CN1117083C - 哒嗪-3-酮衍生物,它们的应用,以及制备它们所用的中间体 - Google Patents

哒嗪-3-酮衍生物,它们的应用,以及制备它们所用的中间体 Download PDF

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CN1117083C
CN1117083C CN96197700A CN96197700A CN1117083C CN 1117083 C CN1117083 C CN 1117083C CN 96197700 A CN96197700 A CN 96197700A CN 96197700 A CN96197700 A CN 96197700A CN 1117083 C CN1117083 C CN 1117083C
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片山忠
河村伸一
实光穣
峰洋子
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Abstract

本发明提供了新的可用作除草剂活性成分的式[I]哒嗪-3-酮衍生物,其中R1为卤代烷基;R2和R3相同或不同并为氢,烷基,卤代烷基,或烷氧基烷基;以及Q为[Q-1],[Q-2],[Q-3],[Q-4],或[Q-5]。本发明还提供了它们的应用和制备它们的中间体。

Description

哒嗪-3-酮衍生物,它们 的应用,以及制备它们 所用的中间体
发明领域
本发明涉及哒嗪-3-酮衍生物,它们作为除草剂的应用,以及制备它们所用的中间体。
发明背景
EP-A-0029123中公开了制备取代苯胺的方法,并公开了新的取代苯胺类化合物。更具体讲,该文献教导了用这一方法制得的某些取代苯胺类化合物可用作制备新的取代哒嗪-3-酮衍生物的重要原料,其中所述的哒嗪-3-酮衍生物在芽后施用时具有除草活性。但这些哒嗪-3-酮衍生物不同于本发明化合物,它们在哒嗪酮的2位具有取代的苯氧基苯基作为基本结构单元,而且在哒嗪酮环上进一步具有明显不同的取代基。
发明公开
为寻求具有优越除草活性的化合物,本发明人已进行了广泛研究。结果,我们发现下面式[I]所示的哒嗪-3-酮衍生物具有优良的除草活性,由此完成了本发明。
因此,本发明提供了下述式[I]化合物(以下称作本发明化合物);以及含有其作为活性成分的除草剂:其中R1为C1-C3卤代烷基;R2和R3相同或不同,并且为氢,C1-C3烷基,C1-C3卤代烷基,或C1-C3烷氧基C1-C3烷基;以及Q为下列式[Q-1],[Q-2],[Q-3],[Q-4],或[Q-5]:[Q-1]                       [Q-2]                        [Q-3][Q-4]                       [Q-5]
其中X为氢或卤素;
Y为卤素,硝基,氰基,或三氟甲基;
Z1为氧,硫或NH;
Z2为氧或硫;
n为0或1;
B为氢,卤素,硝基,氰基,氯磺酰基,OR10,SR10,SO2OR10,N(R11)R12,SO2N(R11)R12,NR11(COR13),NR11(SO2R14),N(SO2R14)(SO2R15),N(SO2R14)(COR13),NHCOOR13,COOR10,CON(R11)R12,CSN(R11)R12,COR16,CR17=CR18COR16,CR17=CR18COOR13,CR17=CR18CON(R11)R12,CH2CHWCOOR13,CH2CHWCON(R11)R12,CR17=NOR33,CR17=NN(R11)R12,CR17(Z2R34)2,OCO2R19,或OCOR19
R4为氢或C1-C3烷基;
R5为氢,C1-C6烷基,C1-C6卤代烷基,C3-C8环烷基烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,氰基-C1-C6烷基,C2-C8烷氧基烷基,C3-C8烷氧基烷氧基烷基,羧基C1-C6烷基,(C1-C6烷氧基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基,(C3-C8环烷氧基)羰基C1-C6烷基,CH2CON(R11)R12,CH2COON(R11)R12,CH(C1-C4烷基)CON(R11)R12,CH(C1-C4烷基)COON(R11)R12,C2-C8烷硫基烷基,或羟基C1-C6烷基;
R6为C1-C6烷基,C1-C6卤代烷基,甲酰基,氰基,羧基,羟基C1-C6烷基,C1-C6烷氧基C1-C6烷基,C1-C6烷氧基C1-C6烷氧基C1-C6烷基,(C1-C6烷基)羰氧基C1-C6烷基,(C1-C6卤代烷基)羰氧基C1-C6烷基,(C1-C6烷氧基)羰基,或(C1-C6烷基)羰基;
R7为氢或C1-C6烷基;和
R8为氢,C1-C6烷基,C1-C6卤代烷基,羟基C1-C6烷基,C2-C8烷氧基烷基,C3-C10烷氧基烷氧基烷基,(C1-C5烷基)羰氧基C1-C6烷基,(C1-C6卤代烷基)羰氧基C1-C6烷基,羧基,羧基C1-C6烷基,(C1-C8烷氧基)羰基,(C1-C6卤代烷氧基)羰基,(C3-C10环烷氧基)羰基,(C3-C8链烯氧基)羰基,(C3-C8炔氧基)羰基,氨基羰基,(C1-C6烷基)氨基羰基,二(C1-C6烷基)氨基羰基,(C1-C6烷基)氨基羰氧基C1-C6烷基,或二(C1-C6烷基)氨基羰氧基C1-C6烷基;
其中R10为氢,C1-C6烷基,C1-C6卤代烷基,C3-C8环烷基,苄基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,氰基C1-C6烷基,C2-C8烷氧基烷基,C2-C8烷硫基烷基,羧基C1-C6烷基,(C1-C8烷氧基)羰基C1-C6烷基,(C1-C6卤代烷氧基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基,(C3-C8环烷氧基)羰基C1-C6烷基,(C1-C6烷基)羰基C1-C6烷基,(C1-C6卤代烷基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷基}羰基C1-C6烷基,(C3-C8环烷基)羰基C1-C6烷基,CH2CON(R11)R12,CH2COON(R11)R12,CH(C1-C4烷基)CON(R11)R12,CH(C1-C4烷基)COON(R11)R12,{(C1-C6烷氧基)羰基C1-C6烷基}氧羰基C1-C6烷基,或羟基C1-C6烷基;
R11和R12独立地为氢,C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6炔基,氰基C1-C6烷基,C2-C8烷氧基烷基,C2-C8烷硫基烷基,羧基C1-C6烷基,(C1-C6烷氧基)羰基C1-C6烷基,(C3-C8环烷氧基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基,或者R11和R12结合形成四亚甲基,五亚甲基,或3-氧杂-1,5-亚戊基;
R13为氢,C1-C6烷基,C1-C6卤代烷基,C3-C8环烷基,或C3-C6链烯基;
R14和R15独立地为C1-C6烷基,C1-C6卤代烷基,或被甲基或硝基任选取代的苯基;
R16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,C2-C8烷氧基烷基,或羟基C1-C6烷基;
R17和R18独立地为氢或C1-C6烷基;
R19为C1-C6烷基;
R33为氢,C1-C6烷基,C1-C6卤代烷基,C3-C8环烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,氰基C1-C6烷基,或(C1-C6烷氧基)羰基C1-C6烷基;
R34为C1-C6烷基,或者两个R34结合形成(CH2)2或(CH2)3;和
W为氢,氯,或溴。
本发明还提供了式[2]化合物:
Figure C9619770000141
其中R3的定义同上,且Q1为下式[Q1-1],[Q-2],[Q1-3],[Q-4],或[Q-5]:
Figure C9619770000142
[Q1-1]                    [Q-2]                     [Q1-3]
Figure C9619770000143
[Q-4]                         [Q-5]其中X,Y,Z1,Z2,n,R4,R5,R7和R8的定义同上;B1为氢,卤素,硝基,氰基,OR27,SR27,SO2OR27,N(R11)R12,SO2NR11(R12),NR11(COR13),NR11(SO2R14),N(SO2R14)(SO2R15),N(SO2R14)(COR13),NHCOOR13,COOR27,CONR11(R12),CSNR11(R12),CR17=CR18COOR13,CR17=CR18CONR11(R12),CH2CHWCOOR13,CH2CHWCONR11(R12),CR17=NOR33,CR17=NNR11(R12),CR17(Z2R34)2,OCO2R19,或OCOR19;R9为C1-C6烷基,C1-C6卤代烷基,氰基,羧基,羟基C1-C6烷基,C1-C6烷氧基C1-C6烷基,C1-C6烷氧基C1-C6烷氧基C1-C6烷基,(C1-C6烷基)羰氧基C1-C6烷基,(C1-C6卤代烷基)羰氧基C1-C6烷基,(C1-C6烷氧基)羰基,或(C1-C6烷基)羰基;其中R19的定义同上;R27为氢,C1-C6烷基,C1-C6卤代烷基,C3-C8环烷基,苄基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,氰基C1-C6烷基,C2-C8烷氧基烷基,C2-C8烷硫基烷基,羧基C1-C6烷基,(C1-C8烷氧基)羰基C1-C6烷基,(C1-C6卤代烷氧基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基,(C3-C8环烷氧基)羰基C1-C6烷基,CH2CON(R11)R12,CH2COON(R11)R12,CH(C1-C4烷基)CON(R11)R12,CH(C1-C4烷基)COON(R11)R12,{(C1-C6烷氧基)羰基C1-C6烷基}氧羰基C1-C6烷基,或羟基C1-C6烷基;以及R11,R12,R13,R14,R15,R17,R18,R19,R33,R34,和Z2的定义同上。
在上述本发明化合物的定义中,各取代基的定义举例说明如下:
R1所代表的C1-C3卤代烷基的实例包括三氟甲基和氯二氟甲基。
R2和R3所代表的C1-C3烷基的实例包括甲基,乙基,和异丙基。
R2和R3所代表的C1-C3卤代烷基的实例包括三氯甲基,三氟甲基,二氟甲基,氯二氟甲基,和五氟乙基。
R2和R3所代表的C1-C3烷氧基C1-C3烷基的实例包括甲氧基甲基。
X,Y,和B所代表的卤素的实例包括氯,氟,溴或碘。
R10所代表的C1-C6烷基的实例包括甲基,乙基,异丙基,丙基,异丁基,丁基,叔丁基,戊基,异戊基和叔戊基。
R10所代表的C1-C6卤代烷基的实例包括2-氯乙基,3-氯丙基,和2,2,2-三氟乙基。
R10所代表的C3-C8环烷基的实例包括环丙基,环丁基,环戊基和环己基。
R10所代表的C3-C6链烯基的实例包括烯丙基,1-甲基-2-丙烯基,3-丁烯基,2-丁烯基、3-甲基-2-丁烯基,和2-甲基-3-丁烯基。
R10所代表的C3-C6卤代链烯基的实例包括2-氯-2-丙烯基和3,3-二氯-2-丙烯基。
R10所代表的C3-C6炔基的实例包括丙炔基,1-甲基-2-丙炔基,2-丁炔基,和1,1-二甲基-2-丙炔基。
R10所代表的C3-C6卤代炔基的实例包括4-溴-2-丁炔基。
R10所代表的氰基C1-C6烷基的实例包括氰甲基。
R10所代表的C2-C8烷氧基烷基的实例包括甲氧基甲基,甲氧基乙基,乙氧基甲基,和乙氧基乙基。
R10所代表的C2-C8烷硫基烷基的实例包括甲硫基甲基。
R10所代表的羧基C1-C6烷基的实例包括羧甲基,1-羧基乙基,和2-羧基乙基。
R10所代表的(C1-C8烷氧基)羰基C1-C6烷基的实例包括甲氧羰基甲基,乙氧羰基甲基,丙氧羰基甲基,异丙氧基羰基甲基,丁氧基羰基甲基,异丁氧基羰基甲基,叔丁氧基羰基甲基,戊氧基羰基甲基,异戊氧基羰基甲基,叔戊氧基羰基甲基,1-甲氧羰基乙基,1-乙氧羰基乙基,1-丙氧羰基乙基,1-异丙氧基羰基乙基,1-丁氧羰基乙基,1-异丁氧羰基乙基,1-叔丁氧基羰基乙基,1-戊氧基羰基乙基,1-异戊氧基羰基乙基,和1-叔戊氧基羰基乙基。
R10所代表的(C1-C6卤代烷氧基)羰基C1-C6烷基的实例包括2-氯乙氧基羰基甲基。
R10所代表的{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基的实例包括甲氧基甲氧羰基甲基和1-甲氧基甲氧羰基乙基。
R10所代表的(C3-C8环烷氧基)羰基C1-C6烷基的实例包括环丁氧基羰基甲基,环戊氧基羰基甲基,环己氧基羰基甲基,1-环丁氧基羰基乙基,1-环戊氧基羰基乙基和1-环己氧基羰基乙基。
R10所代表的(C1-C6烷基)羰基C1-C6烷基的实例包括甲基羰基甲基。
R10所代表的(C1-C6卤代烷基)羰基C1-C6烷基的实例包括氯甲基羰基甲基。
R10所代表的{(C1-C4烷氧基)C1-C4烷基}羰基C1-C6烷基的实例包括2-甲氧基乙基羰基甲基。
R10所代表的(C3-C8环烷基)羰基C1-C6烷基的实例包括环戊基羰基甲基。
R10所代表的{(C1-C6烷氧基)羰基C1-C6烷基}氧羰基C1-C6烷基的实例包括(乙氧羰基)甲氧基羰基甲基。
R11和R12所代表的C1-C6烷基的实例包括甲基,乙基,丙基,丁基,异丙基,和异丁基。
R11和R12所代表的C1-C6卤代烷基的实例包括氯乙基和溴乙基。
R11和R12所代表的C3-C6链烯基的实例包括烯丙基,1-甲基-2-丙烯基,和3-丁烯基。
R11和R12所代表的C3-C6炔基的实例包括丙炔基和1-甲基-2-丙炔基。
