 H             H        H          OH        C=O
B272          CH3SO                H             H        H          OH        C=O
B273          CH3SO2              H             H        H          OH        C=O
B274          Ph                    H             H        H          OH        C=O
B275          CH3O                 H             H        H          OH        C=O
B276          CH3OC(O)             H             H        H          OH        C=O
B277          CH3CH2OC(O)         H             H        H          OH        C=O
B278          CH2=CHCH2          H             H        H          OH        C=O
B279          HCCCH2               H             H        H          OH        C=O
B280          CF3                  H             H        H          OH        C=O
B281          (CH3)2NSO2         H             H        H          OH        C=O
B282          (CH3)2N             H             H        H          OH        C=O
B283          PhO                    H             H        H          OH        C=O
B284          PhS                    H             H        H          OH        C=O
B285          PhSO                   H             H        H          OH        C=O
B286          PhSO2                 H             H        H          OH        C=O
基团            R6               R7            R8        R9       R10        W
B287            CN                H               H          H          OH         C=O
B288            CH3              CH3           H          H          OH         C=O
B289            CH3CH2          CH3           H          H          OH         C=O
B290            CH3CH2CH2      CH3           H          H          OH         C=O
B291            (CH3)2CH        CH3           H          H          OH         C=O
B292            (CH3)3C         CH3           H          H          OH         C=O
B293            CH3S             CH3           H          H          OH         C=O
B294            CH3SO            CH3           H          H          OH         C=O
B295            CH3SO2          CH3           H          H          OH         C=O
B296            Ph                CH3           H          H          OH         C=O
B297            CH3O             CH3           H          H          OH         C=O
B298            CH3OC(O)         CH3           H          H          OH         C=O
B299            CH3CH2OC(O)     CH3           H          H          OH         C=O
B300            CH2=CHCH2      CH3           H          H          OH         C=O
B301            HCCCH2           CH3           H          H          OH         C=O
B302            CF3              CH3           H          H          OH         C=O
B303            (CH3)2NSO2     CH3           H          H          OH         C=O
B304            (CH3)2N         CH3           H          H          OH         C=O
B305            PhO                CH3           H          H          OH         C=O
B306            PhS                CH3           H          H          OH         C=O
B307            PhSO               CH3           H          H          OH         C=O
B308            PhSO2             CH3           H          H          OH         C=O
B309            CN                 CH3           H          H          OH         C=O
B310            CH3               H              CH3       H          OH         C=O
B311            CH3CH2           H              CH3       H          OH         C=O
B312            CH3CH2CH2      H              CH3       H          OH         C=O
B313            (CH3)2CH        H              CH3       H          OH         C=O
B314            (CH3)3C         H              CH3       H          OH         C=O
B315            CH3S             H              CH3       H          OH         C=O
B316            CH3SO            H              CH3       H          OH         C=O
B317            CH3SO2          H              CH3       H          OH         C=O
B318            Ph                 H              CH3       H          OH         C=O
B319            CH3O             H              CH3       H          OH         C=O
基团             R6                  R7            R8          R9      R10       W
B320             CH3OC(O)            H              CH3         H         OH         C=O
B321             CH3CH2OC(O)        H              CH3         H         OH         C=O
B322             CH2=CHCH2         H              CH3         H         OH         C=O
B323             HCCCH2              H              CH3         H         OH         C=O
B324             CF3                 H              CH3         H         OH         C=O
B325             (CH3)2NSO2        H              CH3         H         OH         C=O
B326             (CH3)2N            H              CH3         H         OH         C=O
B327             PhO                   H              CH3         H         OH         C=O
B328             PhS                   H              CH3         H         OH         C=O
B329             PhSO                  H              CH3         H         OH         C=O
B330             PhSO2                H              CH3         H         OH         C=O
B331             CN                    H              CH3         H         OH         C=O
B332             CH3                 CH3           CH3         H         OH         C=O
B333             CH3CH2             CH3           CH3         H         OH         C=O
B334             CH3CH2CH2         CH3           CH3         H         OH         C=O
B335             (CH3)2CH           CH3           CH3         H         OH         C=O
B336             (CH3)3C            CH3           CH3         H         OH         C=O
B337             CH3S                CH3           CH3         H         OH         C=O
B338             CH3SO               CH3           CH3         H         OH         C=O
B339             CH3SO2             CH3           CH3         H         OH         C=O
B340             Ph                   CH3           CH3         H         OH         C=O
B341             CH3O                CH3           CH3         H         OH         C=O
B342             CH3OC(O)            CH3           CH3         H         OH         C=O
B343             CH3CH2OC(O)        CH3           CH3         H         OH         C=O
B344             CH3=CHCH2         CH3           CH3         H         OH         C=O
B345             HCCCH2              CH3           CH3         H         OH         C=O
B346             CF3                 CH3           CH3         H         OH         C=O
B347             (CH3)2NSO2        CH3           CH3         H         OH         C=O
B348             (CH3)2N            CH3           CH3         H         OH         C=O
B349             PhO                   CH3           CH3         H         OH         C=O
B350             PhS                   CH3           CH3         H         OH         C=O
B351             PhSO                  CH3           CH3         H         OH         C=O
B352             PhSO2                CH3           CH3         H         OH         C=O
基团            R6                 R7              R8           R9            R10          W
B353            CN                  CH3             CH3          H               OH            C=O
B354            CH3                CH3             CH3          CH3           OH            C=O
B355            CH3CH2            CH3             CH3          CH3           OH            C=O
B356            CH3CH2CH2        CH3             CH3          CH3           OH            C=O
B357            (CH3)2CH          CH3             CH3          CH3           OH            C=O
B358            (CH3)3C           CH3             CH3          CH3           OH            C=O
B359            CH3S               CH3             CH3          CH3           OH            C=O
B360            CH3SO              CH3             CH3          CH3           OH            C=O
B361            CH3SO2            CH3             CH3          CH3           OH            C=O
B362            Ph                  CH3             CH3          CH3           OH            C=O
B363            CH3O               CH3             CH3          CH3           OH            C=O
B364            CH3OC(O)           CH3             CH3          CH3           OH            C=O
B365            CH3CH2OC(O)       CH3             CH3          CH3           OH            C=O
B366            CH2=CHCH2        CH3             CH3          CH3           OH            C=O
B367            HCCCH2             CH3             CH3          CH3           OH            C=O
B368            CF3                CH3             CH3          CH3           OH            C=O
B369            (CH3)2NSO2       CH3             CH3          CH3           OH            C=O
B370            (CH3)2N           CH3             CH3          CH3           OH            C=O
B371            PhO                  CH3             CH3          CH3           OH            C=O
B372            PhS                  CH3             CH3          CH3           OH            C=O
B373            PhSO                 CH3             CH3          CH3           OH            C=O
B374            PhSO2               CH3             CH3          CH3           OH            C=O
B375            CN                   CH3             CH3          CH3           OH            C=O
B376            CH3CH2            CH3CH2         H             H               OH            C=O
B377            CH3CH2CH2        CH3CH2         H             H               OH            C=O
B378            (CH3)2CH          CH3CH2         H             H               OH            C=O
B379            (CH3)3C           CH3CH2         H             H               OH            C=O
B380            CH3S               CH3CH2         H             H               OH            C=O
B381            CH3SO              CH3CH2         H             H               OH            C=O
B382            CH3SO2            CH3CH2         H             H               OH            C=O
B383            Ph                  CH3CH2         H             H               OH            C=O
B384            CH3O               CH3CH2         H             H               OH            C=O
B385            CH3OC(O)           CH3CH2         H             H               OH            C=O
基团           R6                   R7             R8          R9          R10          W
B386           CH3CH2OC(O)         CH3CH2        H            H            OH            C=O
B387           CH2=CHCH2          CH3CH2        H            H            OH            C=O
B388           HCCCH2               CH3CH2        H            H            OH            C=O
B389           CF3                  CH3CH2        H            H            OH            C=O
B390           (CH3)2NSO2         CH3CH2        H            H            OH            C=O
B391           (CH3)2N             CH3CH2        H            H            OH            C=O
B392           PhO                   CH3CH2        H            H            OH            C=O
B393           PhS                   CH3CH2        H            H            OH            C=O
B394           PhSO                  CH3CH2        H            H            OH            C=O
B395           PhSO2                CH3CH2        H            H            OH            C=O
B396           CN                    CH3CH2        H            H            OH            C=O
B397           H                     H                H            H            OH            N-CH3
B398           CH3                  H                H            H            OH            N-CH3
B399           CH3CH2              H                H            H            OH            N-CH3
B400           CH3CH2CH2          H                H            H            OH            N-CH3
B401           (CH3)2CH            H                H            H            OH            N-CH3
B402           (CH3)3C             H                H            H            OH            N-CH3
B403           CH3S                 H                H            H            OH            N-CH3
B404           CH3SO                H                H            H            OH            N-CH3
B405           CH3SO2              H                H            H            OH            N-CH3
B406           Ph                    H                H            H            OH            N-CH3
B407           CH3O                 H                H            H            OH            N-CH3
B408           CH3OC(O)             H                H            H            OH            N-CH3
B409           CH3CH2OC(O)         H                H            H            OH            N-CH3
B410           CH2=CHCH2          H                H            H            OH            N-CH3
B411           HCCCH2               H                H            H            OH            N-CH3
B412           CF3                  H                H            H            OH            N-CH3
B413           (CH3)2NSO2        H                H            H            OH            N-CH3
B414           (CH3)2N            H                H            H            OH            N-CH3
B415           PhO                   H                H            H            OH            N-CH3
B416           PhS                   H                H            H            OH            N-CH3
B417           PhSO                  H                H            H            OH            N-CH3
B418           PhSO2                H                H            H            OH            N-CH3
基团           R6                  R7            R8          R9         R10          W
B419           CN                   H               H            H           OH            N-CH3
B420           CH3                 CH3           H            H           OH            N-CH3
B421           CH3CH2            CH3            H            H           OH            N-CH3
B422           CH3CH2CH2        CH3            H            H           OH            N-CH3
B423           (CH3)2CH          CH3            H            H           OH            N-CH3
B424           (CH3)3C           CH3            H            H           OH            N-CH3
B425           CH3S               CH3            H            H           OH            N-CH3
B426           CH3SO              CH3            H            H           OH            N-CH3
B427           CH3SO2            CH3            H            H           OH            N-CH3
B428           Ph                  CH3            H            H           OH            N-CH3
B429           CH3O               CH3            H            H           OH            N-CH3
B430           CH3OC(O)           CH3            H            H           OH            N-CH3
B431           CH3CH2OC(O)       CH3            H            H           OH            N-CH3
B432           CH2=CHCH2        CH3            H            H           OH            N-CH3
B433           HCCCH2             CH3            H            H           OH            N-CH3
B434           CF3                CH3            H            H           OH            N-CH3
B435           (CH3)2NSO2      CH3            H            H           OH            N-CH3
B436           (CH3)2N          CH3            H            H           OH            N-CH3
B437           PhO                 CH3            H            H           OH            N-CH3
B438           PhS                 CH3            H            H           OH            N-CH3
B439           PhSO                CH3            H            H           OH            N-CH3
B440           PhSO2              CH3            H            H           OH            N-CH3
B441           CN                  CH3            H            H           OH            N-CH3
B442           CH3                H               CH3         H           OH            N-CH3
B443           CH3CH2           H               CH3         H           OH            N-CH3
B444           CH3CH2CH2       H               CH3         H           OH            N-CH3
B445           (CH3)2CH         H               CH3         H           OH            N-CH3
B446           (CH3)3C          H               CH3         H           OH            N-CH3
B447           CH3S              H               CH3         H           OH            N-CH3
B448           CH3SO             H               CH3         H           OH            N-CH3
B449           CH3SO2           H               CH3         H           OH            N-CH3
B450           Ph                 H               CH3         H           OH            N-CH3
B451           CH3O              H               CH3         H           OH            N-CH3
基团           R6                  R7             R8           R9         R10         W
B452           CH3OC(O)            H               CH3           H           OH          N-CH3
B453           CH3CH2OC(O)        H               CH3           H           OH          N-CH3
B454           CH2=CHCH2         H               CH3           H           OH          N-CH3
B455           HCCCH2              H               CH3           H           OH          N-CH3
B456           CF3                 H               CH3           H           OH          N-CH3
B457           (CH3)2NSO2       H               CH3           H           OH          N-CH3
B458           (CH3)2N           H               CH3           H           OH          N-CH3
B459           PhO                  H               CH3           H           OH          N-CH3
B460           PhS                  H               CH3           H           OH          N-CH3
B461           PhSO                 H               CH3           H           OH          N-CH3
B462           PhSO2               H               CH3           H           OH          N-CH3
B463           CN                   H               CH3           H           OH          N-CH3
B464           CH3                 CH3            CH3           H           OH          N-CH3
B465           CH3CH2            CH3            CH3           H           OH          N-CH3
B466           CH3CH2CH2        CH3            CH3           H           OH          N-CH3
B467           (CH3)2CH          CH3            CH3           H           OH          N-CH3
B468           (CH3)3C           CH3            CH3           H           OH          N-CH3
B469           CH3S               CH3            CH3           H           OH          N-CH3
B470           CH3SO              CH3            CH3           H           OH          N-CH3
B471           CH3SO2            CH3            CH3           H           OH          N-CH3
B472           Ph                  CH3            CH3           H           OH          N-CH3
B473           CH3O               CH3            CH3           H           OH          N-CH3
B474           CH3OC(O)           CH3            CH3           H           OH          N-CH3
B475           CH3CH2OC(O)       CH3            CH3           H           OH          N-CH3
B476           CH2=CHCH2        CH3            CH3           H           OH          N-CH3
B477           HCCCH2             CH3            CH3           H           OH          N-CH3
B478           CF3                CH3            CH3           H           OH          N-CH3
B479           (CH3)2NSO2      CH3            CH3           H           OH          N-CH3
B480           (CH3)2N          CH3            CH3           H           OH          N-CH3
B481           PhO                 CH3            CH3           H           OH          N-CH3
B482           PhS                 CH3            CH3           H           OH          N-CH3
B483           PhSO                CH3            CH3           H           OH          N-CH3
B484           PhSO2              CH3            CH3           H           OH          N-CH3
基团           R6                R7           R8           R9            R10          W
B485           CN                 CH3          CH3           H              OH           N-CH3
B486           CH3               CH3          CH3          CH3           OH           N-CH3
B487           CH3CH2           CH3          CH3          CH3           OH           N-CH3
B488           CH3CH2CH2       CH3          CH3          CH3           OH           N-CH3
B489           (CH3)2CH         CH3          CH3          CH3           OH           N-CH3
B490           (CH3)3C          CH3          CH3          CH3           OH           N-CH3
B491           CH3S              CH3          CH3          CH3           OH           N-CH3
B492           CH3SO             CH3          CH3          CH3           OH           N-CH3
B493           CH3SO2           CH3          CH3          CH3           OH           N-CH3
B494           Ph                 CH3          CH3          CH3           OH           N-CH3
B495           CH3O              CH3          CH3          CH3           OH           N-CH3
B496           CH3OC(O)          CH3          CH3          CH3           OH           N-CH3
B497           CH3CH2OC(O)      CH3          CH3          CH3           OH           N-CH3
B498           CH2=CHCH2       CH3          CH3          CH3           OH           N-CH3
B499           HCCCH2            CH3          CH3          CH3           OH           N-CH3
B500           CF3               CH3          CH3          CH3           OH           N-CH3
B501           (CH3)2NSO2     CH3          CH3          CH3           OH           N-CH3
B502           (CH3)2N         CH3          CH3          CH3           OH           N-CH3
B503           PhO                CH3          CH3          CH3           OH           N-CH3
B504           PhS                CH3          CH3          CH3           OH           N-CH3
B505           PhSO               CH3          CH3          CH3           OH           N-CH3
B506           PhSO2             CH3          CH3          CH3           OH           N-CH3
B507           CN                 CH3          CH3          CH3           OH           N-CH3
B508           CH3CH2          CH3CH2      H             H              OH           N-CH3
B509           CH3CH2CH2      CH3CH2      H             H              OH           N-CH3
B510           (CH3)2CH        CH3CH2      H             H              OH           N-CH3
B511           (CH3)3C         CH3CH2      H             H              OH           N-CH3
B512           CH3S             C3CH2       H             H              OH           N-CH3
B513           CH3SO            C3CH2       H             H              OH           N-CH3
B514           CH3SO2          CH3CH2      H             H              OH           N-CH3
B515           Ph                 CH3CH2      H             H              OH           N-CH3
B516           CH3O             CH3CH2      H             H              OH           N-CH3
B517           CH3OC(O)         CH3CH2      H             H              OH           N-CH3
基团            R6                   R7            R8         R9        R10         W
B518            CH3CH2OC(O)         CH3CH2       H           H          OH           N-CH3
B519            CH2=CHCH2          CH3CH2       H           H          OH           N-CH3
B520            HCCCH2               CH3CH2       H           H          OH           N-CH3
B521            CF3                  CH3CH2       H           H          OH           N-CH3
B522            (CH3)2NSO2        CH3CH2       H           H          OH           N-CH3
B523            (CH3)2N            CH3CH2       H           H          OH           N-CH3
B524            PhO                   CH3CH2       H           H          OH           N-CH3
B525            PhS                   CH3CH2       H           H          OH           N-CH3
B526            PhSO                  CH3CH2       H           H          OH           N-CH3
B527            PhSO2                CH3CH2       H           H          OH           N-CH3
B528            CN                    CH3CH2       H           H          OH           N-CH3
B529            H                     H               H           H          OH           O
B530            CH3                  H               H           H          OH           O
B531            CH3CH2              H               H           H          OH           O
B532            CH3CH2CH2          H               H           H          OH           O
B533            (CH3)2CH            H               H           H          OH           O
B534            (CH3)3C             H               H           H          OH           O
B535            CH3S                 H               H           H          OH           O
B536            CH3SO                H               H           H          OH           O
B537            CH3SO2              H               H           H          OH           O
B538            Ph                    H               H           H          OH           O
B539            CH3O                 H               H           H          OH           O
B540            CH3OC(O)             H               H           H          OH           O
B541            CH3CH2OC(O)         H               H           H          OH           O
B542            CH2=CHCH2          H               H           H          OH           O
B543            HCCCH2               H               H           H          OH           O
B544            CF3                  H               H           H          OH           O
B545            (CH3)2NSO2        H               H           H          OH           O
B546            (CH3)2N            H               H           H          OH           O
B547            PhO                   H               H           H          OH           O
B548            PhS                   H               H           H          OH           O
B549            PhSO                  H               H           H          OH           O
B550            PhSO2                H               H           H          OH           O
基团           R6                 R7             R8          R9          R10         W
B551           CN                  H               H             H            OH           O
B552           CH3                CH3           H             H            OH           O
B553           CH3CH2           CH3            H             H            OH           O
B554           CH3CH2CH2       CH3            H             H            OH           O
B555           (CH3)2CH         CH3            H             H            OH           O
B556           (CH3)3C          CH3            H             H            OH           O
B557           CH3S              CH3            H             H            OH           O
B558           CH3SO             CH3            H             H            OH           O
B559           CH3SO2           CH3            H             H            OH           O
B560           Ph                  CH3            H             H            OH           O
B561           CH3O              CH3            H             H            OH           O
B562           CH3OC(O)          CH3            H             H            OH           O
B563           CH3CH2OC(O)      CH3            H             H            OH           O
B564           CH2=CHCH2       CH3            H             H            OH           O
B565           HCCCH2            CH3            H             H            OH           O
B566           CF3               CH3            H             H            OH           O
B567           (CH3)2NSO2      CH3            H             H            OH           O
B568           (CH3)2N          CH3            H             H            OH           O
B569           PhO                 CH3            H             H            OH           O
B570           PhS                 CH3            H             H            OH           O
B571           PhSO                CH3            H             H            OH           O
B572           PhSO2              CH3            H             H            OH           O
B573           CN                  CH3            H             H            OH           O
B574           CH3                H               CH3          H            OH           O
B575           CH3CH2           H               CH3          H            OH           O
B576           CH3CH2CH2       H               CH3          H            OH           O
B577           (CH3)2CH         H               CH3          H            OH           O
B578           (CH3)3C          H               CH3          H            OH           O
B579           CH3S              H               CH3          H            OH           O
B580           CH3SO             H               CH3          H            OH           O
B581           CH3SO2           H               CH3          H            OH           O
B582           Ph                  H               CH3          H            OH           O
B583           CH3O               H               CH3          H            OH           O
基团           R6                 R7            R8         R9        R10        W
B584           CH3OC(O)           H              CH3         H          OH          O
B585           CH3CH2OC(O)       H              CH3         H          OH          O
B586           CH2=CHCH2        H              CH3         H          OH          O
B587           HCCCH2             H              CH3         H          OH          O
B588           CF3                H              CH3         H          OH          O
B589           (CH3)2NSO2       H              CH3         H          OH          O
B590           (CH3)2N           H              CH3         H          OH          O
B591           PhO                  H              CH3         H          OH          O
B592           PhS                  H              CH3         H          OH          O
B593           PhSO                 H              CH3         H          OH          O
B594           PhSO2               H              CH3         H          OH          O
B595           CN                   H              CH3         H          OH          O
B596           CH3                 CH3           CH3         H          OH          O
B597           CH3CH2            CH3           CH3         H          OH          O
B598           CH3CH2CH2        CH3           CH3         H          OH          O
B599           (CH3)2CH          CH3           CH3         H          OH          O
B600           (CH3)3C           CH3           CH3         H          OH          O
B601           CH3S               CH3           CH3         H          OH          O
B602           CH3SO              CH3           CH3         H          OH          O
B603           CH3SO2            CH3           CH3         H          OH          O
B604           Ph                  CH3           CH3         H          OH          O
B605           CH3O               CH3           CH3         H          OH          O
B606           CH3OC(O)           CH3           CH3         H          OH          O
B607           CH3CH2OC(O)       CH3           CH3         H          OH          O
B608           CH2=CHCH2        CH3           CH3         H          OH          O
B609           HCCCH2             CH3           CH3         H          OH          O
B610           CF3                CH3           CH3         H          OH          O
B611           (CH3)2NSO2      CH3           CH3         H          OH          O
B612           (CH3)2N          CH3           CH3         H          OH          O
B613           PhO                 CH3           CH3         H          OH          O
B614           PhS                 CH3           CH3         H          OH          O
B615           PhSO                CH3           CH3         H          OH          O
B616           PhSO2              CH3           CH3         H          OH          O
基团            R6                 R7           R8          R9         R10         W
B617            CN                  CH3          CH3         H            OH           O
B618            CH3               CH3          CH3         CH3         OH           O
B619            CH3CH2           CH3          CH3         CH3         OH           O
B620            CH3CH2CH2       CH3          CH3         CH3         OH           O
B621            (CH3)2CH         CH3          CH3         CH3         OH           O
B622            (CH3)3C          CH3          CH3         CH3         OH           O
B623            CH3S              CH3          CH3         CH3         OH           O
B624            CH3SO             CH3          CH3         CH3         OH           O
B625            CH3SO2           CH3          CH3         CH3         OH           O
B626            Ph                 CH3          CH3         CH3         OH           O
B627            CH3O              CH3          CH3         CH3         OH           O
B628            CH3OC(O)          CH3          CH3         CH3         OH           O
B629            CH3CH2OC(O)      CH3          CH3         CH3         OH           O
B630            CH2=CHCH2       CH3          CH3         CH3         OH           O
B631            HCCCH2            CH3          CH3         CH3         OH           O
B632            CF3               CH3          CH3         CH3         OH           O
B633            (CH3)2NSO2      CH3          CH3         CH3         OH           O
B634            (CH3)2N          CH3          CH3         CH3         OH           O
B635            PhO                 CH3          CH3         CH3         OH           O
B636            PhS                 CH3          CH3         CH3         OH           O
B637            PhSO                CH3          CH3         CH3         OH           O
B638            PhSO2              CH3          CH3         CH3         OH           O
B639            CN                  CH3          CH3         CH3         OH           O
B640            CH3CH2           CH3CH2      H            H            OH           O
B641            CH3CH2CH2       CH3CH2      H            H            OH           O
B642            (CH3)2CH         CH3CH2      H            H            OH           O
B643            (CH3)3C          CH3CH2      H            H            OH           O
B644            CH3S              CH3CH2      H            H            OH           O
B645            CH3SO             CH3CH2      H            H            OH           O
B646            CH3SO2           CH3CH2      H            H            OH           O
B647            Ph                 CH3CH2      H            H            OH           O
B648            CH3O              CH3CH2      H            H            OH           O
B649            CH3OC(O)          CH3CH2      H            H            OH           O
基团           R6                   R7            R8        R9        R10        W
B650           CH3CH2OC(O)         CH3CH2       H          H          OH          O
B651           CH2=CHCH2          CH3CH2       H          H          OH          O
B652           HCCCH2               CH3CH2       H          H          OH          O
B653           CF3                  CH3CH2       H          H          OH          O
B654           (CH3)2NSO2        CH3CH2       H          H          OH          O
B655           (CH3)2N            CH3CH2       H          H          OH          O
B656           PhO                   CH3CH2       H          H          OH          O
B657           PhS                   CH3CH2       H          H          OH          O
B658           PhSO                  CH3CH2       H          H          OH          O
B659           PhSO2                CH3CH2       H          H          OH          O
B660           CN                    CH3CH2       H          H          OH          O
B661           H                      H              H          H          OH          S
B662           CH3                  H              H          H          OH          S
B663           CH3CH2              H              H          H          OH          S
B664           CH3CH2CH2          H              H          H          OH          S
B665           (CH3)2CH            H              H          H          OH          S
B666           (CH3)3C             H              H          H          OH          S
B667           CH3S                 H              H          H          OH          S
B668           CH3SO                H              H          H          OH          S
B669           CH3SO2              H              H          H          OH          S
B670           Ph                    H              H          H          OH          S
B671           CH3O                 H              H          H          OH          S
B672           CH3OC(O)             H              H          H          OH          S
B673           CH3CH2OC(O)         H              H          H          OH          S
B674           CH2=CHCH2          H              H          H          OH          S
B675           HCCCH2               H              H          H          OH          S
B676           CF3                  H              H          H          OH          S
B677           (CH3)2NSO2        H              H          H          OH          S
B678           (CH3)2N            H              H          H          OH          S
B679           PhO                   H              H          H          OH          S
B680           PhS                   H              H          H          OH          S
B681           PhSO                  H              H          H          OH          S
B682           PhSO2                H              H          H          OH          S
基团          R6                  R7          R8       R9       R10         W
B683          CN                   H            H          H          OH          S
B684          CH3                CH3         H          H          OH          S
B685          CH3CH2            CH3         H          H          OH          S
B686          CH3CH2CH2        CH3         H          H          OH          S
B687          (CH3)2CH          CH3         H          H          OH          S
B688          (CH3)3C           CH3         H          H          OH          S
B689          CH3S               CH3         H          H          OH          S
B690          CH3SO              CH3         H          H          OH          S
B691          CH3SO2            CH3         H          H          OH          S
B692          Ph                  CH3         H          H          OH          S
B693          CH3O               CH3         H          H          OH          S
B694          CH3OC(O)           CH3         H          H          OH          S
B695          CH3CH2OC(O)       CH3         H          H          OH          S
B696          CH2=CHCH2        CH3         H          H          OH          S
B697          HCCCH2             CH3         H          H          OH          S
B698          CF3                CH3         H          H          OH          S
B699          (CH3)2NSO2      CH3         H          H          OH          S
B700          (CH3)2N          CH3         H          H          OH          S
B701          PhO                 CH3         H          H          OH          S
B702          PhS                 CH3         H          H          OH          S
B703          PhSO                CH3         H          H          OH          S
B704          PhSO2              CH3         H          H          OH          S
B705          CN                  CH3         H          H          OH          S
B706          CH3                H            CH3       H          OH          S
B707          CH3CH2           H             CH3       H          OH          S
B708          CH3CH2CH2       H            CH3       H          OH          S
B709          (CH3)2CH         H            CH3       H          OH          S
B710          (CH3)3C          H            CH3       H          OH          S
B711          CH3S              H            CH3       H          OH          S
B712          CH3SO             H            CH3       H          OH          S
B713          CH3SO2           H            CH3       H          OH          S
B714          Ph                  H            CH3       H          OH          S
B715          CH3O              H            CH3       H          OH          S
基团          R6                  R7        R8        R9        R10        W
B716          CH3OC(O)            H           CH3       H          OH          S
B717          CH3CH2OC(O)        H           CH3       H          OH          S
B718          CH2=CHCH2         H           CH3       H          OH          S
B719          HCCCH2              H           CH3       H          OH          S
B720          CF3                 H           CH3       H          OH          S
B721          (CH3)2NSO2        H           CH3       H          OH          S
B722          (CH3)2N            H           CH3       H          OH          S
B723          PhO                   H           CH3       H          OH          S
B724          PhS                   H           CH3       H          OH          S
B725          PhSO                  H           CH3       H          OH          S
B726          PhSO2                H           CH3       H          OH          S
B727          CN                    H           CH3       H          OH          S
B728          CH3                 CH3        CH3       H          OH          S
B729          CH3CH2             CH3        CH3       H          OH          S
B730          CH3CH2CH2         CH3        CH3       H          OH          S
B731          (CH3)2CH           CH3        CH3       H          OH          S
B732          (CH3)3C            CH3        CH3       H          OH          S
B733          CH3S                CH3        CH3       H          OH          S
B734          CH3SO               CH3        CH3       H          OH          S
B735          CH3SO2             CH3        CH3       H          OH          S
B736          Ph                   CH3        CH3       H          OH          S
B737          CH3O                CH3        CH3       H          OH          S
B738          CH3OC(O)            CH3        CH3       H          OH          S
B739          CH3CH2OC(O)        CH3        CH3       H          OH          S
B740          CH2=CHCH2         CH3        CH3       H          OH          S
B741          HCCCH2              CH3        CH3       H          OH          S
B742          CF3                 CH3        CH3       H          OH          S
B743          (CH3)2NSO2       CH3        CH3       H          OH          S
B744          (CH3)2N           CH3        CH3       H          OH          S
B745          PhO                  CH3        CH3       H          OH          S
B746          PhS                  CH3        CH3       H          OH          S
B747          PhSO                 CH3        CH3       H          OH          S
B748          PhSO2               CH3        CH3       H          OH          S
基团          R6               R7           R8        R9         R10       W
B749          CN                CH3          CH3       H            OH         S
B750          CH3              CH3          CH3       CH3        OH         S
B751          CH3CH2          CH3          CH3       CH3        OH         S
B752          CH3CH2CH2      CH3          CH3       CH3        OH         S
B753          (CH3)2CH        CH3          CH3       CH3        OH         S
B754          (CH3)3C         CH3          CH3       CH3        OH         S
B755          CH3S             CH3          CH3       CH3        OH         S
B756          CH3SO            CH3          CH3       CH3        OH         S
B757          CH3SO2          CH3          CH3       CH3        OH         S
B758          Ph                CH3          CH3       CH3        OH         S
B759          CH3O             CH3          CH3       CH3        OH         S
B760          CH3OC(O)         CH3          CH3       CH3        OH         S
B761          CH3CH2OC(O)     CH3          CH3       CH3        OH         S
B762          CH2=CHCH2      CH3          CH3       CH3        OH         S
B763          HCCCH2            CH3          CH3       CH3        OH         S
B764          CF3               CH3          CH3       CH3        OH         S
B765          (CH3)2NSO2     CH3          CH3       CH3        OH         S
B766          (CH3)2N         CH3          CH3       CH3        OH         S
B767          PhO                CH3          CH3       CH3        OH         S
B768          PhS                CH3          CH3       CH3        OH         S
B769          PhSO               CH3          CH3       CH3        OH         S
B770          PhSO2             CH3          CH3       CH3        OH         S
B771          CN                 CH3          CH3       CH3        OH         S
B772          CH3CH2          CH3CH2      H           H           OH         S
B773          CH3CH2CH2      CH3CH2      H           H           OH         S
B774          (CH3)2CH        CH3CH2      H           H           OH         S
B775          (CH3)3C         CH3CH2      H           H           OH         S
B776          CH3S             CH3CH2      H           H           OH         S
B777          CH3SO            CH3CH2      H           H           OH         S
B778          CH3SO2          CH3CH2      H           H           OH         S
B779          Ph                 CH3CH2     H           H           OH         S
B780          CH3O             CH3CH2      H           H           OH         S
B781          CH3OC(O)         CH3CH2      H           H           OH         S
基团         R6                 R7            R8       R9       R10       W
B782         CH3CH2OC(O)       CH3CH2      H         H          OH        S
B783         CH2=CHCH2        CH3CH2      H         H          OH        S
B784         HCCCH2             CH3CH2      H         H          OH        S
B785         CF3                CH3CH2      H         H          OH        S
B786         (CH3)2NSO2       CH3CH2      H         H          OH        S
B787         (CH3)2N           CH3CH2      H         H          OH        S
B788         PhO                  CH3CH2      H         H          OH        S
B789         PhS                  CH3CH2      H         H          OH        S
B790         PhSO                 CH3CH2      H         H          OH        S
B791         PhSO2               CH3CH2      H         H          OH        S
B792         CN                   CH3CH2      H         H          OH        S
B793         H                    H              H         H          OH        SO2
B794         CH3                 H              H         H          OH        SO2
B795         CH3CH2            H              H         H          OH         SO2
B796         CH3CH2CH2        H              H         H          OH         SO2
B797         (CH3)2CH          H              H         H          OH         SO2