R11和R12所代表的氰基C1-C6烷基的实例包括氰甲基。
R11和R12所代表的C2-C8烷氧基烷基的实例包括甲氧基甲基和乙氧基乙基。
R11和R12所代表的C2-C8烷硫基烷基的实例包括甲硫基甲基和甲硫基乙基。
R11和R12所代表的羧基C1-C6烷基的实例包括羧甲基和1-羧基乙基。
R11和R12所代表的(C1-C6烷氧基)羰基C1-C6烷基的实例包括甲氧羰基甲基,乙氧羰基甲基,丙氧羰基甲基,异丙氧基羰基甲基,丁氧基羰基甲基,异丁氧基羰基甲基,叔丁氧基羰基甲基,戊氧基羰基甲基,异戊氧基羰基甲基,叔戊氧基羰基甲基,1-甲氧羰基乙基,1-乙氧羰基乙基,1-丙氧羰基乙基,1-异丙氧基羰基乙基,1-丁氧羰基乙基,1-异丁氧羰基甲基,1-叔丁氧基羰基乙基,1-戊氧基羰基乙基,1-异戊氧基羰基乙基,和1-叔戊氧基羰基乙基。
R11和R12所代表的(C3-C8环烷氧基)羰基C1-C6烷基的实例包括环戊氧基羰基甲基。
R11和R12所代表的{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基的实例包括甲氧基甲氧羰基甲基和1-甲氧基甲氧羰基乙基。
R13所代表的C1-C6烷基的实例包括甲基,乙基,丙基,丁基,戊基,异丙基,异丁基,和异戊基。
R13所代表的C1-C6卤代烷基的实例包括2,2,2-三氟乙基。
R13所代表的C3-C8环烷基的实例包括环丙基,环丁基,环戊基和环己基。
R13所代表的C3-C6链烯基的实例包括烯丙基。
R14和R15所代表的C1-C6烷基的实例包括甲基,乙基,丙基,丁基,和异丙基。
R14和R15所代表的C1-C6卤代烷基的实例包括三氟甲基,2,2,2-三氟乙基,2-氯乙基,氯甲基,和三氯甲基。
R14和R15所代表的被甲基或硝基任选取代的苯基的实例包括苯基,对-甲基苯基,2-硝基苯基,3-硝基苯基和4-硝基苯基。
R16所代表的C1-C6烷基的实例包括甲基,乙基,丙基,丁基,戊基,异丙基,异丁基,叔丁基,异戊基,和叔戊基。
R16所代表的C1-C6卤代烷基的实例包括氯甲基,二氯甲基,溴甲基,二溴甲基,1-氯乙基,1,1-二氯乙基,1-溴乙基,和1,1-二溴乙基。
R16所代表的C2-C6链烯基的实例包括乙烯基,烯丙基,1-丙烯基,和1-甲基-2-丙烯基。
R16所代表的C2-C6卤代链烯基的实例包括3,3-二氯-2-丙烯基和3,3-二溴-2-丙烯基。
R16所代表的C2-C6炔基的实例包括乙炔基和2-丁炔基。
R16所代表的C2-C6卤代炔基的实例包括3-溴-2-丙炔基。
R16所代表的C2-C8烷氧基烷基的实例包括甲氧基甲基,乙氧基甲基和异丙氧基甲基。
R16所代表的羟基C1-C6烷基的实例包括羟甲基。
R17和R18所代表的C1-C6烷基的实例包括甲基。
R19所代表的C1-C6烷基的实例包括甲基和乙基。
R33所代表的C1-C6烷基的实例包括甲基和乙基。
R33所代表的C1-C6卤代烷基的实例包括2-氯乙基。
R33所代表的C3-C8环烷基的实例包括环戊基。
R33所代表的C3-C6链烯基的实例包括烯丙基。
R33所代表的C3-C6卤代链烯基的实例包括2-氯-2-丙烯基。
R33所代表的C3-C6炔基的实例包括丙炔基。
R33所代表的C3-C6卤代炔基的实例包括4-氯-2-丁炔基。
R33所代表的氰基C1-C6烷基的实例包括2-氰基乙基和氰基甲基。
R33所代表的(C1-C6烷氧基)羰基C1-C6烷基的实例包括乙氧羰基甲基。
R34所代表的C1-C6烷基的实例包括甲基和乙基。
R4所代表的C1-C3烷基的实例包括甲基。
R5所代表的C1-C6烷基的实例包括甲基,乙基,丙基,丁基,戊基,异丙基,异丁基,和异戊基。
R5所代表的C1-C6卤代烷基的实例包括2-氯乙基,2-溴乙基,3-氯丁基,3-溴丁基,二氟甲基,和溴二氟甲基。
R5所代表的C3-C8环烷基烷基的实例包括环戊基甲基。
R5所代表的C3-C6链烯基的实例包括烯丙基,1-甲基-2-丙烯基,3-丁烯基,2-丁烯基,3-甲基-2-丁烯基,和2-甲基-3-丁烯基。
R5所代表的C3-C6卤代链烯基的实例包括2-氯-2-丙烯基和3,3-二氯-2-丙烯基。
R5所代表的C3-C6炔基的实例包括丙炔基,1-甲基-2-丙炔基,2-丁炔基,和1,1-二甲基-2-丙炔基。
R5所代表的C3-C6卤代炔基的实例包括3-碘-2-丙炔基和3-溴-2-丙炔基。
R5所代表的氰基C1-C6烷基的实例包括氰甲基。
R5所代表的C2-C8烷氧基烷基的实例包括甲氧基甲基,乙氧基甲基和1-甲氧基乙基。
R5所代表的C3-C8烷氧基烷氧基烷基的实例包括甲氧基乙氧基甲基。
R5所代表的羧基C1-C6烷基的实例包括羧甲基,1-羧基乙基,和2-羧基乙基。
R5所代表的(C1-C6烷氧基)羰基C1-C6烷基的实例包括甲氧羰基甲基,乙氧羰基甲基,丙氧羰基甲基,异丙氧基羰基甲基,丁氧基羰基甲基,异丁氧基羰基甲基,叔丁氧基羰基甲基,戊氧基羰基甲基,异戊氧基羰基甲基,叔戊氧基羰基甲基,1-甲氧羰基乙基,1-乙氧羰基乙基,1-丙氧羰基乙基,1-异丙氧基羰基乙基,1-丁氧羰基乙基,1-异丁氧羰基乙基,1-叔丁氧基羰基乙基,1-戊氧基羰基乙基,1-异戊氧基羰基乙基,和1-叔戊氧基羰基乙基。
R5所代表的{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基的实例包括甲氧基甲氧羰基甲基和1-甲氧基甲氧羰基乙基。
R5所代表的(C3-C8环烷氧基)羰基C1-C6烷基的实例包括环丁氧基羰基甲基,环戊氧基羰基甲基,环己氧基羰基甲基,1-环丁氧基羰基乙基,1-环戊氧基羰基乙基和1-环己氧基羰基乙基。
R5所代表的C2-C8烷硫基烷基的实例包括甲硫基甲基。
R5所代表的羟基C1-C6烷基的实例包括羟甲基,羟乙基,和羟丙基。
R6所代表的C1-C6烷基的实例包括甲基和乙基。
R6所代表的C1-C6卤代烷基的实例包括溴甲基,二溴甲基,三溴甲基,1-溴乙基,氯甲基,二氯甲基,和三氯甲基。
R6所代表的羟基C1-C6烷基的实例包括羟甲基。
R6所代表的C1-C6烷氧基C1-C6烷基的实例包括甲氧基甲基,乙氧基甲基,丙氧基甲基,和异丙氧基甲基。
R6所代表的C1-C6烷氧基C1-C6烷氧基C1-C6烷基的实例包括甲氧基甲氧基甲基,甲氧基乙氧基甲基,和乙氧基甲氧基甲基。
R6所代表的(C1-C6烷基)羰氧基C1-C6烷基的实例包括乙酰氧基甲基,乙基羰氧基甲基,和异丙基羰氧基甲基。
R6所代表的(C1-C6卤代烷基)羰氧基C1-C6烷基的实例包括三氟乙酰氧基甲基,氯乙酰氧基甲基,和三氯乙酰氧基甲基。
R6所代表的(C1-C6烷氧基)羰基的实例包括甲氧羰基,乙氧羰基,丙氧羰基,丁氧羰基,戊氧羰基,异丙氧羰基,异丁氧羰基,和异戊氧基羰基。
R6所代表的(C1-C6烷基)羰基的实例包括甲基羰基,乙基羰基,和异丙基羰基。
R7所代表的C1-C6烷基的实例包括甲基。
R8所代表的C1-C6烷基的实例包括甲基和乙基。
R8所代表的C1-C6卤代烷基的实例包括氯甲基,溴甲基和氟甲基。
R8所代表的C1-C6羟基烷基的实例包括羟甲基。
R8所代表的C2-C8烷氧基烷基的实例包括甲氧基甲基,乙氧基甲基,异丙氧基甲基,丁氧基甲基,和异丁氧基甲基。
R8所代表的C3-C10烷氧基烷氧基烷基的实例包括甲氧基甲氧基甲基,甲氧基乙氧基甲基,和乙氧基甲基甲基。
R8所代表的(C1-C5烷基)羰氧基C1-C6烷基的实例包括乙酰氧基甲基,乙基羰氧基甲基,和异丙基羰氧基甲基。
R8所代表的(C1-C6卤代烷基)羰氧基C1-C6烷基的实例包括2-氯乙基羰氧基甲基。
R8所代表的羧基C1-C6烷基的实例包括羧甲基。
R8所代表的(C1-C8)烷氧基羰基的实例包括甲氧羰基,乙氧羰基,丙氧羰基,丁氧羰基,戊氧羰基,异丙氧羰基,异丁氧羰基,和异戊氧基羰基。
R8所代表的(C1-C6卤代烷氧基)羰基的实例包括2-氯乙氧基羰基,2-溴乙氧基羰基,3-氯丁氧基羰基,1-氯-2-丙氧基羰基,1,3-二氯-2-丙氧基羰基,2,2-二氯乙氧基羰基,2,2,2-三氟乙氧基羰基,2,2,2-三氯乙氧基羰基和2,2,2-三溴乙氧基羰基。
R8所代表的(C3-C10环烷氧基)羰基的实例包括环丁氧基羰基,环戊氧基羰基,和环己氧基羰基。
R8所代表的(C3-C8链烯氧基)羰基的实例包括烯丙氧基羰基和3-丁烯氧基羰基。
R8所代表的(C3-C8炔氧基)羰基的实例包括丙炔氧基羰基,3-丁炔氧基羰基和1-甲基-2-丙炔氧基羰基。
R8所代表的(C1-C6烷基)氨基羰基的实例包括甲氨基羰基,乙氨基羰基和丙氨基羰基。
R8所代表的二(C1-C6烷基)氨基羰基的实例包括二甲氨基羰基,二乙氨基羰基,和二异丙基氨基羰基。
R8所代表的(C1-C6烷基)氨基羰氧基C1-C6烷基的实例包括甲氨基羰氧基甲基,乙氨基羰氧基甲基,和丙氨基羰氧基甲基。
R8所代表的二(C1-C6烷基)氨基羰氧基C1-C6烷基的实例包括二甲氨基羰氧基烷基和二乙氨基羰氧基烷基。
本发明化合物中,根据它们的除草活性,优选的取代基如下:
R1优选为被一个或多个氟原子取代的甲基(如三氟甲基或氯二氟甲基),或被一个或多个氟原子取代的乙基(如五氟乙基,),而且更优选三氟甲基;
R2优选为C1-C3烷基,如甲基或乙基,或氢,而且更优选甲基或氢;
R3优选为C1-C3烷基如甲基或乙基,或氢,而且更优选甲基或氢;和
Q优选为[Q-1],[Q-2],[Q-3],或[Q-4]。
根据除草活性,本发明化合物的优选实例是包含上述优选取代基的组合所构成的化合物。
当Q为[Q-1]时,更优选的化合物为其中X为氢或氟,而Y为氯的化合物。这些化合物中,更优选其中B为OR10,SR10,N(R11)R12,NR11(SO2R14),或COOR10的化合物。这些化合物之中,更优选的化合物是:其中R10为C1-C6烷基,C3-C6炔基,(C1-C8烷氧基)羰基C1-C6烷基,或(C3-C8环烷氧基)羰基C1-C6烷基;R11为氢;R12为(C1-C6烷氧基)羰基C1-C6烷基;和R14为C1-C6烷基或C1-C6卤代烷基。
当Q为[Q-2]时,较优选的化合物是其中X为氟或氢;Z1为氧;R4为氢;和n为1。这些化合物之中,更优选其中R5为C3-C6炔基的化合物。
优选化合物的代表性实例包括:
7-氟-6-(5-三氟甲基-3-哒嗪酮-2-基)-4-丙炔基-2H-1,4-苯并噁嗪-3-酮;
7-氟-6-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-4-丙炔基-2H-1,4-苯并噁嗪-3-酮;
6-(5-三氟甲基-3-哒嗪酮-2-基)-4-丙炔基-2H-1,4-苯并噁嗪-3-酮;
6-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-4-丙炔基-2H-1,4-苯并噁嗪-3-酮;
2-(4-氯-2-氟-5-异丙氧基苯基)-4-甲基-5-三氟甲基-哒嗪-3-酮;
2-(4-氯-2-氟-5-甲氧基苯基)-4-甲基-5-三氟甲基-哒嗪-3-酮;
2-(4-氯-2-氟-5-乙氧基苯基)-4-甲基-5-三氟甲基哒嗪-3-酮;
2-(4-氯-2-氟-5-丙炔氧基苯基)-4-甲基-5-三氟甲基哒嗪-3-酮;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸甲酯;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸乙酯;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸丙酯;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸异丙酯;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸丁酯;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸戊酯;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸环戊酯;
2-{2-氯-4  氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基}丙酸乙酯;
2-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基}丙酸甲酯;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯硫基乙酸乙酯;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯硫基乙酸甲酯;
2-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯硫基}丙酸乙酯;
2-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯硫基}丙酸甲酯;
2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯氧基}丙酸甲酯;
2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯氧基}丙酸乙酯;
2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯硫基乙酸乙酯;
2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯硫基乙酸甲酯;
2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯硫基}丙酸乙酯;
2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯硫基}丙酸甲酯;
2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯硫基}丙酸异丙酯;
2-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氨基}丙酸乙酯;
2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯氨基}丙酸乙酯;
N-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯基}甲磺酰胺;
N-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯基}氯甲磺酰胺;
N-{2-氯-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯基}甲磺酰胺;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯甲酸甲酯;
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯甲酸乙酯;
2-氯-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯甲酸甲酯;
2-氯-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯甲酸异丙酯;和
2-(4-氯-2-氟-5-丙炔氧基苯基)-6-甲基-5-三氟甲基-哒嗪-3-酮。
在这些化合物中,依据它们的除草活性,更优选下述化合物:
7-氟-6-(5-三氟甲基-3-哒嗪酮-2-基)-4-丙炔基-2H-1,4-苯并噁嗪-3-酮;
7-氟-6-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-4-丙炔基-2H-1,4-苯并噁嗪-3-酮;
6-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-4-丙炔基-2H-1,4-苯并噁嗪-3-酮;
2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯氧基}丙酸乙酯;和
2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯硫基}丙酸乙酯。
另外,基于它们对作物和有害杂草之间的选择性,更优选的化合物如下:
2-(4-氯-2-氟-5-丙炔氧基苯基)-4-甲基-5-三氟甲基哒嗪-3-酮;2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯氧基乙酸乙酯;
N-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯基}甲磺酰胺;和
2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯甲酸乙酯。
本发明化合物可按照例如下文所描述的方法制备。
(制备方法1)
这一方法为制备包含在本发明化合物中的下式化合物的方法:
Figure C9619770000261
其中R1,R2,R3,和Q1的定义同上,上式化合物通过使下式腙衍生物:其中R1,R3,和Q1的定义同上,与下式化合物反应制备:其中R2的定义同上;R28为C1-C6烷基如甲基或乙基;Ar为任选取代的苯基,如苯基。
反应通常在溶剂中进行。反应温度一般为-20℃-150℃,优选0℃-100℃。反应时间通常为瞬间至72小时。尽管采用1摩尔化合物[5]与1摩尔化合物[4]的比例是理想的,但反应中的各反应物用量仍可依据反应条件而任意改变。
可使用的溶剂的实例包括脂族烃,如己烷,庚烷,粗汽油,环己烷,和石油醚;芳烃,如苯,甲苯,和二甲苯;醚类,如乙醚,二异丙醚,二噁烷,四氢呋喃(THF),和乙二醇二甲醚;硝基化合物,如硝基甲烷和硝基苯;酰胺,如甲酰胺,N,N-二甲基甲酰胺和乙酰胺;叔胺,如吡啶,三乙胺,二异丙基乙胺,N,N-二甲基苯胺,N,N-二乙基苯胺,和N-甲基吗啉;含硫化合物,如二甲亚砜和sulforan;醇,如甲醇,乙醇,乙二醇和异丙醇;水;以及它们的混合物。
反应完成之后,从反应混合物中蒸去溶剂,并层析所得残留物;或者将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后如果需要的话,再利用诸如色谱法或重结晶之类技术进行后续纯化。从而得到所需的本发明化合物。
上述反应通过下式中间化合物来进行:
Figure C9619770000271
其中R1,R2,R3,R28,和Q1的定义同上。
此制备方法也可通过分离化合物[6],尔后再分子内使化合物[6]环化来进行。环合通常是在溶剂中进行。反应温度一般在-20℃至150℃范围内,优选50℃-150℃。反应时间通常为瞬间至72小时。
可使用的溶剂的实例包括脂族烃,如己烷,庚烷,粗汽油,环己烷,和石油醚;芳烃,如苯,甲苯,和二甲苯;卤代烃,如氯仿,四氯化碳,二氯甲烷,二氯乙烷,氯苯和二氯苯;醚类,如乙醚,二异丙醚,二噁烷,四氢呋喃,和乙二醇二甲醚;酮,如丙酮,甲乙酮,甲基异丁基酮,异佛尔酮,和环己酮;酯,如甲酸乙酯,乙酸乙酯,乙酸丁酯,和碳酸二乙酯;硝基化合物,如硝基甲烷和硝基苯;腈类,如乙腈和异丁腈;酰胺,如甲酰胺,N,N-二甲基甲酰胺和乙酰胺;叔胺,如吡啶,三乙胺,二异丙基乙胺,N,N-二甲基苯胺,N,N-二乙基苯胺,和N-甲基吗啉;含硫化合物如二甲亚砜和sulforan;脂肪酸,如甲酸,乙酸,和丙酸;醇如甲醇,乙醇,乙二醇和异丙醇;水;以及它们的混合物。
作为反应催化剂,可使用酸,如硫酸,或碱,如甲醇钠。
(制备方法2)
这一制备方法的流程如下:
Figure C9619770000281
其中R51为非氢的取代基,它包括在R5的定义之内;R1,R2,R3,R4,和X的定义同上;R22为C1-C6烷基;以及D为氯,溴,碘,甲磺酰氧基,三氟甲磺酰氧基,或对-甲苯磺酰氧基。
由化合物[7]制备化合物[8]的方法
化合物[8]可通过在溶剂中使化合物[7]和硝化剂反应制备。
硝化剂:硝酸等
硝化剂的用量:每摩尔化合物[7]为1-10摩尔
溶剂:硫酸
温度:-10℃至室温
时间:瞬间至24小时。
由化合物[8]制备化合物[9]的方法
化合物[9]可按下述制备:在氟化钾存在下,在溶剂中使化合物[8]和下式化合物反应:其中R4和R22的定义同上。
化合物[12]用量:每摩尔化合物[8]为1-50摩尔
氟化钾用量:每摩尔化合物[8]为1-50摩尔
溶剂:1,4-二噁烷等
温度:室温至加热回流温度
时间:瞬间-96小时。
由化合物[9]制备化合物[10]的方法
化合物[10]可通过在酸存在下,在溶剂中用铁粉等还原剂还原化合物[9]制备。
铁粉用量;每摩尔化合物[9]为3摩尔至过量
酸:乙酸等
酸用量:1-10摩尔
溶剂:水,乙酸乙酯等
温度:室温至加热回流温度
时间:瞬间-24小时。
由化合物[10]制备化合物[11]的方法
化合物[11]可通过使化合物[10]和下式化合物反应制备:
R51-D[13]
其中R51和D的定义同上。
此反应通常是在碱存在下在溶剂中进行。反应温度一般为-20℃150℃,优选0℃-50℃。反应时间一般为瞬间至48小时。反应中所用各试剂的量相对于每摩尔化合物[10]来说,通常为1-3摩尔化合物[13]和1-2摩尔碱。
所用碱的实例包括无机碱如氢化钠,氢化钾,氢氧化钠,氢氧化钾,碳酸钾,和碳酸钠;和有机碱如三乙胺,二异丙基乙胺,吡啶,4-二甲氨基吡啶,N,N-二甲基苯胺,和N,N-二乙基苯胺。
可使用的溶剂的实例包括脂族烃,如己烷,庚烷,粗汽油,环己烷,和石油醚;芳烃,如苯,甲苯,和二甲苯;卤代烃,如氯苯和二氯苯;醚类,如乙醚,二异丙醚,二噁烷,四氢呋喃,和乙二醇二甲醚;硝基化合物,如硝基苯;酰胺,如甲酰胺,N,N-二甲基甲酰胺和乙酰胺;叔胺,如吡啶,三乙胺,二异丙基乙胺,N,N-二甲基苯胺,N,N-二乙基苯胺,和N-甲基吗啉;以及它们的混合物。
反应完成之后,如果需要的话,将反应混合物倾入水中,再进行常规后处理,如用有机溶剂提取并浓缩,随后如果需要的话,再通过诸如柱层析或重结晶之类技术进行后续纯化。从而可得到本发明化合物[11]。
上述化合物[9]也可以按照下述流程制备:
Figure C9619770000301
其中R1,R2,R3,R4,R22,和X的定义同上。
由化合物[14]制备化合物[15]的方法
化合物[15]可按下述制备:在碱存在下,使化合物[14]与下式化合物在溶剂中反应:
其中R4和R22的定义同上。
化合物[17]用量:每摩尔化合物[14]为1-2摩尔
碱:氢化钠,碳酸钠等
碱用量:每摩尔化合物[14]为1-2摩尔
溶剂:1,4-二噁烷,N,N-二甲基甲酰胺等
温度:0℃-100℃
时间:瞬间-24小时。
由化合物[15]制备化合物[9]的方法
化合物[9]可通过在溶剂中使化合物[15]和硝化剂反应制备。
硝化剂:硝酸等
硝化剂用量:每摩尔化合物[15]为1-10摩尔
溶剂:硫酸,乙酸等
温度:-10℃至室温
时间:瞬间至24小时。
由化合物[14]制备化合物[16]的方法
化合物[16]可通过在溶剂中使化合物[14]和硝化剂反应制备。
硝化剂:硝酸等
硝化剂用量:每摩尔化合物[14]为1-10摩尔
溶剂:硫酸,乙酸等
温度:-10℃至室温
时间:瞬间至24小时。
由化合物[16]制备化合物[9]的方法
化合物[9]可按如下所述制备:在碱存在下,在溶剂中使化合物[16]和化合物[17]反应。
化合物[17]用量:每摩尔化合物[16]为1-2摩尔
碱:氢化钠,碳酸钾等
碱用量:每摩尔化合物[16]为1-2摩尔
溶剂:1,4-二噁烷,N,N-二甲基甲酰胺等
温度:0℃-100℃
时间:瞬间-24小时。
(制备方法3)
此制备方法的反应流程如下:
Figure C9619770000321
其中X,R1,R2,R3,R51,和D的定义同上。
由化合物[18]制备化合物[19]的方法
化合物[19]可通过在酸存在下在溶剂中使化合物[18]和铁粉等还原剂反应制备。
铁粉用量:每摩尔化合物[18]为3摩尔至过量
酸:乙酸等
酸用量:每摩尔化合物[18]为1-10摩尔
溶剂:水,乙酸乙酯等
温度:室温至加热回流温度
时间:瞬间至24小时。
由化合物[20]制备化合物[21]的方法
化合物[20]可按如下所述制备:使化合物[19]在溶剂中与硫氰酸钠,硫氰酸钾等反应,然后再在溶剂中与溴或氯反应。
硫氰酸钠,硫氰酸钾等的用量:每摩尔化合物[19]为1-10摩尔
溴或氯的用量:每摩尔化合物[19]为1-10摩尔
溶剂:盐酸水溶液,乙酸水溶液,硫酸水溶液等
温度:0℃-50℃
时间:瞬间-150小时。
由化合物[20]制备化合物[21]的方法
化合物[21]的制备如下:1)使化合物[20]在溶剂中与亚硝酸钠,亚硝酸钾等反应,然后2)在乙酸溶液中加热。
<反应1>
亚硝酸钠,亚硝酸钾等的用量:每摩尔化合物[20]为1-2摩尔
溶剂:盐酸水溶液或硫酸水溶液
温度;-10℃至10℃
时间;瞬间-5小时。
<反应2>
酸溶液:盐酸水溶液,硫酸水溶液等
温度:70℃至加热回流温度
时间:瞬间-24小时。
由化合物[21]制备化合物[22]的方法
化合物[22]可通过在碱存在下,在溶剂中使化合物[21]和化合物[13]制备。
化合物[13]的用量:每摩尔化合物[21]为1-3摩尔
碱:氢化钠,碳酸钾等
碱用量:每摩尔化合物[21]为1-2摩尔
溶剂:1,4-二噁烷,N,N-二甲基甲酰胺等
温度:0℃-100℃
时间:瞬间-48小时。
(制备方法4)
这一制备方法的流程如下:
Figure C9619770000341
其中X,R1,R2,R3和R5的定义同上。
由化合物[23]制备化合物[24]的方法
化合物[24]可通过在酸存在下,在溶剂中用铁粉等还原剂还原化合物[23]制备。
铁粉用量:每摩尔化合物[23]为3摩尔至过量
酸:乙酸等
酸用量:每摩尔化合物[23]为1-10摩尔
溶剂:水,乙酸乙酯等
温度:室温至加热回流温度
时间:瞬间-24小时。
由化合物[24]制备化合物[25]的方法
化合物[25]的制备如下:1)在溶剂中使化合物[24]与亚硝酸盐反应,形成重氮盐,随后2)升高温度使重氮盐在溶剂中进行环合。
<反应1>
亚硝酸盐:亚硝酸钠,亚硝酸钾等
亚硝酸盐的用量;每摩尔化合物[24]为1-2摩尔
溶剂:盐酸水溶液,硫酸水溶液等
温度:-10℃至10℃
时间:瞬间-5小时。
<反应2>
溶剂:盐酸水溶液,硫酸水溶液等
温度:室温-80℃
时间:瞬间-24小时。
(制备方法5)
这一制备方法的流程如下:
Figure C9619770000351
其中Y1为非硝基的取代基,它包括在Y的定义内;R101为非氢的取代基,它包括在R10的定义内;而X,R1,R2,和R3的定义同上。
由化合物[26]制备化合物[27]的方法
化合物[27]可通过向化合物[26]/溶剂中加入硝酸制备(参见OrganicSynthesis Collective,Vol.1,p.372)。
反应温度一般在0℃-100℃范围内。反应时间通常为瞬间至24小时。尽管在反应中采用1摩尔硝酸化合物与1摩尔化合物[26]的比例是理想的,但各反应物用量仍可根据反应条件而随意改变。
可使用的溶剂的实例包括酸类溶剂(如硫酸)。
由化合物[27]制备化合物[28]的方法
化合物[28]可通过在溶剂中还原化合物[27]来制备(参见OrganicSynthesis Collective,Vol.2,p.471,和ibid.,Vol.5,p.829)。
例如,此方法可通过向乙酸、铁粉和水的混合物内加入纯净形式或溶在溶剂(如乙酸乙酯)中的化合物[27]来进行。反应温度通常为0℃-100℃。反应时间一般为瞬间-24小时。
反应完成之后,过滤反应混合物收集结晶(如果需要的话,可加水沉淀结晶),或者将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后,如果需要的话,用诸如柱层析或重结晶之类技术进行后续纯化。从而可以分离出所需产物。
由化合物[28]制备化合物[29]的方法
化合物[29]的制备如下:1)在溶剂中使化合物[28]和亚硝酸盐反应,和2)随后在酸性溶剂中加热。
<反应1>
亚硝酸盐:亚硝酸钠,亚硝酸钾等
亚硝酸盐用量:每摩尔化合物[28]为1-2摩尔
溶剂:盐酸水溶液,硫酸水溶液等
温度:-10℃至10℃
时间:瞬间-5小时。
<反应2>
酸性溶剂:盐酸水溶液或硫酸水溶液
温度:70℃至加热回流温度