B798         (CH3)3C           H              H         H          OH         SO2
B799         CH3S               H              H         H          OH         SO2
B800         CH3SO              H              H         H          OH         SO2
B801         CH3SO2            H              H         H          OH         SO2
B802         Ph                   H              H         H          OH         SO2
B803         CH3O               H              H         H          OH         SO2
B804         CH3OC(O)           H              H         H          OH         SO2
B805         CH3CH2OC(O)       H              H         H          OH         SO2
B806         CH2=CHCH2        H              H         H          OH         SO2
B807         HCCCH2             H              H         H          OH         SO2
B808         CF3                H              H         H          OH         SO2
B809         (CH3)2NSO2       H             H         H          OH         SO2
B810         (CH3)2N           H              H         H          OH        SO2
B811         PhO                  H             H         H          OH         SO2
B812         PhS                  H             H         H          OH         SO2
B813         PhSO                 H             H         H          OH         SO2
B814         PhSO2              H              H         H          OH         SO2
基团             R6                    R7         R8        R9        R10        W
B815             CN                     H            CH         H          OH          SO2
B816             CH3                  CH3         H          H          OH          SO2
B817             CH3CH2              CH3         H          H          OH          SO2
B818             CH3CH2CH2          CH3         H          H          OH          SO2
B819             (CH3)2CH            CH3         H          H          OH          SO2
B820             (CH3)3C             CH3         H          H          OH          SO2
B821             CH3S                 CH3         H          H          OH          SO2
B822             CH3SO                CH3         H          H          OH          SO2
B823             CH3SO2              CH3         H          H          OH          SO2
B824             Ph                     CH3         H          H          OH          SO2
B825             CH3O                 CH3         H          H          OH          SO2
B826             CH3OC(O)             CH3         H          H          OH          SO2
B827             CH3CH2OC(O)         CH3         H          H          OH          SO2
B828             CH2=CHCH2          CH3         H          H          OH          SO2
B829             HCCCH2               CH3         H          H          OH          SO2
B830             CF3                  CH3         H          H          OH          SO2
B831             (CH3)2NSO2         CH3         H          H          OH          SO2
B832             (CH3)2N             CH3         H          H          OH          SO2
B833             PhO                    CH3         H          H          OH          SO2
B834             PhS                    CH3         H          H          OH          SO2
B835             PhSO                   CH3         H          H          OH          SO2
B836             PhSO2                 CH3         H          H          OH          SO2
B837             CN                     CH3         H          H          OH          SO2
B838             CH3                   H            CH3       H          OH          SO2
B839             CH3CH2              H            CH3       H          OH          SO2
B840             CH3CH2CH2          H            CH3       H          OH          SO2
B841             (CH3)2CH            H            CH3       H          OH          SO2
B842             (CH3)3C             H            CH3       H          OH          SO2
B843             CH3S                 H            CH3       H          OH          SO2
B844             CH3SO                H            CH3       H          OH          SO2
B845             CH3SO2              H            CH3       H          OH          SO2
B846             Ph                     H            CH3       H          OH          SO2
B847             CH3O                  H            CH3       H          OH          SO2
基团          R6                 R7             R8             R9        R10        W
B848          CH3OC(O)           H               CH3            H          OH          SO2
B849          CH3CH2OC(O)       H               CH3            H          OH          SO2
B850          CH2=CHCH2        H               CH3            H          OH          SO2
B851          HCCCH2              H               CH3            H          OH          SO2
B852          CF3                 H               CH3            H          OH          SO2
B853          (CH3)2NSO2       H               CH3            H          OH          SO2
B854          (CH3)2N           H               CH3            H          OH          SO2
B855          PhO                  H               CH3            H          OH          SO2
B856          PhS                  H               CH3            H          OH          SO2
B857          PhSO                 H               CH3            H          OH          SO2
B858          PhSO2               H               CH3            H          OH          SO2
B859          CN                   H               CH3            H          OH          SO2
B860          CH3                CH3            CH3            H          OH          SO2
B861          CH3CH2            CH3            CH3            H          OH          SO2
B862          CH3CH2CH2        CH3            CH3            H          OH          SO2
B863          (CH3)2CH          CH3            CH3            H          OH          SO2
B864          (CH3)3C           CH3            CH3            H          OH          SO2
B865          CH3S               CH3            CH3            H          OH          SO2
B866          CH3SO              CH3            CH3            H          OH          SO2
B867          CH3SO2            CH3            CH3            H          OH          SO2
B868          Ph                   CH3            CH3            H          OH          SO2
B869          CH3O               CH3            CH3            H          OH          SO2
B870          CH3OC(O)           CH3            CH3            H          OH          SO2
B871          CH3CH2OC(O)       CH3            CH3            H          OH          SO2
B872          CH2=CHCH2        CH3            CH3            H          OH          SO2
B873          HCCCH2             CH3            CH3            H          OH          SO2
B874          CF3                CH3            CH3            H          OH          SO2
B875          (CH3)2NSO2       CH3            CH3            H          OH          SO2
B876          (CH3)2N           CH3            CH3            H          OH          SO2
B877          PhO                  CH3            CH3            H          OH          SO2
B878          PhS                  CH3            CH3            H          OH          SO2
B879          PhSO                 CH3            CH3            H          OH          SO2
B880          PhSO2              CH3            CH3            H          OH          SO2
基团         R6                 R7              R8             R9         R10        W
B881         CN                   CH3             CH3            H           OH          SO2
B882         CH3                CH3             CH3            CH3        OH          SO2
B883         CH3CH2            CH3             CH3            CH3        OH          SO2
B884         CH3CH2CH2        CH3             CH3            CH3        OH          SO2
B885         (CH3)2CH          CH3             CH3            CH3        OH          SO2
B886         (CH3)3C           CH3             CH3            CH3        OH          SO2
B887         CH3S               CH3             CH3            CH3        OH          SO2
B888         CH3SO              CH3             CH3            CH3        OH          SO2
B889         CH3SO2            CH3             CH3            CH3        OH          SO2
B890         Ph                   CH3             CH3            CH3        OH          SO2
B891         CH3O               CH3             CH3            CH3        OH          SO2
B892         CH3OC(O)           CH3             CH3            CH3        OH          SO2
B893         CH3CH2OC(O)       CH3             CH3            CH3        OH          SO2
B894         CH2=CHCH2        CH3             CH3            CH3        OH          SO2
B895         HCCCH2             CH3             CH3            CH3        OH          SO2
B896         CF3                CH3             CH3            CH3        OH          SO2
B897         (CH3)2NSO2       CH3             CH3            CH3        OH          SO2
B898         (CH3)2N           CH3             CH3            CH3        OH          SO2
B899         PhO                  CH3             CH3            CH3        OH          SO2
B900         PhS                  CH3             CH3            CH3        OH          SO2
B901         PhSO                 CH3             CH3            CH3        OH          SO2
B902         PhSO2               CH3             CH3            CH3        OH          SO2
B903         CN                   CH3             CH3            CH3        OH          SO2
B904         CH3CH2            CH3CH2         H               H           OH          SO2
B905         CH3CH2CH2        CH3CH2         H               H           OH          SO2
B906         (CH3)2CH          CH3CH2         H               H           OH          SO2
B907         (CH3)3C           CH3CH2         H               H           OH          SO2
B908         CH3S               CH3CH2         H               H           OH          SO2
B909         CH3SO              CH3CH2         H               H           OH          SO2
B910         CH3SO2            CH3CH2         H               H           OH          SO2
B911         Ph                   CH3CH2         H               H           OH          SO2
B912         CH3O               CH3CH2         H               H           OH          SO2
B913         CH3OC(O)           CH3CH2         H               H           OH          SO2
基团           R6                  R7            R8         R9       R10         W
B914           CH3CH2OC(O)        CH3CH2       H           H         OH           SO2
B915           CH2=CHCH2         CH3CH2       H           H         OH           SO2
B916           HCCCH2              CH3CH2       H           H         OH           SO2
B917           CF3                 CH3CH2       H           H         OH           SO2
B918           (CH3)2NSO2        CH3CH2       H           H         OH           SO2
B919           (CH3)2N            CH3CH2       H           H         OH           SO2
B920           PhO                  CH3CH2       H           H         OH           SO2
B921           PhS                  CH3CH2       H           H         OH           SO2
B922           PhSO                 CH3CH2       H           H         OH           SO2
B923           PhSO2               CH3CH2       H           H         OH           SO2
B924           CN                   CH3CH2       H           H         OH           SO2
B925           H                    H              H           H         OH           CHC(O)OCH2CH3
B926           CH3                 H              H           H         OH           CHC(O)OCH2CH3
B927           CH3CH2             H              H           H         OH           CHC(O)OCH2CH3
B928           CH3CH2CH2         H              H           H         OH           CHC(O)OCH2CH3
B929           (CH3)2CH           H              H           H         OH           CHC(O)OCH2CH3
B930           (CH3)3C            H              H           H         OH           CHC(O)OCH2CH3
B931           CH3S                H              H           H         OH           CHC(O)OCH2CH3
B932           CH3SO               H              H           H         OH           CHC(O)OCH2CH3
B933           CH3SO2             H              H           H         OH           CHC(O)OCH2CH3
B934           Ph                    H              H           H         OH           CHC(O)OCH2CH3
B935           CH3O                H              H           H         OH           CHC(O)OCH2CH3
B936           CH3OC(O)            H              H           H         OH           CHC(O)OCH2CH3
B937           CH3CH2OC(O)        H              H           H         OH           CHC(O)OCH2CH3
B938           CH2=CHCH2         H              H           H         OH           CHC(O)OCH2CH3
B939           HCCCH2              H              H           H         OH           CHC(O)OCH2CH3
B940           CF3                 H              H           H         OH           CHC(O)OCH2CH3
B941           (CH3)2NSO2       H              H           H         OH           CHC(O)OCH2CH3
B942           (CH3)2N           H              H           H         OH           CHC(O)OCH2CH3
B943           PhO                  H              H           H         OH           CHC(O)OCH2CH3
B944           PhS                  H              H           H         OH           CHC(O)OCH2CH3
B945           PhSO                 H              H           H         OH           CHC(O)OCH2CH3
B946           PhSO2               H              H           H         OH           CHC(O)OCH2CH3
基团            CR6                R7         R8        R9         R10          W
B947            CN                  H            H          H           OH            CHC(O)OCH2CH3
B948            CH3                CH3         H          H           OH            CHC(O)OCH2CH3
B949            CH3CH2           CH3         H          H           OH            CHC(O)OCH2CH3
B950            CH3CH2CH2       CH3         H          H           OH            CHC(O)OCH2CH3
B951            (CH3)2CH         CH3         H          H           OH            CHC(O)OCH2CH3
B952            (CH3)3C          CH3         H          H           OH            CHC(O)OCH2CH3
B953            CH3S              CH3         H          H           OH            CHC(O)OCH2CH3
B954            CH3SO             CH3         H          H           OH            CHC(O)OCH2CH3
B955            CH3SO2           CH3         H          H           OH            CHC(O)OCH2CH3
B956            Ph                 CH3         H          H           OH            CHC(O)OCH2CH3
B957            CH3O              CH3         H          H           OH            CHC(O)OCH2CH3
B958            CH3OC(O)          CH3         H          H           OH            CHC(O)OCH2CH3
B959            CH3CH2OC(O)      CH3         H          H           OH            CHC(O)OCH2CH3
B960            CH2=CHCH2       CH3         H          H           OH            CHC(O)OCH2CH3
B961            HCCCH2            CH3         H          H           OH            CHC(O)OCH2CH3
B962            CF3               CH3         H          H           OH            CHC(O)OCH2CH3
B963            (CH3)2NSO2      CH3         H          H           OH            CHC(O)OCH2CH3
B964            (CH3)2N          CH3         H          H           OH            CHC(O)OCH2CH3
B965            PhO                 CH3         H          H           OH            CHC(O)OCH2CH3
B966            PhS                 CH3         H          H           OH            CHC(O)OCH2CH3
B967            PhSO                CH3         H          H           OH            CHC(O)OCH2CH3
B968            PhSO2              CH3         H          H           OH            CHC(O)OCH2CH3
B969            CN                  CH3         H          H           OH            CHC(O)OCH2CH3
B970            CH3               H             CH3       H           OH            CHC(O)OCH2CH3
B971            CH3CH2           H             CH3       H           OH            CHC(O)OCH2CH3
B972            CH3CH2CH2       H            CH3       H           OH            CHC(O)OCH2CH3
B973            (CH3)2CH         H            CH3       H           OH            CHC(O)OCH2CH3
B974            (CH3)3C          H            CH3       H           OH            CHC(O)OCH2CH3
B975            CH3S              H            CH3       H           OH            CHC(O)OCH2CH3
B976            CH3SO             H            CH3       H           OH            CHC(O)OCH2CH3
B977            CH3SO2           H            CH3       H           OH            CHC(O)OCH2CH3
B978            Ph                 H            CH3       H           OH            CHC(O)OCH2CH3
B979            CH3O              H            CH3       H           OH            CHC(O)OCH2CH3
基团           R6                 R7          R8             R9        R10        W
B980           CH3OC(O)           H            CH3            H          OH          CHC(O)OCH2CH3
B981           CH3CH2OC(O)       H            CH3            H          OH          CHC(O)OCH2CH3
B982           CH2=CHCH2        H            CH3            H          OH          CHC(O)OCH2CH3
B983           HCCCH2             H            CH3            H          OH          CHC(O)OCH2CH3
B984           CF3                H            CH3            H          OH          CHC(O)OCH2CH3
B985           (CH3)2NSO2       H            CH3            H          OH          CHC(O)OCH2CH3
B986           (CH3)2N           H            CH3            H          OH          CHC(O)OCH2CH3
B987           PhO                  H            CH3            H          OH          CHC(O)OCH2CH3
B988           PhS                  H            CH3            H          OH          CHC(O)OCH2CH3
B989           PhSO                 H            CH3            H          OH          CHC(O)OCH2CH3
B990           PhSO2               H            CH3            H          OH          CHC(O)OCH2CH3
B991           CN                   H            CH3            H          OH          CHC(O)OCH2CH3
B992           CH3                CH3         CH3            H          OH          CHC(O)OCH2CH3
B993           CH3CH2            CH3         CH3            H          OH          CHC(O)OCH2CH3
B994           CH3CH2CH2        CH3         CH3            H          OH          CHC(O)OCH2CH3
B995           (CH3)2CH          CH3         CH3            H          OH          CHC(O)OCH2CH3
B996           (CH3)3C           CH3         CH3            H          OH          CHC(O)OCH2CH3
B997           CH3S               CH3         CH3            H          OH          CHC(O)OCH2CH3
B998           CH3SO              CH3         CH3            H          OH          CHC(O)OCH2CH3
B999           CH3SO2            CH3         CH3            H          OH          CHC(O)OCH2CH3
B1000          Ph                  CH3         CH3            H          OH          CHC(O)OCH2CH3
B1001          CH3O               CH3         CH3            H          OH          CHC(O)OCH2CH3
B1002          CH3OC(O)           CH3         CH3            H          OH          CHC(O)OCH2CH3
B1003          CH3CH2OC(O)       CH3         CH3            H          OH          CHC(O)OCH2CH3
B1004          CH2=CHCH2        CH3         CH3            H          OH          CHC(O)OCH2CH3
B1005          HCCCH2             CH3         CH3            H          OH          CHC(O)OCH2CH3
B1006          CF3                CH3         CH3            H          OH          CHC(O)OCH2CH3
B1007          (CH3)2NSO2      CH3         CH3            H          OH          CHC(O)OCH2CH3
B1008          (CH3)2N          CH3         CH3            H          OH          CHC(O)OCH2CH3
B1009          PhO                 CH3         CH3            H          OH          CHC(O)OCH2CH3
B1010          PhS                 CH3         CH3            H          OH          CHC(O)OCH2CH3
B1011          PhSO                CH3         CH3            H          OH          CHC(O)OCH2CH3
B1012          PhSO2              CH3         CH3            H          OH          CHC(O)OCH2CH3
基团           R6                   R7              R8         R9         R10         W
B1013          CN                    CH3             CH3        H            OH           CHC(O)OCH2CH3
B1014          CH3                  CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1015          CH3CH2              CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1016          CH3CH2CH2          CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1017          (CH3)2CH            CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1018          (CH3)3C             CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1019          CH3S                 CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1020          CH3SO                CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1021          CH3SO2              CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1022          Ph                    CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1023          CH3O                 CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1024          CH3OC(O)             CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1025          CH3CH2OC(O)         CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1026          CH2=CHCH2          CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1027          HCCCH2               CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1028          CF3                  CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1029          (CH3)2NSO2         CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1030          (CH3)2N             CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1031          PhO                    CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1032          PhS                    CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1033          PhSO                   CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1034          PhSO2                 CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1035          CN                     CH3             CH3        CH3        OH           CHC(O)OCH2CH3
B1036          CH3CH2              CH3CH2         H           H           OH           CHC(O)OCH2CH3
B1037          CH3CH2CH2          CH3CH2         H           H           OH           CHC(O)OCH2CH3
B1038          (CH3)2CH            CH3CH2         H           H           OH           CHC(O)OCH2CH3
B1039          (CH3)3C             CH3CH2         H           H           OH           CHC(O)OCH2CH3
B1040          CH3S                 CH3CH2         H           H           OH           CHC(O)OCH2CH3
B1041          CH3SO                CH3CH2         H           H           OH           CHC(O)OCH2CH3
B1042          CH3SO2              CH3CH2         H           H           OH           CHC(O)OCH2CH3
B1043          Ph                    CH3CH2         H           H           OH           CHC(O)OCH2CH3
B1044          CH3O                 CH3CH2         H           H           OH           CHC(O)OCH2CH3
B1045          CH3OC(O)             CH3CH2         H           H           OH           CHC(O)OCH2CH3
基团           R6                 R7             R8       R9        R10        W
B1046          CH3CH2OC(O)       CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1047          CH2=CHCH2        CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1048          HCCCH2             CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1049          CF3                CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1050          (CH3)2NSO2       CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1051          (CH3)2N           CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1052          PhO                 CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1053          PhS                 CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1054          PhSO                CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1055          PhSO2              CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1056          CN                  CH3CH2       H         H          OH          CHC(O)OCH2CH3
B1057          CH3OC(O)           H               H         H          OH          CHPh
B1058          H                   H               H         H          OH          CHPh
B1059          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)2
B1064          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          CH2
B1068          H                   CH3O           H         H          OH          CH2
B1069          CH3O               CH3OC(O)       H         CH3       OH         CH2
B1070          CH3O               H               CH3      H          OH         CH2
B1071          Cl                  H               H         H          OH          CH2
B1072          F                   H               H         H          OH          CH2
B1073          H                   H               H         H          OH          CH(OCH3)2
B1074          H                   H               H         H          OH          CH2OSO2CH3
B1075          CH3               CH3            CH3      CH3      OH           S(O)
B1076          ClCH2CH2         H               H         H          OH          CH2
B1077          HO(CH2)2         H               H         H          OH          CH2
B1078          MsO(CH2)2        H               H         H          OH          CH2
基团             R6                       R7            R8          R9        R10               W
B1079            HOCH(CH3)CH2            H              H            H          OH                 CH2
B1080            MsOCH(CH3)CH2           H              H            H          OH                 CH2
B1081            (CH3)2CH                H              CH3         CH3       OH                 CH2
B1082            HCCCH2                   H              CH3         CH3       OH                 CH2
B1083            H2C=CCH2               H              CH3         CH3       OH                 CH2
B1084            H2C=C(CH3)             H              H            H          OH                 CHCH3
B1085            H                          H              H            H          OH                 CHCONHCH2Ph
B1086            H                         H               H            H          OH                 
Figure C9981578601341
B1087            CH3OC(O)                 CH3           H            H          OH                 C(CH3)2
B1088            H                         H              H            H          OH                 
B1089            CH3CH2                  H             CH3         CH3       OH                 CH2
B1090            CH3OC(O)                 H              H            H          OH                 CF3CH2CH2
B1091            CH3CH2S                CH3CH2       CH3         H          OH                 CH2
B1092            CH3S                     Ph             CH3         H          OH                 CH2
B1093            CH3CH2                 CH3CH2       CH3         H          OH                 CH2
B1094            CH3OC(O)                 H              H            H          OH                 C(CH3)2
B1095            CH3                      H              H            H          OH                 C(CH3)2
B1096            H                         H              H            H          OH                 NCOCH2SCH3
B1097                             H              H            H          OH                 CH2
B1098            1,1-二甲基乙烯基          H              H            H          OH                 CH2
B1099                        H              H            H          OH                 CH2
B1100            H                         H              H            H          -ONH+(CH2CH3)3 CH2
B1101            H                         H              H            H          -ONH+(CH2CH3)3 CH(CH3)
B1102            H                         H              H            H          PhS                CH2
B1103            H                         H              H            H          PhSO               CH2
B1104            H                         H              H            H          PhSO2             CH2
R1105            CH3                     CH3           CH3         CH3       Cl                 C=O
B1106            H                         H              H            H          OH                 CHCH2CH(CH3)2
基团            R6                     R7           R8         R9        R10          W
B1107           CH3                    CH3          CH3        CH3       CH3C(O)O     C=O
B1108           CH3OC(O)CH2           H             H           H           OH            CH2
B1109           CH3OC(O)CH2           CH3          H           H           OH            CH2
B1110           CH3OC(O)CH2           CH3          CH3        H           OH            CH2
B1111           CH3OC(O)CH2           CH3          CH3        CH3        OH            CH2
B1112           CH3OC(O)CH2           H             CH3        CH3        OH            CH2
B1113           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)2
B1119           CH3OC(O)CH2           CH3          H           H           OH            C(CH3)2
B1120           CH3OC(O)CH2           CH3          CH3        H           OH            C(CH3)2
B1121           CH3OC(O)CH2           CH3          CH3        CH3        OH            C(CH3)2
B1122           CH3OC(O)CH2           H             CH3        CH3        OH            C(CH3)2
B1123           CH3CH2OC(O)CH2       H             H           H           OH            CH2
B1124           CH3CH2OC(O)CH2       CH3          H           H           OH            CH2
B1125           CH3CH2OC(O)CH2       CH3          CH3        H           OH            CH2
B1126           CH3CH2OC(O)CH2       CH3          CH3        CH3        OH            CH2
B1127           CH3CH2OC(O)CH2       H             CH3        CH3        OH            CH2
B1128           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)2
B1134           CH3CH2OC(O)CH2       CH3          H           H           OH            C(CH3)2
B1135           CH3CH2OC(O)CH2       CH3          CH3        H           OH            C(CH3)2
B1136           CH3CH2OC(O)CH2       CH3          CH3        CH3        OH            C(CH3)2
B1137           CH3CH2OC(O)CH2       H             CH3        CH3        OH            C(CH3)2
B1138           
Figure C9981578601351
         CH3          H           H            OH            CH2
基团              R6                 R7             R8            R9        R10        W
B1139             CH3SCH2           H               H              H          OH          CH2
B1140             CH3SCH2           CH3            H              H          OH          CH2
B1141             CH3SCH2           CH3            CH3           H          OH          CH2
B1142             CH3SCH2           CH3            CH3           CH3       OH          CH2
B1143             CH3SCH2           H               CH3           CH3       OH          CH2
B1144             CH3SOCH2          H                H              H          OH          CH2
B1145             CH3SOCH2          CH3            H              H          OH          CH2
B1146             CH3SOCH2          CH3            CH3           H          OH          CH2
B1147             CH3SOCH2          CH3            CH3           CH3       OH          CH2
B1148             CH3SOCH2          H               CH3           CH3       OH          CH2
B1149             CH3SO2CH2        H               H              H          OH          CH2
B1150             CH3SO2CH2        CH3            H              H          OH          CH2
B1151             CH3SO2CH2        CH3            CH3           H          OH          CH2
B1152             CH3SO2CH2        CH3            CH3           CH3       OH          CH2
B1153             CH3SO2CH2        H               CH3           CH3       OH          CH2
B1154             HOCH2               H               H              H          OH          CH2
B1155             HOCH2               CH3            H              H          OH          CH2
B1156             HOCH2               CH3            CH3           H          OH          CH2
B1157             HOCH2               CH3            CH3           CH3       OH          CH2
B1158             HOCH2               H               CH3           CH3       OH          CH2
B1159             NCCH2               H               H              H          OH          CH2
B1160             NCCH2               CH3            H              H          OH          CH2
B1161             NCCH2               CH3            CH3           H          OH          CH2
B1162             NCCH2               CH3            CH3           CH3       OH          CH2
B1163             NCCH2               H               CH3           CH3       OH          CH2
B1164             CH3C(O)OCH2        H               H              H          OH          CH2
B1165             CH3C(O)OCH2        CH3            H              H          OH          CH2
B1166             CH3C(O)OCH2        CH3            CH3           H          OH          CH2
B1167             CH3C(O)OCH2        CH3            CH3           CH3       OH          CH2
B1168             CH3C(O)OCH2        H               CH3           CH3       OH          CH2
B1169             CH3OCH2            H               H              H          OH          CH2
B1170             CH3OCH2            CH3            H              H          OH          CH2
B1171             CH3OCH2            CH3            CH3           H          OH          CH2
基团              R6               R7            R8        R9         R10                    W
B1172             CH3OCH2         CH3           CH3       CH3        OH                      CH2
B1173             CH3OCH2         H              CH3       CH3        OH                      CH2
B1174             PhCH2            H              H           H           OH                      CH2
B1175             PhCH2            CH3           H          H            OH                      CH2
B1176             PhCH2            CH3           CH3       H            OH                      CH2
B1177             PhCH2            CH3           CH3       CH3         OH                      CH2
B1178             PhCH2            H              CH3       CH3         OH                      CH2
B1179             H                 H              H           H            O-K+                    CH2
B1180             H                 H              H           H            S(CH2)7CH3          CH2
B1181             H                 H              H           H            S(CH2)7CH3          CH2
B1182             H                 H              H           H            SO(CH2)7CH3         CH2
B1183             H                 H              H           H            SO2(CH2)7CH3       CH2
B1184             H                 H              H           H            NHSO2CH3             CH2
B1185             H                 H              H           H            NH(CO)S(CH2)7CH3    CH2
B1186             H                 H              H           H            Cl                      CH2
B1187             H                 H              H           H            NH2                    CH2
B1188             H                 H              H           H            OC(O)C(CH3)3          CH2
B1189             H                 H              H           H            OC(O)CH3               CH2
B1190             H                 H              H           H            OC(O)Ph                 CH2
B1191             H                 H              H           H            OC(O)-环丙基            CH2
B1192             H                 H              H           H            OC(O)CH2CH3          CH2
B1193             H                 H              H           H            OC(O)CH=CH2          CH2
B1194             H                 H              H           H            OC(O)CH=CHCH3        CH2
B1195             H                 H              H           H            OC(O)SCH3             CH2
B1196             H                 H              H           H            OC(O)S(CH2)7CH3     CH2
B1197             H                 H              H           H            OC(O)OCH2CH3         CH2
B1198             H                 H              H           H            OC(O)N(CH2CH3)2     CH2
B1199             H                 H              H           H            S-(4-Cl-苯基)           CH2
B1200             H                 H              H           H            SO-(4-Cl-苯基)          CH2
B1201             H                 H              H           H            SO2-(4-Cl-苯基)        CH2
B1202             H                 H              H           H            S-(4-CF3-苯基)         CH2
B1203             H                 H              H           H            SO-(4-CF3-苯基)        CH2
B1204             H                 H              H           H            SO2-(4-CF3-苯基)      CH2
基团             R6        R7           R8            R9           R10                      W
B1205            H          H              H              H             S-(4-NO2-苯基)           CH2
B1206            H          H              H              H             SO-(4-NO2-苯基)          CH2
B1207            H          H              H              H             SO2-(4-NO2-苯基)        CH2
B1208            H          H              H              H                                 CH2
B1209            H          H              H              H             
Figure C9981578601382
                    CH2
B1210            H          H              H              H                                 CH2
B1211            H          H              H              H             
Figure C9981578601384
                CH2
B1212            H          H              H              H                               CH2
B1179            CH3       CH3           H              H             O-K+                      CH2
B1180            CH3       CH3           H              H             S(CH2)7CH3            CH2
B1181            CH3       CH3           H              H             S(CH2)7CH3            CH2
B1182            CH3       CH3           H              H             SO(CH2)7CH3           CH2
B1183            CH3       CH3           H              H             SO2(CH2)7CH3         CH2
B1184            CH3       CH3           H              H             NHSO2CH3               CH2
B1185            CH3       CH3           H              H             NH(CO)S(CH2)7CH3      CH2
B1186            CH3       CH3           H              H             Cl                        CH2
B1187            CH3       CH3           H              H             NH2                      CH2
B1188            CH3       CH3           H              H             OC(O)C(CH3)3            CH2
B1189            CH3       CH3           H              H             OC(O)CH3                 CH2
B1190            CH3       CH3           H              H             OC(O)Ph                   CH2
B1191            CH3       CH3           H              H             OC(O)-环丙基              CH2
B1192            CH3       CH3           H              H             OC(O)CH2CH3             CH2
B1193            CH3       CH3           H              H             OC(O)CH=CH2             CH2
B1194            CH3       CH3           H              H             OC(O)CH=CHCH3           CH2
B1195            CH3       CH3           H              H             OC(O)SCH3                CH2
B1196            CH3       CH3           H              H             OC(O)S(CH2)7CH3       CH2
B1197            CH3       CH3           H              H             OC(O)OCH2CH3            CH2
B1198            CH3       CH3           H              H             OC(O)N(CH2CH3)2       CH2
B1199            CH3       CH3           H              H             S-(4-Cl-苯基)             CH2
B1200            CH3       CH3           H              H             SO-(4-Cl-苯基)            CH2
基团           R6            R7         R8        R9         R10                     W
B1201          CH3           CH3         H          H           SO2-(4-Cl-苯基)         CH2
B1202          CH3           CH3         H          H           S-(4-CF3-苯基)          CH2
B1203          CH3           CH3         H          H           SO-(4-CF3-苯基)         CH2
B1204          CH3           CH3         H          H           SO2-(4-CF3-苯基)       CH2
B1205          CH3           CH3         H          H           S-(4-NO2-苯基)          CH2
B1206          CH3           CH3         H          H           SO-(4-NO2-苯基)         CH2
B1207          CH3           CH3         H          H           SO2-(4-NO2-苯基)       CH2
B1208          CH3           CH3         H          H           
Figure C9981578601391
                  CH2
B1209          CH3           CH3         H          H                               CH2
B1210          CH3           CH3         H          H                              CH2
B1211          CH3           CH3         H          H           
Figure C9981578601394
               CH2
B1212          CH3           CH3         H          H                            CH2
B1213          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
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           W
C1           H                   H            H            OH         1           CH2
C2           CH3                H            H            OH         1           CH2
C3           CH3CH2            H            H            OH         1           CH2
C4           CH3CH2CH2        H            H            OH         1           CH2
C5           (CH3)2CH          H            H            OH         1           CH2
C6           (CH3)3C           H            H            OH         1           CH2
C7           CH3S               H            H            OH         1           CH2
C8           CH3SO              H            H            OH         1           CH2
C9           CH3SO2           H            H            OH         1           CH2
C10          Ph                  H            H            OH         1           CH2
C11          CH3O               H            H            OH         1           CH2
C12          CH3OC(O)           H            H            OH         1           CH2
C13          CH3CH2OC(O)       H            H            OH         1           CH2
C14          CH2=CHCH2        H            H            OH         1           CH2
C15          HCCCH2             H            H            OH         1           CH2
C16          CF3                H            H            OH         1           CH2
C17          (CH3)2NSO2       H            H            OH         1           CH2
C18          (CH3)2N           H            H            OH         1           CH2
C19          PhO                  H            H            OH         1           CH2
C20          PhS                  H            H            OH         1           CH2
C21          PhSO                 H            H            OH         1           CH2
C22          PhSO2               H            H            OH         1           CH2
C23          CN                   H            H            OH         1           CH2
C24          CH3                CH3         H            OH         1           CH2
C25          CH3CH2            CH3         H            OH         1           CH2
C26          CH3CH2CH2        CH3         H            OH         1           CH2
C27          (CH3)2CH          CH3         H            OH         1           CH2
C28          (CH3)3C           CH3         H            OH         1           CH2
C29          CH3S               CH3         H            OH         1           CH2
C30          CH3SO              CH3         H            OH         1           CH2
C31          CH3SO2            CH3         H            OH         1           CH2
C32          Ph                  CH3         H            OH         1           CH2
基团          R6                   R7            R16        R10       p           W
C33           CH3O                 CH3           H           OH         1           CH2
C34           CH3OC(O)             CH3           H           OH         1           CH2
C35           CH3CH2OC(O)         CH3           H           OH         1           CH2
C36           CH2=CHCH2          CH3           H           OH         1           CH2
C37           HCCCH2               CH3           H           OH         1           CH2
C38           CF3                  CH3           H           OH         1           CH2
C39           (CH3)2NSO2         CH3           H           OH         1           CH2
C40           (CH3)2N             CH3           H           OH         1           CH2
C41           PhO                   CH3           H           OH         1           CH2
C42           PhS                   CH3           H           OH         1           CH2
C43           PhSO                  CH3           H           OH         1           CH2
C44           PhSO2                CH3           H           OH         1           CH2
C45           CN                    CH3           H           OH         1           CH2
C46           H                     H              H           OH         4           CH2
C47           CH3                  H              H           OH         4           CH2
C48           CH3CH2              H              H           OH         4           CH2
C49           CH3CH2CH2          H              H           OH         4           CH2
C50           (CH3)2CH            H              H           OH         4           CH2
C51           (CH3)3C             H              H           OH         4           CH2
C52           CH3S                 H              H           OH         4           CH2
C53           CH3SO                H              H           OH         4           CH2
C54           CH3SO2             H              H           OH         4           CH2
C55           Ph                    H              H           OH         4           CH2
C56           CH3O                 H              H           OH         4           CH2
C57           CH3OC(O)             H              H           OH         4           CH2
C58           CH3CH2OC(O)         H              H           OH         4           CH2
C59           CH2=CHCH2          H              H           OH         4           CH2
C60           HCCCH2               H              H           OH         4           CH2
C61           CF3                  H              H           OH         4           CH2
C62           (CH3)2NSO2        H              H           OH         4           CH2
C63           (CH3)2N            H              H           OH         4           CH2