时间:瞬间-24小时。
由化合物[29]制备化合物[30]的方法
化合物[30]可按如下所述制备:在碱存在下,使化合物[29]在溶剂中与下式化合物反应:
R101-D                                        [31]
其中R101和D的定义同上。
反应通常在溶剂中进行。反应温度通常为-20℃至150℃,优选0℃-100℃。反应时间通常为瞬间至72小时。尽管在反应中采用1摩尔化合物[31]和1摩尔碱与1摩尔化合物[29]的比例是理想的,但各反应物用量仍可依据反应条件而随意改变。
可使用的碱的实例包括无机碱和有机碱,如碳酸钾,氢氧化钠,和氢化钠。
可使用的溶剂的实例包括脂族烃,如己烷,庚烷,粗汽油,环己烷,和石油醚;芳烃,如苯,甲苯,和二甲苯;卤代烃,如氯仿,四氯化碳,二氯甲烷,二氯乙烷,氯苯和二氯苯;醚类,如乙醚,二异丙醚,二噁烷,四氢呋喃,和乙二醇二甲醚;酮,如丙酮,甲乙酮,甲基异丁基酮,异佛尔酮,和环己酮;酯,如甲酸乙酯,乙酸乙酯,乙酸丁酯,和碳酸二乙酯;硝基化合物,如硝基甲烷和硝基苯;腈类,如乙腈和异丁腈;酰胺,如甲酰胺,N,N-二甲基甲酰胺和乙酰胺;叔胺,如吡啶,三乙胺,二异丙基乙胺,N,N-二甲基苯胺,N,N-二乙基苯胺,和N-甲基吗啉;含硫化合物如二甲亚砜和sulforan;以及它们的混合物。
反应完成之后,过滤反应混合物收集结晶(如果需要的话,可加水沉淀结晶),或者将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后,如果需要的话,用诸如柱层析或重结晶之类技术进行后续纯化。从而可以分离出所需产物。
(制备方法6)
这一制备方法的流程如下:
其中R23和R24独立地为非氢的取代基,此取代基包括在R11和R12的定义内;或COR13,SO2R14,SO2R15,或COOR10,其中R10,R13,R14和R15的定义同上;X,Y1,R1,R2,和R3的定义同上。
由化合物[28]制备化合物[32]的方法
化合物[32]的制备如下:使化合物[28 与式[34]化合物反应:
R20-D                                        [34]
其中R20为非氢的取代基,它包括在R11或R12的定义内;或COR13,SO2R14,SO2R15,或COOR10,其中R10,R13,R14和R15的定义同上;且D定义同上;
或与式[35]化合物反应:
(R21)2O                                         [35]
其中R21为COR13,SO2R14,SO2R15,或COOR10,其中R10,R13,R14和R15的定义同上;
上述反应一般是在碱存在下且通常是在溶剂中进行。
反应温度一般为-20℃至200℃,优选0℃-180℃。反应时间通常为瞬间至72小时。尽管在反应中采用1摩尔化合物[34]或[35]与1摩尔化合物[28]的比例是理想的,但各反应物用量仍可依据反应条件而随意改变。
可使用的碱的实例包括有机碱如吡啶和三乙胺,和无机碱。
可使用的溶剂的实例包括脂族烃,如己烷,庚烷,粗汽油,环己烷,和石油醚;芳烃,如苯,甲苯,和二甲苯;卤代烃,如氯仿,四氯化碳,二氯甲烷,二氯乙烷,氯苯和二氯苯;醚类,如乙醚,二异丙醚,二噁烷,四氢呋喃,和乙二醇二甲醚;酮,如丙酮,甲乙酮,甲基异丁基酮,异佛尔酮,和环己酮;酯,如甲酸乙酯,乙酸乙酯,乙酸丁酯,和碳酸二乙酯;硝基化合物,如硝基甲烷和硝基苯;腈类,如乙腈和异丁腈;酰胺,如甲酰胺,N,N-二甲基甲酰胺和乙酰胺;叔胺,如吡啶,三乙胺,二异丙基乙胺,N,N-二甲基苯胺,N,N-二乙基苯胺,和N-甲基吗啉;含硫化合物如二甲亚砜和sulforan;以及它们的混合物。
反应完成之后,过滤反应混合物收集沉淀出的结晶,或者将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后,如果需要的话,用诸如柱层析或重结晶之类技术进行后续纯化。从而可以分离出所需产物。
由化合物[32]制备化合物[33]的方法
化合物[33]可通过使化合物[32]和化合物[34]或[35]反应制备。此制备方法以由化合物[28]制备化合物[32]的制备方法为基础。
(制备方法7)
这一制备方法的流程如下:其中X,Y,R1,R2,R3,R10,R11,和R12的定义同上。
由化合物[36]制备化合物[37]的方法
化合物[37]可通过在无任何溶剂存在下或在溶剂中使化合物[36]和氯磺酸反应来制备。
氯磺酸用量:每摩尔化合物[36]为1摩尔至过量
溶剂:硫酸
温度:0℃-70℃
时间:瞬间-24小时
(参见Org.Syn.Coll.,Vol. 1,8(1941))
由化合物[37]制备化合物[38]的方法
化合物[38]可按如下所述制备:在碱存在下,在无任何溶剂或有溶剂存在的条件下,使化合物[37]和式[40]化合物反应:
R10-OH
其中R10的定义同上。                          [40]
化合物[24]的用量:每摩尔化合物[37]为1摩尔至过量
碱:有机碱如三乙胺或无机碱如碳酸钾
碱用量:每摩尔化合物[37]为1-2摩尔
溶剂:N,N-二甲基甲酰胺,1,4-二噁烷等
温度:0℃-100℃
时间:瞬间-24小时
由化合物[37]制备化合物[39]的方法
化合物[39]的制备如下:在有或无碱存在下,在无任何溶剂的条件下或在溶剂中使化合物[37]和下式化合物反应:
R11R12NH[41]
其中R11和R12的定义同上。
化合物[41]用量:每摩尔化合物[37]为1摩尔至过量
碱:有机碱如三乙胺或无机碱如碳酸钾
碱用量:每摩尔化合物[37]为1-2摩尔
溶剂:1,4-二噁烷,N,N-二甲基甲酰胺等
温度:0℃-100℃
时间:瞬间-24小时
(制备方法8)
此制备方法的反应流程如下:
其中X,Y,R1,R2,R3,R11,R12,R17,R18和R22的定义同上。
由化合物[42]制备化合物[43]的方法
化合物[43]可按照JP-A5-294920/1993,pp.15-16中描述的方法由化合物[42]制得。
由化合物[43]制备化合物[44]的方法
化合物[44]可按如下所述制备:在溶剂中使化合物[43]与下面式[45]化合物或式[46]化合物反应,而且当使用化合物[46]时,反应是在碱存在下进行:
(C6H5)3P=CR18COOR22                          [45]
(C2H5O)2P(O)CHR18COOR22                       [46]其中R18和R22的定义同上。
化合物[45]或[46]的用量:每摩尔化合物[43]为1-2摩尔
溶剂:四氢呋喃,甲苯等
碱:氢化钠等
碱用量:每摩尔化合物[43]为1-2摩尔
温度:0℃-50℃
时间:瞬间-24小时
由化合物[44]制备化合物[45]的方法
化合物[45]可经化合物[44]与化合物]41]反应制备。
(制备方法9)
这一制备方法的流程如下:
Figure C9619770000411
其中W2为氯或溴;而X,Y,R1,R2,R3和R13的定义则同上。
反应条件见USP 5,208,212中所述。
此制备可按如下所述完成:在氢氯酸,氢溴酸等溶液中,采用常规方法转化化合物[48]形成重氮盐,随后在铜盐(如氯化铜(II)或溴化铜(II))存在下,在溶剂如乙腈中,使该重氮盐与下式化合物反应:
CH2=CHCO2R13                            [50]
其中R13定义同上。
反应温度通常为-20℃至150℃,优选为0℃至60℃。反应时间一般为瞬间至72小时。
反应完成之后,过滤反应混合物收集结晶(如果需要的话,可加水沉淀结晶),或者将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后,如果需要的话,用诸如柱层析或重结晶之类技术进行后续纯化。从而可以分离出所需产物。
(制备方法10)
此制备方法的反应流程如下:其中W3为溴或碘;且X,Y1,R1,R2,R3,和R13的定义同上。
由化合物[28]制备化合物[51]的方法
化合物[51]可按如下所述制备:1)在溶剂中由化合物[28]形成重氮盐,2)随后再在溶剂中与碘化钾或溴化铜(I)反应。
<反应1>
重氮化剂:亚硝酸钠,亚硝酸钾等
重氮化剂的用量;每摩尔化合物[28]为1-2摩尔
溶剂:氢溴酸水溶液,硫酸水溶液等
温度:-10℃至10℃
时间:瞬间-5小时。
<反应2>
碘化钾或溴化铜(I)的用量:每摩尔化合物[28]为1摩尔至过量
溶剂:氢溴酸水溶液,硫酸水溶液等
温度:0℃-80℃
时间:瞬间-24小时。
(参见Org.Syn.Coll.,Vol. 2,604(1943),和ibid.,Vol. 1,136(1941))
由化合物[51]制备化合物[52]的方法
化合物[52]的制备如下:在一氧化碳气氛中,在过渡金属催化剂和碱存在下,使化合物[51]在溶剂中与下式化合物反应:
   R13-OH     [53]
其中R13的定义同上。
催化剂:PdCl2(PPh3)2
催化剂用量:每摩尔化合物[51]为催化量至0.5摩尔
化合物[53]用量:每摩尔化合物[51]为1摩尔至过量
碱:有机碱如二乙胺
碱用量:每摩尔化合物[51]为1-2摩尔
溶剂:N,N-二甲基甲酰胺等
一氧化碳压力:1-150atm.
温度:0℃-100℃
时间:瞬间-72小时
(参见 日本化学会会誌(Bull.Chem.Soc.Jpn.), 48(7)2075(1975))
(制备方法11)
这一制备方法的流程如下:其中X,Y,R1,R2,R3,和R19的定义同上。
化合物[55]可按如下所述制备:在酸性溶剂(如硫酸)中水解化合物[54],或在酸(如三溴化硼)存在下,在溶剂,如二氯甲烷中水解化合物[54]。
反应温度通常为-20℃至150℃,优选0℃至100℃。反应时间一般为瞬间至72小时。
尽管在反应中采用1摩尔酸与1摩尔化合物[54]的比例是理想的,但各反应物用量仍可依据反应条件而随意改变。
反应完成之后,过滤反应混合物收集结晶(如果需要的话,可加水沉淀结晶),或者将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后,如果需要的话,用诸如柱层析或重结晶之类技术进行后续纯化。从而可以分离出所需产物。
(制备方法12)
这一制备方法的流程如下:其中X,Y,R1,R2,R3,Z2和R17的定义同上;Z3为氧或硫;R25为氢或C1-C5烷基,且R26为C1-C6烷基,C3-C6链烯基,或C3-C6炔基。
化合物[57]可通过在有或无催化剂存在下,通常是在溶剂中使化合物[56[和下式化合物反应来制备:
R26Z3H    [58]其中R26和Z3的定义同上。
尽管在反应中采用1摩尔化合物[58]与1摩尔化合物[56]的比例是理想的,但化合物[58]的用量仍可依据反应条件而随意改变。
可使用的催化剂的实例包括对-甲苯磺酸。可使用的溶剂的实例包括甲苯,二甲苯等,或化合物[56]。
反应温度通常为0℃至200℃,优选50℃至150℃。反应时间一般为瞬间至72小时。
反应完成之后,过滤反应混合物收集结晶(如果需要的话,可加水沉淀结晶),或者将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后,如果需要的话,用诸如柱层析或重结晶之类技术进行后续纯化。从而可以分离出所需产物。
(制备方法13)
这一制备方法的流程如下:
Figure C9619770000451
其中R61为非甲基的取代基,它包括在R6的定义内,而X,Y,R1,R2,和R3的定义则同上。
由化合物[55]制备化合物[59]的方法
化合物[59]可通过在碱存在下,在溶剂中使化合物[55]与化合物2,3-二氯丙烯反应制备。
2,3-二氯丙烯的用量:每摩尔化合物[55]为1-3摩尔
碱:无机碱如碳酸钾
碱用量:每摩尔化合物[55]为1-2摩尔
溶剂:N,N-二甲基甲酰胺等
温度:0℃-70℃
时间:瞬间-24小时
由化合物[59]制备化合物[60]的方法
化合物[60]可通过在溶剂中加热化合物[59]来制备。
溶剂:N,N-二甲基甲酰胺,N,N-二甲基苯胺,N,N-二乙基苯胺,对-二异丙基苯等
温度:70℃-200℃
时间:瞬间-24小时
由化合物[60]制备化合物[61]的方法
化合物[61]可以化合物[62]为原料按照USP 5,308,829,2-11栏中描述的方法制备,其中苯并呋喃环的2位上的甲基被其它取代基代替。
(制备方法14)
此制备方法的流程如下:
Figure C9619770000461
其中X,Y,R1,R2,R3,和R7的定义同上。
由化合物[55]制备化合物[62]的方法
化合物[62]可制备如下:在碱存在下,在溶剂中使化合物[55]和式[65]化合物反应:
CH2=CR7CH2W2                      [65]
其中W2和R7的定义同上。
化合物[65]用量:每摩尔化合物[55]为1-5摩尔
碱:无机碱如碳酸钾
碱用量:每摩尔化合物[55]为1-2摩尔
溶剂:N,N-二甲基甲酰胺,1,4-二噁烷等
温度:0℃-70℃
时间:瞬间-24小时
由化合物[62]制备化合物[63]的方法
化合物[63]可通过在溶剂中加热化合物[62]来制备。
溶剂:N,N-二甲基甲苯胺,N,N-二乙基苯胺,对-二异丙基苯等
温度:100℃-200℃
小时:瞬间-24小时
由化合物[63]制备化合物[64]的方法
化合物[64]可通过在酸存在下在溶剂中加热化合物[63]制备。
酸:有机酸如对-甲苯磺酸;和无机酸如硫酸
酸用量:每摩尔化合物[63]为催化量至1摩尔
溶剂:甲苯,二甲苯等
温度:100℃-250℃
时间:瞬间-24小时
(制备方法15)
这一制备方法的流程如下:
Figure C9619770000471
其中R81为非甲基和羟甲基的取代基,它包括在R8的定义之内;而X,Y,R1,R2,R3,和R7的定义则同上。
由化合物[63]制备化合物[66]的方法
化合物[66]可通过在溶剂中使化合物[63]和过酸反应制备。
过酸:间-氯过苯甲酸或过乙酸
过酸用量:每摩尔化合物[63]为1摩尔至过量
溶剂:卤代烃如二氯甲烷;和有机酸如乙酸
温度:-20℃至室温
时间:瞬间-24小时
由化合物[66]制备化合物[67]的方法
化合物[67]可通过在碱存在下在溶剂中反应化合物[66]制备。
碱:碳酸钾等
碱用量:每摩尔化合物[66]为1-2摩尔
溶剂:甲醇,乙醇等
温度:0℃-50℃
时间:瞬间-5小时
由化合物[67]制备化合物[68]的方法
化合物[68]可以化合物[67]为原料按照USP 5,411,935,第5-10栏中描述的方法制备,其中二氢苯并呋喃环的2位上的羟烷基被其它取代基代替。
(制备方法16)
此制备方法的流程如下:
Figure C9619770000491
其中W1为卤素,优选氯;R32为氢或C1-C5烷基;且X,Y,Z2,R1,R2,R3,R11,R12,R33和R34的定义同上。
由化合物[42]制备化合物[69]的方法
化合物[69]可采用常规方法在溶剂中使化合物[42]和卤化剂(如亚硫酰氯)反应制备。
由化合物[69]制备化合物[70]的方法
化合物[70]可按如下所述制备:使化合物[69]与下式化合物反应:
Figure C9619770000501
其中M_为碱金属阳离子,优选锂阳离子或钠阳离子;且R19,R22,和R32的定义同上,
得到下式化合物:其中X,Y,R1,R2,R3,R19,R22和R32的定义同上,
然后水解并将化合物[75]脱羧基化。
头一反应通常是在溶剂中进行。反应温度一般为-20℃至50℃,优选室温。反应时间通常为瞬间至72小时。
可使用的溶剂的实例包括脂族烃如己烷,庚烷,粗汽油,环己烷,和石油醚;醚,如二乙醚,二异丙醚,二噁烷,四氢呋喃,和乙二醇二甲醚;酰胺,如甲酰胺,N,N-二甲基甲酰胺,和乙酰胺;含硫化合物,如二甲亚砜和sulforane;以及它们的混合物。
后一反应是在硫酸、氢溴酸等存在下,在溶剂如低级羧(如乙酸)中,或在无任何溶剂条件下进行。反应温度通常为80℃至140℃,优选100℃至120℃。反应时间一般为瞬间至72小时。
由化合物[70]制备化合物[71]的方法
化合物[71]可通过使化合物[70]和式[76]化合物反应制备:
H2N-O-R33                       [76]其中R33的定义同上。
此反应是在低级醇如甲醇,乙醇或异丙醇中,或在这类低级醇和水的混合溶液中进行。反应温度为0℃至80℃。反应时间为瞬间至72小时。
化合物[76]可以游离碱形式或酸加成盐(如盐酸盐或硫酸盐)形式使用。
上述反应中,也可以加入碱性催化剂来进行,如有机碱(如吡啶);碱金属碳酸盐(如碳酸钠,碳酸钾等);碱金属碳酸氢盐;或碱土金属碳酸盐。
化合物[71]还可以按如下所述制备:在碱存在下,通常在溶剂中使下式化合物:
Figure C9619770000511
其中X,Y,R1,R2,R3,和R32的定义同上,与式[78]的化合物反应:
R33-D                  [78]
其中R33和D的定义同上。
可使用的碱的实例包括碱金属醇盐和碱金属氢化物(如氢化钠)。
尽管在反应中采用约1摩尔化合物[78]和1-2摩尔碱与1摩尔化合物[77]的比例是理想的,但各反应物的用量仍可依据反应条件而随意改变。
可使用的溶剂的实例包括醚,如二乙醚,二异丙醚,二噁烷,四氢呋喃,和乙二醇二甲醚;酰胺,如甲酰胺,N,N-二甲基甲酰胺,和乙酰胺;含硫化合物,如二甲亚砜和sulforane;醇,如甲醇,乙醇,乙二醇和异丙醇;以及它们的混合物。
上述反应的反应温度通常为-10℃至100℃,优选0℃至80℃。反应时间一般为瞬间至72小时。
由化合物[70]制备化合物[72]的方法
化合物[72]可通过使化合物[70]和下式化合物反应制备:其中R11和R12的定义同上。
反应在低级醇(如甲醇,乙醇或异丙醇),或低级醇和水的混合溶液中进行。反应温度为0℃至80℃。反应时间为瞬间至72小时。
化合物[79]可以游离碱形式或其酸加成盐(如盐酸盐或硫酸盐)形式使用。
上述反应中也可以加入碱性催化剂来进行,如有机碱(如吡啶),碱金属碳酸盐(如碳酸钠,碳酸钾等);碱金属碳酸氢盐;或碱土金属碳酸盐。
由化合物[70]制备化合物[73]的方法
化合物[73]的制备如下:通常在催化量至过量酸(如对-甲苯磺酸,盐酸或硫酸)存在下,在有机溶剂(如苯或氯仿)中使化合物[70]和下式化合物反应:
R34-Z2H                         [80]
其中Z2和R34的定义同上。
反应温度为-30℃至反应混合物的沸点。反应时间为瞬间至72小时。
(制备方法17)
这一制备方法的流程如下:
Figure C9619770000531
其中Q1和R1的定义同上。
化合物[82]通过在溶剂中使化合物[81]和下式化合物反应制备:
Figure C9619770000532
其中R19和R22的定义同上。
反应温度通常在30℃至120℃范围内,优选40℃至80℃。反应时间一般为5至72小时。尽管在反应中采用1摩尔化合物[83]与1摩尔化合物[81]的比例是理想的,但各反应物的用量仍可依据反应条件而改变。
可使用的溶剂的实例包括叔胺如三乙胺。
反应完成之后,从反应混合物中蒸除溶剂,并将残留物进行色谱纯化,或者将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后,如果需要的话,用柱色谱或重结晶等方法进行后续纯化。从而可以分离出所需产物。
(制备方法18)
这一制备方法的流程如下:其中B3为OR35,SR35,COOR35,COR16,或CR17=CR18COR16(其中R35为(C1-C6烷基)羰基C1-C6烷基(C1-C6卤代烷基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷基}羰基C1-C6烷基,或(C3-C8环烷基)羰基C1-C6烷基;且R16,R17,和R18的定义同上);B4为用醇保护B3中的酮或醛部分而衍生得到的取代基;和X,Y,R1,R2,和R3的定义同上。
由化合物[99]制备化合物[100]的方法
化合物[100]按与制备方法1中所述相同的方式制备,其中只是用化合物[99]代替化合物[4]。
由化合物[100]制备化合物[101]的方法
化合物[101]通过用常规方法使化合物[100]的缩酮或缩醛部分脱保护制备。
化合物[99]可用与下文制备化合物[4]的方法中所述相同的方式制备,其中只是下述式[102]化合物中的取代基B3的酮或醛部分被醇(如甲醇)保护:其中X,Y,和B3的定义同上,得到式[103]化合物:其中X,Y和B4的定义同上,并用化合物[103]代替化合物[91],如下所述。
在本发明化合物的制备方法1中用作起始化合物之一的化合物[5]可以从市场上购得,或者可以按照例如Jikken Kagaku Kouza(MaruzenK.K.),4th ed.,Vol. 24,pp.259-260中描述的方法制备。
制备方法1中所用的另一起始物质化合物[4]可按如下所述制备:在碱存在下,使下式化合物:其中R1和R3的定义同上;V为碘,溴,或氯,
与水反应,得到式[85]化合物(此反应以下称作反应1)其中R1和R3的定义同上;
然后使化合物[85]与下式化合物反应(以下称作反应2):
Q1-NHNH2  [86]其中Q1的定义同上。
化合物[85]也可以其水合物或缩醛衍生物形式在水或醇中进行反应。
反应1通常在溶剂中进行。反应温度一般在20℃至100℃范围内。反应时间为瞬间至24小时。尽管在反应中采用2摩尔水和2摩尔碱与1摩尔化合物[84]的比例是理想的,但如果需要的话,各反应物的用量可以改变。
可使用的碱的实例包括有机碱和无机碱如乙酸钠和乙酸钾。
可使用的溶剂的实例包括脂族烃,如己烷,庚烷,粗汽油,环己烷,和石油醚;芳烃如苯,甲苯,和二甲苯;卤代烃,如氯苯和二氯苯;醚类,如乙醚,二异丙醚,二噁烷,四氢呋喃,和乙二醇二甲醚;酯,如甲酸乙酯,乙酸乙酯,乙酸丁酯,和碳酸二乙酯;硝基化合物,如硝基甲烷和硝基苯;腈类,如乙腈和异丁腈;酰胺,如N,N-二甲基甲酰胺;叔胺,如吡啶,三乙胺,二异丙基乙胺,N,N-二甲基苯胺,N,N-二乙基苯胺,和N-甲基吗啉;含硫化合物,如二甲亚砜和sulforan;醇,如甲醇,乙醇,乙二醇,和异丙醇;水;以及它们的混合物。
反应2通常是在溶剂中进行。反应温度一般为-20℃至200℃。反应时间往往为瞬间至72小时。尽管在反应中采用1摩尔化合物[86]与1摩尔化合物[84]的比例是理想的,但各反应物的用量仍可依据反应条件而任意改变。如果需要的话,也可以使用化合物[86]的盐酸盐或硫酸盐。
可使用的溶剂的实例包括脂族烃,如己烷,庚烷,粗汽油,环己烷,和石油醚;芳烃,如苯,甲苯,和二甲苯;卤代烃,如氯仿,四氯化碳,二氯甲烷,二氯乙烷,氯苯和二氯苯;醚类,如乙醚,二异丙醚,二噁烷,四氢呋喃,和乙二醇二甲醚;酯,如甲酸乙酯,乙酸乙酯,乙酸丁酯,和碳酸二乙酯;硝基化合物,如硝基甲烷和硝基苯;腈类,如乙腈和异丁腈;酰胺,如甲酰胺,N,N-二甲基甲酰胺,和乙酰胺;叔胺,如吡啶,三乙胺,二异丙基乙胺,N,N-二甲基苯胺,N,N-二乙基苯胺,和N-甲基吗啉;含硫化合物,如二甲亚砜和sulforan;脂肪酸,如甲酸,乙酸,和丙酸;醇,如甲醇,乙醇,乙二醇,和异丙醇;水;以及它们的混合物。
反应完成之后,过滤反应混合物收集结晶(如果需要的话,可加水沉淀结晶),或者将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后,如果需要的话,用诸如柱层析或重结晶之类技术进行后续纯化。从而可以分离出所需产物。
在化合物[4]的实例中,下式化合物:其中X的定义同上;Y2为卤素;和B2为氢,卤素,C1-C6烷氧基,或C1-C6烷硫基,
还可以按照下述流程制备:
Figure C9619770000572
其中X,Y2,B2,和R22的定义同上。
由化合物[88]制备化合物[89]的方法
化合物[89]可按如下所述制备:在盐酸或硫酸中,使化合物[88]与亚硝酸盐反应,转化成重氮盐,然后再在碱(如乙酸钠或吡啶)存在下,将重氮盐与下式化合物反应:其中R22的定义同上。
(例如参见 四面体(Tetrahedron),Vol.35,p.2013(1979))
由化合物[89]制备化合物[90]的方法
化合物[90]可通过水解化合物[89]制备,水解通常是在碱存在下在溶剂中进行。
反应温度为0℃至150℃,优选20℃至100℃。反应时间为1至24小时,优选1至10小时。尽管在反应中采用1摩尔碱与1摩尔化合物[89]的比例是理想的,但如果需要的话,反应中所用各试剂的用量仍可变化。
可使用的碱的实例包括无机碱如氢氧化钾,氢氧化锂,氢氧化钡,和氢氧化钠。
可使用的溶剂的实例包括脂族烃,如己烷,庚烷,粗汽油,环己烷,和石油醚;芳烃,如苯,甲苯,和二甲苯;卤代烃,如氯苯和二氯苯;醚类,如乙醚,二异丙醚,二噁烷,四氢呋喃,和乙二醇二甲醚;酮,如丙酮,甲乙酮,甲基异丁基酮,异佛尔酮,和环己酮;硝基化合物,如硝基甲烷和硝基苯;酰胺,如N,N-二甲基甲酰胺;叔胺如吡啶,三乙胺,二异丙基乙胺,N,N-二甲基苯胺,N,N-二乙基苯胺,和N-甲基吗啉;含硫化合物,如二甲亚砜和sulforan;醇,如甲醇,乙醇,乙二醇,和异丙醇;水;以及它们的混合物。
由化合物[90]制备化合物[87]的方法
化合物[87]可通过在溶剂中加热化合物[90]制备。
反应温度为50℃至200℃,优选50℃至150℃。反应时间为瞬间至72小时。
可使用的溶剂的实例包括脂族烃,如己烷,庚烷,粗汽油,环己烷,和石油醚;芳烃,如苯,甲苯,和二甲苯;卤代烃,如氯仿,四氯化碳,二氯甲烷,二氯乙烷,氯苯和二氯苯;醚类,如乙醚,二异丙醚,二噁烷,四氢呋喃,和乙二醇二甲醚;酮,如丙酮,甲乙酮,甲基异丁基酮,异佛尔酮,和环己酮;酯,如甲酸乙酯,乙酸乙酯,乙酸丁酯,和碳酸二乙酯;硝基化合物,如硝基甲烷和硝基苯;腈类,如乙腈和异丁腈;酰胺,如甲酰胺,N,N-二甲基甲酰胺,和乙酰胺;叔胺,如吡啶,三乙胺,二异丙基乙胺,N,N-二甲基苯胺,N,N-二乙基苯胺,和N-甲基吗啉;含硫化合物,如二甲亚砜和sulforan;脂肪酸,如甲酸,乙酸,和丙酸;醇,如甲醇,乙醇,乙二醇,和异丙醇;水;以及它们的混合物。
上述反应还可以采用金属(如铜)作为催化剂来进行。
反应完成之后,过滤反应混合物收集沉淀出的结晶,或者将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后,如果需要的话,用诸如柱层析或重结晶之类技术进行后续纯化。从而可以分离出所需产物。
化合物[86]也可以按照下述流程制备:其中Q1定义同上。
(参见Organic Synthesis Collective,Vol.1,p.442)
化合物[91]是已知的,或可用下述文献中所述的方法制备:EP-61741-A;USP 4,670,046,USP 4,770,695,USP 4,709,049,USP 4,640,707,USP 4,720,297,USP 5,169,431;和JP-A 63-156789/1988。
化合物[91]的某些实例也可以按照下述流程制备:其中R31为COR16或COOR10
由化合物[94]制备化合物[95]的方法
化合物[95]可以通过在溶剂中使化合物[94]和硝酸反应制备。
反应温度通常为0℃至100℃。反应时间一般为瞬间至24小时。尽管在反应中采用1摩尔硝酸与1摩尔化合物[94]的比例是理想的,但反应中所用各试剂的用量仍可依据反应条件而任意改变。
可使用的溶剂的实例包括酸性溶剂如硝酸和硫酸的混合物。
(参见Organic Synthesis Collective,Vo].1,p.372)
由化合物[95]制备化合物[96]的方法
化合物[96]可通过在乙酸、铁粉和水的混合物中还原化合物[95]加以制备。
反应温度通常为0℃至100℃。反应时间一般为瞬间至24小时。
反应完成之后,将反应混合物进行常规后处理,如用有机溶剂提取并浓缩,随后,如果需要的话,用诸如柱层析或重结晶之类技术进行后续纯化。从而可以分离出所需产物。
(参见Organic Synthesis Collective,Vol.2,p.471和ibid.,Vol.5,p.829)