C64           PhO                   H              H           OH         4           CH2
C65           PhS                   H              H           OH         4           CH2
基团           R6                 R7          R16         R10         p         W
C66            PhSO                H             H            OH           4         CH2
C67            PhSO2              H             H            OH           4         CH2
C68            CN                  H             H            OH           4         CH2
C69            CH3                CH3          H            OH           4         CH2
C70            CH3CH2           CH3          H            OH           4         CH2
C71            CH3CH2CH2       CH3          H            OH           4         CH2
C72            (CH3)2CH         CH3          H            OH           4         CH2
C73            (CH3)3C          CH3          H            OH           4         CH2
C74            CH3S              CH3          H            OH           4         CH2
C75            CH3SO             CH3          H            OH           4         CH2
C76            CH3SO2           CH3          H            OH           4         CH2
C77            Ph                  CH3          H            OH           4         CH2
C78            CH3O               CH3          H            OH           4         CH2
C79            CH3OC(O)           CH3          H            OH           4         CH2
C80            CH3CH2OC(O)       CH3          H            OH           4         CH2
C81            CH2=CHCH2        CH3          H            OH           4         CH2
C82            HCCCH2             CH3          H            OH           4         CH2
C83            CF3                CH3          H            OH           4         CH2
C84            (CH3)2NSO2      CH3          H            OH           4         CH2
C85            (CH3)2N          CH3          H            OH           4         CH2
C86            PhO                 CH3          H            OH           4         CH2
C87            PhS                 CH3          H            OH           4         CH2
C88            PhSO                CH3          H            OH           4         CH2
C89            PhSO2              CH3          H            OH           4         CH2
C90            CN                  CH3          H            OH           4         CH2
C91            H                   H             H            OH           3         CH2
C92            CH3                H             H            OH           3         CH2
C93            CH3CH2           H             H            OH           3         CH2
C94            CH3CH2CH2       H             H            OH           3         CH2
C95            (CH3)2CH         H             H            OH           3         CH2
C96            (CH3)3C          H             H            OH           3         CH2
C97            CH3S              H             H            OH           3         CH2
C98            CH3SO             H             H            OH           3         CH2
基团             R6                 R7            R16           R10            p                W
C99              CH3SO2            H              H              OH              3                CH2
C100             Ph                  H              H              OH              3                CH2
C101             CH3O               H              H              OH              3                CH2
C102             CH3OC(O)           H              H              OH              3                CH2
C103             CH3CH2OC(O)       H              H              OH              3                CH2
C104             CH2=CHCH2        H              H              OH              3                CH2
C105             HCCCH2             H              H              OH              3                CH2
C106             CF3                H              H              OH              3                CH2
C107             (CH3)2NSO2       H              H              OH              3                CH2
C108             (CH3)2N           H              H              OH              3                CH2
C109             PhO                  H              H              OH              3                CH2
C110             PhS                  H              H              OH              3                CH2
C111             PhSO                 H              H              OH              3                CH2
C112             PhSO2               H              H              OH              3                CH2
C113             CN                   H              H              OH              3                CH2
C114             CH3                CH3           H              OH              3                CH2
C115             CH3CH2            CH3           H              OH              3                CH2
C116             CH3CH2CH2        CH3           H              OH              3                CH2
C117             (CH3)2CH          CH3           H              OH              3                CH2
C118             (CH3)3C           CH3           H              OH              3                CH2
C119             CH3S               CH3           H              OH              3                CH2
C120             CH3SO              CH3           H              OH              3                CH2
C121             CH3SO2            CH3           H              OH              3                CH2
C122             Ph                   CH3           H              OH              3                CH2
C123             CH3O               CH3           H              OH              3                CH2
C124             CH3OC(O)           CH3           H              OH              3                CH2
C125             CH3CH2OC(O)       CH3           H              OH              3                CH2
C126             CH2=CHCH2        CH3           H              OH              3                CH2
C127             HCCCH2             CH3           H              OH              3                CH2
C128             CF3                CH3           H              OH              3                CH2
C129             (CH3)2NSO2       CH3           H              OH              3                CH2
C130             (CH3)2N           CH3           H              OH              3                CH2
C131             PhO                  CH3           H              OH              3                CH2
基团            R6               R7               R16          R10          p          W
C132            PhS               CH3              H             OH            3          CH2
C133            PhSO              CH3              H             OH            3          CH2
C134            PhSO2            CH3              H             OH            3          CH2
C135            CN                CH3              H             OH            3          CH2
C136            CH3CH2          CH3CH2         H             OH            1          CH2
C137            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          CH2
C144            CH3              CH3              CH3          OH            1          CH2
C145            CH3CH2          CH3CH2          CH3          OH            1          CH2
C146            H                 H                  H             OH            2          CH2
C147            CH3               CH3              H             OH            2          CH2
C148            CH3CH2          CH3CH2          H             OH            2          CH2
C149            H                 H                  H             OH            5          CH2
C150            CH3               CH3              H             OH            5          CH2
C151            CH3CH2          CH3CH2          H             OH            5          CH2
C152            CH3              H                  H             OH            2          CH2
下表4中,Q代表Q3
Figure C9981578601441
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        R10       o
D1            H                     H           H           H           OH         2
D2            CH3                  H           H           H           OH         2
D3            CH3CH2              H           H           H           OH         2
D4            CH3CH2CH2          H           H           H           OH         2
D5            (CH3)2CH            H           H           H           OH         2
D6            (CH3)3C             H           H           H           OH         2
D7            CH3S                 H           H           H           OH         2
D8            CH3SO                H           H           H           OH         2
D9            CH3SO2              H           H           H           OH         2
D10           Ph                    H           H           H           OH         2
D11           CH3O                 H           H           H           OH         2
D12           CH2=CHCH2          H           H           H           OH         2
D13           HCCCH2               H           H           H           OH         2
D14           CF3                  H           H           H           OH         2
D15           PhO                   H           H           H           OH         2
D16           PhS                   H           H           H           OH         2
D17           PhSO                  H           H           H           OH         2
D18           PhSO2                H           H           H           OH         2
D19           CH3                  CH3        H           H           OH         2
D20           CH3CH2              CH3        H           H           OH         2
D21           CH3CH2CH2          CH3        H           H           OH         2
D22           (CH3)2CH            CH3        H           H           OH         2
D23           (CH3)3C             CH3        H           H           OH         2
D24           CH3S                 CH3        H           H           OH         2
D25           CH3SO                CH3        H           H           OH         2
D26           CH3SO2              CH3        H           H           OH         2
D27           Ph                     CH3        H           H           OH         2
D28           CH3O                 CH3        H           H           OH         2
D29           CH2=CHCH2          CH3        H           H           OH         2
D30           HCCCH2               CH3        H           H           OH         2
D31           CF3                  CH3        H           H           OH         2
D32           PhO                   CH3        H           H           OH         2
基团          R6                R7            R8        R12          R10           o
D33           PhS                CH3           H           H             OH             2
D34           PhSO               CH3           H           H             OH             2
D35           PhSO2             CH3           H           H             OH             2
D36           H                  H              H           H             OH             3
D37           CH3               H              H           H             OH             3
D38           CH3CH2           H              H           H             OH             3
D39           CH3CH2CH2       H              H           H             OH             3
D40           (CH3)2CH         H              H           H             OH             3
D41           (CH3)3C          H              H           H             OH             3
D42           CH3S              H              H           H             OH             3
D43           CH3SO             H              H           H             OH             3
D44           CH3SO2           H              H           H             OH             3
D45           Ph                 H              H           H             OH             3
D46           CH3O              H              H           H             OH             3
D47           CH2=CHCH2       H              H           H             OH             3
D48           HCCCH2            H              H           H             OH             3
D49           CF3               H              H           H             OH             3
D50           PhO                H              H           H             OH             3
D51           PhS                H              H           H             OH             3
D52           PhSO               H              H           H             OH             3
D53           PhSO2             H              H           H             OH             3
D54           CH3               CH3           H           H             OH             3
D55           CH3CH2           CH3           H           H             OH             3
D56           CH3CH2CH2      CH3           H           H             OH             3
D57           (CH3)2CH         CH3           H           H             OH             3
D58           (CH3)3C          CH3           H           H             OH             3
D59           CH3S              CH3           H           H             OH             3
D60           CH3SO             CH3           H           H             OH             3
D61           CH3SO2           CH3           H           H             OH             3
D62           Ph                 CH3           H           H             OH             3
D63           CH3O              CH3           H           H             OH             3
D64           CH2=CHCH2       CH3           H           H             OH             3
D65           HCCCH2            CH3           H           H             OH             3
基团           R6                 R7           R8         R12        R10       o
D66            CF3                CH3          H           H           OH          3
D67            PhO                 CH3          H           H           OH          3
D68            PhS                 CH3          H           H           OH          3
D69            PhSO                CH3          H           H           OH          3
D70            PhSO2              CH3          H           H           OH          3
D71            H                   H             H           H           OH          4
D72            CH3                H             H           H           OH          4
D73            CH3CH2            H             H           H           OH          4
D74            CH3CH2CH2        H             H           H           OH          4
D75            (CH3)2CH          H             H           H           OH          4
D76            (CH3)3C           H             H           H           OH          4
D77            CH3S               H             H           H           OH          4
D78            CH3SO              H             H           H           OH          4
D79            CH3SO2            H             H           H           OH          4
D80            Ph                  H             H           H           OH          4
D81            CH3O               H             H           H           OH          4
D82            CH2=CHCH2        H             H           H           OH          4
D83            HCCCH2             H             H           H           OH          4
D84            CF3                H             H           H           OH          4
D85            PhO                 H             H           H           OH          4
D86            PhS                 H             H           H           OH          4
D87            PhSO                H             H           H           OH          4
D88            PhSO2              H             H           H           OH          4
D89            CH3                CH3          H           H           OH          4
D90            CH3CH2           CH3          H           H           OH          4
D91            CH3CH2CH2       CH3          H           H           OH          4
D92            (CH3)2CH         CH3          H           H           OH          4
D93            (CH3)3C          CH3          H           H           OH          4
D94            CH3S              CH3          H           H           OH          4
D95            CH3SO             CH3          H           H           OH          4
D96            CH3SO2          CH3          H           H           OH          4
D97            Ph                 CH3          H           H           OH          4
D98            CH3O              CH3          H           H           OH          4
基团             R6                 R7              R8        R12         R10          o
D99              CH2=CHCH2        CH3             H          H            OH            4
D100             HCCCH2             CH3             H          H            OH            4
D101             CF3                CH3             H          H            OH            4
D102             PhO                 CH3             H          H            OH            4
D103             PhS                 CH3             H          H            OH            4
D104             PhSO                CH3             H          H            OH            4
D105             PhSO2              CH3             H          H            OH            4
D106             H                   H                H          CH3         OH            4
D107             H                   H                H          CH3         OH            3
D108             H                   H                H          H            OH            1
D109             CH3                H                H          H            OH            1
D110             CH3OC(O)           CH3             H          H            OH            1
D111             CH3CH2OC(O)       CH3             H          H            OH            1
D112             CH3O               CH3             H          H            OH            1
D113             CH3S               CH3             H          H            OH            1
D114             CH3SO              CH3             H          H            OH            1
D115             CH3SO2            CH3             H          H            OH            1
D116             CH3CH2            H                H          H            OH            1
D117             CH3OC(O)           CH3CH2         H          H            OH            1
D118             CH3CH2OC(O)       CH3CH2         H          H            OH            1
D119             CH3O               CH3CH2         H          H            OH            1
D120             CH3S               CH3CH2         H          H            OH            1
D121             CH3SO              CH3CH2         H          H            OH            1
D122             CH3SO2            CH3CH2         H          H            OH            1
D123             CH3CH2S           CH3             H          H            OH            1
D124             CH3CH2SO          CH3             H          H            OH            1
D125             CH3CH2SO2        CH3             H          H            OH            1
D126             CH3CH2S           CH3CH2         H          H            OH            1
D127             CH3CH2SO          CH3CH2         H          H            OH            1
D128             CH3CH2SO2        CH3CH2         H          H            OH            1
D129             H                    H                CH3       H            OH            1
D130             CH3                 H                CH3       H            OH            1
D131             CH3OC(O)            CH3             CH3       H            OH            1
基团            R6                   R7            R8          R12        R10      o
D132            CH3CH2OC(O)         CH3           CH3         H           OH        1
D133            CH3O                 CH3           CH3         H           OH        1
D134            CH3S                 CH3           CH3         H           OH        1
D135            CH3SO                CH3           CH3         H           OH        1
D136            CH3SO2              CH3           CH3         H           OH        1
D137            H                      H              H            CH3        OH        1
D138            CH3                   H              H            CH3        OH        1
D139            H                      H              CH3         CH3        OH        1
D140            CH3CH2OC(O)         CH3           H            H           OH        4
下表5中,Q代表Q4
Figure C9981578601491
并且Q4代表下列基团E:
表5:基团E:
基团            R6               R7            R10         X           Y          W          q
E1              H                 H              OH           S           CH2       CH2       2
E2              CH3              H              OH           S           CH2       CH2       2
E3              CH3              CH3           OH           S           CH2       CH2       2
E4              CH3OC(O)         H              OH           S           CH2       CH2       2
E5              CH3              CH3OC(O)      OH           S           CH2       CH2       2
E6              H                 H              OH           SO          CH2       CH2       2
E7              CH3              H              OH           SO          CH2       CH2       2
E8              CH3              CH3           OH           SO          CH2       CH2       2
E9              CH3OC(O)         H              OH           SO          CH2       CH2       2
E10             CH3              CH3OC(O)      OH           SO          CH2       CH2       2
E11             H                 H              OH           SO2        CH2       CH2       2
基团         R6           R7             R10           X            Y            W            q
E12          CH3          H               OH             SO2         CH2         CH2         2
E13          CH3          CH3            OH             SO2         CH2         CH2         2
E14          CH3OC(O)     H               OH             SO2         CH2         CH2         2
E15          CH3          CH3OC(O)       OH             SO2         CH2         CH2         2
E46          H             H               OH              CO           O            CH2         2
E17          CH3          H               OH              CO           O            CH2         2
E18          CH3          CH3            OH             CO           O            CH2          2
E19          CH3OC(O)     H               OH              CO           O            CH2         2
E20          CH3          CH3OC(O)       OH             CO           O            CH2          2
E21          H             H               OH              CO           O            CH2         2
E22          CH3          H               OH             CO           O            CH2          2
E23          CH3          CH3            OH             CO           O            CH2         2
E24          CH3OC(O)     H               OH             CO           O            CH2         2
E25          CH3          CH3OC(O)       OH             CO           O            CH2         2
E26          H             H               OH             CO           O            CH2         2
E27          CH3          H               OH             CO           O            CH2         2
E28          CH3          CH3            OH             CO           O            CH2         2
E29          CH3OC(O)     H               OH             CO           O            CH2         2
E30          CH3          CH3OC(O)       OH             CO           O            CH2         2
下表6中,Q代表Q5
Figure C9981578601501
并且Q5代表下列基团F:
表6:基团F:
基团         R6           R7            R8            R10
F1           H             H               H              OH
F2           CH3          H               H              OH
基团                R6             R7            R8          R10
F3                  CH3            CH3           H            OH
F4                  CH3            CH3           CH3         OH
F5                  H               H               CH3         OH
F6                  H               CH3           CH3         OH
表7:式Ia化合物
Figure C9981578601511
化合物序号          R2            R3           R4           R5         Q1           p
A1                  H              H              H            CF3         B24           0
A2                  CH3           H              H            CF3         B24           0
A3                  CH3CH2       H              H            CF3         B24           0
A4                  (CH3)2CH     H              H            CF3         B24           0
A5                  (CH3)3C      H              H            CF3         B24           0
A6                  环丙基          H              H            CF3         B24           0
A7                  CH3(CH2)2   H              H            CF3         B24           0
A8                  CH3OCH2      H              H            CF3         B24           0
A9                  CH3O(CH2)2  H              H            CF3         B24           0
A10                 Ph              H              H            CF3         B24           0
A11                 PhO             H              H            CF3         B24           0
A12                 PhS             H              H            CF3         B24           0
A13                 PhSO            H              H            CF3         B24           0
A14                 PhSO2          H              H            CF3         B24           0
A15                 CH3S           H              H            CF3         B24           0
A16                 CH3SO          H              H            CF3         B24           0
A17                 CF3            H              H            CF3         B24           0
A18                 F2CH           H              H            CF3         B24           0
化合物序号          R2                          R3             R4            R5              Q1           p
A19                 HCC                          H                H              CF3             B24            0
A20                 CH3CC                       H                H              CF3             B24            0
A21                 CH2=CH                     H                H              CF3             B24            0
A22                 CH2=CHCH2                H                H              CF3             B24            0
A23                 CH3SO2N(CH3)             H                H              CF3             B24            0
A24                 (CH3)2N                   H                H              CF3             B24            0
A25                 (CH3)2NSO2               H                H              CF3             B24            0
A26                 ClCH2                      H                H              CF3             B24            0
A27                 CH3SCH2                   H                H              CF3             B24            0
A28                 CH3SOCH2                  H                H              CF3             B24            0
A29                 CH3SO2CH2                H                H              CF3             B24            0
A30                 [1.2.4]-三唑-1-基甲基        H                H              CF3             B24            0
A31                 CH3                        CF3             H              CH3             B24            0
A32                 CH3                        CH3             H              CF3             B24            0
A33                 H                            H                H             CF3CF2         B24            0
A34                 CH3                         H                H             CF3CF2         B24            0
A35                 CH3CH2                    H                H              CF3CF2         B24            0
A36                 环丙基                       H                H              CF3CF2         B24            0
A37                 (CH3)3C                   H                H              CF3CF2         B24            0
A38                 (CH3)2CH                  H                H              CF3CF2         B24            0
A39                 CH3(CH2)2                H                H              CF3CF2         B24            0
A40                 CH3OCH2                   H                H              CF3CF2         B24            0
A41                 CH3O(CH2)2               H                H              CF3CF2         B24            0
A42                 Ph                           H                H              CF3CF2         B24            0
A43                 PhO                          H                H              CF3CF2         B24            0
A44                 PhS                          H                H              CF3CF2         B24            0
A45                 PhSO                         H                H              CF3CF2         B24            0
A46                 PhSO2                       H                H              CF3CF2         B24            0
A47                 CH3S                        H                H              CF3CF2         B24            0
A48                 CH3SO                       H                H              CF3CF2         B24            0
A49                 CF3                         H                H              CF3CF2         B24            0
化合物序号        R2                         R3              R4            R5                     Q1            p
A50               F2CH                       H                H              CF3CF2                B24             0
A51               HCC                         H                H              CF3CF2                B24             0
A52               CH3CC                      H                H              CF3CF2                B24             0
A53               CH2=CH                    H                H              CF3CF2                B24             0
A54               CH2=CHCH2                H                H              CF3CF2                B24             0
A55               CH3SO2N(CH3)             H                H              CF3CF2                B24             0
A56               (CH3)2N                   H                H              CF3CF2                B24             0
A57               (CH3)2NSO2               H                H              CF3CF2                B24             0
A58               ClCH2                      H                H              CF3CF2                B24             0
A59               CH3SCH2                   H                H              CF3CF2                B24             0
A60               CH3SOCH2                  H                H              CF3CF2                B24             0
A61               CH3SO2CH2                H                H              CF3CF2                B24             0
A62               [1.2.4]-三唑-1-基甲基        H                H              CF3CF2                B24             0
A63               H                            H                H              CF3CF2CF2            B24             0
A64               CH3                         H                H              CF3CF2CF2            B24             0
A65               CH3CH2                    H                H              CF3CF2CF2            B24             0
A66               环丙基                       H                H              CF3CF2CF2            B24             0
A67               (CH3)3C                   H                H              CF3CF2CF2            B24             0
A68               (CH3)2CH                  H                H              CF3CF2CF2            B24             0
A69               CH3(CH2)2                H                H              CF3CF2CF2            B24             0
A70               CH3OCH2                   H                H              CF3CF2CF2            B24             0
A71               CH3O(CH2)2              H                H              CF3CF2CF2            B24             0
A72               Ph                          H                H              CF3CF2CF2            B24             0
A73               PhO                         H                H              CF3CF2CF2            B24             0
A74               PhS                         H                H              CF3CF2CF2            B24             0
A75               PhSO                        H                H              CF3CF2CF2            B24             0
A76               PhSO2                      H                H              CF3CF2CF2            B24             0
A77               CH3S                       H                H              CF3CF2CF2            B24             0
A78               CH3SO                      H                H              CF3CF2CF2            B24             0
A79               CF3                        H                H              CF3CF2CF2            B24             0
A80               F2CH                       H                H              CF3CF2CF2            B24             0
化合物序号         R2                             R3             R4             R5                Q1           p
A81                HCC                             H               H               CF3CF2CF2       B24            0
A82                CH3CC                          H               H               CF3CF2CF2       B24            0
A83                CH2=CH                        H               H               CF3CF2CF2       B24            0
A84                CH2=CHCH2                    H               H               CF3CF2CF2       B24            0
A85                CH3SO2N(CH3)                 H               H               CF3CF2CF2       B24            0
A86                (CH3)2N                       H               H               CF3CF2CF2       B24            0
A87                (CH3)2NSO2                   H               H               CF3CF2CF2       B24            0
A88                ClCH2                          H               H               CF3CF2CF2       B24            0
A89                CH3SCH2                       H               H               CF3CF2CF2       B24            0
A90                CH3SOCH2                      H               H               CF3CF2CF2       B24            0
A91                CH3SO2CH2                    H               H               CF3CF2CF2       B24            0
A92                [1.2.4]-三唑-1-基甲基            H               H               CF3CF2CF2       B24            0
A93                H                                H               H               CF2Cl              B24            0
A94                CH3                             H               H               CF2Cl              B24            0
A95                CH3CH2                         H              H               CF2Cl              B24            0
A96                环丙基                           H               H               CF2Cl              B24            0
A97                (CH3)3C                       H               H               CF2Cl              B24            0
A98                (CH3)2CH                      H               H               CF2Cl              B24            0
A99                CH3(CH2)2                    H               H               CF2Cl              B24            0
A100               CH3OCH2                       H               H               CF2Cl              B24            0
A101               CH3O(CH2)2                   H               H               CF2Cl              B24            0
A102               Ph                               H               H               CF2Cl              B24            0
A103               PhO                              H               H               CF2Cl              B24            0
A104               PhS                              H               H               CF2Cl              B24            0
A105               PhSO                             H               H               CF2Cl              B24            0
A106               PhSO2                           H               H               CF2Cl              B24            0
A107               CH3S                            H               H               CF2Cl              B24            0
A108               CH3SO                           H               H               CF2Cl              B24            0
A109               CF3                             H               H               CF2Cl              B24            0
A110               F2CH                            H               H               CF2Cl              B24            0
A111               HCC                              H               H               CF2Cl              B24            0
化合物序号        R2                             R3            R4          R5             Q1          p
A112              CH3CC                          H              H            CF2Cl          B24           0
A113              CH2=CH                        H              H            CF2Cl          B24           0
A114              CH2=CHCH2                    H              H            CF2Cl          B24           0
A115              CH3SO2N(CH3)                 H              H            CF2Cl          B24           0
A116              (CH3)2N                       H              H            CF2Cl          B24           0
A117              (CH3)2NSO2                   H              H            CF2Cl          B24           0
A118              ClCH2                           H              H            CF2Cl          B24           0
A119              CH3SCH2                       H              H            CF2Cl          B24           0
A120              CH3SOCH2                      H              H            CF2Cl          B24           0
A121              CH3SO2CH2                    H              H            CF2Cl          B24           0
A122              [1.2.4]-三唑-1-基甲基            H              H            CF2Cl          B24           0
A123              H                                H              H            CHF2           B24           0
A124              CH3                             H              H            CHF2           B24           0
A125              CH3CH2                        H              H            CHF2           B24           0
A126              环丙基                           H              H            CHF2           B24           0
A127              (CH3)3C                       H              H            CHF2           B24           0
A128              (CH3)2CH                      H              H            CHF2           B24           0
A129              CH3(CH2)2                    H              H            CHF2           B24           0
A130              CH3OCH2                       H              H            CHF2           B24           0
A131              CH3O(CH2)2                   H              H            CHF2           B24           0
A132              Ph                               H              H            CHF2           B24           0
A133              PhO                              H              H            CHF2           B24           0
A134              PhS                              H              H            CHF2           B24           0
A135              PhSO                             H              H            CHF2           B24           0
A136              PhSO2                           H              H            CHF2           B24           0
A137              CH3S                            H              H            CHF2           B24           0
A138              CH3SO                           H              H            CHF2           B24           0
A139              CF3                             H              H            CHF2           B24           0
A140              F2CH                            H              H            CHF2           B24           0
A141              HCC                              H              H            CHF2           B24           0
A142              CH3CC                           H              H            CHF2           B24           0
化合物序号       R2                                R3            R4           R5            Q1         p
A143             CH2=CH                           H              H             CHF2          B24          0
A144             CH2=CHCH2                       H              H             CHF2          B24          0
A145             CH3SO2N(CH3)                    H              H             CHF2          B24          0
A146             (CH3)2N                          H              H             CHF2          B24          0
A147             (CH3)2NSO2                      H              H             CHF2          B24          0
A148             ClCH2                             H              H             CHF2          B24          0
A149             CH3SCH2                          H              H             CHF2          B24          0
A150             CH3SOCH2                         H              H             CHF2          B24          0
A151             CH3SO2CH2                       H              H             CHF2          B24          0
A152             [1.2.4]-三唑-1-基甲基               H              H             CHF2          B24          0
A153             H                                   H              H             CCl3          B24          0
A154             CH3                                H              H             CCl3          B24          0
A155             CH3CH2                           H              H             CCl3          B24          0
A156             环丙基                              H              H             CCl3          B24          0
A157             (CH3)3C                          H              H             CCl3          B24          0
A158             (CH3)2CH                         H              H             CCl3          B24          0
A159             CH3(CH2)2                       H              H             CCl3          B24          0
A160             CH3OCH2                          H              H             CCl3          B24          0
A161             CH3O(CH2)2                      H              H             CCl3          B24          0
A162             Ph                                  H              H             CCl3          B24          0
A163             PhO                                 H              H             CCl3          B24          0
A164             PhS                                 H              H             CCl3          B24          0
A165             PhSO                                H              H             CCl3          B24          0
A166             PhSO2                              H              H             CCl3          B24          0
A167             CH3S                               H              H             CCl3          B24          0
A168             CH3SO                              H              H             CCl3          B24          0
A169             CF3                                H              H             CCl3          B24          0
A170             F2CH                               H              H             CCl3          B24          0
A171             HCC                                 H              H             CCl3          B24          0
A172             CH3CC                              H              H             CCl3          B24          0
A173             CH2=CH                            H              H             CCl3          B24          0
化合物序号        R2                            R3            R4           R5           Q1          p
A174              CH2=CHCH2                   H              H             CCl3         B24          0
A175              CH3SO2N(CH3)                H              H             CCl3         B24          0
A176              (CH3)2N                      H              H             CCl3         B24          0
A177              (CH3)2NSO2                  H              H             CCl3         B24          0
A178              ClCH2                         H              H             CCl3         B24          0
A179              CH3SCH2                      H              H             CCl3         B24          0
A180              CH3SOCH2                     H              H             CCl3         B24          0
A181              CH3SO2CH2                  H              H             CCl3         B24          0
A182              [1.2.4]-三唑-1-基甲基          H              H             CCl3         B24          0
A183              H                              H              CH3          CF3          B24          0
A184              CH3                           H              CH3          CF3          B24          0
A185              CH3CH2                      H              CH3          CF3          B24          0
A186              环丙基                         H              CH3          CF3          B24          0
A187              (CH3)3C                     H              CH3          CF3          B24          0
A188              (CH3)2CH                    H              CH3          CF3          B24          0
A189              CH3(CH2)2                  H              CH3          CF3          B24          0
A190              CH3OCH2                     H              CH3          CF3          B24          0
A191              CH3O(CH2)2                 H              CH3          CF3          B24          0
A192              Ph                             H              CH3          CF3          B24          0
A193              PhO                            H              CH3          CF3          B24          0
A194              PhS                            H              CH3          CF3          B24          0
A195              PhSO                           H              CH3          CF3          B24          0
A196              PhSO2                         H              CH3          CF3          B24          0
A197              CH3S                          H              CH3          CF3          B24          0
A198              CH3SO                         H              CH3          CF3          B24          0
A199              CF3                           H              CH3          CF3          B24          0
A200              F2CH                          H              CH3          CF3          B24          0
A201              HCC                            H              CH3          CF3          B24          0
A202              CH3CC                         H              CH3          CF3          B24          0
A203              CH2=CH                       H              CH3          CF3          B24          0
A204              CH2=CHCH2                   H              CH3          CF3          B24          0
化合物序号       R2                     R3          R4           R5               Q1         p
No.