本发明化合物具有优良的除草活性,而且它们中的一些还显示出对作物和有害杂草具有极好的选择性。更具体讲,本发明化合物对下文所列举的各种有害杂草具有除草活性,它们在对旱田进行叶面处理和土壤处理时可将其破坏。
蓼科:
卷茎蓼(Polygonum convolvulus),酸模叶蓼(Polygonumlapathifolium),宾洲蓼(Polygonum pensylvanicum),春蓼(Polygonumpersicaria),皱叶酸模(Rumex crispus),阔叶酸模(Rumex obtusifolius),虎杖(Polygonum cuspidatum)
马齿苋科:
马齿苋(Portulaca oleracea)
石竹科:
繁缕(Stellaria media)
藜科:
藜(Chenopodium album),扫帚菜(Kochia scoparia)
苋科:
西风谷(Amaranthus retroflexus),绿穗苋(Amaranthus hybridus)
Crusiferae:
野生萝卜(Raphanus raphanistrum),野生芥末(Sinapis arvensis),荠菜(Capsella bursa-pastoris)
豆科:
高田菁(Sesbania exaltata),加拿大筛子芥(Cassia obtusifolia),扭曲山马蝗(Desmodium tortuosum),白车轴草(trifolium repens)
锦葵科:
青麻(Abutilon theophrasti),刺黄花稔(Sida spinosa)
堇菜科:
田堇菜(Viola arvensis),三色堇(Viola tricolor)
茜草科:
猪殃殃(Galium aparine)
旋花科:
裂叶牵牛(Ipomoea hederacea),圆叶牵牛(Ipomoea purpurea),全叶裂叶牵牛(Ipomoea hederacea var.integriuscula),多洼牵牛(Ipomoealacunosa),田旋花(Convolvulus arvensis)
唇形科:
小野芝麻(Laminum purpureum),宝盖草(Lamium amplexicaule)
茄科:
曼陀罗(Datura stramonium),龙葵(Solanum nigrum)
玄参科:
波斯水苦苣(Veronica persica),常春藤叶婆婆纳(Veronicahederaefolia)
菊科:
宾州苍耳(Xanthium pensylvanicum),向日葵(Helianthus annuus),淡甘菊(Matricaria perforata or inodora),珍珠菊(Chrysanthemumsegetum),香甘菊(Matricaria matricarioides),美洲豚草(Ambrosiaartemisiifolia),三裂叶豚草(Ambrosia trifida),加拿大飞蓬(Erigeroncanadensis),蒌蒿(Artemisia princeps),极高一枝黄花(Solidagoaltissima)
紫草科:
田野勿望草(Myosotis arvensis)
萝摩科:
叙利亚马利筋(Asclepias syriaca)
大戟科:
泽漆(Eurphorbia helioscopia),美洲地锦草(Euphorbia maculata)
禾本科:
稗草(Echinochla crus-galli),狗尾草(Setaria viridis),费氏狗尾草(Setaria faberi),马唐(Digitaria sanguinalis),牛筋草(Eleusine indica),早熟禾(Poa annua),看麦娘(Aloecurus myosuroides),野燕麦(Avenafatua),阿刺伯高粱(Sorghum halepense),匍匐冰草(Agropyronrepens),旱雀麦(Bromus tectorum),狗牙根(Cynodon dactylon),秋稷(Panicum dichotomiflorum),得克萨斯稷(Panicum texanum),二色蜀黍(Sorghum vulgare)
鸭跖草科:
鸭跖草(Commelina communis)
木贼科:
问荆(Equisetum arvense)
莎草科:
碎米莎草(Cyperus iria),香附子(Cyperus rotundus),铁荸荠(Cyperus esculentus)
此外,本发明的一些化合物对主要农作物,如玉米(Zea mays),小麦(Triticum aestivum),大麦(Hordeum vulgare),稻(Oryza sativa),高粱(Sorghum bicolor),大豆(Glycine max),棉花(Gossypium spp.),甜菜(Beta vulgaris),花生(Arachis hypogaea),向日葵(Helianthus annuus)和蔓菁(Brassica napus);园艺作物(如花和观赏植物);和菜蔬类作物无造成危害的植物毒性。
本发明化合物能够有效防除非耕种培植的大豆(Glycine max),玉米(Zea mays),和小麦(Triticum aestivum)间的有害杂草。而且,它们中的一些还显示出对作物无造成危害的植物毒性。
本发明化合物在水田漫灌处理情况下,对下文所列的各种有害杂草具有除草活性。
禾本科:
稗(Echinochloa oryzicola)
玄参科:
陌上草(Lindernia procumbens)
千屈菜科:
节节菜,多花水苋
沟繁缕科:
三蕊沟繁缕
莎草科:
异型莎草(Cyperus difformis),萤蔺(Scirpus juncoides),牛毛毡(Eleocharis acicularis),水莎草,木贼状荸荠
雨久花科:
鸭舌草
泽泻科:
矮慈茹,慈茹,窄叶泽泻
眼子菜科:
眼子菜(Potamogeton distinctus)
伞形科:
水芹
此外,本发明一些化合物对移植水稻无造成危害的植物毒性。
本发明化合物能够有效防除果园,草地,空地,森林,排水沟,水道,或其它非栽培地中的各种有害杂草。
本发明还对生长在排水沟,水道等地方的各种水生植物如风眼兰(Eichhornia crassipes)具有除草活性。
本发明化合物与国际专利申请WO95/34659中所述的除草化合物有着基本相同的特性。在栽培引入了上述申请中所述的除草耐受性基因而获得具有耐受性的作物时,可使用比栽培无耐受性的常规作物所用剂量较大的本发明化合物,因此能够有效防治其它有害植物。
当本发明化合物用作除草剂的活性成分时,通常将它们与固体或液体载体或稀释剂,表面活性剂,和其它助剂混合配制成诸如乳油,可湿性粉剂,洗动剂,颗粒剂,浓乳剂,和水分散性颗粒剂。
这些制剂可含有任一种本发明化合物作为活性成分,其用量按制剂总重量计为0.001-80%,优选0.005%-70%。
固体载体或稀释剂的实例包括细粉或颗粒状下述物质:矿物质如高岭土,硅镁土,膨润土,白土,叶蜡石,滑石,硅藻土,和方解石;有机物质如胡桃壳粉;水溶性有机物质如尿素;无机盐如硫酸铵;和合成水合氧化硅。液体载体或稀释剂的实例包括芳香烃类,如甲基萘,苯基二甲苯基乙烷,和烷基苯(二甲苯);醇类,如异丙醇,乙二醇,和2-乙氧基乙醇;酯类,如邻苯二甲酸二烷基酯;酮类如丙酮,环己酮,和异佛尔酮;矿物油,如机油;植物油如豆油和棉籽油;二甲基亚砜,N,N-二甲基甲酰胺,乙腈,N-甲基吡咯烷酮,水,等。
用于乳化,分散,或扩散的表面活性剂的实例可包括阴离子型表面活性剂,如烷基硫酸盐,烷基磺酸盐,烷基芳基磺酸盐,磺基琥珀酸二烷基酯,和聚氧乙烯烷基芳基醚的磷酸盐;和非离子型的表面活性剂,如聚氧乙烯烷基醚,聚氧乙烯烷基芳基醚,聚氧乙烯聚氧丙烯嵌段共聚物,失水山梨糖醇脂肪酸酯,和聚氧乙烯失水山梨糖醇脂肪酸酯。
制剂中使用的助剂的实例可包括木质素磺酸盐,藻酸盐,聚乙烯醇,阿拉伯树胶,羧甲基纤维素(CMC),和磷酸异丙基酯(PAP)。
通常将本发明化合物配制成上述制剂,然后用于苗前或苗后土壤,叶面,或漫灌处理有害杂草。土壤处理包括土壤表面处理和拌土。叶面处理包括施用于植物整体和直接施用,即将化合物仅施用于杂草而不接触作物。
如果需要,本发明化合物可与具有除草活性的其它化合物混用。与本发明化合物混用的化合物的实例包括在农业化学品手册目录1995版(Meister公司出版)(Catalog 1995 Edition of farm Chemical Handbook),农药新化合物综述,13卷,1995(农药信息服务)(AG CHEM NEWCOMPOUND REVIEW(AG CHEM INFORMATION SERVICE));或JOSOUZAI KENKYU SOURAN(Hakuyu-sha)中描述的多种化合物。上述化合物的典型实例如下述:阿特拉津,草净津,二甲丙乙净,嗪草酮,扑草净,西马津,西草净,氯麦隆,敌草隆,dymuron,伏草隆,异丙隆,利谷隆,甲基苯噻隆,溴苯腈,碘苯腈,乙丁烯氟灵,胺硝草,氟乐灵,氟锁草醚,氟锁草醚钠,甲羧除草醚,甲氧除草醚,氟黄胺草醚,克阔乐,噁草酮,氟硝草醚,carfentrazone,flumiclorac-pentyl,flumioxazine,fluthiacet-methyl,sulfentrazone,thidiazimin,双苯唑快,敌草快,百草枯,2,4-滴,2,4-滴丁酸,氯酞酸甲酯,二甲四氯,二甲四氯丙酸,稗草胺,二氯吡啶酸,麦草畏,氟硫草定,氟草烟,二甲四氯丙酸盐,萘丙胺,二甲四氯乙硫酯,二氯喹啉酸,绿草定,乙草胺,甲草胺,丁草胺,乙酰甲草胺,乙基乙草胺,丙草胺,扑草胺,苄嘧黄隆,氯黄隆,氯嘧黄隆,卤甲黄隆,甲黄隆,烟嘧黄隆,氟嘧黄隆,吡嘧黄隆,嘧黄隆,噻苯隆,醚苯黄隆,苯磺隆,azimsulfuron,cloransulam-methyl,cyclosulfamuron,flumeturam,flupyrsulfuron,啶嘧黄隆,imazosulfuron,metosulam,prosulfuron,rimsulfuron,triflusulfuron-mrthyl,咪草酯,灭草烟,灭草喹,咪草烟,咪草酯,imazamox,bispyribac-sodium,pyriminobac-methyl,pyrithiobac-sodium,枯杀达,烯草酮,噻草酮,肟草酮,禾草灵,噁唑禾草灵-乙酯,高噁唑禾草灵,吡氟禾草灵,高吡氟禾草灵,吡氟氯禾灵,喹禾灵,cyhalofop-butyl,clodinafop-propargyl,吡草酮,异噁草胺,吡氟草胺,达草灭,吡唑特,苄草唑,isoxaflutole,sulcotrione,草铵膦,草甘膦,噻草平,杀草丹,溴丁酰草胺,抑草磷,丁草特,哌草丹,dimethenamid,甲胂钠,扑草灭,禾草畏,异噁草胺,苯噻草胺,草达灭,甲肾一钠,哌草磷,pributycarb,敌稗,哒草特,野麦畏,cafenstrol,胺草唑,和thiafluamide。
下面描述这类组合混用的代表性实例,其中本发明化合物用表1-5中所示的各化合物编号表示。
1.选自化合物1-495,1-496,1-499,1-503和1-577中的任一种化合物和选自莠去净,草津浸,溴苯腈和噻草平中的任一种化合物以1∶1-100重量比混合的混合物。
2.选自化合物1-495,1-496,1-499,1-503和1-577中的任一种化合物与选自稀草酮,噻草酮,禾草灵,喹禾灵,克阔乐,氟锁草醚,氟锁草醚钠(acifluorfen-sodium),flumiclorac-pentyl和麦草畏的任一种化合物以1∶0.5-50的重量比混合的混合物。
3.选自化合物1-495,1-496,1-499,1-503和1-577的任一种化合物与选自烟嘧磺隆,氟嘧磺隆,prosulfuron,氯嘧磺隆(chlorimuran-ethyl),噻磺隆,imsulfuon,卤黄隆,噁磺隆(oxasulfuron),isoxaflutole,醚草烟和imazamox的任一种化合物以1∶0.1-10的重量比混合的混合物。
4.选自化合物1-439,1-482,1-486,1-496,1-1076,1-1123和1-1441的任一种化合物与选自异丙隆和绿麦隆的任一种化合物以1∶1-100的重量比混合的混合物。
5.选自化合物1-439,1-482,1-486,1-496,1-1076,1-1123和1-1441的任一种化合物与选自2甲4氯丙酸,fluroxypyr和碘苯腈的任一种化合物以1∶0.5-50的重量比混合的混合物。
6.选自化合物1-439,1-482,1-486,1-496,1-1076,1-1123和1-1441的任一种化合物与选自吡氟草胺,甲磺隆,噁唑禾草灵-乙酯和clodinafop-propargyl的任一种化合物以1∶0.1-10的重量比混合的混合物。
7.选自化合物1-1141,1-1222和2-203的任一种化合物与选自草甘膦,草铵膦和对草快的任一种化合物以1∶1-100的重量比混合的混合物。
此外,本发明化合物还可与杀虫剂,杀螨剂,杀线虫剂,杀菌剂,植物生长调节剂,肥料,土壤改良剂等混合使用。
当本发明化合物用作除草剂的活性成分时,其施用量通常为每公顷0.01-10,000g,优选1-8000g,当然该用量可以依据气候条件,制剂类型,施用时间,施用方法,土壤状况,作物种类,杂草种类等而变。在使用乳油、可湿性粉剂、流动剂、浓乳剂、水分散性颗粒剂等时,一般是在加水稀释后以每公顷大约10-1000升的预定量施用,如果需要,可以加入诸如分散剂之类的助剂。在使用颗粒剂或某些类型的流动剂时,一般不需要稀释而直接施用。
如果需要的话,除上述表面活性剂外,还可使用的助剂的实例包括聚氧乙烯树脂酸(酯),木质素磺酸盐,松香酯,二萘基甲烷磺酸盐,作物油浓缩物,和植物油如豆油,玉米油,棉子油和葵花油。
本发明化合物还可用作收获酸如用于棉花的脱叶剂和干燥剂,以及马铃薯的干燥剂的活性成分。在这些情况下,本发明化合物通常按用作除草剂的活性成分的情况相同的方法配制,而且可以在作物收获之前单独或与其它收获酸结合用于叶面处理。
本发明化合物用下述制备实施例、参考实施例、制剂实施例和试验实施例进一步说明,但本发明并不局限于这些实施例。
下面描述本发明化合物和用作中间体的式[2]腙类化合物的制备实施例,其中本发明化合物用表1-5中所示的化合物编号表示。
制备实施例1(制备化合物2-631)
在冰冷却下,向8.0g(97.2mmol)乙酸钠和50ml水的混合溶液中加入6.6g(24.3mmol)1,1-二溴-3,3,3-三氟丙酮,并使反应在80℃进行30分钟。然后,冷却反应混合物至0℃,向其中加入4.4g(18.7mmol)7-氟-6-肼基-4-丙炔基-2H-1,4-苯并噁嗪-3-酮,并在室温下搅拌反应混合物2小时。过滤收集沉淀出的结晶,用10ml水洗涤两次,并干燥,得到6.3g(18.37mmol)7-氟-6-三氟乙酰基亚甲基肼基-4-丙炔基-2H-1,4-苯并噁嗪-3-酮[其它名称:3,3,3-三氟-2-氧代丙醛1-(7-氟-3-氧代-4-丙炔基-2H-1,4-苯并噁嗪-6-基腙)],m.p.190.6℃(分解)。
向6.0g(17.5mmol)上述化合物和50ml甲苯的混合溶液中加入9.1g(26.2mmol)乙酯基亚甲基三苯基磷烷,并加热回流混合物1小时。减压蒸除甲苯,将所得残留物进行硅胶柱层析,得到1.3g(3.5mmol)7-氟-6-[5-三氟甲基-3-哒嗪酮-2-基]-4-丙炔基-2H-1,4-苯并噁嗪-3-酮(化合物2-631)。
制备实施例2(制备化合物1-476)
在冰冷却下,向5.3g(53.5mmol)乙酸钠和约100ml水的混合溶液内加入6.6g(24.3mmol)1,1-二溴-3,3,3-三氟丙酮,并使反应在70℃进行20分钟。尔后冷却反应混合物至室温,向其中加入溶在约20ml乙醚中的2-氟-4-氯-5-异丙氧基苯肼(5.8g,21.5mmol),并室温搅拌反应混合物1小时。分离醚层并浓缩。然后向残留物中加入约60ml THF,再加入8.3g(23.0mmol)乙酯基亚乙基三苯基磷烷,并加热回流混合物2小时。减压蒸除甲苯,硅胶柱层析所得残留物,得到3.8g(10.5mmol)2-[2-氟-4-氯-5-异丙氧基苯基]-4-甲基-5-三氟甲基哒嗪-3-酮(化合物1-476)。
Figure C9619770000681
制备实施例3(制备化合物1-391)
首先,在冰冷却下,将3.5g(9.7mmol)2-[2-氟-4-氯-5-异丙氧基苯基]-4-甲基-5-三氟甲基哒嗪-3-酮(化合物1-476)溶于大约10ml浓硫酸中,并将溶液温热至室温。10分钟之后,向反应混合物内加入大约100ml水,过滤收集所沉淀的结晶,用20ml水洗涤两次并用10ml己烷洗涤一次。这些结晶用异丙醇重结晶,得到3.2g(9.0mmol)2-[2-氟-4-氯-5-羟基苯基]-4-甲基-5-三氟甲基哒嗪-3-酮(化合物1-391)。
Figure C9619770000682
制备实施例4(制备化合物1-486)
首先,将3.2g(10mmol)化合物1-391溶于50ml DMF中,然后在室温下加入2.0g(13mmol)碳酸钾,随后再加入1.3g(11mmol)丙炔溴,并室温搅拌混合物30分钟,尔后加入100ml水。过滤收集沉淀出的结晶,用己烷洗涤,并用异丙醇重结晶,得到3.4g(9mmol)化合物1-486。
Figure C9619770000691
制备实施例5(制备化合物1-496)
首先,将3.2g(10mmol)化合物1-391溶于大约50ml DMF内,加入0.44g(11mmol)氢化钠(60wt.%,油分散物),并室温静置混合物30分钟,接着在冰冷却下加入1.8g(11mmol)溴乙酸乙酯、室温搅拌1小时后,用乙醚提取反应混合物。有机层依次用10%盐酸,碳酸氢钠水溶液,氯化钠饱和溶液洗涤,并用无水硫酸镁干燥。减压蒸除溶剂,并硅胶柱层析所得残留物,得到2.4g(5.5mmol)化合物1-496。
制备实施例6(制备化合物2-251)
在冰冷却下,向5.3g(53.5mmol)乙酸钠和约50ml水的混合溶液中加入6.6g(24.3mmol)1,1-二溴-3,3,3-三氟丙酮,并使反应在80℃进行1小时。然后,冷却反应混合物至0℃,向其中加入4.4g(18.7mmol)7-氟-6-肼基-4-丙炔基-2H-1,4-苯并噁嗪-3-酮,并在室温下搅拌反应混合物2小时。过滤收集沉淀出的结晶,用10ml水洗涤两次和10ml己烷洗涤一次,然后不经干燥而直接溶于50ml甲苯中。向此溶液内加入8.8g(24.3mmol)乙酯基亚乙基三苯基磷烷,并加热回流混合物1小时,同时进行共沸脱水。减压蒸除甲苯,残留物进行硅胶柱层析,得到3.5g(9.01mmol)化合物2-251。
Figure C9619770000701
制备实施例7(制备化合物2-328)
在冰冷却下,向5.3g(53.5mmol)乙酸钠和约50ml水的混合溶液中加入6.6g(24.3mmol)1,1-二溴-3,3,3-三氟丙酮,并使反应在80℃进行1小时。然后,冷却反应混合物至0℃,向其中加入4.8g(18.7mmol)6-氟-5-肼基-3-仲丁基-1,3-苯并噻唑-2-酮,并将反应混合物室温下搅拌2小时。然后,向反应混合物中加入100ml乙醚,接着搅拌并进行析相作用,浓缩有机层。将残留物溶于50mlTHF,加入8.8g(24.3mmol)乙酯基亚乙基三苯基磷烷,并加热回流混合物1小时。减压蒸除THF,将残留物进行硅胶柱层析,得到3.7g(9.6mmol)化合物2-328。
制备实施例8(制备化合物1-347)
首先,将50ml浓硫酸用冰冷却,并在其中溶入7.0g(22.8mmol)化合物1-341。然后,在5℃或更低的温度下,逐滴加入1.51g(24mmol)发烟硝酸接着在0℃-5℃下熟化1小时。将混合物倾入到300ml冰水中,并用50ml乙醚提取三次。合并的醚层用大约100ml水洗涤,并用100ml碳酸氢钠水溶液中和,继之进行相分离。有机层用硫酸镁干燥并浓缩至一半体积,尔后将残留物进行硅胶柱层析,得到6.1g(17.4mmol)化合物1-347。
制备实施例9(制备化合物1-353)
首先,混合5.0g铁粉、75ml乙酸和10ml水,并温热混合物至约80℃,接着熟化15分钟。然后,将6.0g(17.1mmol)化合物1-347溶于40ml乙酸乙酯,在80℃或更低的温度下将其滴加到上述混合物内。在大约80℃熟化1小时后,静置反应混合物使之冷却至室温,并用100ml乙酸乙酯提取。合并的乙酸乙酯层用50ml水洗涤两次,并用碳酸氢钠水溶液中和,继之进行相分离。有机层用硫酸镁干燥,然后减压蒸乙酸乙酯。硅胶柱层析残留物,得到5.1g(15.9mmol)化合物1-353。
Figure C9619770000712
制备实施例10(制备化合物1-420)
首先,将500mg(1.6mmol)化合物1-353与10ml(77.3mmol)2-溴丙酸乙酯混合,并在大约160℃下加热回流此混合物约12小时。放置冷却后,将反应混合物进行硅胶柱色谱纯化,得到60mg(0.6mmol)化合物1-420。
制备实施例11(制备化合物1-1622)
首先,在5ml乙腈中一同混合6ml(55.4mmol)丙烯酸乙酯、0.5g(4.8mmol)亚硝酸叔丁酯和0.6g(4.5mmol)氯化铜(II),接着用冰冷却。然后在5℃或更低温度下逐滴加入溶在5ml乙腈中的化合物1-353(1.0g,3.1mmol),接着室温熟化过夜。将反应混合物倾入冰水中,用100ml乙酸乙酯提取两次。合并的乙酸乙酯层用50ml稀盐酸洗涤,并用硫酸镁干燥。减压蒸除溶剂,并硅胶柱层析所得残留物,得到0.51g(1.2mmol)化合物1-1622。
Figure C9619770000722
制备实施例12(制备化合物1-1221)
在冰冷却下,向含5.3g(53.5mmol)乙酸钠和约50ml水的混合溶液中加入6.6g(24.3mmol)1,1-二溴-3,3,3-三氟丙酮,并使反应在80℃进行1小时。然后,冷却反应混合物至0℃,向其中加入5.2g(18.7mmol)2-(2-氯-4-氟-5-肼基苯硫基)丙酸甲酯,并室温搅拌反应混合物2小时。过滤收集沉淀出的结晶,用10ml水洗涤两次和10ml己烷洗涤一次,并干燥。将残留物溶于50ml THF,向其中加入8.4g(22.4mmol)乙酯基亚甲基三苯基磷烷,室温搅拌溶液3小时。减压蒸除THF,并将残留物通过硅胶柱色谱纯化,得到3.8g(9.0mmol)化合物1-1221。
Figure C9619770000731
制备实施例13(制备化合物2-821)
在冰冷却下,向含8.0g(97.2mmol)乙酸钠和约50ml水的混合溶液中加入6.9g(24.3mmol)3,3-二溴-1,1,1-三氟丁酮,并使反应在80℃进行30分钟。然后,冷却反应混合物至0℃,向其中加入4.4g(18.7mmol)7-氟-6-肼基-4-丙炔基-2H-1,4-苯并噁嗪-3-酮,并室温搅拌反应混合物2小时。过滤收集沉淀出的结晶,用10ml水洗涤两次,并干燥。得到6.1g(17.0mmol)1,1,1-三氟-2,3-丁二酮3-(7-氟-3-氧代-4-丙炔基-2H-1,4-苯并噁嗪-6-基腙)。
向6.1g(17.0mmol)上述化合物和50ml THF的混合溶液中加入7.1g(20.4mmol)乙酯基亚甲基三苯基磷烷,并加热回流混合物1小时。减压蒸除THF,并将残留物通过硅胶柱色谱纯化,得到0.61g(1.6mmol)7-氟-6-(6-甲基-5-三氟甲基-3-哒嗪酮-2-基)-4-丙炔基-2H-1,4-苯并噁嗪-3-酮(化合物2-821)。
Figure C9619770000741
参考实施例1
该实施例为制备实施例13中所用的3,3-二溴-1,1,1-三氟-2-丁酮的制备实施例。
首先,将34.0g乙酸钠溶于270ml乙酸中,向其中加入25g(0.20mol)1,1,1-三氟-2-丁酮,并在15℃-20℃的温度下,于45分钟内滴加入66.3g(0.42mol)溴。搅拌反应混合物5小时,期间保持温度为15℃-20℃。室温下放置68小时,取出上清液,用600ml浓硫酸洗涤。再用307ml浓硫酸进一步洗涤并常压蒸馏,得到28g(0.10mol)3,3-二溴-1,1,1-三氟-2-丁酮。
制备实施例14(制备化合物1-1346)
在冰冷却下,向含5.3g(53.5mmol)乙酸钠和约50ml水的混合溶液中加入6.9g(24.3mmol)3,3-二溴-1,1,1-三氟-2-丁酮,并使反应在80℃进行1小时。然后,冷却反应混合物至0℃,向其中加入3.3g(18.7mmol)2-氯-4-氟-5-肼基苯酚,并室温搅拌反应混合物2小时。过滤收集沉淀出的结晶,用10ml水洗涤两次和10ml己烷洗涤一次,干燥,然后将残留物溶于50ml THF。向此溶液中加入8.8g(24.3mmol)乙酯基亚甲基三苯基磷烷,并将混合物室温搅拌3小时。减压蒸除THF,并硅胶柱层析所得残留物,得到0.51g(1.6mmol)化合物1-1346。
Figure C9619770000751
制备实施例15(制备化合物1-1441)
首先,将3.2g(10mmol)化合物1-1346溶于约50ml DMF中,室温下向其中加入2.0g(13mmol)碳酸钾,然后再加入1.3g(11mmol)丙炔溴,并室温搅拌混合物30分钟,接着加入100ml水。过滤收集沉淀结晶,己烷洗涤,并用异丙醇重结晶,得到3.2g(8.5mmol)化合物1-1441。
Figure C9619770000752
制备实施例16(制备化合物1-499)
此实施例按制备实施例5中所述的方法进行,只是其中用1.8g(1.1mmol)氯乙酸正戊酯代替溴乙酸乙酯。加入此化合物之后,将反应混合物在40℃搅拌3小时,尔后用乙醚提取。有机层用10%HCl、碳酸氢钠水溶液和饱和氯化钠溶液洗涤,并用无水硫酸镁干燥。减压蒸除溶剂,并将残留物通过硅胶色谱纯化,得到3.8g(8.0mmol)化合物1-499。
制备实施例17(制备化合物2-203)
在冰冷却下,向含5.3g(53.5mmol)乙酸钠和约50ml水的混合溶液中加入6.6g(24.3mmol)1,1-二溴-3,3,3-三氟丙酮,并使反应在80℃进行1小时。然后,冷却反应混合物至0℃,向其中加入4.0g(18.7mmol)6-肼基-4-丙炔基-2H-1,4-苯并噁嗪-3-酮,并室温搅拌反应混合物2小时。过滤收集沉淀出的结晶,用10ml水洗涤两次和10ml己烷洗涤一次,然后不经干燥直接溶于50ml THF。向此溶液中加入8.8g(24.3mmol)乙酯基亚乙基三苯基磷烷,并加热回流混合物3小时。减压蒸除THF,并硅胶柱层析所得残留物,得到3.3g(8.8mmol)化合物2-203。
制备实施例18(制备化合物1-1222)
在冰冷却下,向含5.3g(53.5mmol)乙酸钠和约50ml水的混合溶液中加入6.6g(24.3mmol)1,1-二溴-3,3,3-三氟丙酮,并使反应在80℃进行1小时。然后,冷却反应混合物至0℃,向其中加入5.5g(18.7mmol)2-(2-氯-4-氟-5-肼基苯硫基)丙酸乙酯,并室温搅拌反应混合物2小时。过滤收集沉淀出的结晶,用10ml水洗涤两次和10ml己烷洗涤一次,干燥,然后溶于50ml THF。向此溶液中加入8.4g(22.4mmol)乙酯基亚甲基三苯基磷烷,并室温搅拌混合物3小时。减压蒸除THF,并硅胶柱层析所得残留物,得到4.3g(9.9mmol)化合物1-1222。
Figure C9619770000771
制备实施例19(制备化合物1-476)
在冰冷却下,向含5.3g(53.5mmol)乙酸钠和约100ml水的混合溶液中加入6.6g(24.3mmol)1,1-二溴-3,3,3-三氟丙酮,并使反应在70℃进行20分钟。然后,冷却反应混合物至室温,向其中加入溶在约20ml乙醚中的2-氟-4-氯-5-异丙氧基苯肼(5.8g,21.5mmol)溶液,并室温搅拌反应混合物1小时。分离乙醚层,用10ml氯化钠饱和溶液洗涤一次,并用硫酸镁干燥。蒸除乙醚,得到6.5g(20.0mmol)3,3,3-三氟-2-氧代-丙醛1-(4-氯-2-氟-5-异丙氧基苯腙)。
    1H-NMR(250MHz,CDCl3,TMSδ(ppm))1.39(6H,d,J=6.0Hz),
4.38-4.52(1H,m),7.15(1H,d,J=10.5Hz),7.22(1H,d,J=7.3Hz),7.43(1H,q,
J=1.7Hz),9.18(1H,br).