A205             CH3SO2N(CH3)         H            CH3          CF3              B24         0
A206             (CH3)2N               H            CH3          CF3              B24         0
A207             (CH3)2NSO2           H            CH3          CF3              B24         0
A208             ClCH2                  H            CH3          CF3              B24         0
A209             CH3SCH2               H            CH3          CF3              B24         0
A210             CH3SOCH2              H            CH3          CF3              B24         0
A211             CH3SO2CH2            H            CH3          CF3              B24         0
A212             H                        H            CH3          CF3CF2         B24         0
A213             CH3                     H            CH3          CF3CF2         B24         0
A214             CH3CH2                H            CH3          CF3CF2          B24         0
A215             环丙基                   H            CH3          CF3CF2          B24         0
A216             (CH3)3C               H            CH3          CF3CF2          B24         0
A217             (CH3)2CH              H            CH3          CF3CF2          B24         0
A218             CH3(CH2)2            H            CH3          CF3CF2          B24         0
A219             CH3OCH2               H            CH3          CF3CF2          B24         0
A220             CH3O(CH2)2           H            CH3          CF3CF2          B24         0
A221             Ph                       H            CH3          CF3CF2          B24         0
A222             PhO                      H            CH3          CF3CF2          B24         0
A223             PhS                      H            CH3          CF3CF2          B24         0
A224             PhSO                     H            CH3          CF3CF2          B24         0
A225             PhSO2                   H            CH3          CF3CF2          B24         0
A226             CH3S                    H            CH3          CF3CF2          B24         0
A227             CH3SO                   H            CH3          CF3CF2          B24         0
A228             CF3                     H            CH3          CF3CF2          B24         0
A229             F2CH                    H            CH3          CF3CF2          B24         0
A230             HCC                      H            CH3          CF3CF2          B24         0
A231             CH3CC                   H            CH3          CF3CF2          B24         0
A232             CH2=CH                 H            CH3          CF3CF2          B24         0
A233             CH2=CHCH2            H            CH3          CF3CF2          B24         0
A234             CH3SO2N(CH3)         H            CH3          CF3CF2          B24         0
A235             (CH3)2N               H            CH3          CF3CF2          B24         0
A236             (CH3)2NSO2           H            CH3          CF3CF2          B24         0
化合物序号         R2                  R3         R4            R5                     Q1         p
A237               ClCH2               H           CH3           CF3CF2                B24         0
A238               CH3SCH2            H           CH3           CF3CF2                B24         0
A239               CH3SOCH2           H           CH3           CF3CF2                B24         0
A240               CH3SO2CH2         H           CH3           CF3CF2                B24         0
A241               H                     H           CH3           CF3CF2CF2            B24         0
A242               CH3                  H           CH3           CF3CF2CF2            B24         0
A243               CH3CH2             H           CH3           CF3CF2CF2            B24         0
A244               环丙基                H           CH3           CF3CF2CF2            B24         0
A245               (CH3)3C            H           CH3           CF3CF2CF2            B24         0
A246               (CH3)2CH           H           CH3           CF3CF2CF2            B24         0
A247               CH3(CH2)2         H           CH3           CF3CF2CF2            B24         0
A248               CH3OCH2            H           CH3           CF3CF2CF2            B24         0
A249               CH3O(CH2)2        H           CH3           CF3CF2CF2            B24         0
A250               Ph                    H           CH3           CF3CF2CF2            B24         0
A251               PhO                   H           CH3           CF3CF2CF2            B24         0
A252               PhS                   H           CH3           CF3CF2CF2            B24         0
A253               PhSO                  H           CH3           CF3CF2CF2            B24         0
A254               PhSO2                H           CH3           CF3CF2CF2            B24         0
A255               CH3S                 H           CH3           CF3CF2CF2            B24         0
A256               CH3SO                H           CH3           CF3CF2CF2            B24         0
A257               CF3                  H           CH3           CF3CF2CF2            B24         0
A258               F2CH                 H           CH3           CF3CF2CF2            B24         0
A259               HCC                   H           CH3           CF3CF2CF2            B24         0
A260               CH3CC                H           CH3           CF3CF2CF2            B24         0
A261               CH2=CH              H           CH3           CF3CF2CF2            B24         0
A262               CH2=CHCH2         H           CH3           CF3CF2CF2            B24         0
A263               CH3SO2N(CH3)      H           CH3           CF3CF2CF2            B24         0
A264               (CH3)2N            H           CH3           CF3CF2CF2            B24         0
A265               (CH3)2NSO2        H           CH3           CF3CF2CF2            B24         0
A266               ClCH2               H            CH3           CF3CF2CF2            B24         0
A267               CH3SCH2            H           CH3           CF3CF2CF2            B24         0
A268               CH3SOCH2           H           CH3           CF3CF2CF2            B24         0
化合物序号          R2                  R3          R4           R5                 Q1        p
A269                CH3SO2CH2        H            CH3          CF3CF2CF2       B24          0
A270                H                    H            CH3          CF2Cl             B24          0
A271                CH3                 H            CH3          CF2Cl             B24          0
A272                CH3CH2            H            CH3          CF2Cl             B24          0
A273                环丙基               H            CH3          CF2Cl             B24          0
A274                (CH3)3C           H            CH3          CF2Cl             B24          0
A275                (CH3)2CH          H            CH3          CF2Cl             B24          0
A276                CH3(CH2)2        H            CH3          CF2Cl             B24          0
A277                CH3OCH2           H            CH3          CF2Cl             B24          0
A278                CH3O(CH2)2       H            CH3          CF2Cl             B24          0
A279                Ph                   H            CH3          CF2Cl             B24          0
A280                PhO                  H            CH3          CF2Cl             B24          0
A281                PhS                  H            CH3          CF2Cl             B24          0
A282                PhSO                 H            CH3          CF2Cl             B24          0
A283                PhSO2               H            CH3          CF2Cl             B24          0
A284                CH3S                H            CH3          CF2Cl             B24          0
A285                CH3SO               H            CH3          CF2Cl             B24          0
A286                CF3                 H            CH3          CF2Cl             B24          0
A287                F2CH                H            CH3          CF2Cl             B24          0
A288                HCC                  H            CH3          CF2Cl             B24          0
A289                CH3CC               H            CH3          CF2Cl             B24          0
A290                CH2=CH             H            CH3          CF2Cl             B24          0
A291                CH2=CHCH2         H            CH3          CF2Cl             B24          0
A292                CH3SO2N(CH3)      H            CH3          CF2Cl             B24          0
A293                (CH3)2N            H            CH3          CF2Cl             B24          0
A294                (CH3)2NSO2        H            CH3          CF2Cl             B24          0
A295                ClCH2                H            CH3          CF2Cl             B24          0
A296                CH3SCH2            H            CH3          CF2Cl             B24          0
A297                CH3SOCH2           H            CH3          CF2Cl             B24          0
A298                CH3SO2CH2         H            CH3          CF2Cl             B24          0
A299                H                     H            CH3          CHF2              B24          0
A300                CH3                  H            CH3          CHF2              B24          0
化合物序号         R2                  R3        R4           R5           Q1          p
A301               CH3CH2             H          CH3          CHF2         B24          0
A302               环丙基                H          CH3          CHF2         B24          0
A303               (CH3)3C            H          CH3          CHF2         B24          0
A304               (CH3)2CH           H          CH3          CHF2         B24          0
A305               CH3(CH2)2         H          CH3          CHF2         B24          0
A306               CH3OCH2            H          CH3          CHF2         B24          0
A307               CH3O(CH2)2        H          CH3          CHF2         B24          0
A308               Ph                    H          CH3          CHF2         B24          0
A309               PhO                   H          CH3          CHF2         B24          0
A310               PhS                   H          CH3          CHF2         B24          0
A311               PhSO                  H          CH3          CHF2         B24          0
A312               PhSO2               H          CH3          CHF2         B24          0
A313               CH3S                H          CH3          CHF2         B24          0
A314               CH3SO               H          CH3          CHF2         B24          0
A315               CF3                 H          CH3          CHF2         B24          0
A316               F2CH                H          CH3          CHF2         B24          0
A317               HCC                  H          CH3          CHF2         B24          0
A318               CH3CC               H          CH3          CHF2         B24          0
A319               CH2=CH             H          CH3          CHF2         B24          0
A320               CH2=CHCH2         H          CH3          CHF2         B24          0
A321               CH3SO2N(CH3)      H          CH3          CHF2         B24          0
A322               (CH3)2N            H          CH3          CHF2         B24          0
A323               (CH3)2NSO2        H          CH3          CHF2         B24          0
A324               ClCH2               H          CH3           CHF2         B24          0
A325               CH3SCH2            H          CH3          CHF2         B24          0
A326               CH3SOCH2           H          CH3          CHF2         B24          0
A327               CH3SO2CH2         H          CH3          CHF2         B24          0
A328               H                     H          CH3          CCl3         B24          0
A329               CH3                  H          CH3          CCl3         B24          0
A330               CH3CH2             H          CH3          CCl3         B24          0
A331               (CH3)3C            H          CH3          CCl3         B24          0
A332               (CH3)2CH           H          CH3          CCl3         B24          0
化合物序号         R2                  R3        R4          R5          Q1        p
A333               环丙基               H          CH3         CCl3        B24         0
A334               CH3(CH2)2        H          CH3         CCl3        B24         0
A335               CH3OCH2           H          CH3         CCl3        B24         0
A336               CH3O(CH2)2       H          CH3         CCl3        B24         0
A337               Ph                   H          CH3         CCl3        B24         0
A338               PhO                  H          CH3         CCl3        B24         0
A339               PhS                  H          CH3         CCl3        B24         0
A340               PhSO                 H          CH3         CCl3        B24         0
A341               PhSO2               H          CH3         CCl3        B24         0
A342               CH3S                H          CH3         CCl3        B24         0
A343               CH3SO               H          CH3         CCl3        B24         0
A344               CF3                 H          CH3         CCl3        B24         0
A345               F2CH                H          CH3         CCl3        B24         0
A346               HCC                  H          CH3         CCl3        B24         0
A347               CH3CC               H          CH3         CCl3        B24         0
A348               CH2=CH             H          CH3         CCl3        B24         0
A349               CH2=CHCH2         H          CH3         CCl3        B24         0
A350               CH3SO2N(CH3)      H          CH3         CCl3        B24         0
A351               (CH3)2N            H          CH3         CCl3        B24         0
A352               (CH3)2NSO2        H          CH3         CCl3        B24         0
A353               ClCH2               H          CH3         CCl3        B24         0
A354               CH3SCH2            H          CH3         CCl3        B24         0
A355               CH3SOCH2           H          CH3         CCl3        B24         0
A356               CH3SO2CH2         H          CH3         CCl3        B24         0
A357               H                     H          Ph           CF3         B24         0
A358               CH3                 H          Ph           CF3          B24         0
A359               CH3CH2             H          Ph           CF3         B24         0
A360               环丙基                H          Ph           CF3         B24         0
A361               (CH3)3C            H          Ph           CF3         B24         0
A362               (CH3)2CH           H          Ph           CF3         B24         0
A363               CH3(CH2)2         H          Ph           CF3         B24         0
A364               CH3OCH2            H          Ph           CF3         B24         0
化合物序号           R2                  R3        R4        R5              Q1       p
A365                 CH3O(CH2)2       H          Ph         CF3             B24        0
A366                 Ph                   H          Ph         CF3             B24        0
A367                 PhO                  H          Ph         CF3             B24        0
A368                 PhS                  H          Ph         CF3             B24        0
A369                 PhSO                 H          Ph         CF3             B24        0
A370                 PhSO2               H          Ph         CF3             B24        0
A371                 CH3S                H          Ph         CF3             B24        0
A372                 CH3SO               H          Ph         CF3             B24        0
A373                 CF3                 H          Ph         CF3             B24        0
A374                 F2CH                H          Ph         CF3             B24        0
A375                 HCC                  H          Ph         CF3             B24        0
A376                 CH3CC               H          Ph         CF3             B24        0
A377                 CH2=CH             H          Ph         CF3             B24        0
A378                 CH2=CHCH2         H          Ph         CF3             B24        0
A379                 CH3SO2N(CH3)      H          Ph         CF3             B24        0
A380                 (CH3)2N            H          Ph         CF3             B24        0
A381                 (CH3)2NSO2       H          Ph          CF3             B24        0
A382                 ClCH2               H          Ph         CF3             B24        0
A383                 CH3SCH2            H          Ph         CF3             B24        0
A384                 CH3SOCH2           H          Ph         CF3             B24        0
A385                 CH3SO2CH2        H          Ph         CF3             B24        0
A386                 H                    H          Ph         CF3CF2         B24        0
A387                 CH3                 H          Ph         CF3CF2         B24        0
A388                 CH3CH2             H          Ph         CF3CF2         B24        0
A389                 环丙基               H          Ph          CF3CF2         B24        0
A390                 (CH3)3C            H          Ph         CF3CF2         B24        0
A391                 (CH3)2CH           H          Ph         CF3CF2         B24        0
A392                 CH3(CH2)2         H          Ph         CF3CF2         B24        0
A393                 CH3OCH2            H          Ph         CF3CF2         B24        0
A394                 CH3O(CH2)2        H          Ph         CF3CF2         B24        0
A395                 Ph                    H          Ph         CF3CF2         B24        0
A396                 PhO                   H          Ph         CF3CF2         B24        0
化合物序号          R2                   R3          R4         R5             Q1      p
A397                PhS                   H            Ph          CF3CF2        B24       0
A398                PhSO                  H            Ph          CF3CF2        B24       0
A399                PhSO2                H            Ph          CF3CF2        B24       0
A400                CH3S                 H            Ph          CF3CF2        B24       0
A401                CH3SO                H            Ph          CF3CF2        B24       0
A402                CF3                  H            Ph          CF3CF2        B24       0
A403                F2CH                 H            Ph          CF3CF2        B24       0
A404                HCC                   H            Ph          CF3CF2        B24       0
A405                CH3CC                H            Ph          CF3CF2        B24       0
A406                CH2=CH              H            Ph          CF3CF2        B24       0
A407                CH2=CHCH2          H            Ph          CF3CF2        B24       0
A408                CH3SO2N(CH3)       H            Ph          CF3CF2        B24       0
A409                (CH3)2N             H            Ph          CF3CF2        B24       0
A410                (CH3)2NSO2         H            Ph          CF3CF2        B24       0
A411                ClCH2                H            Ph          CF3CF2         B24       0
A412                CH3SCH2             H            Ph          CF3CF2         B24       0
A413                CH3SOCH2            H            Ph          CF3CF2         B24       0
A414                CH3SO2CH2          H            Ph          CF3CF2        B24       0
A415                H                      H            Ph          CF3CF2CF2    B24       0
A416                CH3                  H            Ph          CF3CF2CF2     B24       0
A417                CH3CH2              H            Ph          CF3CF2CF2     B24       0
A418                环丙基                 H            Ph          CF3CF2CF2     B24       0
A419                (CH3)3C             H            Ph          CF3CF2CF2     B24       0
A420                (CH3)2CH            H            Ph          CF3CF2CF2     B24       0
A421                CH3(CH2)2          H            Ph          CF3CF2CF2     B24       0
A422                CH3OCH2             H            Ph          CF3CF2CF2     B24       0
A423                CH3O(CH2)2         H            Ph          CF3CF2CF2     B24       0
A424                Ph                     H            Ph          CF3CF2CF2     B24       0
A425                PhO                    H            Ph          CF3CF2CF2     B24       0
A426                PhS                    H            Ph          CF3CF2CF2     B24       0
A427                PhSO                   H            Ph          CF3CF2CF2     B24       0
A428                PhSO2                 H            Ph          CF3CF2CF2     B24       0
化合物序号          R2                   R3        R4         R5               Q1         p
A429                CH3S                 H          Ph          CF3CF2CF2      B24         0
A430                CH3SO                H          Ph          CF3CF2CF2      B24         0
A431                CF3                  H          Ph          CF3CF2CF2      B24         0
A432                F2CH                 H          Ph          CF3CF2CF2      B24         0
A433                HCC                   H          Ph          CF3CF2CF2      B24         0
A434                CH3CC                H          Ph          CF3CF2CF2      B24         0
A435                CH2=CH              H          Ph          CF3CF2CF2      B24         0
A436                CH2=CHCH2          H          Ph          CF3CF2CF2      B24         0
A437                CH3SO2N(CH3)       H          Ph          CF3CF2CF2      B24         0
A438                (CH3)2N             H          Ph          CF3CF2CF2      B24         0
A439                (CH3)2NSO2         H          Ph          CF3CF2CF2      B24         0
A440                ClCH2                H          Ph          CF3CF2CF2      B24         0
A441                CH3SCH2             H          Ph          CF3CF2CF2      B24         0
A442                CH3SOCH2            H          Ph          CF3CF2CF2      B24         0
A443                CH3SO2CH2          H          Ph          CF3CF2CF2      B24         0
A444                H                      H          Ph          CF2Cl            B24         0
A445                CH3                   H          Ph          CF2Cl            B24         0
A446                CH3CH2              H          Ph          CF2Cl             B24         0
A447                环丙基                 H          Ph          CF2Cl             B24         0
A448                (CH3)3C             H          Ph          CF2Cl             B24         0
A449                (CH3)2CH            H          Ph          CF2Cl             B24         0
A450                CH3(CH2)2          H          Ph          CF2Cl             B24         0
A451                CH3OCH2             H          Ph          CF2Cl             B24         0
A452                CH3O(CH2)2         H          Ph          CF2Cl             B24         0
A453                Ph                     H          Ph          CF2Cl             B24         0
A454                PhO                    H          Ph          CF2Cl             B24         0
A455                PhS                    H          Ph          CF2Cl             B24         0
A456                PhSO                   H          Ph          CF2Cl             B24         0
A457                PhSO2                 H          Ph          CF2Cl             B24         0
A458                CH3S                  H          Ph          CF2Cl             B24         0
A459                CH3SO                 H          Ph          CF2Cl             B24         0
A460                CF3                   H          Ph          CF2Cl             B24         0
化合物序号           R2                  R3        R4        R5           Q1        p
A461                 F2CH                H          Ph         CF2Cl        B24         0
A462                 HCC                  H          Ph         CF2Cl        B24         0
A463                 CH3CC               H          Ph         CF2Cl        B24         0
A464                 CH2=CH             H          Ph         CF2Cl        B24         0
A465                 CH2=CHCH2         H          Ph         CF2Cl        B24         0
A466                 CH3SO2N(CH3)      H          Ph         CF2Cl        B24         0
A467                 (CH3)2N            H          Ph         CF2Cl        B24         0
A468                 (CH3)2NSO2        H          Ph         CF2Cl        B24         0
A469                 ClCH2               H          Ph         CF2Cl        B24         0
A470                 CH3SCH2            H          Ph         CF2Cl        B24         0
A471                 CH3SOCH2           H          Ph         CF2Cl        B24         0
A472                 CH3SO2CH2         H          Ph         CF2Cl        B24         0
A473                 H                     H          Ph         CHF2         B24         0
A474                 CH3                 H          Ph         CHF2         B24         0
A475                 CH3CH2             H          Ph         CHF2         B24         0
A476                 环丙基                H          Ph         CHF2         B24         0
A477                 (CH3)3C            H          Ph         CHF2         B24         0
A478                 (CH3)2CH           H          Ph         CHF2         B24         0
A479                 CH3(CH2)2         H          Ph         CHF2         B24         0
A480                 CH3OCH2            H          Ph         CHF2         B24         0
A481                 CH3O(CH2)2        H          Ph         CHF2         B24         0
A482                 Ph                    H          Ph         CHF2         B24         0
A483                 PhO                   H          Ph         CHF2         B24         0
A484                 PhS                   H          Ph         CHF2         B24         0
A485                 PhSO                  H          Ph         CHF2         B24         0
A486                 PhSO2               H          Ph         CHF2         B24         0
A487                 CH3S                H          Ph         CHF2         B24         0
A488                 CH3SO               H          Ph         CHF2         B24         0
A489                 CF3                 H          Ph         CHF2         B24         0
A490                 F2CH                H          Ph         CHF2         B24         0
A491                 HCC                  H          Ph         CHF2         B24         0
A492                 CH3CC               H          Ph         CHF2         B24         0
化合物序号            R2                   R3          R4        R5            Q1         p
A493                  CH2=CH              H            Ph         CHF2           B24         0
A494                  CH2=CHCH2          H            Ph         CHF2           B24         0
A495                  CH3SO2N(CH3)       H            Ph         CHF2           B24         0
A496                  (CH3)2N             H            Ph         CHF2           B24         0
A497                  (CH3)2NSO2         H            Ph         CHF2           B24         0
A498                  ClCH2                H            Ph         CHF2           B24         0
A499                  CH3SCH2             H            Ph         CHF2           B24         0
A500                  CH3SOCH2            H            Ph         CHF2           B24         0
A501                  CH3SO2CH2          H            Ph         CHF2           B24         0
A502                  H                      H            Ph         CCl3           B24         0
A503                  CH3                  H            Ph         CCl3           B24         0
A504                  CH3CH2              H            Ph         CCl3           B24         0
A505                  环丙基                 H            Ph         CCl3           B24         0
A506                  (CH3)3C             H            Ph         CCl3           B24         0
A507                  (CH3)2CH            H            Ph         CCl3           B24         0
A508                  CH3(CH2)2          H            Ph         CCl3           B24         0
A509                  CH3OCH2             H            Ph         CCl3           B24         0
A510                  CH3O(CH2)2        H            Ph         CCl3           B24         0
A511                  Ph                    H            Ph         CCl3           B24         0
A512                  PhO                   H            Ph         CCl3           B24         0
A513                  PhS                   H            Ph         CCl3           B24         0
A514                  PhSO                  H            Ph         CCl3           B24         0
A515                  PhSO2                H            Ph         CCl3           B24         0
A516                  CH3S                 H            Ph         CCl3           B24         0
A517                  CH3SO                H            Ph         CCl3           B24         0
A518                  CF3                  H            Ph         CCl3           B24         0
A519                  F2CH                 H            Ph         CCl3           B24         0
A520                  HCC                   H            Ph         CCl3           B24         0
A521                  CH3CC                H            Ph         CCl3           B24         0
A522                  CH2=CH              H            Ph         CCl3           B24         0
A523                  CH2=CHCH2          H            Ph         CCl3           B24         0
A524                  CH3SO2N(CH3)      H            Ph         CCl3           B24         0
化合物序号         R2                R3                 R4         R5           Q1        p
A525               (CH3)2N          H                   Ph          CCl3         B24         0
A526               (CH3)2NSO2      H                   Ph          CCl3         B24         0
A527               ClCH2             H                   Ph          CCl3          B24         0
A528               CH3SCH2          H                   Ph          CCl3          B24         0
A529               CH3SOCH2         H                   Ph          CCl3          B24         0
A530               CH3SO2CH2       H                   Ph          CCl3          B24         0
A531               H                   CH3                H           CF3          B24         0
A532               H                   CH3CH2            H           CF3          B24         0
A533               H                   环丙基               H           CF3          B24         0
A534               H                   (CH3)3CH          H           CF3          B24         0
A535               H                   (CH3)2CH          H           CF3          B24         0
A536               H                   CH3(CH2)2        H           CF3          B24         0
A537               H                   CH3OCH2           H           CF3          B24         0
A538               H                   CH3O(CH2)2       H           CF3          B24         0
A539               H                   Ph                   H           CF3          B24         0
A540               H                   PhO                  H           CF3          B24         0
A541               H                   PhS                  H           CF3          B24         0
A542               H                   PhSO                 H           CF3          B24         0
A543               H                   PhSO2               H           CF3          B24         0
A544               H                   CH3S                H           CF3          B24         0
A545               H                   CH3SO               H           CF3          B24         0
A546               H                   CF3                 H           CF3          B24         0
A547               H                   F2CH                H           CF3          B24         0
A548               H                   HCC                  H           CF3          B24         0
A549               H                   CH3CC               H           CF3          B24         0
A550               H                   CH2=CH             H           CF3          B24         0
A551               H                   CH2=CHCH2         H           CF3          B24         0
A552               H                   CH3SO2N(CH3)      H           CF3          B24         0
A553               H                   (CH3)2N            H           CF3          B24         0
A554               H                   (CH3)2NSO2        H           CF3          B24         0
A555               H                   CH3SCH2            H           CF3          B24         0
A556               H                   CH3SOCH2           H           CF3          B24         0
化合物序号      R2          R3                  R4          R5                Q1         p
A557            H            CH3SO2CH2         H            CF3               B24         0
A558            H            CH3                 H            CF3CF2           B24         0
A559            H            CH3CH2             H            CF3CF2           B24         0
A560            H            环丙基                H            CF3CF2           B24         0
A561            H            (CH3)3C            H            CF3CF2           B24         0
A562            H            (CH3)2CH           H            CF3CF2           B24         0
A563            H            CH3(CH2)2         H            CF3CF2           B24         0
A564            H            CH3OCH2            H            CF3CF2           B24         0
A565            H            CH3O(CH2)2        H            CF3CF2           B24         0
A566            H            Ph                    H            CF3CF2           B24         0
A567            H            PhO                   H            CF3CF2           B24         0
A568            H            PhS                   H            CF3CF2           B24         0
A569            H            PhSO                  H            CF3CF2           B24         0
A570            H            PhSO2               H            CF3CF2           B24         0
A571            H            CH3S                H            CF3CF2           B24         0
A572            H            CH3SO               H            CF3CF2           B24         0
A573            H            CF3                 H            CF3CF2           B24         0
A574            H            F2CH                H            CF3CF2           B24         0
A575            H            HCC                  H            CF3CF2           B24         0
A576            H            CH3CC               H            CF3CF2           B24         0
A577            H            CH2=CH             H            CF3CF2           B24         0
A578            H            CH2=CHCH2         H            CF3CF2           B24         0
A579            H            CH3SO2N(CH3)      H            CF3CF2           B24         0
A580            H            (CH3)2N            H            CF3CF2           B24         0
A581            H            (CH3)2NSO2        H            CF3CF2           B24         0
A582            H            CH3SCH2            H            CF3CF2           B24         0
A583            H            CH3SOCH2           H            CF3CF2           B24         0
A584            H            CH3SO2CH2         H            CF3CF2           B24         0
A585            H            CH3                 H            CF3CF2CF2       B24         0
A586            H            CH3CH2             H            CF3CF2CF2       B24         0
A587            H            环丙基                H            CF3CF2CF2       B24         0
A588            H            (CH3)3C            H            CF3CF2CF2       B24         0
化合物序号       R2          R3                  R4          R5                    Q1          p
A589             H            (CH3)2CH           H            CF3CF2CF2           B24          0
A590             H            CH3(CH2)2         H            CF3CF2CF2           B24          0
A591             H            CH3OCH2            H            CF3CF2CF2           B24          0
A592             H            CH3O(CH2)2        H            CF3CF2CF2           B24          0
A593             H            Ph                    H            CF3CF2CF2           B24          0
A594             H            PhO                   H            CF3CF2CF2           B24          0
A595             H            PhS                   H            CF3CF2CF2           B24          0
A596             H            PhSO                  H            CF3CF2CF2           B24          0
A597             H            PhSO2               H            CF3CF2CF2           B24          0
A598             H            CH3S                H            CF3CF2CF2           B24          0
A599             H            CH3SO               H            CF3CF2CF2           B24          0
A600             H            CF3                 H            CF3CF2CF2           B24          0
A601             H            F2CH                H            CF3CF2CF2           B24          0
A602             H            HCC                  H            CF3CF2CF2           B24          0
A603             H            CH3CC               H            CF3CF2CF2           B24          0
A604             H            CH2=CH             H            CF3CF2CF2           B24          0
A605             H            CH2=CHCH2         H            CF3CF2CF2           B24          0
A606             H            CH3SO2N(CH3)      H            CF3CF2CF2           B24          0
A607             H            (CH3)2N            H            CF3CF2CF2           B24          0
A608             H            (CH3)2NSO2        H            CF3CF2CF2           B24          0
A609             H            CH3SCH2            H            CF3CF2CF2           B24          0
A610             H            CH3SOCH2           H            CF3CF2CF2           B24          0
A611             H            CH3SO2CH2         H            CF3CF2CF2           B24          0
A612             H            CH3                 H             CF2Cl                 B24          0
A613             H            CH3CH2             H            CF2Cl                  B24          0
A614             H            环丙基                H            CF2Cl                  B24          0
A615             H            (CH3)3C            H            CF2Cl                  B24          0
A616             H            (CH3)2CH           H            CF2Cl                  B24          0
A617             H            CH3(CH2)2         H            CF2Cl                  B24          0
A618             H            CH3OCH2            H            CF2Cl                  B24          0
A619             H            CH3O(CH2)2        H            CF2Cl                  B24          0
A620             H            Ph                    H            CF2Cl                  B24          0
化合物         R2         R3                  R4         R5          Q1        p
A621           H           PhO                  H           CF2Cl        B24        0
A622           H           PhS                  H           CF2Cl        B24        0
A623           H           PhSO                 H           CF2Cl        B24        0
A624           H           PhSO2               H           CF2Cl        B24        0
A625           H           CH3S                H           CF2Cl        B24        0
A626           H           CH3SO               H           CF2Cl        B24        0
A627           H           CF3                 H           CF2Cl        B24        0
A628           H           F2CH                H           CF2Cl        B24        0
A629           H           HCC                  H           CF2Cl        B24        0
A630           H           CH3CC               H           CF2Cl        B24        0
A631           H           CH2=CH             H           CF2Cl        B24        0
A632           H           CH2=CHCH2         H           CF2Cl        B24        0
A633           H           CH3SO2N(CH3)      H           CF2Cl        B24        0
A634           H           (CH3)2N            H           CF2Cl        B24        0
A635           H           (CH3)2NSO2        H           CF2Cl        B24        0
A636           H           CH3SCH2            H           CF2Cl        B24        0
A637           H           CH3SOCH2           H           CF2Cl        B24        0
A638           H           CH3SO2CH2         H           CF2Cl        B24        0
A639           H           CH3                 H            CHF2         B24        0
A640           H           CH3CH2             H           CHF2         B24        0
A641           H           环丙基                H           CHF2         B24        0
A642           H           (CH3)3C            H           CHF2         B24        0
A643           H           (CH3)2CH           H           CHF2         B24        0
A644           H           CH3(CH2)2         H           CHF2         B24        0
A645           H           CH3OCH2            H           CHF2         B24        0
A646           H           CH3O(CH2)2        H           CHF2         B24        0
A647           H           Ph                    H           CHF2         B24        0
A648           H           PhO                   H           CHF2         B24        0
A649           H           PhS                   H           CHF2         B24        0
A650           H           PhSO                  H           CHF2         B24        0
A651           H           PhSO2                H           CHF2         B24        0
A652           H           CH3S                 H           CHF2         B24        0
化合物序号       R2        R3                  R4         R5           Q1         p
A653             H          CH3SO               H           CHF2         B24          0
A654             H          CF3                 H           CHF2         B24          0
A655             H          F2CH                H           CHF2         B24          0
A656             H          HCC                  H           CHF2         B24          0
A657             H          CH3CC               H           CHF2         B24          0
A658             H          CH2=CH             H           CHF2         B24          0
A659             H          CH2=CHCH2         H           CHF2         B24          0
A660             H          CH3SO2N(CH3)      H           CHF2         B24          0
A661             H          (CH3)2N            H           CHF2         B24          0
A662             H          (CH3)2NSO2        H           CHF2         B24          0
A663             H          CH3SCH2            H           CHF2         B24          0
A664             H          CH3SOCH2           H           CHF2         B24          0
A665             H          CH3SO2CH2         H           CHF2         B24          0
A666             H          CH3                 H           CCl3         B24          0
A667             H          CH3CH2             H           CCl3         B24          0
A668             H          环丙基                H           CCl3         B24          0
A669             H          (CH3)3C            H           CCl3         B24          0
A670             H          (CH3)2CH           H           CCl3         B24          0
A671             H          CH3(CH2)2         H           CCl3         B24          0
A672             H          CH3OCH2            H           CCl3         B24          0
A673             H          CH3O(CH2)2        H           CCl3         B24          0
A674             H          Ph                    H           CCl3         B24          0
A675             H          PhO                   H           CCl3         B24          0
A676             H          PhS                   H           CCl3         B24          0
A677             H          PhSO                  H           CCl3         B24          0
A678             H          PhSO2                H           CCl3         B24          0
A679             H          CH3S                 H           CCl3         B24          0
A680             H          CH3SO                H           CCl3         B24          0
A681             H          CF3                  H           CCl3         B24          0
A682             H          F2CH                 H           CCl3         B24          0
A683             H          HCC                   H           CCl3         B24          0
A684             H          CH3CC                H           CCl3         B24          0
化合物序号      R2            R3                R4          R5          Q1       p
A685            H              CH2=CH           H            CCl3        B24        0
A686            H              CH2=CHCH2       H            CCl3        B24        0
A687            H              CH3SO2N(CH3)    H            CCl3        B24        0
A688            H              (CH3)2N          H            CCl3        B24        0
A689            H              (CH3)2NSO2      H            CCl3        B24        0
A690            H              CH3SCH2          H            CCl3        B24        0
A691            H              CH3SOCH2         H            CCl3        B24        0
A692            H              CH3SO2CH2       H            CCl3        B24        0
A693            H              CH3               CH3         CF3         B24        0
A694            H              CH3CH2           CH3         CF3         B24        0
A695            H              环丙基              CH3         CF3         B24        0
A696            H              (CH3)3C          CH3         CF3         B24        0
A697            H              (CH3)2CH         CH3         CF3         B24        0
A698            H              CH3(CH2)2       CH3         CF3         B24        0
A699            H              CH3OCH2          CH3         CF3         B24        0
A700            H              CH3O(CH2)2      CH3         CF3         B24        0
A701            H              Ph                  CH3         CF3         B24        0
A702            H              PhO                 CH3         CF3         B24        0
A703            H              PhS                 CH3         CF3         B24        0
A704            H              PhSO                CH3         CF3         B24        0
A705            H              PhSO2              CH3         CF3         B24        0
A706            H              CH3S               CH3         CF3         B24        0
A707            H              CH3SO              CH3         CF3         B24        0
A708            H              CF3                CH3         CF3         B24        0
A709            H              F2CH               CH3         CF3         B24        0
A710            H              HCC                 CH3         CF3         B24        0
A711            H              CH3CC              CH3         CF3         B24        0
A712            H              CH2=CH            CH3         CF3         B24        0
A713            H              CH2=CHCH2        CH3         CF3         B24        0
A714            H              CH3SO2N(CH3)     CH3         CF3         B24        0
A715            H              (CH3)2N           CH3         CF3         B24        0
A716            H              (CH3)2NSO2       CH3         CF3         B24        0
化合物序号       R2         R3               R4          R5               Q1        p
A717             H           CH3SCH2         CH3         CF3              B24         0
A718             H           CH3SOCH2        CH3         CF3              B24         0
A719             H           CH3SO2CH2      CH3         CF3              B24         0
A720             H           CH3              CH3         CF3CF2          B24         0
A721             H           CH3CH2          CH3         CF3CF2          B24         0
A722             H           环丙基             CH3         CF3CF2          B24         0
A723             H           (CH3)3C         CH3         CF3CF2          B24         0
A724             H           (CH3)2CH        CH3         CF3CF2          B24         0
A725             H           CH3(CH2)2      CH3         CF3CF2          B24         0
A726             H           CH3OCH2         CH3         CF3CF2          B24         0
A727             H           CH3O(CH2)2     CH3         CF3CF2          B24         0
A728             H           Ph                 CH3         CF3CF2          B24         0
A729             H           PhO                CH3         CF3CF2          B24         0
A730             H           PhS                CH3         CF3CF2          B24         0
A731             H           PhSO               CH3         CF3CF2          B24         0
A732             H           PhSO2             CH3         CF3CF2          B24         0
A733             H           CH3S              CH3         CF3CF2          B24         0
A734             H           CH3SO             CH3         CF3CF2          B24         0
A735             H           CF3               CH3         CF3CF2          B24         0
A736             H           F2CH              CH3         CF3CF2          B24         0
A737             H           HCC                CH3         CF3CF2          B24         0
A738             H           CH3CC             CH3         CF3CF2          B24         0
A739             H           CH2=CH           CH3         CF3CF2          B24         0
A740             H           CH2=CHCH2       CH3         CF3CF2          B24         0
A741             H           CH3SO2N(CH3)    CH3         CF3CF2          B24         0
A742             H           (CH3)2N          CH3         CF3CF2          B24         0
A743             H           (CH3)2NSO2      CH3         CF3CF2          B24         0
A744             H           CH3SCH2          CH3         CF3CF2          B24         0
A745             H           CH3SOCH2         CH3         CF3CF2          B24         0
A746             H           CH3SO2CH2       CH3         CF3CF2          B24         0
A747             H           CH3               CH3         CF3CF2CF2      B24         0
A748             H           CH3CH2           CH3         CF3CF2CF2      B24         0
化合物序号      R2         R3                R4          R5                    Q1         p
No.
A749            H           环丙基             CH3         CF3CF2CF2           B24         0
A750            H           (CH3)3C         CH3         CF3CF2CF2           B24         0
A751            H           (CH3)2CH        CH3         CF3CF2CF2           B24         0
A752            H           CH3(CH2)2      CH3         CF3CF2CF2           B24         0
A753            H           CH3OCH2         CH3         CF3CF2CF2           B24         0
A754            H           CH3O(CH2)2     CH3         CF3CF2CF2           B24         0
A755            H           Ph                 CH3         CF3CF2CF2           B24         0
A756            H           PhO                CH3         CF3CF2CF2           B24         0
A757            H           PhS                CH3         CF3CF2CF2           B24         0
A758            H           PhSO               CH3         CF3CF2CF2           B24         0
A759            H           PhSO2             CH3         CF3CF2CF2           B24         0
A760            H           CH3S              CH3         CF3CF2CF2           B24         0
A761            H           CH3SO             CH3         CF3CF2CF2           B24         0
A762            H           CF3               CH3         CF3CF2CF2           B24         0
A763            H           F2CH              CH3         CF3CF2CF2           B24         0
A764            H           HCC                CH3         CF3CF2CF2           B24         0
A765            H           CH3CC             CH3         CF3CF2CF2           B24         0
A766            H           CH2=CH           CH3         CF3CF2CF2           B24         0
A767            H           CH2=CHCH2       CH3         CF3CF2CF2           B24         0
A768            H           CH3SO2N(CH3)    CH3         CF3CF2CF2           B24         0
A769            H           (CH3)2N          CH3         CF3CF2CF2           B24         0
A770            H           (CH3)2NSO2      CH3         CF3CF2CF2           B24         0
A771            H           CH3SCH2          CH3         CF3CF2CF2           B24         0
A772            H           CH3SOCH2         CH3         CF3CF2CF2           B24         0
A773            H           CH3SO2CH2       CH3         CF3CF2CF2           B24         0
A774            H           CH3               CH3         CF2Cl                  B24         0
A775            H           CH3CH2           CH3         CF2Cl                  B24         0
A776            H           环丙基             CH3         CF2Cl                  B24         0
A777            H           (CH3)3C          CH3         CF2Cl                  B24         0
A778            H           (CH3)2CH         CH3         CF2Cl                  B24         0
A779            H           CH3(CH2)2       CH3         CF2Cl                  B24         0
A780            H           CH3OCH2          CH3         CF2Cl                  B24         0
化合物序号      R2         R3                  R4          R5          Q1        p
A781            H           CH3O(CH2)2       CH3         CF2Cl       B24         0
A782            H           Ph                   CH3         CF2Cl       B24         0
A783            H           PhO                  CH3         CF2Cl       B24         0
A784            H           PhS                  CH3         CF2Cl       B24         0
A785            H           PhSO                 CH3         CF2Cl       B24         0
A786            H           PhSO2               CH3         CF2Cl       B24         0
A787            H           CH3S                CH3         CF2Cl       B24         0
A788            H           CH3SO               CH3         CF2Cl       B24         0
A789            H           CF3                 CH3         CF2Cl       B24         0
A790            H           F2CH                CH3         CF2Cl       B24         0
A791            H           HCC                  CH3         CF2Cl       B24         0
A792            H           CH3CC               CH3         CF2Cl       B24         0
A793            H           CH2=CH             CH3         CF2Cl       B24         0
A794            H           CH2=CHCH2         CH3         CF2Cl       B24         0
A795            H           CH3SO2N(CH3)      CH3         CF2Cl       B24         0
A796            H           (CH3)2N            CH3         CF2Cl       B24         0
A797            H           (CH3)2NSO2        CH3         CF2Cl       B24         0
A798            H           CH3SCH2            CH3         CF2Cl       B24         0
A799            H           CH3SOCH2           CH3         CF2Cl       B24         0
A800            H           CH3SO2CH2         CH3         CF2Cl       B24         0
A801            H           CH3                  CH3         CHF2        B24         0
A802            H           CH3CH2             CH3         CHF2        B24         0
A803            H           环丙基                CH3         CHF2        B24         0
A804            H           (CH3)3C            CH3         CHF2        B24         0
A805            H           (CH3)2CH           CH3         CHF2        B24         0
A806            H           CH3(CH2)2         CH3         CHF2        B24         0
A807            H           CH3OCH2            CH3         CHF2        B24         0
A808            H           CH3O(CH2)2        CH3         CHF2        B24         0
A809            H           Ph                    CH3         CHF2        B24         0
A810            H           PhO                   CH3         CHF2        B24         0
A811            H           PhS                   CH3         CHF2        B24         0
A812            H           PhSO                  CH3         CHF2        B24         0
化合物序号      R2         R3                 R4          R5          Q1         p
A813            H           PhSO2              CH3         CHF2        B24         0
A814            H           CH3S               CH3         CHF2        B24         0
A815            H           CH3SO              CH3         CHF2        B24         0
A816            H           CF3                CH3         CHF2        B24         0
A817            H           F2CH               CH3         CHF2        B24         0
A818            H           HCC                 CH3         CHF2        B24         0
A819            H           CH3CC              CH3         CHF2        B24         0
A820            H           CH2=CH            CH3         CHF2        B24         0
A821            H           CH2=CHCH2        CH3         CHF2        B24         0
A822            H           CH3SO2N(CH3)     CH3         CHF2        B24         0
A823            H           (CH3)2N           CH3         CHF2        B24         0
A824            H           (CH3)2NSO2       CH3         CHF2        B24         0
A825            H           CH3SCH2           CH3         CHF2        B24         0
A826            H           CH3SOCH2          CH3         CHF2        B24         0
A827            H           CH3SO2CH2        CH3         CHF2        B24         0
A828            H           CH3                CH3         CCl3        B24         0
A829            H           CH3CH2            CH3         CCl3        B24         0
A830            H           环丙基              CH3         CCl3        B24         0
A831            H           (CH3)3C          CH3         CCl3        B24         0
A832            H           (CH3)2CH         CH3         CCl3        B24         0
A833            H           CH3(CH2)2       CH3         CCl3        B24         0
A834            H           CH3OCH2          CH3         CCl3        B24         0
A835            H           CH3O(CH2)2      CH3         CCl3        B24         0
A836            H           Ph                  CH3         CCl3        B24         0
A837            H           PhO                 CH3         CCl3        B24         0
A838            H           PhS                 CH3         CCl3        B24         0
A839            H           PhSO                CH3         CCl3        B24         0
A840            H           PhSO2              CH3         CCl3        B24         0
A841            H           CH3S               CH3         CCl3        B24         0
A842            H           CH3SO              CH3         CCl3        B24         0
A843            H           CF3                CH3         CCl3        B24         0
A844            H           F2CH               CH3         CCl3        B24         0
化合物序号       R2         R3                 R4         R5             Q1        p
A845             H           HCC                 CH3        CCl3           B24         0
A846             H           CH3CC              CH3        CCl3           B24         0
A847             H           CH2=CH            CH3        CCl3           B24         0
A848             H           CH2=CHCH2        CH3        CCl3           B24         0
A849             H           CH3SO2N(CH3)     CH3        CCl3           B24         0
A850             H           (CH3)2N           CH3        CCl3           B24         0
A851             H           (CH3)2NSO2       CH3        CCl3           B24         0
A852             H           CH3SCH2           CH3        CCl3           B24         0
A853             H           CH3SOCH2          CH3        CCl3           B24         0
A854             H           CH3SO2CH2        CH3       CCl3           B24         0
A855             H           CH3                Ph          CF3            B24         0
A856             H           CH3CH2            Ph          CF3            B24         0
A857             H           (CH3)2CH          Ph          CF3            B24         0
A858             H           (CH3)2CH          Ph          CF3            B24         0
A859             H           环丙基               Ph          CF3            B24         0
A860             H           CH3(CH2)2        Ph          CF3            B24         0
A861             H           CH3OCH2           Ph          CF3            B24         0
A862             H           CH3O(CH2)2       Ph          CF3            B24         0
A863             H           Ph                   Ph          CF3            B24         0
A864             H           PhO                  Ph          CF3            B24         0
A865             H           PhS                  Ph          CF3            B24         0
A866             H           PhSO                 Ph          CF3            B24         0
A867             H           PhSO2              Ph          CF3             B24         0
A868             H           CH3S               Ph          CF3             B24         0
A869             H           CH3SO              Ph          CF3             B24         0
A870             H           CF3                Ph          CF3             B24         0
A871             H           F2CH               Ph          CF3             B24         0
A872             H           HCC                 Ph          CF3             B24         0
A873             H           CH3CC              Ph          CF3             B24         0
A874             H           CH2=CH            Ph          CF3             B24         0
A875             H           CH2=CHCH2        Ph          CF3             B24         0
A876             H           CH3SO2N(CH3)     Ph          CF3             B24         0
化合物序号       R2          R3                  R4         R5               Q1        p
A877             H            (CH3)2N            Ph          CF3              B24         0
A878             H            (CH3)2NSO2        Ph          CF3              B24         0
A879             H            CH3SCH2            Ph          CF3              B24         0
A880             H            CH3SOCH2           Ph          CF3              B24         0
A881             H            CH3SO2CH2         Ph          CF3              B24         0
A882             H            CH3                 Ph          CF3CF2          B24         0
A883             H            CH3CH2             Ph          CF3CF2          B24         0
A884             H            环丙基                Ph          CF3CF2          B24         0
A885             H            (CH3)3C            Ph          CF3CF2          B24         0
A886             H            (CH3)2CH           Ph          CF3CF2          B24         0
A887             H            CH3(CH2)2         Ph          CF3CF2          B24         0
A888             H            CH3OCH2            Ph          CF3CF2          B24         0
A889             H            CH3O(CH2)2        Ph          CF3CF2          B24         0
A890             H            Ph                    Ph          CF3CF2          B24         0
A891             H            PhO                   Ph          CF3CF2          B24         0
A892             H            PhS                   Ph          CF3CF2          B24         0
A893             H            PhSO                  Ph          CF3CF2          B24         0
A894             H            PhSO2                Ph          CF3CF2          B24         0
A895             H            CH3S                 Ph          CF3CF2          B24         0
A896             H            CH3SO                Ph          CF3CF2          B24         0
A897             H            CF3                  Ph          CF3CF2          B24         0
A898             H            F2CH                 Ph          CF3CF2          B24         0
A899             H            HCC                   Ph          CF3CF2          B24         0
A900             H            CH3CC                Ph          CF3CF2          B24         0
A901             H            CH2=CH              Ph          CF3CF2          B24         0
A902             H            CH2=CHCH2          Ph          CF3CF2          B24         0
A903             H            CH3SO2N(CH3)      Ph          CF3CF2          B24         0
A904             H            (CH3)2N            Ph          CF3CF2          B24         0
A905             H            (CH3)2NSO2        Ph          CF3CF2          B24         0
A906             H            CH3SCH2            Ph          CF3CF2          B24         0
A907             H            CH3SOCH2           Ph          CF3CF2          B24         0
A908             H            CH3SO2CH2         Ph          CF3CF2          B24         0
化合物序号      R2         R3               R4         R5                Q1          p
A909            H           CH3              Ph          CF3CF2CF2      B24           0
A910            H           CH3CH2          Ph          CF3CF2CF2      B24           0
A911            H           环丙基             Ph          CF3CF2CF2      B24           0
A912            H           (CH3)3C         Ph          CF3CF2CF2      B24           0
A913            H           (CH3)2CH        Ph          CF3CF2CF2      B24           0
A914            H           CH3(CH2)2      Ph          CF3CF2CF2      B24           0
A915            H           CH3OCH2         Ph          CF3CF2CF2      B24           0
A916            H           CH3O(CH2)2     Ph          CF3CF2CF2      B24           0
A917            H           Ph                 Ph          CF3CF2CF2      B24           0
A918            H           PhO                Ph          CF3CF2CF2      B24           0
A919            H           PhS                Ph          CF3CF2CF2      B24           0
A920            H           PhSO               Ph          CF3CF2CF2      B24           0
A921            H           PhSO2             Ph          CF3CF2CF2      B24           0
A922            H           CH3S              Ph          CF3CF2CF2      B24           0
A923            H           CH3SO             Ph          CF3CF2CF2      B24           0
A924            H           CF3               Ph          CF3CF2CF2      B24           0
A925            H           F2CH              Ph          CF3CF2CF2      B24           0
A926            H           HCC                Ph          CF3CF2CF2      B24           0
A927            H           CH3CC             Ph          CF3CF2CF2      B24           0
A928            H           CH2=CH           Ph          CF3CF2CF2      B24           0
A929            H           CH2=CHCH2       Ph          CF3CF2CF2      B24           0
A930            H           CH3SO2N(CH3)    Ph          CF3CF2CF2      B24           0
A931            H           (CH3)2N          Ph          CF3CF2CF2      B24           0
A932            H           (CH3)2NSO2      Ph          CF3CF2CF2      B24           0
A933            H           CH3SCH2          Ph          CF3CF2CF2      B24           0
A934            H           CH3SOCH2         Ph          CF3CF2CF2      B24           0
A935            H           CH3SO2CH2       Ph          CF3CF2CF2      B24           0
A936            H           CH3               Ph          CF2Cl             B24           0
A937            H           CH3CH2           Ph          CF2Cl             B24           0
A938            H           环丙基              Ph          CF2Cl             B24           0
A939            H           (CH3)3C          Ph          CF2Cl             B24           0
A940            H           (CH3)2CH         Ph          CF2Cl             B24           0
化合物序号       R2         R3                 R4         R5          Q1        p
A941             H           CH3(CH2)2       Ph          CF2Cl        B24        0
A942             H           CH3OCH2          Ph          CF2Cl        B24        0
A943             H           CH3O(CH2)2      Ph          CF2Cl        B24        0
A944             H           Ph                  Ph          CF2Cl        B24        0
A945             H           PhO                 Ph          CF2Cl        B24        0
A946             H           PhS                 Ph          CF2Cl        B24        0
A947             H           PhSO                Ph          CF2Cl        B24        0
A948             H           PhSO2              Ph          CF2Cl        B24        0
A949             H           CH3S               Ph          CF2Cl        B24        0
A950             H           CH3SO              Ph          CF2Cl        B24        0
A951             H           CF3                Ph          CF2Cl        B24        0
A952             H           F2CH               Ph          CF2Cl        B24        0
A953             H           HCC                 Ph          CF2Cl        B24        0
A954             H           CH3CC              Ph          CF2Cl        B24        0
A955             H           CH2=CH            Ph          CF2Cl        B24        0
A956             H           CH2=CHCH2        Ph          CF2Cl        B24        0
A957             H           CH3SO2N(CH3)     Ph          CF2Cl        B24        0
A958             H           (CH3)2N           Ph          CF2Cl        B24        0
A959             H           (CH3)2NSO2       Ph          CF2Cl        B24        0
A960             H           CH3SCH2           Ph          CF2Cl        B24        0
A961             H           CH3SOCH2          Ph          CF2Cl        B24        0
A962             H           CH3SO2CH2        Ph          CF2Cl        B24        0
A963             H           CH3                Ph          CHF2         B24        0
A964             H           CH3CH2            Ph          CHF2         B24        0
A965             H           (CH3)3C           Ph          CHF2         B24        0
A966             H           (CH3)2CH          Ph          CHF2         B24        0
A967             H           环丙基               Ph          CHF2         B24        0
A968             H           CH3(CH2)2        Ph          CHF2         B24        0
A969             H           CH3OCH2           Ph          CHF2         B24        0
A970             H           CH3O(CH2)2       Ph          CHF2         B24        0
A971             H           Ph                   Ph          CHF2         B24        0
A972             H           PhO                  Ph          CHF2         B24        0
化合物序号      R2        R3                R4         R5         Q1         p
A973            H          PhS                Ph          CHF2        B24         0
A974            H          PhSO               Ph          CHF2        B24         0
A975            H          PhSO2             Ph          CHF2        B24         0
A976            H          CH3S              Ph          CHF2        B24         0
A977            H          CH3SO             Ph          CHF2        B24         0
A978            H          CF3               Ph          CHF2        B24         0
A979            H          F2CH              Ph          CHF2        B24         0
A980            H          HCC                Ph          CHF2        B24         0
A981            H          CH3CC             Ph          CHF2        B24         0
A982            H          CH2=CH           Ph          CHF2        B24         0
A983            H          CH2=CHCH2       Ph          CHF2        B24         0
A984            H          CH3SO2N(CH3)    Ph          CHF2        B24         0
A985            H          (CH3)2N          Ph          CHF2        B24         0
A986            H          (CH3)2NSO2      Ph          CHF2        B24         0
A987            H          CH3SCH2          Ph          CHF2        B24         0
A988            H          CH3SOCH2         Ph          CHF2        B24         0
A989            H          CH3SO2CH2       Ph          CHF2        B24         0
A990            H          CH3               ph          CCl3        B24         0
A991            H          CH3CH2           Ph          CCl3        B24         0
A992            H          (CH3)3C          Ph          CCl3        B24         0
A993            H          (CH3)2CH         Ph          CCl3        B24         0
A994            H          环丙基              Ph          CCl3        B24         0
A995            H          CH3(CH2)2       Ph          CCl3        B24         0
A996            H          CH3OCH2          Ph          CCl3        B24         0
A997            H          CH3O(CH2)2      Ph          CCl3        B24         0
A998            H          Ph                  Ph          CCl3        B24         0
A999            H          PhO                 Ph          CCl3        B24         0
A1000           H          PhS                 Ph          CCl3        B24         0
A1001           H          PhSO                Ph          CCl3        B24         0
A1002           H          PhSO2              Ph          CCl3        B24         0
A1003           H          CH3S               Ph          CCl3        B24         0
A1004           H          CH3SO              Ph          CCl3        B24         0
化合物序号       R2                              R3                R4           R5            Q1           p
A1005            H                                CF3               Ph            CCl3          B24            0
A1006            H                                F2CH              Ph            CCl3          B24            0
A1007            H                                HCC                Ph            CCl3          B24            0
A1008            H                                CH3CC             Ph            CCl3          B24            0
A1009            H                                CH2=CH           Ph            CCl3          B24            0
A1010            H                                CH2=CHCH2       Ph            CCl3          B24            0
A1011            H                                CH3SO2N(CH3)    Ph            CCL3          B24            0
A1012            H                                (CH3)2N          Ph            CCl3          B24            0
A1013            H                                (CH3)2NSO2      Ph            CCl3          B24            0
A1014            H                                CH3SCH2          Ph            CCl3          B24            0
A1015            H                                CH3SOCH2         Ph            CCl3          B24            0
A1016            H                                CH3SO2CH2       Ph            CCl3          B24            0
A1017            F                                H                   H             CF3           B24            0
A1018            Cl                               H                   H             CF3           B24            0
A1019            Br                               H                   H             CF3           B24            0
A1020            NC                               H                   H             CF3           B24            0
A1021            CH3SO2O                        H                  H             CF3           B24            0
A1022            CH3O                            H                  H             CF3           B24            0
A1023            CH3CH2O                        H                  H             CF3           B24            0
A1024            CH2CH=CH2O                    H                  H             CF3           B24            0
A1025            HCCCH2O                         H                  H             CF3           B24            0
A1026            PhCH2S                          H                  H             CF3           B24            0
A1027            PhCH2SO2                       H                  H             CF3           B24            0
A1028            ClCH2CH2                       H                  H             CF3           B24            0
A1029            BrCH2                           H                  H             CF3           B24            0
A1030            FCH2                            H                  H             CF3           B24            0
A1031            CHF2CH2                        H                  H             CF3           B24            0
A1032            CF3CH2                         H                  H             CF3           B24            0
A1033            [1,3]-咪唑-1-基甲基              H                  H             CF3           B24            0
A1034            CHCl2CH2                       H                  H             CF3           B24            0
A1035            ClCH=CH                          H                  H             CF3           B24            0
化合物序号      R2                R3                 R4          R5         Q1         p
A1036           Cl2C=CH          H                   H            CF3        B24          0
A1037           CF3CH=CH         H                   H            CF3        B24          0
A1038           ClCC               H                   H            CF3        B24          0
A1039           PhCH2             H                   H            CF3        B24          0
A1040           CH3CH2           CH3               H            CF3        B24          0
A1041           CH3               OH                  H            CF3        B24          0
A1042           CH3               F                   H            CF3        B24          0
A1043           CH3               Cl                  H            CF3        B24          0
A1044           F                  CH3                H            CF3        B24          0
A1045           Cl                 CH3                H            CF3        B24          0
A1046           H                  F                   H            CF3        B24          0
A1047           H                  Cl                  H            CF3        B24          0
A1048           H                  Br                  H            CF3        B24          0
A1049           H                  OH                  H            CF3        B24          0
A1050           H                  OCH3               H            CF3        B24          0
A1051           H                  OCHF2              H            CF3        B24          0
A1052           H                  OSO2CH3           H            CF3        B24          0
A1053           H                  OSO2CF3           H            CF3        B24          0
A1054           H                  ClCH2              H            CF3        B24          0
A1055           H                  BrCH2              H            CF3        B24          0
A1056           H                  FCH2               H            CF3        B24          0
A1057           H                  CHF2CH2           H            CF3        B24          0
A1058           H                  CF3CH2            H            CF3        B24          0
A1059           H                  三唑基甲基           H            CF3        B24          0
A1060           H                  CHCl2CH2          H            CF3        B24          0
A1061           H                  ClCH=CH             H            CF3        B24          0
A1062           H                  Cl2C=CH           H            CF3        B24          0
A1063           H                  CF3CH=CH          H            CF3        B24          0
A1064           H                  ClCC                H            CF3        B24          0
A1065           H                  CH3C(O)            H            CF3        B24          0
A1066           H                  Ph                  H            CF3        B24          0
A1067           H                  SO2CH3            H            CF3        B24          0
化合物序号       R2                  R3          R4        R5          Q1         p
A1068            H                    SO2CF3     H          CF3         B24         0
A1069            H                    NC            H          CF3         B24         0
A1070            H                    NO2          H          CF3         B24         0
A1071            CH3                 H             F          CF3         B24         0
A1072            CH3                 H             Cl         CF3         B24         0
A1073            CH3                 H             Br         CF3         B24         0
A1074            CH3                 H             NC         CF3         B24         0
A1075            CH3                 H             CH3O      CF3         B24         0
A1076            CH3                 H             CH3S      CF3         B24         0
A1077            CH3                 H             CH3SO     CF3         B24         0
A1078            CH3                 H             CH3SO2   CF3         B24         0
A1079            CH3CH2OCH2       H             H          CF3         B24         0
A1080            PhOCH2              H             H          CF3         B24         0
A1081            
Figure C9981578601851
           H             H          CF3         B24         0
A1082            (CH3)2CH2OCH2   H             H          CF3         B24         0
A1083            BrCH2CH2           H             H          CF3         B24         0
A1084            FCH2CH2            H             H          CF3         B24         0
A1085            
Figure C9981578601852
          H             H          CF3                     0
A1086            
Figure C9981578601853
         H             H          CF3         B24         0
A1087                      H             H          CF3         B24         0
A1088            
Figure C9981578601855
        H             H          CF3         B24         0
A1089                    H             H          CF3         B24         0
A1090            
Figure C9981578601857
      H             H          CF3         B24         0
化合物序号        R2                             R3         R4         R5         Q1        p
No.
A1091             环丙基-CH2                     H           H           CF3        B24         0
A1092             2,2-二氯环丙-1-基               H           H           CF3        B24         0
A1093             CH3OC(O)CH=CH                 H           H           CF3        B24         0
A1094             CH3CH2OC(O)CH=CH             H           H           CF3        B24         0
A1095             ClCH2CH=CH                    H           H           CF3                    0
A1096             CH=C=CH                       H           H           CF3        B24         0
A1097             (CH3)2NCH2                  H           H           CF3        B24         0
A1098             HOCH2                          H           H           CF3        B24         0
A1099             CH3C(O)OCH2                   H           H           CF3        B24         0
A1100             PhC(O)OCH2                     H           H           CF3        B24         0
A1101             PhCH2CH2                      H           H           CF3        B24         0
A1102             CH3OC(O)CH2                   H           H           CF3        B24         0
A1103             NCCH2                          H           H           CF3        B24         0
A1104             CH3(CH2)7SCH2              H           H           CF3        B24         0
A1105             CH3(CH2)7SOCH2             H           H           CF3        B24         0
A1106             CH3(CH2)7SO2CH2           H           H           CF3        B24         0
A1107             
Figure C9981578601861
                    H           H           CF3        B24         0
A1108             ClCH2CC                        H           H           CF3        B24         0
A1109             CHF2CH2CH2                  H           H           CF3        B24         0
A1110             CHCl2CH2CH2                 H           H           CF3        B24         0
A1111             CF3SO2O                      H           H           CF3        B24         0
A1112             
Figure C9981578601862
                   H           H           CF3        B24         0
A1113                                 H           H           CF3        B24         0
A1114             
Figure C9981578601864
                   H           H           CF3        B24         0
A1115             
Figure C9981578601865
                       H           H           CF3        B24         0
化合物序号         R2                           R3           R4          R5          Q1          p
A1116              
Figure C9981578601871
                      H            H            CF3          B24          0
A1117                                     H            H            CF3          B24          0
A1118              CH3ON=CHCH2                 H            H            CF3          B24          0
A1119              O=CHCH2                      H            H            CF3          B24          0
A1120              CH3CH2OCH2                 H            H            CF2Cl        B24          0
A1121              PhOCH2                        H            H            CF2Cl        B24          0
A1122                                    H            H            CF2Cl        B24          0
A1123              (CH3)2CH2OCH2             H            H            CF2Cl        B24          0
A1124              BrCH2                         H            H            CF2Cl        B24          0
A1125              FCH2                          H            H            CF2Cl        B24          0
A1126              
Figure C9981578601874
                   H            H            CF2Cl        B24          0
A1127                                 H            H            CF2Cl        B24          0
A1128                                H            H            CF2Cl        B24          0
A1129              
Figure C9981578601877
                 H            H            CF2Cl        B24          0
A1130                               H            H            CF2Cl        B24          0
A1131                              H            H            CF2Cl        B24          0
A1132              环丙基-CH2                    H            H            CF2Cl        B24          0
A1133              2,2-二氯环丙-1-基              H            H            CF2Cl        B24          0
A1134              CH3OC(O)CH=CH                H            H            CF2Cl        B24          0
A1135              CH3CH2OC(O)CH=CH            H            H            CF2Cl        B24          0
化合物序号        R2                       R3        R4        R5             Q1       p
A1136             ClCH2CH=CH              H          H          CF2Cl          B24        0
A1137             CH=C=CH                 H          H          CF2Cl          B24        0
A1138             (CH3)2NCH2            H          H          CF2Cl          B24        0
A1139             HOCH2                    H          H          CF2Cl          B24        0
A1140             CH3C(O)OCH2             H          H          CF2Cl          B24        0
A1141             PhC(O)OCH2               H          H          CF2Cl          B24        0
A1142             PhCH2                    H          H          CF2Cl          B24        0
A1143             CH3OC(O)CH2             H          H          CF2Cl          B24        0
A1144             NCCH2                    H          H          CF2Cl          B24        0
A1145             CH3(CH2)7SCH2        H          H          CF2Cl          B24        0
A1146             CH3(CH2)7SOCH2       H          H          CF2Cl          B24        0
A1147             CH3(CH2)7SO2CH2     H          H          CF2Cl          B24        0
A1148                            H          H          CF2Cl          B24        0
A1149             ClCH2CC                  H          H          CF2Cl          B24        0
A1150             Br                        H          H          CF2Cl          B24        0
A1151             Cl                        H          H          CF2Cl          B24        0
A1152             CF3SO2O                H          H          CF2Cl          B24        0
A1153                            H          H          CF2Cl          B24        0
A1154                           H          H          CF2Cl          B24        0
A1155                           H          H          CF2C1          B24        0
A1156             
Figure C9981578601885
                 H          H          CF2Cl          B24        0
A1157                               H          H          CF2Cl          B24        0
A1158                               H          H          CF2Cl          B24        0
A1159             CH3ON=CHCH2            H          H          CF2Cl          B24        0
A1160             O=CHCH2                 H          H          CF2Cl          B24        0
化合物序号       R2                             R3           R4          R5            Q1          p
A1161            CH3CH2OCH2                  H              H            CF2H          B24          0
A1162            PhOCH2                         H              H            CF2H          B24          0
A1163            
Figure C9981578601891
                      H              H            CF2H          B24          0
A1164            (CH3)2CH2OCH2              H              H            CF2H          B24          0
A1165            BrCH2                          H              H            CF2H          B24          0
A1166            FCH2                           H              H            CF2H          B24          0
A1167            
Figure C9981578601892
                    H              H            CF2H          B24          0
A1168                                H              H            CF2H          B24          0
A1169                               H              H            CF2H          B24          0
A1170                               H              H            CF2H          B24          0
A1171            
Figure C9981578601896
                 H              H            CF2H          B24          0
A1172                             H              H            CF2H          B24          0
A1173            环丙基-CH2                     H              H            CF2H          B24          0
A1174            2,2-二氯环丙-1-基               H              H            CF2H          B24          0
A1175            CH3OC(O)CH=CH                 H              H            CF2H          B24          0
A1176            CH3CH2OC(O)CH=CH             H              H            CF2H          B24          0
A1177            ClCH2CH=CH                    H              H            CF2H          B24          0
A1178            CH=C=CH                       H              H            CF2H          B24          0
A1179            (CH3)2NCH2                  H              H            CF2H          B24          0
A1180            HOCH2                          H              H            CF2H          B24          0
A1181            CH3C(O)OCH2                   H              H            CF2H          B24          0
A1182            PhC(O)OCH2                     H              H            CF2H          B24          0
化合物序号          R2                      R3        R4         R5         Q1        p
A1183               PhCH2                   H          H           CF2H       B24         0
A1184               CH3OC(O)CH2            H          H           CF2H       B24         0
A1185               NCCH2                   H          H           CF2H       B24         0
A1186               CH3(CH2)7SCH2       H          H           CF2H       B24         0
A1187               CH3(CH2)7SOCH2      H          H           CF2H       B24         0
A1188               CH3(CH2)7SO2CH2    H          H           CF2H       B24         0
A1189               
Figure C9981578601901
             H          H           CF2H       B24         0
A1190               ClCH2CC                 H          H           CF2H       B24         0
A1191               Br                        H          H           CF2H       B24         0
A1192               Cl                        H          H           CF2H       B24         0
A1193               CF3SO2O                H          H           CF2H       B24         0
A1194                             H          H           CF2H       B24         0
A1195               
Figure C9981578601903
            H          H           CF2H       B24         0
A1196               
Figure C9981578601904
            H          H           CF2H       B24         0
A1197               
Figure C9981578601905
                H          H           CF2H       B24         0
A1198                                H          H           CF2H       B24         0
A1199                                H          H           CF2H       B24         0
A1200               CH3ON=CHCH2           H          H           CF2H       B24         0
A1201               O=CHCH2                H          H           CF2H       B24         0
A1202               CH3CH=CH               H          H           CF3        B24         0
A1203               CH3SO2NH               H          H           CF3        B24         0
A1204               CH3CH2CH2O           H          CH3        CF3        B24         0
A1205               Cl                       CH3       H           CF3        B24         0
A1206               F2CHO                   H          H           CF3        B24         0
A1207               CH3CH2C(O)OCH2       H          H           CF3        B24         0
化合物序号        R2                         R3        R4        R5           Q1          p
A1208             CH3CH2OC(O)OCH2         H           H          CF3          B24          0
A1209             CH3OCH2OCH2             H           H          CF3          B24          0
A1210             CH3                        H           H          CF3          B24          1
A1211             CH3CH2                   H           H          CF3          B24          1
A1212             环丙基                      H           H          CF3          B24          1
A1213             CH3(CH2)2               H           H          CF3          B24          1
A1214             CH3OCH2                   H           H          CF3          B24          1
A1215             CF3                        H           H          CF3          B24          1
A1216             F2CH                       H           H          CF3          B24          1
A1217             ClCH2                      H           H          CF3          B24          1
A1218             CH3SO2CH2               H           H          CF3          B24          1
A1219             CH3                        CF3        H          CH3          B24          1
A1220             CH3CH2OCH2              H           H          CF3          B24          1
A1221             PhOCH2                     H           H          CF3          B24          1
A1222             (CH3)2CH2OCH2          H           H          CF3          B24          1
A1223             BrCH2                      H           H          CF3          B24          1
A1224             FCH2                       H           H          CF3          B24          1
A1225                            H           H          CF3          B24          1
A1226             
Figure C9981578601912
            H           H          CF3          B24          1
A1227             环丙基-CH2                 H           H          CF3          B24          1
A1228             2,2-二氯环丙-1-基          H           H          CF3          B24          1
A1229             (CH3)2NCH2              H           H          CF3          B24          1
A1230             HOCH2                      H           H          CF3          B24          1
A1231             CH3C(O)OCH2               H           H          CF3          B24          1
A1232             PhC(O)OCH2                 H           H          CF3          B24          1
A1233             PhCH2                      H           H          CF3          B24          1
A1234             CH3OC(O)CH2               H           H          CF3          B24          1
A1235             NCCH2                      H           H          CF3          B24          1
化合物序号       R2                        R3           R4         R5           Q1          p
A1236            CH3(CH2)7SO2CH2      H             H           CF3          B24          1
A1237            Br                         H             H            CF3          B24          1
A1238            Cl                         H             H            CF3          B24          1
A1239            O=CHCH2                  H             H            CF3          B24          1
A1240            CH3                       H             H            CF2Cl        B24          1
A1241            CH3CH2                   H             H            CF2Cl        B24          1
A1242            环丙基                      H             H            CF2Cl        B24          1
A1243            CH3(CH2)2               H             H            CF2Cl        B24          1
A1244            CH3OCH2                  H             H            CF2Cl        B24          1
A1245            CF3                       H             H            CF2Cl        B24          1
A1246            F2CH                      H             H            CF2Cl        B24          1
A1247            ClCH2                     H             H            CF2Cl        B24          1
A1248            CH3SO2CH2              H             H            CF2Cl        B24          1
A1249            CH3                       CF3          H            CF2Cl        B24          1
A1250            CH3CH2OCH2             H             H            CF2Cl        B24          1
A1251            PhOCH2                    H             H            CF2Cl        B24          1
A1252            (CH3)2CH2OCH2         H             H            CF2Cl        B24          1
A1253            BrCH2                     H             H            CF2Cl        B24          1
A1254            FCH2                      H             H            CF2Cl        B24          1
A1255            
Figure C9981578601921
              H             H            CF2Cl        B24          1
A1256            
Figure C9981578601922
           H             H            CF2Cl        B24          1
A1257            环丙基-CH2                H             H            CF2Cl        B24          1
A1258            2,2-二氯环丙-1-基          H             H            CF2Cl        B24          1
A1259            (CH3)2NCH2             H             H            CF2Cl        B24          1
A1260            HOCH2                     H             H            CF2Cl        B24          1
A1261            CH3C(O)OCH2              H             H            CF2Cl        B24          1
A1262            PhC(O)OCH2                H             H            CF2Cl        B24          1
A1263            PhCH2                     H             H            CF2Cl        B24          1
化合物序号         R2                           R3          R4         R5           Q1        p
A1264              CH3OC(O)CH2                 H            H           CF2Cl        B24         1
A1265              NCCH2                        H            H           CF2Cl        B24         1
A1266              CH3(CH2)7SO2CH2         H            H           CF2Cl        B24         1
A1267              Br                             H            H           CF2Cl        B24         1
A1268              Cl                             H            H           CF2Cl        B24         1
A1269              O=CHCH2                      H            H           CF2Cl        B24         1
A1270              CH3                           H            H           CF2H         B24         1
A1271              CH3CH2                       H            H           CF2H         B24         1
A1272              环丙基                          H            H           CF2H         B24         1
A1273              CH3(CH2)2                   H            H           CF2H         B24         1
A1274              CH3OCH2                      H            H           CF2H         B24         1
A1275              CF3                           H            H           CF2H         B24         1
A1276              F2CH                          H            H           CF2H         B24         1
A1277              ClCH2                         H            H           CF2H         B24         1
A1278              CH3SO2CH2                  H            H           CF2H         B24         1
A1279              CH3                           CF3         H           CF2H         B24         1
A1280              CH3CH2OCH2                 H            H           CF2H         B24         1
A1281              PhOCH2                        H            H           CF2H         B24         1
A1282              (CH3)2CH2OCH2             H            H           CF2H         B24         1
A1283              BrCH2                         H            H           CF2H         B24         1
A1284              FCH2                          H            H           CF2H         B24         1
A1285              
Figure C9981578601931
                 H            H           CF2H         B24         1
A1286                              H            H           CF2H         B24         1
A1287              环丙基-CH2                    H            H           CF2H         B24         1
A1288              2,2-二氯环丙-1-基              H            H           CF2H         B24         1
A1289              (CH3)2NCH2                 H            H           CF2H         B24         1
A1290              HOCH2                         H            H           CF2H         B24         1
A1291              CH3C(O)OCH2                  H            H           CF2H         B24         1
化合物序号      R2                     R3           R4              R5           Q1         p
A1292           PhC(O)OCH2             H             H                CF2H          B24         1
A1293           PhCH2                  H             H                CF2H          B24         1
A1294           CH3OC(O)CH2           H             H                CF2H          B24         1
A1295           NCCH2                  H             H                CF2H          B24         1
A1296           CH3(CH2)7SO2CH2   H             H                CF2H          B24         1
A1297           Br                      H             H                CF2H          B24         1
A1298           Cl                      H             H                CF2H          B24         1
A1299           O=CHCH2               H             H                CF2H          B24         1
A1300           CH3                    H             H                CF3CF2       B24         1
A1301           HO                      H             Ph                CF3           B24         0
A1302           CH3                    H             CH2=CH         CF3           B24         0
A1303           CH3                    H             CH3CH2O        CF3           B24         0
A1304           HO                      CH3          H                CF3           B24         0
A1305           HO                      H             H                CF3           B24         0
A1306           (CH3CH2)2N(O)CO     H             H                CF3           B24         0
A1307           CH3                    H             甲苯磺酰基-O     CF3           B24         0
A1308           CH3                    H             CH3CC           CF3           B24         0
A1309           CH3                    H             HCC              CF3           B24         0
A1310           CH3                    H             ClCH2CC         CF3           B24         0
A1311           CH3                    H             PhCH2O          CF3           B24         0
A1312           CH3                    H             CF3SO2O        CF3           B24         0
A1313           CH3                    H             (CH3)2N        CF3           B24         0
A1314           CH3                    H             CH3C(O)O        CF3           B24         0
A1315           CH3                    H             CH3CH2C(O)     CF3           B24         0
                                                      O
A1316           CH3                    H             PhC(O)O          CF3           B24         0
A1317           CH3                    H             3-吡啶基         CF3           B24         0
A1318           CH3OCH2OCH2         H             H                CF2Cl         B24         0
A1319           CH3OCH2OCH2         H             H                CF2H          B24         0
A1320           CH3OCH2OCH2         H             H                CF2CF3       B24         0
A1321           CH3OCH2OCH2         H             H                CF3           B24         1
A1322           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):
Q1          Q1          Q1           Q1          Q1         Q1        Q1        Q1       Q1       Q1        Q1     Q1
B1          B2           B3           B4          B5          B6        B7        B8        B9       B10       B11     B12
B13         B14          B15          B16         B17         B18       B19       B20       B21      B22       B23     -
B25         B26          B27          B28         B29         B30       B31       B32       B33      B34       B35     B36
B37         B38          B39          B40         B41         B42       B43       B44       B45      B46       B47     B48
B49         B50          B51          B52         B53         B54       B55       B56       B57      B58       B59     B60
B61         B62          B63          B64         B65         B66       B67       B68       B69      B70       B71     B72
B73         B74          B75          B76         B77         B78       B79       B80       B81      B82       B83     B84
B85         B86          B87          B88         B89         B90       B91       B92       B93      B94       B95     B96
B97         B98          B99          B100        B101        B102      B103      B104      B105     B106      B107    B108
B109        B110         B111         B112        B113        B114      B115      B116      B117     B118      B119    B120
B121        B122         B123         B124        B125        B126      B127      B128      B129     B130      B131    B132
B133        B134         B135         B136        B137        B138      B139      B140      B141     B142      B143    B144
B145        B146         B147         B148        B149        B150      B151      B152      B153     B154      B155    B156
B157        B158         B159         B160        B161        B162      B163      B164      B165     B166      B167    B168
B169        B170         B171         B172        B173        B174      B175      B176      B177     B178      B179    B180
B181        B182         B183         B184        B185        B186      B187      B188      B189     B190      B191    B192
B193        B194         B195         B196        B197        B198      B199      B200      B201     B202      B203    B204
B205        B206         B207         B208        B209        B210      B211      B212      B213     B214      B215    B216
B217        B218         B219         B220        B221        B222      B223      B224      B225     B226      B227    B228
B229        B230         B231         B232        B233        B234      B235      B236      B237     B238      B239    B240
B241        B242         B243         B244        B245        B246      B247      B248      B249     B250      B251    B252
B253        B254         B255         B256        B257        B258      B259      B260      B261     B262      B263    B264
B265        B266         B267         B268        B269        B270      B271      B272      B273     B274      B275    B276
B277        B278         B279         B280        B281        B282      B283      B284      B285     B286      B287    B288
B289        B290         B291         B292        B293        B294      B295      B296      B297     B298      B299    B300
Q1      Q1      Q1     Q1      Q1      Q1     Q1      Q1      Q1     Q1      Q1      Q1
B301    B302    B303    B304    B305    B306    B307    B308    B309    B310    B311    B312
B313    B314    B315    B316    B317    B318    B319    B320    B321    B322    B323    B324
B325    B326    B327    B328    B329    B330    B331    B332    B333    B334    B335    B336
B337    B338    B339    B340    B341    B342    B343    B344    B345    B346    B347    B348
B349    B350    B351    B352    B353    B354    B355    B356    B357    B358    B359    B360
B361    B362    B363    B364    B365    B366    B367    B368    B369    B370    B371    B372
B373    B374    B375    B376    B377    B378    B379    B380    B381    B382    B383    B384
B385    B386    B387    B388    B389    B390    B391    B392    B393    B394    B395    B396
B397    B398    B399    B400    B401    B402    B403    B404    B405    B406    B407    B408
B409    B410    B411    B412    B413    B414    B415    B416    B417    B418    B419    B420
B421    B422    B423    B424    B425    B426    B427    B428    B429    B430    B431    B432
B433    B434    B435    B436    B437    B438    B439    B440    B441    B442    B443    B444
B445    B446    B447    B448    B449    B450    B451    B452    B453    B454    B455    B456
B457    B458    B459    B460    B461    B462    B463    B464    B465    B466    B467    B468
B469    B470    B471    B472    B473    B474    B475    B476    B477    B478    B479    B480
B481    B482    B483    B484    B485    B486    B487    B488    B489    B490    B491    B492
B493    B494    B495    B496    B497    B498    B499    B500    B501    B502    B503    B504
B505    B506    B507    B508    B509    B510    B511    B512    B513    B514    B515    B516
B517    B518    B519    B520    B521    B522    B523    B524    B525    B526    B527    B528
B529    B530    B531    B532    B533    B534    B535    B536    B537    B538    B539    B540
B541    B542    B543    B544    B545    B546    B547    B548    B549    B550    B551    B552
B553    B554    B555    B556    B557    B558    B559    B560    B561    B562    B563    B564
B565    B566    B567    B568    B569    B570    B571    B572    B573    B574    B575    B576
B577    B578    B579    B580    B581    B582    B583    B584    B585    B586    B587    B588
B589    B590    B591    B592    B593    B594    B595    B596    B597    B598    B599    B600
B601    B602    B603    B604    B605    B606    B607    B608    B609    B610    B611    B612
B613    B614    B615    B616    B617    B618    B619    B620    B621    B622    B623    B624
B625    B626    B627    B628    B629    B630    B631    B632    B633    B634    B635    B636
B637    B638    B639    B640    B641    B642    B643    B644    B645    B646    B647    B648
B649    B650    B651    B652    B653    B654    B655    B656    B657    B658    B659    B660
B661    B662    B663    B664    B665    B666    B667    B668    B669    B670    B671    B672
B773    B774    B775    B776    B777    B778    B779    B780    B781    B782    B783    B784
B785    B786    B787    B788    B789    B790    B791    B792    B793    B794    B795    B796
Q1      Q1      Q1      Q1       Q1      Q1     Q1       Q1       Q1      Q1       Q1       Q1
B797    B798    B799     B800     B801    B802    B803     B804     B805     B806     B807     B808
B809    B810    B811     B812     B813    B814    B815     B816     B817     B818     B819     B820
B821    B822    B823     B824     B825    B826    B827     B828     B829     B830     B831     B832
B833    B834    B835     B836     B837    B838    B839     B840     B841     B842     B843     B844
B845    B846    B847     B848     B849    B850    B851     B852     B853     B854     B855     B856
B857    B858    B859     B860     B861    B862    B863     B864     B865     B866     B867     B868
B869    B870    B871     B872     B873    B874    B875     B876     B877     B878     B879     B880
B881    B882    B883     B884     B885    B886    B887     B888     B889     B890     B891     B892
B893    B894    B895     B896     B897    B898    B899     B900     B901     B902     B903     B904
B905    B906    B907     B908     B909    B910    B911     B912     B913     B914     B915     B916
B917    B918    B919     B920     B921    B922    B923     B924     B925     B926     B927     B928
B929    B930    B931     B932     B933    B934    B935     B936     B937     B938     B939     B940
B941    B942    B943     B944     B945    B946    B947     B948     B949     B950     B951     B952
B953    B954    B955     B956     B957    B958    B959     B960     B961     B962     B963     B964
B965    B966    B967     B968     B969    B970    B971     B972     B973     B974     B975     B976
B977    B978    B979     B980     B981    B982    B983     B984     B985     B986     B987     B988
B989    B990    B991     B992     B993    B994    B995     B996     B997     B998     B999     B1000
B1001   B1002   B1003    B1004    B1005   B1006   B1007    B1008    B1009    B1010    B1011    B1012
B1013   B1014   B1015    B1016    B1017   B1018   B1019    B1020    B1021    B1022    B1023    B1024
B1025   B1026   B1027    B1028    B1029   B1030   B1031    B1032    B1033    B1034    B1035    B1036
B1037   B1038   B1039    B1040    B1041   B1042   B1043    B1044    B1045    B1046    B1047    B1048
B1049   B1050   B1051    B1052    B1053   B1054   B1055    B1056    B1057    B1058    B1059    B1060
B1061   B1062   B1063    B1064    B1065   B1066   B1067    B1068    B1069    B1070    B1071    B1072
B1073   B1074   B1075    B1076    B1077   B1078   B1079    B1080    B1081    B1082    B1083    B1084
B1085   B1086   B1087    B1088    B1089   B1090   B1091    B1092    B1093    B1094    B1095    B1096
B1097   B1098   B1099    B1100    B1101   B1102   B1103    B1104    B1105    B1106    B1107    B1108
B1109   B1110   B1111    B1112    B1113   B1114   B1115    B1116    B1117    B1118    B1119    B1120
B1121   B1122   B1123    B1124    B1125   B1126   B1127    B1128    B1129    B1130    B1131    B1132
B1133   B1134   B1135    B1136    B1137   B1138   B1139    B1140    B1141    B1142    B1143    B1144
B1145   B1146   B1147    B1148    B1149   B1150   B1151    B1152    B1153    B1154    B1155    B1156
B1157   B1158   B1159    B1160    B1161   B1162   B1163    B1164    B1165    B1166    B1167    B1168
B1169   B1170   B1171    B1172    B1173   B1174   B1175    B1176    B1177    B1178    B1179    B1180
B1181   B1182   B1183    B1184    B1185   B1186   B1187    B1188    B1189    B1190    B1191    B1192
Q1      Q1      Q1     Q1      Q1      Q1     Q1      Q1      Q1      Q1     Q1      Q1
B1193   B1194   B1195   B1196   B1197   B1198   B1199   B1200   B1201   B1202   B1203   B1204
B1205   B1206   B1207   B1208   B1209   B1210   B1211   B1212   B1213   B1214   B1215   B1216
B1217
表9:式Ic化合物(P为0或1):
Figure C9981578601991
Q1      Q1     Q1      Q1      Q1     Q1      Q1      Q1     Q1      Q1      Q1     Q1
B1      B2      B3      B4      B5      B6      B7      B8      B9      B10     B11    B12
B13     B14     B15     B16     B17     B18     B19     B20     B21     B22     B23    -
B25     B26     B27     B28     B29     B30     B31     B32     B33     B34     B35    B36
B37     B38     B39     B40     B41     B42     B43     B44     B45     B46     B47    B48
B49     B50     B51     B52     B53     B54     B55     B56     B57     B58     B59    B60
B61     B62     B63     B64     B65     B66     B67     B68     B69     B70     B71    B72
B73     B74     B75     B76     B77     B78     B79     B80     B81     B82     B83    B84
B85     B86     B87     B88     B89     B90     B91     B92     B93     B94     B95    B96
B97     B98     B99     B100    B101    B102    B103    B104    B105    B106    B107   B108
B109    B110    B111    B112    B113    B114    B115    B116    B117    B118    B119   B120
B121    B122    B123    B124    B125    B126    B127    B128    B129    B130    B131   B132
B133    B134    B135    B136    B137    B138    B139    B140    B141    B142    B143   B144
B145    B146    B147    B148    B149    B150    B151    B152    B153    B154    B155   B156
B157    B158    B159    B160    B161    B162    B163    B164    B165    B166    B167   B168
B169    B170    B171    B172    B173    B174    B175    B176    B177    B178    B179   B180
B181    B182    B183    B184    B185    B186    B187    B188    B189    B190    B191   B192
B193    B194    B195    B196    B197    B198    B199    B200    B201    B202    B203   B204
B205    B206    B207    B208    B209    B210    B211    B212    B213    B214    B215   B216
B217    B218    B219    B220    B221    B222    B223    B224    B225    B226    B227   B228
B229    B230    B231    B232    B233    B234    B235    B236    B237    B238    B239   B240
B241    B242    B243    B244    B245    B246    B247    B248    B249    B250    B251   B252
Q1      Q1      Q1     Q1      Q1      Q1     Q1      Q1     Q1     Q1      Q1      Q1
B253    B254    B255    B256    B257    B258    B259    B260   B261    B262    B263    B264
B265    B266    B267    B268    B269    B270    B271    B272   B273    B274    B275    B276
B277    B278    B279    B280    B281    B282    B283    B284   B285    B286    B287    B288
B289    B290    B291    B292    B293    B294    B295    B296   B297    B298    B299    B300
B301    B302    B303    B304    B305    B306    B307    B308   B309    B310    B311    B312
B313    B314    B315    B316    B317    B318    B319    B320   B321    B322    B323    B324
B325    B326    B327    B328    B329    B330    B331    B332   B333    B334    B335    B336
B337    B338    B339    B340    B341    B342    B343    B344   B345    B346    B347    B348
B349    B350    B351    B352    B353    B354    B355    B356   B357    B358    B359    B360
B361    B362    B363    B364    B365    B366    B367    B368   B369    B370    B371    B372
B373    B374    B375    B376    B377    B378    B379    B380   B381    B382    B383    B384
B385    B386    B387    B388    B389    B390    B391    B392   B393    B394    B395    B396
B397    B398    B399    B400    B401    B402    B403    B404   B405    B406    B407    B408
B409    B410    B411    B412    B413    B414    B415    B416   B417    B418    B419    B420
B421    B422    B423    B424    B425    B426    B427    B428   B429    B430    B431    B432
B433    B434    B435    B436    B437    B438    B439    B440   B441    B442    B443    B444
B445    B446    B447    B448    B449    B450    B451    B452   B453    B454    B455    B456
B457    B458    B459    B460    B461    B462    B463    B464   B465    B466    B467    B468
B469    B470    B471    B472    B473    B474    B475    B476   B477    B478    B479    B480
B481    B482    B483    B484    B485    B486    B487    B488   B489    B490    B491    B492
B493    B494    B495    B496    B497    B498    B499    B500   B501    B502    B503    B504
B505    B506    B507    B508    B509    B510    B511    B512   B513    B514    B515    B516
B517    B518    B519    B520    B521    B522    B523    B524   B525    B526    B527    B528
B529    B530    B531    B532    B533    B534    B535    B536   B537    B538    B539    B540
B541    B542    B543    B544    B545    B546    B547    B548   B549    B550    B551    B552
B553    B554    B555    B556    B557    B558    B559    B560   B561    B562    B563    B564
B565    B566    B567    B568    B569    B570    B571    B572   B573    B574    B575    B576
B577    B578    B579    B580    B581    B582    B583    B584   B585    B586    B587    B588
B589    B590    B591    B592    B593    B594    B595    B596   B597    B598    B599    B600
B601    B602    B603    B604    B605    B606    B607    B608   B609    B610    B611    B612
B613    B614    B615    B616    B617    B618    B619    B620   B621    B622    B623    B624
B625    B626    B627    B628    B629    B630    B631    B632   B633    B634    B635    B636
B637    B638    B639    B640    B641    B642    B643    B644   B645    B646    B647    B648
Q1       Q1       Q1      Q1       Q1       Q1      Q1       Q1       Q1      Q1       Q1       Q1
B649     B650     B651     B652     B653     B654     B655     B656     B657     B658     B659     B660
B661     B662     B663     B664     B665     B666     B667     B668     B669     B670     B671     B672
B773     B774     B775     B776     B777     B778     B779     B780     B781     B782     B783     B784
B785     B786     B787     B788     B789     B790     B791     B792     B793     B794     B795     B796
B797     B798     B799     B800     B801     B802     B803     B804     B805     B806     B807     B808
B809     B810     B811     B812     B813     B814     B815     B816     B817     B818     B819     B820
B821     B822     B823     B824     B825     B826     B827     B828     B829     B830     B831     B832
B833     B834     B835     B836     B837     B838     B839     B840     B841     B842     B843     B844
B845     B846     B847     B848     B849     B850     B851     B852     B853     B854     B855     B856
B857     B858     B859     B860     B861     B862     B863     B864     B865     B866     B867     B868
B869     B870     B871     B872     B873     B874     B875     B876     B877     B878     B879     B880
B881     B882     B883     B884     B885     B886     B887     B888     B889     B890     B891     B892
B893     B894     B895     B896     B897     B898     B899     B900     B901     B902     B903     B904
B905     B906     B907     B908     B909     B910     B911     B912     B913     B914     B915     B916
B917     B918     B919     B920     B921     B922     B923     B924     B925     B926     B927     B928
B929     B930     B931     B932     B933     B934     B935     B936     B937     B938     B939     B940
B941     B942     B943     B944     B945     B946     B947     B948     B949     B950     B951     B952
B953     B954     B955     B956     B957     B958     B959     B960     B961     B962     B963     B964
B965     B966     B967     B968     B969     B970     B971     B972     B973     B974     B975     B976
B977     B978     B979     B980     B981     B982     B983     B984     B985     B986     B987     B988
B989     B990     B991     B992     B993     B994     B995     B996     B997     B998     B999     B1000
B1001    B1002    B1003    B1004    B1005    B1006    B1007    B1008    B1009    B1010    B1011    B1012
B1013    B1014    B1015    B1016    B1017    B1018    B1019    B1020    B1021    B1022    B1023    B1024
B1025    B1026    B1027    B1028    B1029    B1030    B1031    B1032    B1033    B1034    B1035    B1036
B1037    B1038    B1039    B1040    B1041    B1042    B1043    B1044    B1045    B1046    B1047    B1048
B1049    B1050    B1051    B1052    B1053    B1054    B1055    B1056    B1057    B1058    B1059    B1060
B1061    B1062    B1063    B1064    B1065    B1066    B1067    B1068    B1069    B1070    B1071    B1072
B1073    B1074    B1075    B1076    B1077    B1078    B1079    B1080    B1081    B1082    B1083    B1084
B1085    B1086    B1087    B1088    B1089    B1090    B1091    B1092    B1093    B1094    B1095    B1096
B1097    B1098    B1099    B1100    B1101    B1102    B1103    B1104    B1105    B1106    B1107    B1108
B1109    B1110    B1111    B1112    B1113    B1114    B1115    B1116    B1117    B1118    B1119    B1120
B1121    B1122    B1123    B1124    B1125    B1126    B1127    B1128    B1129    B1130    B1131    B1132
B1133    B1134    B1135    B1136    B1137    B1138    B1139    B1140    B1141    B1142    B1143    B1144
Q1      Q1      Q1      Q1     Q1      Q1      Q1    Q1     Q1     Q1      Q1       Q1
B1145   B1146   B1147   B1148   B1149   B1150   B1151  B1152  B1153   B1154   B1155    B1156
B1157   B1158   B1159   B1160   B1161   B1162   B1163  B1164  B1165   B1166   B1167    B1168
B1169   B1170   B1171   B1172   B1173   B1174   B1175  B1176  B1177   B1178   B1179    B1180
B1181   B1182   B1183   B1184   B1185   B1186   B1187  B1188  B1189   B1190   B1191    B1192
B1193   B1194   B1195   B1196   B1197   B1198   B1199  B1200  B1201   B1202   B1203    B1204
B1205   B1206   B1207   B1208   B1209   B1210   B1211  B1212  B1213   B1214   B1215    B1216
B1217
表10:式Id化合物(P为0或1):
Q1      Q1     Q1      Q1      Q1     Q1      Q1     Q1    Q1      Q1      Q1      Q1
B1      B2      B3      B4      B5      B6      B7     B8     B9      B10     B11      B12
B13     B14     B15     B16     B17     B18     B19    B20    B21     B22     B23      -
B25     B26     B27     B28     B29     B30     B31    B32    B33     B34     B35      B36
B37     B38     B39     B40     B41     B42     B43    B44    B45     B46     B47      B48
B49     B50     B51     B52     B53     B54     B55    B56    B57     B58     B59      B60
B61     B62     B63     B64     B65     B66     B67    B68    B69     B70     B71      B72
B73     B74     B75     B76     B77     B78     B79    B80    B81     B82     B83      B84
B85     B86     B87     B88     B89     B90     B91    B92    B93     B94     B95      B96
B97     B98     B99     B100    B101    B102    B103   B104   B105    B106    B107     B108
B109    B110    B111    B112    B113    B114    B115   B116   B117    B118    B119     B120
B121    B122    B123    B124    B125    B126    B127   B128   B129    B130    B131     B132
B133    B134    B135    B136    B137    B138    B139   B140   B141    B142    B143     B144
B145    B146    B147    B148    B149    B150    B151   B152   B153    B154    B155     B156
B157    B158    B159    B160    B161    B162    B163   B164   B165    B166    B167     B168
B169    B170    B171    B172    B173    B174    B175   B176   B177    B178    B179     B180
B181    B182    B183    B184    B185    B186    B187   B188   B189    B190    B191     B192
B193    B194    B195    B196    B197    B198    B199   B200   B201    B202    B203     B204
Q1       Q1       Q1      Q1      Q1      Q1     Q1      Q1     Q1      Q1     Q1      Q1
B205     B206     B207     B208    B209    B210    B211    B212    B213    B214   B215    B216
B217     B218     B219     B220    B221    B222    B223    B224    B225    B226   B227    B228
B229     B230     B231     B232    B233    B234    B235    B236    B237    B238   B239    B240
B241     B242     B243     B244    B245    B246    B247    B248    B249    B250   B251    B252
B253     B254     B255     B256    B257    B258    B259    B260    B261    B262   B263    B264
B265     B266     B267     B268    B269    B270    B271    B272    B273    B274   B275    B276
B277     B278     B279     B280    B281    B282    B283    B284    B285    B286   B287    B288
B289     B290     B291     B292    B293    B294    B295    B296    B297    B298   B299    B300
B301     B302     B303     B304    B305    B306    B307    B308    B309    B310   B311    B312
B313     B314     B315     B316    B317    B318    B319    B320    B321    B322   B323    B324
B325     B326     B327     B328    B329    B330    B331    B332    B333    B334   B335    B336
B337     B338     B339     B340    B341    B342    B343    B344    B345    B346   B347    B348
B349     B350     B351     B352    B353    B354    B355    B356    B357    B358   B359    B360
B361     B362     B363     B364    B365    B366    B367    B368    B369    B370   B371    B372
B373     B374     B375     B376    B377    B378    B379    B380    B381    B382   B383    B384
B385     B386     B387     B388    B389    B390    B391    B392    B393    B394   B395    B396
B397     B398     B399     B400    B401    B402    B403    B404    B405    B406   B407    B408
B409     B410     B411     B412    B413    B414    B415    B416    B417    B418   B419    B420
B421     B422     B423     B424    B425    B426    B427    B428    B429    B430   B431    B432
B433     B434     B435     B436    B437    B438    B439    B440    B441    B442   B443    B444
B445     B446     B447     B448    B449    B450    B451    B452    B453    B454   B455    B456
B457     B458     B459     B460    B461    B462    B463    B464    B465    B466   B467    B468
B469     B470     B471     B472    B473    B474    B475    B476    B477    B478   B479    B480
B481     B482     B483     B484    B485    B486    B487    B488    B489    B490   B491    B492
B493     B494     B495     B496    B497    B498    B499    B500    B501    B502   B503    B504
B505     B506     B507     B508    B509    B510    B511    B512    B513    B514   B515    B516
B517     B518     B519     B520    B521    B522    B523    B524    B525    B526   B527    B528
B529     B530     B531     B532    B533    B534    B535    B536    B537    B538   B539    B540
B541     B542     B543     B544    B545    B546    B547    B548    B549    B550   B551    B552
B553     B554     B555     B556    B557    B558    B559    B560    B561    B562   B563    B564
B565     B566     B567     B568    B569    B570    B571    B572    B573    B574   B575    B576
B577     B578     B579     B580    B581    B582    B583    B584    B585    B586   B587    B588
B589     B590     B591     B592    B593    B594    B595    B596    B597    B598   B599    B600
Q1         Q1         Q1       Q1        Q1       Q1       Q1        Q1       Q1       Q1        Q1       Q1
B601       B602       B603      B604      B605     B606      B607      B608      B609     B610      B611     B612
B613       B614       B615      B616      B617     B618      B619      B620      B621     B622      B623     B624
B625       B626       B627      B628      B629     B630      B631      B632      B633     B634      B635     B636
B637       B638       B639      B640      B641     B642      B643      B644      B645     B646      B647     B648
B649       B650       B651      B652      B653     B654      B655      B656      B657     B658      B659     B660
B661       B662       B663      B664      B665     B666      B667      B668      B669     B670      B671     B672
B773       B774       B775      B776      B777     B778      B779      B780      B781     B782      B783     B784
B785       B786       B787      B788      B789     B790      B791      B792      B793     B794      B795     B796
B797       B798       B799      B800      B801     B802      B803      B804      B805     B806      B807     B808
B809       B810       B811      B812      B813     B814      B815      B816      B817     B818      B819     B820
B821       B822       B823      B824      B825     B826      B827      B828      B829     B830      B831     B832
B833       B834       B835      B836      B837     B838      B839      B840      B841     B842      B843     B844
B845       B846       B847      B848      B849     B850      B851      B852      B853     B854      B855     B856
B857       B858       B859      B860      B861     B862      B863      B864      B865     B866      B867     B868
B869       B870       B871      B872      B873     B874      B875      B876      B877     B878      B879     B880
B881       B882       B883      B884      B885     B886      B887      B888      B889     B890      B891     B892
B893       B894       B895      B896      B897     B898      B899      B900      B901     B902      B903     B904
B905       B906       B907      B908      B909     B910      B911      B912      B913     B914      B915     B916
B917       B918       B919      B920      B921     B922      B923      B924      B925     B926      B927     B928
B929       B930       B931      B932      B933     B934      B935      B936      B937     B938      B939     B940
B941       B942       B943      B944      B945     B946      B947      B948      B949     B950      B951     B952
B953       B954       B955      B956      B957     B958      B959      B960      B961     B962      B963     B964
B965       B966       B967      B968      B969     B970      B971      B972      B973     B974      B975     B976
B977       B978       B979      B980      B981     B982      B983      B984      B985     B986      B987     B988
B989       B990       B991      B992      B993     B994      B995      B996      B997     B998      B999     B1000
B1001      B1002      B1003     B1004     B1005    B1006     B1007     B1008     B1009    B1010     B1011    B1012
B1013      B1014      B1015     B1016     B1017    B1018     B1019     B1020     B1021    B1022     B1023    B1024
B1025      B1026      B1027     B1028     B1029    B1030     B1031     B1032     B1033    B1034     B1035    B1036
B1037      B1038      B1039     B1040     B1041    B1042     B1043     B1044     B1045    B1046     B1047    B1048
B1049      B1050      B1051     B1052     B1053    B1054     B1055     B1056     B1057    B1058     B1059    B1060
B1061      B1062      B1063     B1064     B1065    B1066     B1067     B1068     B1069    B1070     B1071    B1072
B1073      B1074      B1075     B1076     B1077    B1078     B1079     B1080     B1081    B1082     B1083    B1084
B1085      B1086      B1087     B1088     B1089    B1090     B1091     B1092     B1093    B1094     B1095    B1096
Q1        Q1        Q1        Q1       Q1        Q1       Q1        Q1       Q1        Q1        Q1        Q1
B1097     B1098     B1099     B1100     B1101     B1102    B1103     B1104     B1105      B1106     B1107     B1108
B1109     B1110     B1111     B1112     B1113     B1114    B1115     B1116     B1117      B1118     B1119     B1120
B1121     B1122     B1123     B1124     B1125     B1126    B1127     B1128     B1129      B1130     B1131     B1132
B1133     B1134     B1135     B1136     B1137     B1138    B1139     B1140     B1141      B1142     B1143     B1144
B1145     B1146     B1147     B1148     B1149     B1150    B1151     B1152     B1153      B1154     B1155     B1156
B1157     B1158     B1159     B1160     B1161     B1162    B1163     B1164     B1165      B1166     B1167     B1168
B1169     B1170     B1171     B1172     B1173     B1174    B1175     B1176     B1177      B1178     B1179     B1180
B1181     B1182     B1183     B1184     B1185     B1186    B1187     B1188     B1189      B1190     B1191     B1192
B1193     B1194     B1195     B1196     B1197     B1198    B1199     B1200     B1201      B1202     B1203     B1204
B1205     B1206     B1207     B1208     B1209     B1210    B1211     B1212     B1213      B1214     B1215     B1216
B1217
表11:式Ie化合物(P为0或1):
Q1        Q1       Q1        Q1        Q1       Q1        Q1        Q1       Q1         Q1        Q1       Q1
B1        B2        B3        B4        B5        B6        B7        B8        B9         B10       B11       B12
B13       B14       B15       B16       B17       B18       B19       B20       B21        B22       B23       -
B25       B26       B27       B28       B29       B30       B31       B32       B33        B34       B35       B36
B37       B38       B39       B40       B41       B42       B43       B44       B45        B46       B47       B48
B49       B50       B51       B52       B53       B54       B55       B56       B57        B58       B59       B60
B61       B62       B63       B64       B65       B66       B67       B68       B69        B70       B71       B72
B73       B74       B75       B76       B77       B78       B79       B80       B81        B82       B83       B84
B85       B86       B87       B88       B89       B90       B91       B92       B93        B94       B95       B96
B97       B98       B99       B100      B101      B102      B103      B104      B105       B106      B107      B108
B109      B110      B111      B112      B113      B114      B115      B116      B117       B118      B119      B120
B121      B122      B123      B124      B125      B126      B127      B128      B129       B130      B131      B132
B133      B134      B135      B136      B137      B138      B139      B140      B141       B142      B143      B144
B145      B146      B147      B148      B149      B150      B151      B152      B153       B154      B155      B156
Q1       Q1       Q1       Q1        Q1       Q1      Q1       Q1       Q1      Q1       Q1       Q1
B157     B158     B159      B160      B161     B162     B163     B164     B165     B166     B167     B168
B169     B170     B171      B172      B173     B174     B175     B176     B177     B178     B179     B180
B181     B182     B183      B184      B185     B186     B187     B188     B189     B190     B191     B192
B193     B194     B195      B196      B197     B198     B199     B200     B201     B202     B203     B204
B205     B206     B207      B208      B209     B210     B211     B212     B213     B214     B215     B216
B217     B218     B219      B220      B221     B222     B223     B224     B225     B226     B227     B228
B229     B230     B231      B232      B233     B234     B235     B236     B237     B238     B239     B240
B241     B242     B243      B244      B245     B246     B247     B248     B249     B250     B251     B252
B253     B254     B255      B256      B257     B258     B259     B260     B261     B262     B263     B264
B265     B266     B267      B268      B269     B270     B271     B272     B273     B274     B275     B276
B277     B278     B279      B280      B281     B282     B283     B284     B285     B286     B287     B288
B289     B290     B291      B292      B293     B294     B295     B296     B297     B298     B299     B300
B301     B302     B303      B304      B305     B306     B307     B308     B309     B310     B311     B312
B313     B314     B315      B316      B317     B318     B319     B320     B321     B322     B323     B324
B325     B326     B327      B328      B329     B330     B331     B332     B333     B334     B335     B336
B337     B338     B339      B340      B341     B342     B343     B344     B345     B346     B347     B348
B349     B350     B351      B352      B353     B354     B355     B356     B357     B358     B359     B360
B361     B362     B363      B364      B365     B366     B367     B368     B369     B370     B371     B372
B373     B374     B375      B376      B377     B378     B379     B380     B381     B382     B383     B384
B385     B386     B387      B388      B389     B390     B391     B392     B393     B394     B395     B396
B397     B398     B399      B400      B401     B402     B403     B404     B405     B406     B407     B408
B409     B410     B411      B412      B413     B414     B415     B416     B417     B418     B419     B420
B421     B422     B423      B424      B425     B426     B427     B428     B429     B430     B431     B432
B433     B434     B435      B436      B437     B438     B439     B440     B441     B442     B443     B444
B445     B446     B447      B448      B449     B450     B451     B452     B453     B454     B455     B456
B457     B458     B459      B460      B461     B462     B463     B464     B465     B466     B467     B468
B469     B470     B471      B472      B473     B474     B475     B476     B477     B478     B479     B480
B481     B482     B483      B484      B485     B486     B487     B488     B489     B490     B491     B492
B493     B494     B495      B496      B497     B498     B499     B500     B501     B502     B503     B504
B505     B506     B507      B508      B509     B510     B511     B512     B513     B514     B515     B516
B517     B518     B519      B520      B521     B522     B523     B524     B525     B526     B527     B528
B529     B530     B531      B532      B533     B534     B535     B536     B537     B538     B539     B540
B541     B542     B543      B544      B545     B546     B547     B548     B549     B550     B551     B552
Q1        Q1        Q1       Q1        Q1        Q1       Q1        Q1       Q1        Q1        Q1        Q1
B553      B554      B555      B556      B557      B558      B559      B560      B561      B562      B563      B564
B565      B566      B567      B568      B569      B570      B571      B572      B573      B574      B575      B576
B577      B578      B579      B580      B581      B582      B583      B584      B585      B586      B587      B588
B589      B590      B591      B592      B593      B594      B595      B596      B597      B598      B599      B600
B601      B602      B603      B604      B605      B606      B607      B608      B609      B610      B611      B612
B613      B614      B615      B616      B617      B618      B619      B620      B621      B622      B623      B624
B625      B626      B627      B628      B629      B630      B631      B632      B633      B634      B635      B636
B637      B638      B639      B640      B641      B642      B643      B644      B645      B646      B647      B648
B649      B650      B651      B652      B653      B654      B655      B656      B657      B658      B659      B660
B661      B662      B663      B664      B665      B666      B667      B668      B669      B670      B671      B672
B773      B774      B775      B776      B777      B778      B779      B780      B781      B782      B783      B784
B785      B786      B787      B788      B789      B790      B791      B792      B793      B794      B795      B796
B797      B798      B799      B800      B801      B802      B803      B804      B805      B806      B807      B808
B809      B810      B811      B812      B813      B814      B815      B816      B817      B818      B819      B820
B821      B822      B823      B824      B825      B826      B827      B828      B829      B830      B831      B832
B833      B834      B835      B836      B837      B838      B839      B840      B841      B842      B843      B844
B845      B846      B847      B848      B849      B850      B851      B852      B853      B854      B855      B856
B857      B858      B859      B860      B861      B862      B863      B864      B865      B866      B867      B868
B869      B870      B871      B872      B873      B874      B875      B876      B877      B878      B879      B880
B881      B882      B883      B884      B885      B886      B887      B888      B889      B890      B891      B892
B893      B894      B895      B896      B897      B898      B899      B900      B901      B902      B903      B904
B905      B906      B907      B908      B909      B910      B911      B912      B913      B914      B915      B916
B917      B918      B919      B920      B921      B922      B923      B924      B925      B926      B927      B928
B929      B930      B931      B932      B933      B934      B935      B936      B937      B938      B939      B940
B941      B942      B943      B944      B945      B946      B947      B948      B949      B950      B951      B952
B953      B954      B955      B956      B957      B958      B959      B960      B961      B962      B963      B964
B965      B966      B967      B968      B969      B970      B971      B972      B973      B974      B975      B976
B977      B978      B979      B980      B981      B982      B983      B984      B985      B986      B987      B988
B989      B990      B991      B992      B993      B994      B995      B996      B997      B998      B999      B1000
B1001     B1002     B1003     B1004     B1005     B1006     B1007     B1008     B1009     B1010     B1011     B1012
B1013     B1014     B1015     B1016     B1017     B1018     B1019     B1020     B1021     B1022     B1023     B1024
B1025     B1026     B1027     B1028     B1029     B1030     B1031     B1032     B1033     B1034     B1035     B1036
B1037     B1038     B1039     B1040     B1041     B1042     B1043     B1044     B1045     B1046     B1047     B1048
Q1        Q1        Q1       Q1        Q1        Q1       Q1        Q1        Q1         Q1        Q1        Q1
B1049     B1050     B1051     B1052     B1053     B1054     B1055     B1056     B1057      B1058      B1059     B1060
B1061     B1062     B1063     B1064     B1065     B1066     B1067     B1068     B1069      B1070      B1071     B1072
B1073     B1074     B1075     B1076     B1077     B1078     B1079     B1080     B1081      B1082      B1083     B1084
B1085     B1086     B1087     B1088     B1089     B1090     B1091     B1092     B1093      B1094      B1095     B1096
B1097     B1098     B1099     B1100     B1101     B1102     B1103     B1104     B1105      B1106      B1107     B1108
B1109     B1110     B1111     B1112     B1113     B1114     B1115     B1116     B1117      B1118      B1119     B1120
B1121     B1122     B1123     B1124     B1125     B1126     B1127     B1128     B1129      B1130      B1131     B1132
B1133     B1134     B1135     B1136     B1137     B1138     B1139     B1140     B1141      B1142      B1143     B1144
B1145     B1146     B1147     B1148     B1149     B1150     B1151     B1152     B1153      B1154      B1155     B1156
B1157     B1158     B1159     B1160     B1161     B1162     B1163     B1164     B1165      B1166      B1167     B1168
B1169     B1170     B1171     B1172     B1173     B1174     B1175     B1176     B1177      B1178      B1179     B1180
B1181     B1182     B1183     B1184     B1185     B1186     B1187     B1188     B1189      B1190      B1191     B1192
B1193     B1194     B1195     B1196     B1197     B1198     B1199     B1200     B1201      B1202      B1203     B1204
B1205     B1206     B1207     B1208     B1209     B1210     B1211     B1212     B1213      B1214      B1215     B1216
B1217
表12:式If化合物
Figure C9981578602081
Q1        Q1       Q1        Q1        Q1       Q1        Q1        Q1       Q1      Q1         Q1        Q1
B1        B2        B3        B4        B5        B6        B7        B8        B9      B10        B11       B12
B13       B14       B15       B16       B17       B18       B19       B20       B21     B22        B23       -
B25       B26       B27       B28       B29       B30       B31       B32       B33     B34        B35       B36
B37       B38       B39       B40       B41       B42       B43       B44       B45     B46        B47       B48
B49       B50       B51       B52       B53       B54       B55       B56       B57     B58        B59       B60
B61       B62       B63       B64       B65       B66       B67       B68       B69     B70        B71       B72
B73       B74       B75       B76       B77       B78       B79       B80       B81     B82        B83       B84
B85       B86       B87       B88       B89       B90       B91       B92       B93     B94        B95       B96
B97       B98       B99       B100      B101      B102      B103      B104      B105    B106       B107      B108
Q1       Q1       Q1      Q1       Q1        Q1       Q1       Q1        Q1      Q1       Q1        Q1
B109     B110     B111     B112     B113      B114      B115     B116      B117     B118     B119      B120
B121     B122     B123     B124     B125      B126      B127     B128      B129     B130     B131      B132
B133     B134     B135     B136     B137      B138      B139     B140      B141     B142     B143      B144
B145     B146     B147     B148     B149      B150      B151     B152      B153     B154     B155      B156
B157     B158     B159     B160     B161      B162      B163     B164      B165     B166     B167      B168
B169     B170     B171     B172     B173      B174      B175     B176      B177     B178     B179      B180
B181     B182     B183     B184     B185      B186      B187     B188      B189     B190     B191      B192
B193     B194     B195     B196     B197      B198      B199     B200      B201     B202     B203      B204
B205     B206     B207     B208     B209      B210      B211     B212      B213     B214     B215      B216
B217     B218     B219     B220     B221      B222      B223     B224      B225     B226     B227      B228
B229     B230     B231     B232     B233      B234      B235     B236      B237     B238     B239      B240
B241     B242     B243     B244     B245      B246      B247     B248      B249     B250     B251      B252
B253     B254     B255     B256     B257      B258      B259     B260      B261     B262     B263      B264
B265     B266     B267     B268     B269      B270      B271     B272      B273     B274     B275      B276
B277     B278     B279     B280     B281      B282      B283     B284      B285     B286     B287      B288
B289     B290     B291     B292     B293      B294      B295     B296      B297     B298     B299      B300
B301     B302     B303     B304     B305      B306      B307     B308      B309     B310     B311      B312
B313     B314     B315     B316     B317      B318      B319     B320      B321     B322     B323      B324
B325     B326     B327     B328     B329      B330      B331     B332      B333     B334     B335      B336
B337     B338     B339     B340     B341      B342      B343     B344      B345     B346     B347      B348
B349     B350     B351     B352     B353      B354      B355     B356      B357     B358     B359      B360
B361     B362     B363     B364     B365      B366      B367     B368      B369     B370     B371      B372
B373     B374     B375     B376     B377      B378      B379     B380      B381     B382     B383      B384
B385     B386     B387     B388     B389      B390      B391     B392      B393     B394     B395      B396
B397     B398     B399     B400     B401      B402      B403     B404      B405     B406     B407      B408
B409     B410     B411     B412     B413      B414      B415     B416      B417     B418     B419      B420
B421     B422     B423     B424     B425      B426      B427     B428      B429     B430     B431      B432
B433     B434     B435     B436     B437      B438      B439     B440      B441     B442     B443      B444
B445     B446     B447     B448     B449      B450      B451     B452      B453     B454     B455      B456
B457     B458     B459     B460     B461      B462      B463     B464      B465     B466     B467      B468
B469     B470     B471     B472     B473      B474      B475     B476      B477     B478     B479      B480
B481     B482     B483     B484     B485      B486      B487     B488      B489     B490     B491      B492
B493     B494     B495     B496     B497      B498      B499     B500      B501     B502     B503      B504
Q1       Q1       Q1      Q1       Q1       Q1      Q1       Q1       Q1      Q1       Q1       Q1
B505     B506     B507     B508     B509     B510     B511     B512     B513     B514     B515     B516
B517     B518     B519     B520     B521     B522     B523     B524     B525     B526     B527     B528
B529     B530     B531     B532     B533     B534     B535     B536     B537     B538     B539     B540
B541     B542     B543     B544     B545     B546     B547     B548     B549     B550     B551     B552
B553     B554     B555     B556     B557     B558     B559     B560     B561     B562     B563     B564
B565     B566     B567     B568     B569     B570     B571     B572     B573     B574     B575     B576
B577     B578     B579     B580     B581     B582     B583     B584     B585     B586     B587     B588
B589     B590     B591     B592     B593     B594     B595     B596     B597     B598     B599     B600
B601     B602     B603     B604     B605     B606     B607     B608     B609     B610     B611     B612
B613     B614     B615     B616     B617     B618     B619     B620     B621     B622     B623     B624
B625     B626     B627     B628     B629     B630     B631     B632     B633     B634     B635     B636
B637     B638     B639     B640     B641     B642     B643     B644     B645     B646     B647     B648
B649     B650     B651     B652     B653     B654     B655     B656     B657     B658     B659     B660
B661     B662     B663     B664     B665     B666     B667     B668     B669     B670     B671     B672
B773     B774     B775     B776     B777     B778     B779     B780     B781     B782     B783     B784
B785     B786     B787     B788     B789     B790     B791     B792     B793     B794     B795     B796
B797     B798     B799     B800     B801     B802     B803     B804     B805     B806     B807     B808
B809     B810     B811     B812     B813     B814     B815     B816     B817     B818     B819     B820
B821     B822     B823     B824     B825     B826     B827     B828     B829     B830     B831     B832
B833     B834     B835     B836     B837     B838     B839     B840     B841     B842     B843     B844
B845     B846     B847     B848     B849     B850     B851     B852     B853     B854     B855     B856
B857     B858     B859     B860     B861     B862     B863     B864     B865     B866     B867     B868
B869     B870     B871     B872     B873     B874     B875     B876     B877     B878     B879     B880
B881     B882     B883     B884     B885     B886     B887     B888     B889     B890     B891     B892
B893     B894     B895     B896     B897     B898     B899     B900     B901     B902     B903     B904
B905     B906     B907     B908     B909     B910     B911     B912     B913     B914     B915     B916
B917     B918     B919     B920     B921     B922     B923     B924     B925     B926     B927     B928
B929     B930     B931     B932     B933     B934     B935     B936     B937     B938     B939     B940
B941     B942     B943     B944     B945     B946     B947     B948     B949     B950     B951     B952
B953     B954     B955     B956     B957     B958     B959     B960     B961     B962     B963     B964
B965     B966     B967     B968     B969     B970     B971     B972     B973     B974     B975     B976
B977     B978     B979     B980     B981     B982     B983     B984     B985     B986     B987     B988
B989     B990     B991     B992     B993     B994     B995     B996     B997     B998     B999     B1000
Q1        Q1        Q1 #160;     Q1        Q1        Q1       Q1        Q1        Q1        Q1       Q1        Q1
B1001     B1002     B1003     B1004     B1005     B1006     B1007     B1008     B1009     B1010     B1011     B1012
B1013     B1014     B1015     B1016     B1017     B1018     B1019     B1020     B1021     B1022     B1023     B1024
B1025     B1026     B1027     B1028     B1029     B1030     B1031     B1032     B1033     B1034     B1035     B1036
B1037     B1038     B1039     B1040     B1041     B1042     B1043     B1044     B1045     B1046     B1047     B1048
B1049     B1050     B1051     B1052     B1053     B1054     B1055     B1056     B1057     B1058     B1059     B1060
B1061     B1062     B1063     B1064     B1065     B1066     B1067     B1068     B1069     B1070     B1071     B1072
B1073     B1074     B1075     B1076     B1077     B1078     B1079     B1080     B1081     B1082     B1083     B1084
B1085     B1086     B1087     B1088     B1089     B1090     B1091     B1092     B1093     B1094     B1095     B1096
B1097     B1098     B1099     B1100     B1101     B1102     B1103     B1104     B1105     B1106     B1107     B1108
B1109     B1110     B1111     B1112     B1113     B1114     B1115     B1116     B1117     B1118     B1119     B1120
B1121     B1122     B1123     B1124     B1125     B1126     B1127     B1128     B1129     B1130     B1131     B1132
B1133     B1134     B1135     B1136     B1137     B1138     B1139     B1140     B1141     B1142     B1143     B1144
B1145     B1146     B1147     B1148     B1149     B1150     B1151     B1152     B1153     B1154     B1155     B1156
B1157     B1158     B1159     B1160     B1161     B1162     B1163     B1164     B1165     B1166     B1167     B1168
B1169     B1170     B1171     B1172     B1173     B1174     B1175     B1176     B1177     B1178     B1179     B1180
B1181     B1182     B1183     B1184     B1185     B1186     B1187     B1188     B1189     B1190     B1191     B1192
B1193     B1194     B1195     B1196     B1197     B1198     B1199     B1200     B1201     B1202     B1203     B1204
B1205     B1206     B1207     B1208     B1209     B1210     B1211     B1212     B1213     B1214     B1215     B1216
B1217
表13:式Ig化合物(P为0或1):
Q1        Q1        Q1       Q1        Q1        Q1       Q1        Q1        Q1       Q1        Q1        Q1
B1        B2        B3        B4        B5        B6        B7        B8        B9        B10       B11       B12
B13       B14       B15       B16       B17       B18       B19       B20       B21       B22       B23       -
B25       B26       B27       B28       B29       B30       B31       B32       B33       B34       B35       B36
B37       B38       B39       B40       B41       B42       B43       B44       B45       B46       B47       B48
B49       B50       B51       B52       B53       B54       B55       B56       B57       B58       B59       B60
B61       B62       B63       B64       B65       B66       B67       B68       B69       B70       B71       B72
Q1       Q1       Q1      Q1        Q1       Q1      Q1        Q1 #160;     Q1        Q1        Q1        Q1
B73      B74      B75      B76       B77      B78      B79       B80       B81       B82       B83       B84
B85      B86      B87      B88       B89      B90      B91       B92       B93       B94       B95       B96
B97      B98      B99      B100      B101     B102     B103      B104      B105      B106      B107      B108
B109     B110     B111     B112      B113     B114     B115      B116      B117      B118      B119      B120
B121     B122     B123     B124      B125     B126     B127      B128      B129      B130      B131      B132
B133     B134     B135     B136      B137     B138     B139      B140      B141      B142      B143      B144
B145     B146     B147     B148      B149     B150     B151      B152      B153      B154      B155      B156
B157     B158     B159     B160      B161     B162     B163      B164      B165      B166      B167      B168
B169     B170     B171     B172      B173     B174     B175      B176      B177      B178      B179      B180
B181     B182     B183     B184      B185     B186     B187      B188      B189      B190      B191      B192
B193     B194     B195     B196      B197     B198     B199      B200      B201      B202      B203      B204
B205     B206     B207     B208      B209     B210     B211      B212      B213      B214      B215      B216
B217     B218     B219     B220      B221     B222     B223      B224      B225      B226      B227      B228
B229     B230     B231     B232      B233     B234     B235      B236      B237      B238      B239      B240
B241     B242     B243     B244      B245     B246     B247      B248      B249      B250      B251      B252
B253     B254     B255     B256      B257     B258     B259      B260      B261      B262      B263      B264
B265     B266     B267     B268      B269     B270     B271      B272      B273      B274      B275      B276
B277     B278     B279     B280      B281     B282     B283      B284      B285      B286      B287      B288
B289     B290     B291     B292      B293     B294     B295      B296      B297      B298      B299      B300
B301     B302     B303     B304      B305     B306     B307      B308      B309      B310      B311      B312
B313     B314     B315     B316      B317     B318     B319      B320      B321      B322      B323      B324
B325     B326     B327     B328      B329     B330     B331      B332      B333      B334      B335      B336
B337     B338     B339     B340      B341     B342     B343      B344      B345      B346      B347      B348
B349     B350     B351     B352      B353     B354     B355      B356      B357      B358      B359      B360
B361     B362     B363     B364      B365     B366     B367      B368      B369      B370      B371      B372
B373     B374     B375     B376      B377     B378     B379      B380      B381      B382      B383      B384
B385     B386     B387     B388      B389     B390     B391      B392      B393      B394      B395      B396
B397     B398     B399     B400      B401     B402     B403      B404      B405      B406      B407      B408
B409     B410     B411     B412      B413     B414     B415      B416      B417      B418      B419      B420
B421     B422     B423     B424      B425     B426     B427      B428      B429      B430      B431      B432
B433     B434     B435     B436      B437     B438     B439      B440      B441      B442      B443      B444
B445     B446     B447     B448      B449     B450     B451      B452      B453      B454      B455      B456
B457     B458     B459     B460      B461     B462     B463      B464      B465      B466      B467      B468
Q1        Q1        Q1       Q1       Q1       Q1      Q1       Q1       Q1     Q1       Q1      Q1
B469      B470      B471      B472     B473     B474     B475     B476     B477    B478     B479    B480
B481      B482      B483      B484     B485     B486     B487     B488     B489    B490     B491    B492
B493      B494      B495      B496     B497     B498     B499     B500     B501    B502     B503    B504
B505      B506      B507      B508     B509     B510     B511     B512     B513    B514     B515    B516
B517      B518      B519      B520     B521     B522     B523     B524     B525    B526     B527    B528
B529      B530      B531      B532     B533     B534     B535     B536     B537    B538     B539    B540
B541      B542      B543      B544     B545     B546     B547     B548     B549    B550     B551    B552
B553      B554      B555      B556     B557     B558     B559     B560     B561    B562     B563    B564
B565      B566      B567      B568     B569     B570     B571     B572     B573    B574     B575    B576
B577      B578      B579      B580     B581     B582     B583     B584     B585    B586     B587    B588
B589      B590      B591      B592     B593     B594     B595     B596     B597    B598     B599    B600
B601      B602      B603      B604     B605     B606     B607     B608     B609    B610     B611    B612
B613      B614      B615      B616     B617     B618     B619     B620     B621    B622     B623    B624
B625      B626      B627      B628     B629     B630     B631     B632     B633    B634     B635    B636
B637      B638      B639      B640     B641     B642     B643     B644     B645    B646     B647    B648
B649      B650      B651      B652     B653     B654     B655     B656     B657    B658     B659    B660
B661      B662      B663      B664     B665     B666     B667     B668     B669    B670     B671    B672
B773      B774      B775      B776     B777     B778     B779     B780     B781    B782     B783    B784
B785      B786      B787      B788     B789     B790     B791     B792     B793    B794     B795    B796
B797      B798      B799      B800     B801     B802     B803     B804     B805    B806     B807    B808
B809      B810      B811      B812     B813     B814     B815     B816     B817    B818     B819    B820
B821      B822      B823      B824     B825     B826     B827     B828     B829    B830     B831    B832
B833      B834      B835      B836     B837     B838     B839     B840     B841    B842     B843    B844
B845      B846      B847      B848     B849     B850     B851     B852     B853    B854     B855    B856
B857      B858      B859      B860     B861     B862     B863     B864     B865    B866     B867    B868
B869      B870      B871      B872     B873     B874     B875     B876     B877    B878     B879    B880
B881      B882      B883      B884     B885     B886     B887     B888     B889    B890     B891    B892
B893      B894      B895      B896     B897     B898     B899     B900     B901    B902     B903    B904
B905      B906      B907      B908     B909     B910     B911     B912     B913    B914     B915    B916
B917      B918      B919      B920     B921     B922     B923     B924     B925    B926     B927    B928
B929      B930      B931      B932     B933     B934     B935     B936     B937    B938     B939    B940
B941      B942      B943      B944     B945     B946     B947     B948     B949    B950     B951    B952
B953      B954      B955      B956     B957     B958     B959     B960     B961    B962     B963    B964
Q1       Q1        Q1       Q1        Q1        Q1       Q1        Q1        Q1       Q1       Q1       Q1
B965     B966      B967      B968      B969      B970      B971      B972      B973      B974     B975     B976
B977     B978      B979      B980      B981      B982      B983      B984      B985      B986     B987     B988
B989     B990      B991      B992      B993      B994      B995      B996      B997      B998     B999     B1000
B1001    B1002     B1003     B1004     B1005     B1006     B1007     B1008     B1009     B1010    B1011    B1012
B1013    B1014     B1015     B1016     B1017     B1018     B1019     B1020     B1021     B1022    B1023    B1024
B1025    B1026     B1027     B1028     B1029     B1030     B1031     B1032     B1033     B1034    B1035    B1036
B1037    B1038     B1039     B1040     B1041     B1042     B1043     B1044     B1045     B1046    B1047    B1048
B1049    B1050     B1051     B1052     B1053     B1054     B1055     B1056     B1057     B1058    B1059    B1060
B1061    B1062     B1063     B1064     B1065     B1066     B1067     B1068     B1069     B1070    B1071    B1072
B1073    B1074     B1075     B1076     B1077     B1078     B1079     B1080     B1081     B1082    B1083    B1084
B1085    B1086     B1087     B1088     B1089     B1090     B1091     B1092     B1093     B1094    B1095    B1096
B1097    B1098     B1099     B1100     B1101     B1102     B1103     B1104     B1105     B1106    B1107    B1108
B1109    B1110     B1111     B1112     B1113     B1114     B1115     B1116     B1117     B1118    B1119    B1120
B1121    B1122     B1123     B1124     B1125     B1126     B1127     B1128     B1129     B1130    B1131    B1132
B1133    B1134     B1135     B1136     B1137     B1138     B1139     B1140     B1141     B1142    B1143    B1144
B1145    B1146     B1147     B1148     B1149     B1150     B1151     B1152     B1153     B1154    B1155    B1156
B1157    B1158     B1159     B1160     B1161     B1162     B1163     B1164     B1165     B1166    B1167    B1168
B1169    B1170     B1171     B1172     B1173     B1174     B1175     B1176     B1177     B1178    B1179    B1180
B1181    B1182     B1183     B1184     B1185     B1186     B1187     B1188     B1189     B1190    B1191    B1192
B1193    B1194     B1195     B1196     B1197     B1198     B1199     B1210     B1201     B1202    B1203    B1204
B1205    B1206     B1207     B1208     B1209     B1210     B1211     B1212     B1213     B1214    B1215    B1216
B1217
表14:式Ih化合物(P为0或1):
Q1       Q1        Q1      Q1         Q1        Q1       Q1        Q1        Q1       Q1       Q1      Q1
B1       B2        B3       B4         B5        B6        B7        B8        B9        B10      B11      B12
B13      B14       B15      B16        B17       B18       B19       B20       B21       B22      B23      -
Q1       Q1       Q1       Q1       Q1       Q1      Q1       Q1      Q1       Q1        Q1       Q1
B25      B26      B27       B28      B29      B30      B31      B32      B33      B34       B35      B36
B37      B38      B39       B40      B41      B42      B43      B44      B45      B46       B47      B48
B49      B50      B51       B52      B53      B54      B55      B56      B57      B58       B59      B60
B61      B62      B63       B64      B65      B66      B67      B68      B69      B70       B71      B72
B73      B74      B75       B76      B77      B78      B79      B80      B81      B82       B83      B84
B85      B86      B87       B88      B89      B90      B91      B92      B93      B94       B95      B96
B97      B98      B99       B100     B101     B102     B103     B104     B105     B106      B107     B108
B109     B110     B111      B112     B113     B114     B115     B116     B117     B118      B119     B120
B121     B122     B123      B124     B125     B126     B127     B128     B129     B130      B131     B132
B133     B134     B135      B136     B137     B138     B139     B140     B141     B142      B143     B144
B145     B146     B147      B148     B149     B150     B151     B152     B153     B154      B155     B156
B157     B158     B159      B160     B161     B162     B163     B164     B165     B166      B167     B168
B169     B170     B171      B172     B173     B174     B175     B176     B177     B178      B179     B180
B181     B182     B183      B184     B185     B186     B187     B188     B189     B190      B191     B192
B193     B194     B195      B196     B197     B198     B199     B200     B201     B202      B203     B204
B205     B206     B207      B208     B209     B210     B211     B212     B213     B214      B215     B216
B217     B218     B219      B220     B221     B222     B223     B224     B225     B226      B227     B228
B229     B230     B231      B232     B233     B234     B235     B236     B237     B238      B239     B240
B241     B242     B243      B244     B245     B246     B247     B248     B249     B250      B251     B252
B253     B254     B255      B256     B257     B258     B259     B260     B261     B262      B263     B264
B265     B266     B267      B268     B269     B270     B271     B272     B273     B274      B275     B276
B277     B278     B279      B280     B281     B282     B283     B284     B285     B286      B287     B288
B289     B290     B291      B292     B293     B294     B295     B296     B297     B298      B299     B300
B301     B302     B303      B304     B305     B306     B307     B308     B309     B310      B311     B312
B313     B314     B315      B316     B317     B318     B319     B320     B321     B322      B323     B324
B325     B326     B327      B328     B329     B330     B331     B332     B333     B334      B335     B336
B337     B338     B339      B340     B341     B342     B343     B344     B345     B346      B347     B348
B349     B350     B351      B352     B353     B354     B355     B356     B357     B358      B359     B360
B361     B362     B363      B364     B365     B366     B367     B368     B369     B370      B371     B372
B373     B374     B375      B376     B377     B378     B379     B380     B381     B382      B383     B384
B385     B386     B387      B388     B389     B390     B391     B392     B393     B394      B395     B396
B397     B398     B399      B400     B401     B402     B403     B404     B405     B406      B407     B408
B409     B410     B411      B412     B413     B414     B415     B416     B417     B418      B419     B420
Q1       Q1       Q1      Q1        Q1       Q1      Q1       Q1        Q1      Q1       Q1        Q1
B421     B422     B423     B424      B425     B426     B427     B428      B429     B430     B431      B432
B433     B434     B435     B436      B437     B438     B439     B440      B441     B442     B443      B444
B445     B446     B447     B448      B449     B450     B451     B452      B453     B454     B455      B456
B457     B458     B459     B460      B461     B462     B463     B464      B465     B466     B467      B468
B469     B470     B471     B472      B473     B474     B475     B476      B477     B478     B479      B480
B481     B482     B483     B484      B485     B486     B487     B488      B489     B490     B491      B492
B493     B494     B495     B496      B497     B498     B499     B500      B501     B502     B503      B504
B505     B506     B507     B508      B509     B510     B511     B512      B513     B514     B515      B516
B517     B518     B519     B520      B521     B522     B523     B524      B525     B526     B527      B528
B529     B530     B531     B532      B533     B534     B535     B536      B537     B538     B539      B540
B541     B542     B543     B544      B545     B546     B547     B548      B549     B550     B551      B552
B553     B554     B555     B556      B557     B558     B559     B560      B561     B562     B563      B564
B565     B566     B567     B568      B569     B570     B571     B572      B573     B574     B575      B576
B577     B578     B579     B580      B581     B582     B583     B584      B585     B586     B587      B588
B589     B590     B591     B592      B593     B594     B595     B596      B597     B598     B599      B600
B601     B602     B603     B604      B605     B606     B607     B608      B609     B610     B611      B612
B613     B614     B615     B616      B617     B618     B619     B620      B621     B622     B623      B624
B625     B626     B627     B628      B629     B630     B631     B632      B633     B634     B635      B636
B637     B638     B639     B640      B641     B642     B643     B644      B645     B646     B647      B648
B649     B650     B651     B652      B653     B654     B655     B656      B657     B658     B659      B660
B661     B662     B663     B664      B665     B666     B667     B668      B669     B670     B671      B672
B773     B774     B775     B776      B777     B778     B779     B780      B781     B782     B783      B784
B785     B786     B787     B788      B789     B790     B791     B792      B793     B794     B795      B796
B797     B798     B799     B800      B801     B802     B803     B804      B805     B806     B807      B808
B809     B810     B811     B812      B813     B814     B815     B816      B817     B818     B819      B820
B821     B822     B823     B824      B825     B826     B827     B828      B829     B830     B831      B832
B833     B834     B835     B836      B837     B838     B839     B840      B841     B842     B843      B844
B845     B846     B847     B848      B849     B850     B851     B852      B853     B854     B855      B856
B857     B858     B859     B860      B861     B862     B863     B864      B865     B866     B867      B868
B869     B870     B871     B872      B873     B874     B875     B876      B877     B878     B879      B880
B881     B882     B883     B884      B885     B886     B887     B888      B889     B890     B891      B892
B893     B894     B895     B896      B897     B898     B899     B900      B901     B902     B903      B904
B905     B906     B907     B908      B909     B910     B911     B912      B913     B914     B915      B916
Q1       Q1       Q1       Q1        Q1        Q1       Q1        Q1        Q1       Q1        Q1        Q1
B917     B918     B919      B920      B921      B922      B923      B924      B925      B926      B927      B928
B929     B930     B931      B932      B933      B934      B935      B936      B937      B938      B939      B940
B941     B942     B943      B944      B945      B946      B947      B948      B949      B950      B951      B952
B953     B954     B955      B956      B957      B958      B959      B960      B961      B962      B963      B964
B965     B966     B967      B968      B969      B970      B971      B972      B973      B974      B975      B976
B977     B978     B979      B980      B981      B982      B983      B984      B985      B986      B987      B988
B989     B990     B991      B992      B993      B994      B995      B996      B997      B998      B999      B1000
B1001    B1002    B1003     B1004     B1005     B1006     B1007     B1008     B1009     B1010     B1011     B1012
B1013    B1014    B1015     B1016     B1017     B1018     B1019     B1020     B1021     B1022     B1023     B1024
B1025    B1026    B1027     B1028     B1029     B1030     B1031     B1032     B1033     B1034     B1035     B1036
B1037    B1038    B1039     B1040     B1041     B1042     B1043     B1044     B1045     B1046     B1047     B1048
B1049    B1050    B1051     B1052     B1053     B1054     B1055     B1056     B1057     B1058     B1059     B1060
B1061    B1062    B1063     B1064     B1065     B1066     B1067     B1068     B1069     B1070     B1071     B1072
B1073    B1074    B1075     B1076     B1077     B1078     B1079     B1080     B1081     B1082     B1083     B1084
B1085    B1086    B1087     B1088     B1089     B1090     B1091     B1092     B1093     B1094     B1095     B1096
B1097    B1098    B1099     B1100     B1101     B1102     B1103     B1104     B1105     B1106     B1107     B1108
B1109    B1110    B1111     B1112     B1113     B1114     B1115     B1116     B1117     B1118     B1119     B1120
B1121    B1122    B1123     B1124     B1125     B1126     B1127     B1128     B1129     B1130     B1131     B1132
B1133    B1134    B1135     B1136     B1137     B1138     B1139     B1140     B1141     B1142     B1143     B1144
B1145    B1146    B1147     B1148     B1149     B1150     B1151     B1152     B1153     B1154     B1155     B1156
B1157    B1158    B1159     B1160     B1161     B1162     B1163     B1164     B1165     B1166     B1167     B1168
B1169    B1170    B1171     B1172     B1173     B1174     B1175     B1176     B1177     B1178     B1179     B1180
B1181    B1182    B1183     B1184     B1185     B1186     B1187     B1188     B1189     B1190     B1191     B1192
B1193    B1194    B1195     B1196     B1197     B1198     B1199     B1200     B1201     B1202     B1203     B1204
B1205    B1206    B1207     B1208     B1209     B1210     B1211     B1212     B1213     B1214     B1215     B1216
B1217
表15:式Ik化合物(P为0或1):
Q1      Q1      Q1      Q1       Q1      Q1       Q1       Q1      Q1       Q1       Q1       Q1
B1      B2       B3      B4       B5       B6       B7       B8       B9       B10      B11      B12
B13     B14      B15     B16      B17      B18      B19      B20      B21      B22      B23      -
B25     B26      B27     B28      B29      B30      B31      B32      B33      B34      B35      B36
B37     B38      B39     B40      B41      B42      B43      B44      B45      B46      B47      B48
B49     B50      B51     B52      B53      B54      B55      B56      B57      B58      B59      B60
B61     B62      B63     B64      B65      B66      B67      B68      B69      B70      B71      B72
B73     B74      B75     B76      B77      B78      B79      B80      B81      B82      B83      B84
B85     B86      B87     B88      B89      B90      B91      B92      B93      B94      B95      B96
B97     B98      B99     B100     B101     B102     B103     B104     B105     B106     B107     B108
B109    B110     B111    B112     B113     B114     B115     B116     B117     B118     B119     B120
B121    B122     B123    B124     B125     B126     B127     B128     B129     B130     B131     B132
B133    B134     B135    B136     B137     B138     B139     B140     B141     B142     B143     B144
B145    B146     B147    B148     B149     B150     B151     B152     B153     B154     B155     B156
B157    B158     B159    B160     B161     B162     B163     B164     B165     B166     B167     B168
B169    B170     B171    B172     B173     B174     B175     B176     B177     B178     B179     B180
B181    B182     B183    B184     B185     B186     B187     B188     B189     B190     B191     B192
B193    B194     B195    B196     B197     B198     B199     B200     B201     B202     B203     B204
B205    B206     B207    B208     B209     B210     B211     B212     B213     B214     B215     B216
B217    B218     B219    B220     B221     B222     B223     B224     B225     B226     B227     B228
B229    B230     B231    B232     B233     B234     B235     B236     B237     B238     B239     B240
B241    B242     B243    B244     B245     B246     B247     B248     B249     B250     B251     B252
B253    B254     B255    B256     B257     B258     B259     B260     B261     B262     B263     B264
B265    B266     B267    B268     B269     B270     B271     B272     B273     B274     B275     B276
B277    B278     B279    B280     B281     B282     B283     B284     B285     B286     B287     B288
B289    B290     B291    B292     B293     B294     B295     B296     B297     B298     B299     B300
B301    B302     B303    B304     B305     B306     B307     B308     B309     B310     B311     B312
B313    B314     B315    B316     B317     B318     B319     B320     B321     B322     B323     B324
B325    B326     B327    B328     B329     B330     B331     B332     B333     B334     B335     B336
B337    B338     B339    B340     B341     B342     B343     B344     B345     B346     B347     B348
B349    B350     B351    B352     B353     B354     B355     B356     B357     B358     B359     B360
B361    B362     B363    B364     B365     B366     B367     B368     B369     B370     B371     B372
B373    B374     B375    B376     B377     B378     B379     B380     B381     B382     B383     B384
B385    B386     B387    B388     B389     B390     B391     B392     B393     B394     B395     B396
Q1      Q1      Q1      Q1       Q1        Q1      Q1       Q1        Q1       Q1        Q1        Q1
B397    B398    B399     B400     B401      B402     B403     B404      B405      B406      B407      B408
B409    B410    B411     B412     B413      B414     B415     B416      B417      B418      B419      B420
B421    B422    B423     B424     B425      B426     B427     B428      B429      B430      B431      B432
B433    B434    B435     B436     B437      B438     B439     B440      B441      B442      B443      B444
B445    B446    B447     B448     B449      B450     B451     B452      B453      B454      B455      B456
B457    B458    B459     B460     B461      B462     B463     B464      B465      B466      B467      B468
B469    B470    B471     B472     B473      B474     B475     B476      B477      B478      B479      B480
B481    B482    B483     B484     B485      B486     B487     B488      B489      B490      B491      B492
B493    B494    B495     B496     B497      B498     B499     B500      B501      B502      B503      B504
B505    B506    B507     B508     B509      B510     B511     B512      B513      B514      B515      B516
B517    B518    B519     B520     B521      B522     B523     B524      B525      B526      B527      B528
B529    B530    B531     B532     B533      B534     B535     B536      B537      B538      B539      B540
B541    B542    B543     B544     B545      B546     B547     B548      B549      B550      B551      B552
B553    B554    B555     B556     B557      B558     B559     B560      B561      B562      B563      B564
B565    B566    B567     B568     B569      B570     B571     B572      B573      B574      B575      B576
B577    B578    B579     B580     B581      B582     B583     B584      B585      B586      B587      B588
B589    B590    B591     B592     B593      B594     B595     B596      B597      B598      B599      B600
B601    B602    B603     B604     B605      B606     B607     B608      B609      B610      B611      B612
B613    B614    B615     B616     B617      B618     B619     B620      B621      B622      B623      B624
B625    B626    B627     B628     B629      B630     B631     B632      B633      B634      B635      B636
B637    B638    B639     B640     B641      B642     B643     B644      B645      B646      B647      B648
B649    B650    B651     B652     B653      B654     B655     B656      B657      B658      B659      B660
B661    B662    B663     B664     B665      B666     B667     B668      B669      B670      B671      B672
B773    B774    B775     B776     B777      B778     B779     B780      B781      B782      B783      B784
B785    B786    B787     B788     B789      B790     B791     B792      B793      B794      B795      B796
B797    B798    B799     B800     B801      B802     B803     B804      B805      B806      B807      B808
B809    B810    B811     B812     B813      B814     B815     B816      B817      B818      B819      B820
B821    B822    B823     B824     B825      B826     B827     B828      B829      B830      B831      B832
B833    B834    B835     B836     B837      B838     B839     B840      B841      B842      B843      B844
B845    B846    B847     B848     B849      B850     B851     B852      B853      B854      B855      B856
B857    B858    B859     B860     B861      B862     B863     B864      B865      B866      B867      B868
B869    B870    B871     B872     B873      B874     B875     B876      B877      B878      B879      B880
B881    B882    B883     B884     B885      B886     B887     B888      B889      B890      B891      B892
Q1        Q1        Q1        Q1       Q1         Q1        Q1        Q1        Q1        Q1         Q1        Q1
B893      B894      B895      B896      B897       B898       B899      B900       B901      B902       B903      B904
B905      B906      B907      B908      B909       B910       B911      B912       B913      B914       B915      B916
B917      B918      B919      B920      B921       B922       B923      B924       B925      B926       B927      B928
B929      B930      B931      B932      B933       B934       B935      B936       B937      B938       B939      B940
B941      B942      B943      B944      B945       B946       B947      B948       B949      B950       B951      B952
B953      B954      B955      B956      B957       B958       B959      B960       B961      B962       B963      B964
B965      B966      B967      B968      B969       B970       B971      B972       B973      B974       B975      B976
B977      B978      B979      B980      B981       B982       B983      B984       B985      B986       B987      B988
B989      B990      B991      B992      B993       B994       B995      B996       B997      B998       B999      B1000
B1001     B1002     B1003     B1004     B1005      B1006      B1007     B1008      B1009     B1010      B1011     B1012
B1013     B1014     B1015     B1016     B1017      B1018      B1019     B1020      B1021     B1022      B1023     B1024
B1025     B1026     B1027     B1028     B1029      B1030      B1031     B1032      B1033     B1034      B1035     B1036
B1037     B1038     B1039     B1040     B1041      B1042      B1043     B1044      B1045     B1046      B1047     B1048
B1049     B1050     B1051     B1052     B1053      B1054      B1055     B1056      B1057     B1058      B1059     B1060
B1061     B1062     B1063     B1064     B1065      B1066      B1067     B1068      B1069     B1070      B1071     B1072
B1073     B1074     B1075     B1076     B1077      B1078      B1079     B1080      B1081     B1082      B1083     B1084
B1085     B1086     B1087     B1088     B1089      B1090      B1091     B1092      B1093     B1094      B1095     B1096
B1097     B1098     B1099     B1100     B1101      B1102      B1103     B1104      B1105     B1106      B1107     B1108
B1109     B1110     B1111     B1112     B1113      B1114      B1115     B1116      B1117     B1118      B1119     B1120
B1121     B1122     B1123     B1124     B1125      B1126      B1127     B1128      B1129     B1130      B1131     B1132
B1133     B1134     B1135     B1136     B1137      B1138      B1139     B1140      B1141     B1142      B1143     B1144
B1145     B1146     B1147     B1148     B1149      B1150      B1151     B1152      B1153     B1154      B1155     B1156
B1157     B1158     B1159     B1160     B1161      B1162      B1163     B1164      B1165     B1166      B1167     B1168
B1169     B1170     B1171     B1172     B1173      B1174      B1175     B1176      B1177     B1178      B1179     B1180
B1181     B1182     B1181     B1184     B1185      B1186      B1187     B1188      B1189     B1190      B1191     B1192
B1193     B1194     B1195     B1196     B1197      B1198      B1199     B1200      B1201     B1202      B1203     B1204
B1205     B1206     B1207     B1208     B1209      B1210      B1211     B1212      B1213     B1214      B1215     B1216
B1217
表16:式Im化合物(P为0或1):
Figure C9981578602211
Q1       Q1      Q1       Q1       Q1       Q1        Q1       Q1        Q1        Q1        Q1       Q1
B1       B2       B3       B4       B5        B6        B7        B8        B9        B10       B11       B12
B13      B14      B15      B16      B17       B18       B19       B20       B21       B22       B23       -
B25      B26      B27      B28      B29       B30       B31       B32       B33       B34       B35       B36
B37      B38      B39      B40      B41       B42       B43       B44       B45       B46       B47       B48
B49      B50      B51      B52      B53       B54       B55       B56       B57       B58       B59       B60
B61      B62      B63      B64      B65       B66       B67       B68       B69       B70       B71       B72
B73      B74      B75      B76      B77       B78       B79       B80       B81       B82       B83       B84
B85      B86      B87      B88      B89       B90       B91       B92       B93       B94       B95       B96
B97      B98      B99      B100     B101      B102      B103      B104      B105      B106      B107      B108
B109     B110     B111     B112     B113      B114      B115      B116      B117      B118      B119      B120
B121     B122     B123     B124     B125      B126      B127      B128      B129      B130      B131      B132
B133     B134     B135     B136     B137      B138      B139      B140      B141      B142      B143      B144
B145     B146     B147     B148     B149      B150      B151      B152      B153      B154      B155      B156
B157     B158     B159     B160     B161      B162      B163      B164      B165      B166      B167      B168
B169     B170     B171     B172     B173      B174      B175      B176      B177      B178      B179      B180
B181     B182     B183     B184     B185      B186      B187      B188      B189      B190      B191      B192
B193     B194     B195     B196     B197      B198      B199      B200      B201      B202      B203      B204
B205     B206     B207     B208     B209      B210      B211      B212      B213      B214      B215      B216
B217     B218     B219     B220     B221      B222      B223      B224      B225      B226      B227      B228
B229     B230     B231     B232     B233      B234      B235      B236      B237      B238      B239      B240
B241     B242     B243     B244     B245      B246      B247      B248      B249      B250      B251      B252
B253     B254     B255     B256     B257      B258      B259      B260      B261      B262      B263      B264
B265     B266     B267     B268     B269      B270      B271      B272      B273      B274      B275      B276
B277     B278     B279     B280     B281      B282      B283      B284      B285      B286      B287      B288
B289     B290     B291     B292     B293      B294      B295      B296      B297      B298      B299      B300
B301     B302     B303     B304     B305      B306      B307      B308      B309      B310      B311      B312
B313     B314     B315     B316     B317      B318      B319      B320      B321      B322      B323      B324
Q1       Q1       Q1      Q1       Q1        Q1       Q1       Q1        Q1       Q1        Q1        Q1
B325     B326     B327     B328     B329      B330      B331     B332      B333      B334      B335      B336
B337     B338     B339     B340     B341      B342      B343     B344      B345      B346      B347      B348
B349     B350     B351     B352     B353      B354      B355     B356      B357      B358      B359      B360
B361     B362     B363     B364     B365      B366      B367     B368      B369      B370      B371      B372
B373     B374     B375     B376     B377      B378      B379     B380      B381      B382      B383      B384
B385     B386     B387     B388     B389      B390      B391     B392      B393      B394      B395      B396
B397     B398     B399     B400     B401      B402      B403     B404      B405      B406      B407      B408
B409     B410     B411     B412     B413      B414      B415     B416      B417      B418      B419      B420
B421     B422     B423     B424     B425      B426      B427     B428      B429      B430      B431      B432
B433     B434     B435     B436     B437      B438      B439     B440      B441      B442      B443      B444
B445     B446     B447     B448     B449      B450      B451     B452      B453      B454      B455      B456
B457     B458     B459     B460     B461      B462      B463     B464      B465      B466      B467      B468
B469     B470     B471     B472     B473      B474      B475     B476      B477      B478      B479      B480
B481     B482     B483     B484     B485      B486      B487     B488      B489      B490      B491      B492
B493     B494     B495     B496     B497      B498      B499     B500      B501      B502      B503      B504
B505     B506     B507     B508     B509      B510      B511     B512      B513      B514      B515      B516
B517     B518     B519     B520     B521      B522      B523     B524      B525      B526      B527      B528
B529     B530     B531     B532     B533      B534      B535     B536      B537      B538      B539      B540
B541     B542     B543     B544     B545      B546      B547     B548      B549      B550      B551      B552
B553     B554     B555     B556     B557      B558      B559     B560      B561      B562      B563      B564
B565     B566     B567     B568     B569      B570      B571     B572      B573      B574      B575      B576
B577     B578     B579     B580     B581      B582      B583     B584      B585      B586      B587      B588
B589     B590     B591     B592     B593      B594      B595     B596      B597      B598      B599      B600
B601     B602     B603     B604     B605      B606      B607     B608      B609      B610      B611      B612
B613     B614     B615     B616     B617      B618      B619     B620      B621      B622      B623      B624
B625     B626     B627     B628     B629      B630      B631     B632      B633      B634      B635      B636
B637     B638     B639     B640     B641      B642      B643     B644      B645      B646      B647      B648
B649     B650     B651     B652     B653      B654      B655     B656      B657      B658      B659      B660
B661     B662     B663     B664     B665      B666      B667     B668      B669      B670      B671      B672
B773     B774     B775     B776     B777      B778      B779     B780      B781      B782      B783      B784
B785     B786     B787     B788     B789      B790      B791     B792      B793      B794      B795      B796
B797     B798     B799     B800     B801      B802      B803     B804      B805      B806      B807      B808
B809     B810     B811     B812     B813      B814      B815     B816      B817      B818      B819      B820
Q1        Q1        Q1       Q1        Q1        Q1        Q1         Q1       Q1        Q1         Q1         Q1
B821      B822      B823      B824      B825      B826       B827       B828      B829      B830       B831       B832
B833      B834      B835      B836      B837      B838       B839       B840      B841      B842       B843       B844
B845      B846      B847      B848      B849      B850       B851       B852      B853      B854       B855       B856
B857      B858      B859      B860      B861      B862       B863       B864      B865      B866       B867       B868
B869      B870      B871      B872      B873      B874       B875       B876      B877      B878       B879       B880
B881      B882      B883      B884      B885      B886       B887       B888      B889      B890       B891       B892
B893      B894      B895      B896      B897      B898       B899       B900      B901      B902       B903       B904
B905      B906      B907      B908      B909      B910       B911       B912      B913      B914       B915       B916
B917      B918      B919      B920      B921      B922       B923       B924      B925      B926       B927       B928
B929      B930      B931      B932      B933      B934       B935       B936      B937      B938       B939       B940
B941      B942      B943      B944      B945      B946       B947       B948      B949      B950       B951       B952
B953      B954      B955      B956      B957      B958       B959       B960      B961      B962       B963       B964
B965      B966      B967      B968      B969      B970       B971       B972      B973      B974       B975       B976
B977      B978      B979      B980      B981      B982       B983       B984      B985      B986       B987       B988
B989      B990      B991      B992      B993      B994       B995       B996      B997      B998       B999       B1000
B1001     B1002     B1003     B1004     B1005     B1006      B1007      B1008     B1009     B1010      B1011      B1012
B1013     B1014     B1015     B1016     B1017     B1018      B1019      B1020     B1021     B1022      B1023      B1024
B1025     B1026     B1027     B1028     B1029     B1030      B1031      B1032     B1033     B1034      B1035      B1036
B1037     B1038     B1039     B1040     B1041     B1042      B1043      B1044     B1045     B1046      B1047      B1048
B1049     B1050     B1051     B1052     B1053     B1054      B1055      B1056     B1057     B1058      B1059      B1060
B1061     B1062     B1063     B1064     B1065     B1066      B1067      B1068     B1069     B1070      B1071      B1072
B1073     B1074     B1075     B1076     B1077     B1078      B1079      B1080     B1081     B1082      B1083      B1084
B1085     B1086     B1087     B1088     B1089     B1090      B1091      B1092     B1093     B1094      B1095      B1096
B1097     B1098     B1099     B1100     B1101     B1102      B1103      B1104     B1105     B1106      B1107      B1108
B1109     B1110     B1111     B1112     B1113     B1114      B1115      B1116     B1117     B1118      B1119      B1120
B1121     B1122     B1123     B1124     B1125     B1126      B1127      B1128     B1129     B1130      B1131      B1132
B1133     B1134     B1135     B1136     B1137     B1138      B1139      B1140     B1141     B1142      B1143      B1144
B1145     B1146     B1147     B1148     B1149     B1150      B1151      B1152     B1153     B1154      B1155      B1156
B1157     B1158     B1159     B1160     B1161     B1162      B1163      B1164     B1165     B1166      B1167      B1168
B1169     B1170     B1171     B1172     B1173     B1174      B1175      B1176     B1177     B1178      B1179      B1180
B1181     B1182     B1183     B1184     B1185     B1186      B1187      B1188     B1189     B1190      B1191      B1192
B1193     B1194     B1195     B1196     B1197     B1198      B1199      B1200     B1201     B1202      B1203      B1204
B1205     B1206     B1207     B1208     B1209     B1210      B1211      B1212     B1213     B1214      B1215      B1216
Q1       Q1        Q1        Q1       Q1        Q1        Q1       Q1       Q1         Q1        Q1        Q1
B1217
表17:式In化合物(P为0或1):
Figure C9981578602241
Q1       Q1       Q1        Q1       Q1       Q1        Q1       Q1      Q1       Q1        Q1       Q1
B1       B2        B3        B4       B5        B6        B7       B8       B9       B10       B11       B12
B13      B14       B15       B16      B17       B18       B19      B20      B21      B22       B23       -
B25      B26       B27       B28      B29       B30       B31      B32      B33      B34       B35       B36
B37      B38       B39       B40      B41       B42       B43      B44      B45      B46       B47       B48
B49      B50       B51       B52      B53       B54       B55      B56      B57      B58       B59       B60
B61      B62       B63       B64      B65       B66       B67      B68      B69      B70       B71       B72
B73      B74       B75       B76      B77       B78       B79      B80      B81      B82       B83       B84
B85      B86       B87       B88      B89       B90       B91      B92      B93      B94       B95       B96
B97      B98       B99       B100     B101      B102      B103     B104     B105     B106      B107      B108
B109     B110      B111      B112     B113      B114      B115     B116     B117     B118      B119      B120
B121     B122      B123      B124     B125      B126      B127     B128     B129     B130      B131      B132
B133     B134      B135      B136     B137      B138      B139     B140     B141     B142      B143      B144
B145     B146      B147      B148     B149      B150      B151     B152     B153     B154      B155      B156
B157     B158      B159      B160     B161      B162      B163     B164     B165     B166      B167      B168
B169     B170      B171      B172     B173      B174      B175     B176     B177     B178      B179      B180
B181     B182      B183      B184     B185      B186      B187     B188     B189     B190      B191      B192
B193     B194      B195      B196     B197      B198      B199     B200     B201     B202      B203      B204
B205     B206      B207      B208     B209      B210      B211     B212     B213     B214      B215      B216
B217     B218      B219      B220     B221      B222      B223     B224     B225     B226      B227      B228
B229     B230      B231      B232     B233      B234      B235     B236     B237     B238      B239      B240
B241     B242      B243      B244     B245      B246      B247     B248     B249     B250      B251      B252
B253     B254      B255      B256     B257      B258      B259     B260     B261     B262      B263      B264
Q1       Q1       Q1       Q1        Q1        Q1       Q1        Q1       Q1        Q1        Q1        Q1
B265     B266     B267      B268      B269      B270      B271      B272      B273      B274      B275      B276
B277     B278     B279      B280      B281      B282      B283      B284      B285      B286      B287      B288
B289     B290     B291      B292      B293      B294      B295      B296      B297      B298      B299      B300
B301     B302     B303      B304      B305      B306      B307      B308      B309      B310      B311      B312
B313     B314     B315      B316      B317      B318      B319      B320      B321      B322      B323      B324
B325     B326     B327      B328      B329      B330      B331      B332      B333      B334      B335      B336
B337     B338     B339      B340      B341      B342      B343      B344      B345      B346      B347      B348
B349     B350     B351      B352      B353      B354      B355      B356      B357      B358      B359      B360
B361     B362     B363      B364      B365      B366      B367      B368      B369      B370      B371      B372
B373     B374     B375      B376      B377      B378      B379      B380      B381      B382      B383      B384
B385     B386     B387      B388      B389      B390      B391      B392      B393      B394      B395      B396
B397     B398     B399      B400      B401      B402      B403      B404      B405      B406      B407      B408
B409     B410     B411      B412      B413      B414      B415      B416      B417      B418      B419      B420
B421     B422     B423      B424      B425      B426      B427      B428      B429      B430      B431      B432
B433     B434     B435      B436      B437      B438      B439      B440      B441      B442      B443      B444
B445     B446     B447      B448      B449      B450      B451      B452      B453      B454      B455      B456
B457     B458     B459      B460      B461      B462      B463      B464      B465      B466      B467      B468
B469     B470     B471      B472      B473      B474      B475      B476      B477      B478      B479      B480
B481     B482     B483      B484      B485      B486      B487      B488      B489      B490      B491      B492
B493     B494     B495      B496      B497      B498      B499      B500      B501      B502      B503      B504
B505     B506     B507      B508      B509      B510      B511      B512      B513      B514      B515      B516
B517     B518     B519      B520      B521      B522      B523      B524      B525      B526      B527      B528
B529     B530     B531      B532      B533      B534      B535      B536      B537      B538      B539      B540
B541     B542     B543      B544      B545      B546      B547      B548      B549      B550      B551      B552
B553     B554     B555      B556      B557      B558      B559      B560      B561      B562      B563      B564
B565     B566     B567      B568      B569      B570      B571      B572      B573      B574      B575      B576
B577     B578     B579      B580      B581      B582      B583      B584      B585      B586      B587      B588
B589     B590     B591      B592      B593      B594      B595      B596      B597      B598      B599      B600
B601     B602     B603      B604      B605      B606      B607      B608      B609      B610      B611      B612
B613     B614     B615      B616      B617      B618      B619      B620      B621      B622      B623      B624
B625     B626     B627      B628      B629      B630      B631      B632      B633      B634      B635      B636
B637     B638     B639      B640      B641      B642      B643      B644      B645      B646      B647      B648
B649     B650     B651      B652      B653      B654      B655      B656      B657      B658      B659      B660
Q1        Q1        Q1        Q1       Q1        Q1       Q1        Q1        Q1       Q1        Q1        Q1
B661      B662      B663      B664      B665      B666      B667      B668      B669      B670      B671      B672
B773      B774      B775      B776      B777      B778      B779      B780      B781      B782      B783      B784
B785      B786      B787      B788      B789      B790      B791      B792      B793      B794      B795      B796
B797      B798      B799      B800      B801      B802      B803      B804      B805      B806      B807      B808
B809      B810      B811      B812      B813      B814      B815      B816      B817      B818      B819      B820
B821      B822      B823      B824      B825      B826      B827      B828      B829      B830      B831      B832
B833      B834      B835      B836      B837      B838      B839      B840      B841      B842      B843      B844
B845      B846      B847      B848      B849      B850      B851      B852      B853      B854      B855      B856
B857      B858      B859      B860      B861      B862      B863      B864      B865      B866      B867      B868
B869      B870      B871      B872      B873      B874      B875      B876      B877      B878      B879      B880
B881      B882      B883      B884      B885      B886      B887      B888      B889      B890      B891      B892
B893      B894      B895      B896      B897      B898      B899      B900      B901      B902      B903      B904
B905      B906      B907      B908      B909      B910      B911      B912      B913      B914      B915      B916
B917      B918      B919      B920      B921      B922      B923      B924      B925      B926      B927      B928
B929      B930      B931      B932      B933      B934      B935      B936      B937      B938      B939      B940
B941      B942      B943      B944      B945      B946      B947      B948      B949      B950      B951      B952
B953      B954      B955      B956      B957      B958      B959      B960      B961      B962      B963      B964
B965      B966      B967      B968      B969      B970      B971      B972      B973      B974      B975      B976
B977      B978      B979      B980      B981      B982      B983      B984      B985      B986      B987      B988
B989      B990      B991      B992      B993      B994      B995      B996      B997      B998      B999      B1000
B1001     B1002     B1003     B1004     B1005     B1006     B1007     B1008     B1009     B1010     B1011     B1012
B1013     B1014     B1015     B1016     B1017     B1018     B1019     B1020     B1021     B1022     B1023     B1024
B1025     B1026     B1027     B1028     B1029     B1030     B1031     B1032     B1033     B1034     B1035     B1036
B1037     B1038     B1039     B1040     B1041     B1042     B1043     B1044     B1045     B1046     B1047     B1048
B1049     B1050     B1051     B1052     B1053     B1054     B1055     B1056     B1057     B1058     B1059     B1060
B1061     B1062     B1063     B1064     B1065     B1066     B1067     B1068     B1069     B1070     B1071     B1072
B1073     B1074     B1075     B1076     B1077     B1078     B1079     B1080     B1081     B1082     B1083     B1084
B1085     B1086     B1087     B1088     B1089     B1090     B1091     B1092     B1093     B1094     B1095     B1096
B1097     B1098     B1099     B1100     B1101     B1102     B1103     B1104     B1105     B1106     B1107     B1108
B1109     B1110     B1111     B1112     B1113     B1114     B1115     B1116     B1117     B1118     B1119     B1120
B1121     B1122     B1123     B1124     B1125     B1126     B1127     B1128     B1129     B1130     B1131     B1132
B1133     B1134     B1135     B1136     B1137     B1138     B1139     B1140     B1141     B1142     B1143     B1144
B1145     B1146     B1147     B1148     B1149     B1150     B1151     B1152     B1153     B1154     B1155     B1156
Q1        Q1        Q1        Q1       Q1        Q1        Q1       Q1        Q1        Q1       Q1        Q1
B1157     B1158     B1159     B1160     B1161     B1162     B1163     B1164     B1165     B1166     B1167     B1168
B1169     B1170     B1171     B1172     B1173     B1174     B1175     B1176     B1177     B1178     B1179     B1180
B1181     B1182     B1183     B1184     B1185     B1186     B1187     B1188     B1189     B1190     B1191     B1192
B1193     B1194     B1195     B1196     B1197     B1198     B1199     B1200     B1201     B1202     B1203     B1204
B1205     B1206     B1207     B1208     B1209     B1210     B1211     B1212     B1213     B1214     B1215     B1216
B1217
表18:式Io化合物(P为0或1):
Figure C9981578602271
Q2        Q2        Q2       Q2        Q2        Q2       Q2        Q2       Q2        Q2        Q2       Q2
C1        C2        C3        C4        C5        C6        C7        C8        C9        C10       C11       C12
C13       C14       C15       C16       C17       C18       C19       C20       C21       C22       C23       C24
C25       C26       C27       C28       C29       C30       C31       C32       C33       C34       C35       C36
C37       C38       C39       C40       C41       C42       C43       C44       C45       C46       C47       C48
C49       C50       C51       C52       C53       C54       C55       C56       C57       C58       C59       C60
C61       C62       C63       C64       C65       C66       C67       C68       C69       C70       C71       C72
C73       C74       C75       C76       C77       C78       C79       C80       C81       C82       C83       C84
C85       C86       C87       C88       C89       C90       C91       C92       C93       C94       C95       C96
C97       C98       C99       C100      C101      C102      C103      C104      C105      C106      C107      C108
C109      C110      C111      C112      C113      C114      C115      C116      C117      C118      C119      C120
C121      C122      C123      C124      C125      C126      C127      C128      C129      C130      C131      C132
C133      C134      C135      C136      C137      C138      C139      C140      C141      C142      C143      C144
C145      C146      C147      C148      C149      C150      C151
表19:式Iq化合物(P为0或1):
Q2      Q2       Q2      Q2       Q2       Q2       Q2       Q2      Q2       Q2       Q2       Q2
C1      C2       C3       C4       C5        C6       C7       C8       C9       C10      C11      C12
C13     C14      C15      C16      C17       C18      C19      C20      C21      C22      C23      C24
C25     C26      C27      C28      C29       C30      C31      C32      C33      C34      C35      C36
C37     C38      C39      C40      C41       C42      C43      C44      C45      C46      C47      C48
C49     C50      C51      C52      C53       C54      C55      C56      C57      C58      C59      C60
C61     C62      C63      C64      C65       C66      C67      C68      C69      C70      C71      C72
C73     C74      C75      C76      C77       C78      C79      C80      C81      C82      C83      C84
C85     C86      C87      C88      C89       C90      C91      C92      C93      C94      C95      C96
C97     C98      C99      C100     C101      C102     C103     C104     C105     C106     C107     C108
C109    C110     C111     C112     C113      C114     C115     C116     C117     C118     C119     C120
C121    C122     C123     C124     C125      C126     C127     C128     C129     C130     C131     C132
C133    C134     C135     C136     C137      C138     C139     C140     C141     C142     C143     C144
C145    C146     C147     C148     C149      C150     C151
表20:式Ir化合物(P为0或1):
Figure C9981578602282
Q3      Q3      Q3       Q3       Q3       Q3       Q3       Q3      Q3        Q3      Q3      Q3
D1      D2       D3       D4       D5        D6       D7       D8       D9        D10     D11      D12
D13     D14      D15      D16      D17       D18      D19      D20      D21       D22     D23      D24
D25     D26      D27      D28      D29       D30      D31      D32      D33       D34     D35      D36
D37     D38      D39      D40      D41       D42      D43      D44      D45       D46     D47      D48
Q3       Q3      Q3       Q3       Q3      Q3       Q3       Q3      Q3       Q3       Q3       Q3
D49      D50      D51      D52      D53      D54      D55      D56      D57      D58      D59      D60
D61      D62      D63      D64      D65      D66      D67      D68      D69      D70      D71      D72
D73      D74      D75      D76      D77      D78      D79      D80      D81      D82      D83      D84
D85      D86      D87      D88      D89      D90      D91      D92      D93      D94      D95      D96
D97      D98      D99      D100     D101     D102     D103     D104     D105     D106     D107     D108
D109     D110     D111     D112     D113     D114     D115     D116     D117     D118     D119     D120
D121     D122     D123     D124     D125     D126     D127     D128     D129     D130     D131     D132
D133     D134     D135     D136     D137     D138     D139     D140
表21:式Is化合物(P为0或1):
Q3       Q3      Q3       Q3       Q3      Q3       Q3       Q3      Q3       Q3       Q3      Q3
D1       D2       D3       D4       D5       D6       D7       D8       D9       D10      D11      D12
D13      D14      D15      D16      D17      D18      D19      D20      D21      D22      D23      D24
D25      D26      D27      D28      D29      D30      D31      D32      D33      D34      D35      D36
D37      D38      D39      D40      D41      D42      D43      D44      D45      D46      D47      D48
D49      D50      D51      D52      D53      D54      D55      D56      D57      D58      D59      D60
D61      D62      D63      D64      D65      D66      D67      D68      D69      D70      D71      D72
D73      D74      D75      D76      D77      D78      D79      D80      D81      D82      D83      D84
D85      D86      D87      D88      D89      D90      D91      D92      D93      D94      D95      D96
D97      D98      D99      D100     D101     D102     D103     D104     D105     D106     D107     D108
D109     D110     D111     D112     D113     D114     D115     D116     D117     D118     D119     D120
D121     D122     D123     D124     D125     D126     D127     D128     D129     D130     D131     D132
D133     D134     D135     D136     D137     D138     D139     D140
表22:式It化合物(P为0或1):
Figure C9981578602301
Q4       Q4      Q4       Q4       Q4      Q4      Q4    Q4    Q4    Q4    Q4     Q4     Q4     Q4    Q4
E1       E2       E3       E4       E5       E6      E7     E8    E9    E10    E11    E12    E13    E14    E15
E16      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):
Q4       Q4      Q4       Q4       Q4      Q4      Q4     Q4   Q4    Q4     Q4    Q4     Q4     Q4    Q4
E1       E2       E3       E4       E5       E6      E7     E8    E9    E10    E11    E12    E13    E14    E15
E16      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):
Figure C9981578602303
Q5      Q5       Q5       Q5       Q5      Q5
F1       F2       F3       F4       F5       F6
表25:式Iw化合物(P为0或1):
Figure C9981578602311
Q5     Q5      Q5     Q5    Q5     Q5
F1     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        94-95
A9             73-74            A1022        油
A6             148-150          A1203        结晶
A26            143-144          A21          无定形
A34            170-171          A1023        110-111
A1026          结晶             A1085        188-191
A1304          结晶             A1088        157-158
A1301          结晶             A1092        结晶
A1018          110-111          A1095        136-138
A1             195-197          A1096        194-196
A2             150-151          A124         135-136
A15            164-166          A31          209-210
A27            107-108          H-B1057      166-167
A29            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      150-152
A10            166-167          H-B1067      122-123
A8             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        116-118
A64              134-135         H-C24       172-175
A94              134-135         A1205       结晶
A531             结晶            H-D113      油
A1 045           结晶            H-F5        油
A1322            结晶            H-F16       145-148
A184             146-147         A1088       157-158
A358             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-B1092            -           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-C152             -           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2kg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        1
A2-B1082        2000         2          2         2           2        1        2
A2-B1083        2000         2          3         3           4        2        3
A2-B90          2000         1          1         1           1        1        1
A2-B68          2000         1          2         1           2        1        2
A2-B24          2000         1          1         1           2        1        1
A2-B73          2000         3          4         2           2        2        2
A2-B75          2000         2          3         2           2        1        2
A2-B95          2000         2          4         2           2        1        2
A2-B93          2000         2          4         2           2        1        2
A3-B1           2000         2          2         4           2        3        2
A94-B1          2000         1          2         2           1        1        2
A2-B1063        2000         1          2         1           2        1        2
A2-B1061        2000         3          3         2           2        1        2
A2-B133         2000         1          2         2           2        1        2
A64-B24         2000         4          4         2           2        1        2
A2-B1089        2000         1          2         2           2        1        2
A2-B31          2000         2          3         4           2        1        2
A2-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       2
A2-B91           2000         1         2         1          2        1       2
A2-B2            2000         1         1         1          1        1       2
A2-B25           2000         2         3         2          2        1       2
A2-B1067         2000         2         3         2          2        3       3
A2-B1068         2000         2         2         2          2        1       2
A2-B1070         2000         2         3         3          2        2       2
A2-C146          2000         1         2         2          2        1       2
A2-B354          2000         1         1         1          1        1       2
A34-B1           2000         1         2         2          2        2       3
A9-B1            2000         2         1         2          1        1       2
A184-B1          2000         2         4         2          2        1       2
A184-B24         2000         1         3         2          2        1       2
A3-B24           2000         1         3         2          2        1       2
A8-B24           2000         1         2         2          2        1       3
A18-B24          2000         1         1         1          1        1       2
A2-B552          2000         1         2         2          2        1       2
A2-C152          2000         1         1         2          2        1       2
A2-B69           2000         1         4         2          2        1       1
A2-D36           2000         1         2         2          2        1       1
A2-B618          2000         1         1         1          2        1       1
A2-B33           2000         1         3         2          2        1       3
A2-B34           2000         1         3         2          2        1       2
A2-B35           2000         2         4         2          2        2       2
A2-B1095         2000         3         4         2          2        1       2
A2-C147          2000         2         4         2          2        2       2
A2-B49           2000         2         4         2          2        1       2
A2-C1            2000         2         3         1          2        1       2
A2-B1100         2000         1         3         1          2        1       2
A8-B2            2000         1         3         2          2        1       2
A8-B1064         2000         2         4         3          2        1       3
A8-B1101         2000         2         4         2          2        1       1
A2-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       4
A2-B134              2000       1        2         1         2        1       1
A1210-B354           2000       2        3         2         1        1       2
A2-C2                2000       2        3         1         1        1       1
A2-D36               2000       1        2         1         2        3       1
A2-D113(lsom.A)      2000       4        4         2         1        3       3
A2-D115              2000       3        3         2         2        2       3
A8-B34               2000       2        3         2         2        2       2
A8-B1103             2000       1        3         2         1        1       2
A2-C24               2000       1        2         1         1        1       2
表B1b:芽前作用
化合物               g/ha       稷       马唐      稗        苘麻     苋      藜
A8-B1                250        2        2         2         1        1       1
A1022-B24            250        2        4         4         3        4       1
A2-B145              250        2        2         4         2        3       1
A1208-B354           250        1        1         1         1        1       1
A8-B1063             250        2        3         3         2        4       1
A8-B552              250        2        3         4         1        4       1
A8-B156              250        3        3         3         3        4       2
A1210-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      2
A2-B1082          2000       1        2          2         1         1      2
A2-B1083          2000       1        4          2         1         1      2
A2-B90            2000       1        2          2         1         2      2
A2-B68            2000       1        2          2         1         1      2
A2-B24            2000       1        2          2         1         2      2
A2-B73            2000       1        3          2         1         1      2
A2-B75            2000       2        2          3         1         2      2
A2-B95            2000       1        2          2         1         2      2
A2-B93            2000       1        2          2         1         2      2
A3-B1             2000       1        3          2         1         1      2
A94-B1            2000       1        2          2         1         1      1
A2-B1063          2000       2        2          4         1         2      2
A2-B1061          2000       2        2          2         1         2      2
A2-B133           2000       1        2          2         1         2      2
A2-B1058          2000       1        2          4         1         2      2
A64-B24           2000       2        2          4         1         2      2
A64-B1            2000       2        3          4         1         1      2
A2-B1089          2000       1        2          2         1         1      2
A2-831            2000       2        2          2         1         2      2
A2-B1090          2000       2        4          4         2         2      2
A2-B46(顺式)      2000       1        2          3         1         2      2
A2-B46(反式)      2000       1        2          2         1         1      2
A2-B91            2000       1        2          2         1         2      2
A2-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      2
A2-B1066         2000       1       3         2         1       2      2
A2-B25           2000       1       2         2         2       1      2
A2-B1068         2000       1       2         4         1       1      2
A2-B1070         2000       2       4         2         2       2      2
A2-B5            2000       1       2         2         1       2      2
A2-C149          2000       1       3         2         1       2      2
A2-C146          2000       1       2         2         1       2      2
A2-B112          2000       2       3         2         1       2      2
A2-B354          2000       2       2         2         2       2      2
A2-E16           2000       2       3         2         2       2      2
A6-B24           2000       1       3         2         1       1      2
A34-B1           2000       1       2         2         1       1      2
A9-B1            2000       2       4         2         2       2      2
A184-B1          2000       1       3         2         1       2      2
A184-B24         2000       1       2         2         1       2      2
A7-B24           2000       1       2         2         1       2      2
A3-B24           2000       2       2         2         1       2      2
A34-B24          2000       1       2         2         1       2      2
A8-B24           2000       2       2         2         1       2      2
A18-B24          2000       1       2         2         1       2      2
A2-C152          2000       2       2         3         1       2      2
A2-B69           2000       1       2         2         1       2      2
A2-D36           2000       2       2         2         1       2      2
A2-B618          2000       2       2         2         1       2      2
A2-B49           2000       2       2         2         1       2      2
A2-B1093         2000       2       2         2         1       2      2
A2-B33           2000       2       4         2         1       2      2
A2-B34           2000       1       3         2         1       1      2
A2-B35           2000       1       3         2         1       1      2
A2-B1087         2000       1       4         3         1       2      2
A531-B24         2000       2       2         2         1       2      2
A2-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      2
A2-B70                2000     3       4        3       1       2      2
A2-B49                2000     2       2        2       1       2      2
A2-C1                 2000     3       2        2       1       2      2
A2-B1100              2000     2       2        3       1       1      2
A8-B2                 2000     2       2        2       2       2      3
A8-B1064              2000     2       4        2       1       1      2
A8-B133               2000     2       4        2       1       2      2
A8-B1101              2000     2       3        2       1       2      2
A2-B1101              2000     2       2        2       1       1      3
A2-B156               2000     1       2        2       1       2      2
A2-B134               2000     2       2        1       1       1      2
A1210-B354            2000     2       2        2       1       1      2
A2-C2                 2000     2       1        1       1       1      1
A2-D36                2000     2       1        1       1       1      1
A2-D113(lsom.A)       2000     2       1        1       1       1      2
A2-D113(lsom.B)       2000     2       2        2       2       1      2
A2-D114               2000     2       1        1       1       1      1
A2-D115               2000     1       2        1       1       1      1
A8-B34                2000     2       2        2       2       2      2
A8-B1103              2000     1       4        1       1       1      1
A2-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   lpopur. 藜
                g/ha
A8-B1           250     4       3        3      3       3     3       2
A2-B1091        250     4       4        2      3       4     3       3
A2-B1094        250     2       3        2      3       3     3       2
A2-B145         250     2       2        2      3       3     3       1
A1208-B354      250     3       4        2      1       2     2       2
A1210-B1        250     2       2        2      2       2     2       1
A8-B552         250     2       3        3      2       2     2       2
A8-B156         250     2       3        3      1       2     2       1
A1210-B1105     250     1       2        3      2       2     2       1
A8-B134         250     3       3        3      2       3     3       2
A8-D36          250     3       3        2      2       3     3       2
A2-D111(顺式)   250     2       2        4      2       1     2       2
A2-D111(反式)   250     3       3        3      3       1     3       2
A8-D111         250     3       3        3      3       1     2       3
A8-D109         250     3       3        3      3       1     2       3
A8-F5           250     4       3        4      3       3     3       3
A2-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 (13)

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 C998157860002C1
其中
p为0或1;
R5为C1-C6卤代烷基;
R2为C1-C6烷基,C1-C6卤代烷基,C3-C6环烷基,C1-C6烷氧基,C3-C6炔氧基,C1-C6卤代烷氧基,C1-C4烷氧基-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--C6烷基羰氧基-C1-C4烷基;
R3为氢;
R4为氢或C1-C6烷基;
Q为Q1
其中
R6为氢,C1-C6烷基,C2-C6链烯基,C2-C6炔基,C1-C6烷基-S(O)n17,其中n17是0,1或2,C1-C6烷氧基羰基、C1-C6烷氧基;
R7是氢,C1-C6烷基、C1-C6烷氧基、C1-C6烷氧基羰基;
R8是氢,C1-C6烷基;
R9是氢,C1-C6烷基;
或者相邻的R8与R9一起表示-(CH2)m-,其中m为2,3或6,或C(O)O(CH2)n20
其中n20为2;
W为氧,-CR11R12-,-CR63R64CR65R66,-C(O)-;
R63、R64、R65和R66为氢,或者R65与R9一起形成直接键;
R11为氢,C1-C4烷氧基羰基,苯基,C1-C4烷基,C1-C4卤代烷基;
或者R11与R9一起代表基团-(CH2)0-;
o为1,3或4;
R12为氢,C1-C4烷基,
R10为羟基,O-M+,其中M+为-NH+(CH2CH3)3,苯硫基,苯基亚磺酰基,苯基磺酰基或卤素。
2.根据权利要求1的化合物,其中R10为羟基或O-M+
3.根据权利要求1的化合物,其中W为氧,-CR11R12-或-C(O)-。
4.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。
5.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。
6.根据权利要求1的化合物,其中R2为甲基和R3为氢。
7.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,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,二氟甲基或三氟甲基。
8.根据权利要求1的化合物,其中R4为氢或甲基。
9.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。
10.除草与抑制植物生长的组合物,其包括除草活性量的如权利要求1-9之任一项所定义的式I化合物和惰性载体。
11.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如权利要求1-9之任一项所定义的式I活性成分或包含这种活性成分的组合物。
12.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如权利要求1-9之任一项所定义的式I活性成分或包含这种活性成分的组合物。
13.权利要求10的组合物在防治不需要植物生长方面的应用。
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Families Citing this family (37)

* 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
EP1330459B1 (en) 2000-10-02 2006-08-02 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
EP1450607A1 (en) * 2001-12-03 2004-09-01 Syngenta Participations AG Herbicidal composition
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
PT1601653E (pt) 2003-03-07 2009-04-27 Syngenta Participations Ag Processo para a produção de ésteres de ácido nicotínico substituído
US7214825B2 (en) * 2003-10-17 2007-05-08 Honeywell International Inc. O-(3-chloropropenyl) hydroxylamine free base
EP1740524B1 (en) * 2004-04-30 2012-12-12 Syngenta Participations AG Process for the production of cyclic diketones
AU2005238195B2 (en) * 2004-04-30 2011-07-28 Syngenta Limited Process for the production of cyclic diketones
WO2006059103A2 (en) * 2004-12-03 2006-06-08 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
JP2012512821A (ja) * 2008-12-18 2012-06-07 ビーエーエスエフ ソシエタス・ヨーロピア 除草作用を有するヘテロ環ジケトン誘導体
JP5511693B2 (ja) 2009-02-03 2014-06-04 クミアイ化学工業株式会社 縮合環化した2−ピリドン誘導体及び除草剤
CA2762680C (en) 2009-05-21 2018-04-17 Chlorion Pharma, Inc. Methyl sulfanyl pyrmidmes useful as antiinflammatories, analgesics, and antiepileptics
WO2011064188A1 (en) * 2009-11-27 2011-06-03 Basf Se Insecticidal methods using nitrogen-containing heteroaromatic compounds
BR112014011685A2 (pt) 2011-11-18 2017-05-30 Basf Se composto, utilização de um composto e método
RS55269B1 (sr) * 2011-11-30 2017-02-28 Syngenta Ltd 2-(supstituisani-fenil)-ciklopentan-1,3-dion jedinjenja, i derivati od toga
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
EP2997014B1 (en) 2013-07-19 2016-09-21 Lonza Ltd Method for preparation of 6-trifluoromethylpyridine-3-carboxylic acid derivatives from trifluoroacetylacetic acid
MX2016017019A (es) 2014-06-26 2017-05-12 Lonza Ag Metodo para la preparacion de 4-alcoxi-1,1,1-trifluorobut-3-en-2-o nas de 1,1,1 trifluoroacetona.
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
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
IL277071B1 (en) 2018-03-08 2024-03-01 Incyte Corp Aminopyrizine diol compounds as PI3K–y inhibitors
US11834434B2 (en) * 2018-06-25 2023-12-05 Bayer Aktiengesellschaft Substituted 2-heteroaryloxypyridines and salts thereof and their use as herbicidal agents
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
AU2022309257A1 (en) * 2021-07-12 2024-01-04 Fortephest Ltd Novel derivatives of non-coded amino acids and their use as herbicides

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
GB2205316B (en) 1987-06-05 1991-09-11 Sandoz Ltd Herbicidal benzoyl pyran compounds
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
WO1992022203A1 (en) * 1991-06-12 1992-12-23 E.I. Du Pont De Nemours And Company Substituted pyridine herbicides
JP4240531B2 (ja) * 1995-02-24 2009-03-18 ビーエーエスエフ ソシエタス・ヨーロピア ベンゾイル誘導体
JPH11509202A (ja) * 1995-07-10 1999-08-17 イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー 除草性スルホンアミド
GB2305174A (en) * 1995-09-15 1997-04-02 Zeneca Ltd Chemical process
US6063732A (en) 1996-03-15 2000-05-16 Novartis Crop Protection, Inc. Herbicidal synergistic composition and method of weed control
AU3297397A (en) * 1996-06-06 1998-01-05 E.I. Du Pont De Nemours And Company Herbicidal pyridinyl and pyrazolylphenyl ketones
ES2244214T3 (es) * 1998-09-15 2005-12-01 Syngenta Participations Ag Piridincetonas utiles como herbicidas.

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