将这一化合物溶于50ml THF。向此溶液中加入8.3g(23.0mmol)乙酯基亚乙基三苯基磷烷,并加热回流混合物2小时。减压蒸除THF,残留物通过硅胶柱色谱纯化,得到3.8g(10.5mmol)2-[2-氟-4-氯-5-异丙氧基苯基]-4-甲基-5-三氟甲基哒嗪-3-酮(化合物1-476)。
制备实施例20(制备化合物1-642)
在冰冷却下,向含5.3g(53.5mmol)乙酸钠和约100ml水的混合溶液中加入6.6g(24.3mmol)1,1-二溴-3,3,3-三氟丙酮,并使反应在70℃进行20分钟。然后,冷却反应混合物至室温。另外,单独将5.8g(21.5mmol)粗制2-氯-4-氟-5-肼基苯甲酸乙酯盐酸盐溶于30ml水中,并加入100ml乙醚,在冷却下,将混合物通过加入碳酸氢钠饱和溶液中和,接着用氯化钠饱和溶液洗涤,得到2-氯-4-氟-5-肼基苯甲酸乙酯的乙醚溶液。将此溶液加入到上述反应混合物中,接着在室温下剧烈搅拌2小时。分离乙醚层,用10ml氯化钠饱和溶液洗涤一次,并用硫酸镁干燥。蒸除乙醚。将残留物溶于50ml THF中,加入8.3g(23.0mmol)乙酯基亚乙基三苯基磷烷,并加热回流混合物2小时。减压蒸除THF,残留物通过硅胶柱色谱纯化,得到3.8g(10.0mmol)化合物1-642。
参考实施例2
此实施例为制备实施例20中所用的2-氯-4-氟-5-肼基苯甲酸乙酯盐酸盐的制备实施例。
首先,在室温下将50g(0.29mol)2-氯-4-氟苯甲酸溶于150ml盐酸中,并在35-45℃下滴加入含28ml(0.31mol)发烟硝酸和56ml浓硫酸的混酸。然后,将此溶液在40℃搅拌1小时,再倾入到250ml冰水内。过滤收集沉淀出的结晶并用己烷和乙酸乙酯的混合溶液重结晶,得到55g(0.25mol)2-氯-4-氟-5-硝基苯甲酸。随后将55g(0.25mol)2-氯-4-氟-5-硝基苯甲酸溶于50ml乙酸乙酯中,加入33g(0.28mol)亚硫酰氯,并加热回流混合物3小时,尔后放置冷却至室温。然后在冰冷却下加入20ml乙醇和30g三乙胺,并室温搅拌混合物2小时。蒸除溶剂,残留物通过硅胶色谱纯化,得到57g(0.23mol)2-氯-4-氟-5-硝基苯甲酸乙酯。
随后,混合60g铁粉和500ml 10%乙酸,并将混合物加热至40℃。另外,独立地将50g(0.20mol)2-氯-4-氟-5-硝基苯甲酸乙酯溶于含20ml乙酸和20ml乙酸乙酯的混合溶液中,并滴加到上述铁粉-乙酸混合溶液内。尔后将反应混合物在50℃搅拌1小时,通过硅藻土过滤。滤液用100ml乙酸乙酯提取。乙酸乙酯层用碳酸氢钠水溶液和氯化钠饱和溶液洗涤,并用硫酸镁干燥。蒸除溶剂,残留物通过硅胶色谱纯化,得到40g(0.18mol)5-氨基-2-氯-4-氟苯甲酸乙酯。
然后,将19g(87.4mmol)5-氨基-2-氯-4-氟苯甲酸乙酯溶于120ml盐酸中,继之冷却至0℃,在10℃或更低温度下滴加入6.3g(91.7mmol)亚硝酸钠的水(10ml)溶液。将混合物在0℃搅拌30分钟,然后冷却至-30℃,向其中加入58g(0.31mol)无水氯化锡(II)的盐酸(40ml)溶液,接着在0℃下进一步搅拌3小时。过滤收集沉淀出的结晶,然后干燥,得到13.6g(50.7mmol)粗制2-氯-4-氟-5-肼基苯甲酸乙酯盐酸盐。
制备实施例21(制备化合物1-1789)
首先,将5.0g(15.5mmol)化合物1-391溶于约50ml DMF中,室温下向其中加入2.8g(20.2mmol)碳酸钾,然后再加入1.5g(17.1mmol)3-溴-2-甲基-1-丙烯,并室温搅拌混合物30分钟,接着加入100ml水。过滤收集沉淀结晶,己烷洗涤,并用异丙醇重结晶,得到4.4g(13.2mmol)化合物1-1789。
Figure C9619770000801
制备实施例22(制备化合物4-451)
首先,将4.0g(12.0mmol)化合物1-1789溶于20ml N,N-二甲基苯胺中,并将此溶液在180℃加热3小时。冷却至室温后,加入100ml乙酸乙酯,混合物用1N盐酸和氯化钠饱和溶液洗涤,并用硫酸镁干燥。蒸除溶剂,沉淀的结晶用异丙醇重结晶,得到3.4g(10.2mmol)2-[4-氯-6-氟-3-羟基-2-(2-甲基-2-丙烯基)]-4-甲基-5-三氟甲基哒嗪-3-酮,m.p.133.2℃。
将产物溶于30ml二甲苯中,加入催化量对-甲苯磺酸,并加热回流混合物1小时。冷却至室温后,加入100ml乙酸乙酯,混合物用碳酸氢钠水溶液和氯化钠溶液洗涤,并用硫酸镁干燥。蒸除溶剂,残留物通过硅胶柱色谱纯化,得到3.0g(9.0mmol)化合物4-451。
Figure C9619770000811
制备实施例23(制备化合物1-483)
首先,将5.0g(15.5mmol)化合物1-391溶于约20ml DMF中,室温下向其中加入2.4g(17.1mmol)碳酸钾。将溶液加热至大约40℃,加入1.7g(17.1mmol)2,3-二氯丙烯,1小时后,放置使混合物冷却并倒入冰水中。过滤收集沉淀结晶,己烷洗涤,并用异丙醇重结晶,得到5.2g(13.1mmol)化合物1-483。
Figure C9619770000812
制备实施例24(制备化合物3-139)
首先,将3.0g(7.6mmol)化合物1-436溶于10ml N,N-二甲基苯胺中,并将此溶液加热回流3小时。冷却至室温后,加入50ml乙酸乙酯,混合物用1N盐酸和氯化钠饱和溶液洗涤,并用硫酸镁干燥。蒸除溶剂,沉淀的结晶用异丙醇重结晶,得到2.2g(5.6mmol)2-[4-氯-6-氟-3-羟基-2-(2-氯-2-丙烯基)]-4-甲基-5-三氟甲基哒嗪-3-酮。
    1H-NMR(300MHz,CDCl3,TMSδ(ppm))2.41(3H,q,J=1.9Hz),3.56
(1H,d,J=16.3Hz),3.72(1H,d,J=16.3Hz),4.91(1H,q,J=1.4Hz),5.12(1H,
d,J=1.5Hz),5.72(1H,s),7.25(1H,d,J=8.7Hz),8.00(1H,s)
将产物溶于冰冷却的10ml三氟甲磺酸中,并在冰冷却下搅拌此溶液。30分钟后,将溶液倾入冰水内,过滤收集沉淀结晶并通过硅胶柱色谱纯化,得到1.9g(5.4mmol)化合物3-139。
制备实施例25(制备化合物1-1744)
此实施例按制备实施例20中的方法进行,只是其中用6.1g(21.5mmol)2,4-二氯-5-肼基苯甲酸乙酯盐酸盐代替2-氯-4-氟-5-肼基苯甲酸乙酯盐酸盐。得到4.8g(12.2mmol)化合物1-1744。
Figure C9619770000822
上面所用的2,4-二氯-5-肼基苯甲酸乙酯盐酸盐采用与参考实施例2所示相同的方法由2,4-二氯苯甲酸制备。
制备实施例26(制备化合物1-1279)
在冰冷却下,向含5.3g(53.5mmol)乙酸钠和约100ml水的混合溶液中加入6.6g(24.3mmol)1,1-二溴-3,3,3-三氟丙酮,并使反应在70℃进行20分钟。然后,冷却反应混合物至室温。另外,独立地将5.8g(21.5mmol)2-氯-4-氟-5-肼基苯甲酸乙酯盐酸盐溶于30ml水中,加入100ml乙醚,并在冷却下,加入碳酸氢钠饱和溶液中和混合物,接着用氯化钠饱和溶液洗涤,得到2-氯-4-氟-5-肼基苯甲酸乙酯的乙醚溶液。将此溶液加入到上述反应混合物中,接着在室温下剧烈搅拌2小时。分离乙醚层,用10ml氯化钠饱和溶液洗涤一次,并用硫酸镁干燥。蒸出乙醚,加入少量己烷,得到4.3g(12.6mmol)2-氯-4-氟-5-(2-氧代-3,3,3-三氟亚戊基肼基)苯甲酸乙酯。将该产物溶于50ml THF中,加入5.0g(14.4mmol)乙酯基亚甲基三苯基磷烷,并加热回流混合物2小时。减压蒸除THF,残留物通过硅胶柱色谱纯化,得到3.6g(9.7mmol)化合物1-1279。
Figure C9619770000831
制备实施例27(制备化合物1-1780)
首先,将50g(0.61mol)乙酸钠和41g(0.14mol)1,1-二溴-3,3,3三氟丙酮与500ml水混合,并将混合物在80℃搅拌30分钟,然后冷却至0℃。随后在10℃或更低温度下加入45g(0.14mol)4-溴-2-氟-5-异丙氧基苯肼盐酸盐,并将混合物在10℃或更低温度下搅拌3小时。过滤收集沉淀结晶并干燥,得到35g(94.3mmol)3,3,3-三氟-2-氧代丙醛1-(4-溴-2-氟-5-异丙氧基苯腙)。
然后,在室温下,将16g(46.0mmol)乙酯基亚甲基三苯基磷烷和16g(43.1mmol)3,3,3-三氟-2-氧代丙醛1-(4-溴-2-氟-5-异丙氧基苯腙)在100ml THF中搅拌4小时。反应完成之后,浓缩反应混合物,并将残留物进行硅胶层析,得到9.4g(23.8mmol)化合物1-1780。
参考实施例3
此实施例为制备实施例27中所用的4-溴-2-氟-5-异丙氧基苯肼盐酸盐的制备实施例。
首先,将93g(0.49mol)2-溴-4-氟苯酚悬浮在200ml水中。在10℃或更低温度下,向其中一起倾入55g(0.59mol)氯甲酸甲酯和21.5g(0.51mol)氢氧化钠的水(60ml)溶液,并在同样温度下搅拌混合物2小时。过滤收集沉淀结晶,水洗,在真空烘箱中干燥,得到111.6g(0.45mol)2-溴-4-氟苯氧基甲酸甲酯。
然后,将110g(0.44mol)2-溴-4-氟苯氧基甲酸甲酯溶于250ml硫酸中,在5℃或更低温度下滴加入含30g发烟硝酸和30ml硫酸的混酸,并搅拌混合物2小时。将反应混合物倾倒在冰上,过滤收集沉淀出的结晶,水洗,干燥,得到126g(0.43mol)2-溴-4-氟-5-硝基苯氧基甲酸甲酯。
随后,将125g(0.43mol)2-溴-4-氟-5-硝基苯氧基甲酸甲酯悬浮在200ml水中,加入19g(0.47mol)氢氧化钠,将混合物在50℃-60℃下搅拌4小时。反应完成之后,将反应混合物冷却至室温并用氯仿洗涤。水层用盐酸水溶液酸化并用乙酸乙酯提取。干燥并浓缩乙酸乙酯层,得到104g(0.43mol)2-溴-4-氟-5-硝基苯酚。
尔后,将100g(0.42mol)2-溴-4-氟-5-硝基苯酚溶于400ml二甲基甲酰胺中,加入70g(0.50mol)碳酸钾,随后温热至50℃,逐滴加入94g(0.55mol)异丙基碘,并在45-50℃下搅拌混合物1小时。反应完成之后,将反应混合物倒入水中,并用乙酸乙酯提取。乙酸乙酯层用水和稀盐酸依次洗涤,干燥,并浓缩。柱层析所得残留物,得到99.8g(0.36mol)2-溴-4-氟-5-硝基苯基异丙基醚。
然后,将60g(0.22mol)2-溴-4-氟-5-硝基苯基异丙基醚溶于300ml乙酸乙酯中,加入1.0g 10%钯-炭,在氢气氛中氢化。反应完成后,滤除钯-炭,并浓缩滤液,得到52g(0.21mol)4-溴-2-氟-5-异丙氧基苯胺。
随后,将108g(0.57mol)氯化锡(II)溶于100ml浓盐酸中,接着冷却至-30℃,然后在0℃或更低温度下滴加入重氮盐溶液[由47g(0.19mol)4-溴-2-氟-5-异丙氧基苯胺,13.5g(0.20mol)亚硝酸钠,和120ml盐酸制得],并将混合物在室温下搅拌2小时。过滤收集沉淀出的结晶,在真空烘箱中干燥,得到45g(0.14mol)粗产物,4-溴-2-氟-5-异丙氧基苯肼盐酸盐。
Figure C9619770000861
制备实施例28(制备化合物1-1783)
首先,将19g(52.4mmol)乙酯基亚乙基三苯基磷烷和19g(63.2mmol)3,3,3-三氟-2-氧代丙醛1-(4-溴-2-氟-5-异丙氧基苯腙)在100ml THF中加热回流5小时。反应完成后,浓缩反应混合物,并硅胶层析所得残留物,得到9.1g(22.2mmol)化合物1-1783。
Figure C9619770000862
制备实施例29(制备化合物1-1748)
该实施例按照制备实施例27的方法进行,其中只是用41g(0.41mol)2,4-二氯-5-异丙氧基苯肼盐酸盐代替4-溴-2-氟-5-异丙氧基苯肼盐酸盐,得到31.3g(91.3mmol)3,3,3-三氟-2-氧代丙醛1-(2,4-二氯-5-异丙氧基苯腙)。然后,将此化合物和40g(0.11mol)乙酯基亚乙基三苯基磷烷在100ml THF中加热回流5小时。反应完成后,浓缩反应混合物,并硅胶柱层析所得残留物,得到21g(54.8mmol)化合物1-1748。
上面所用的2,4-二氯-5-异丙氧基苯肼用与参考实施例3中所述相同的方法由2,4-二氯苯酚制得。。
制备实施例30(制备化合物1-1029)
首先,将9g(22.8mmol)2-(4-溴-2-氟-5-异丙氧基苯基)-5-三氟甲基哒嗪-3-酮加到50ml硫酸中,并搅拌此混合物1小时。反应完成之后,将反应混合物倒在冰上,用乙酸乙酯提取。干燥并浓缩乙酸乙酯层,并柱层析所得残留物(洗脱剂:己烷∶乙酸乙酯=5∶1),得到5.9g(16.7mmol)化合物1-1029。
制备实施例31(制备化合物1-392)
首先,将9g(22.0mmol)2-(4-溴-2-氟-5-异丙氧基苯基)-4-甲基-5-三氟甲基哒嗪-3-酮加到50ml硫酸中,并搅拌此混合物1小时。反应完成之后,将反应混合物倒在冰上,用乙酸乙酯提取。干燥并浓缩乙酸乙酯层,并柱层析所得残留物(洗脱剂:己烷∶乙酸乙酯=5∶1),得到4.2g(11.5mmol)化合物1-392。
制备实施例32(制备化合物1-1274)
首先,将7.4g(90.2mmol)乙酸钠和8.0g(28.2mmol)1,1-二溴-3,3,3三氟丙酮与70ml水混合,并将混合物在80℃搅拌30分钟,然后冷却,在10℃或更低温度下加入7.0g 2-氯-5-肼基肉桂酸乙酯,并搅拌混合物3小时。过滤收集沉淀结晶并干燥,得到9.6g(27.5mmol)2-氯-5-(3,3,3-三氟-2-氧代亚丙基肼基)肉桂酸乙酯。
    1H-NMR(250MHz,CDCl3,TMSδ(ppm))1.36(3H,t,J=6.9Hz),4.30(2H,q,J=6.9Hz),6.4-6.6(1H,m),7.2-7.5(3H,m),7.65(1H,d,J=2.5Hz),8.0-8.1(1H,m)
然后,在室温下,将1.0g(2.9mmol)乙酯基亚甲基三苯基磷烷和1.0g(2.9mmol)2-氯-5-(3,3,3-三氟-2-氧代亚丙基肼基)肉桂酸乙酯在10ml THF中搅拌1小时。反应完成之后,浓缩反应混合物,并将残留物进行柱层析(洗脱剂:己烷∶乙酸乙酯=5∶1),得到0.43g(11.5mmol)化合物1-1274。
Figure C9619770000891
参考实施例4
制备实施例32中所用的2-氯-5-肼基肉桂酸乙酯用下述方法制备:
首先,将60g氯化锡(II)溶于60ml浓盐酸中,接着将混合物冷却至-30℃,然后在0℃或更低温度下滴加入重氮盐溶液[由19g 5-氨基-2-氯肉桂酸乙酯和6.3g亚硝酸钠制得],并将混合物在室温下搅拌1小时。过滤收集沉淀出的结晶,将这些结晶加到冰水中,用2N氢氧化钠水溶液中和,并用氯仿提取。干燥并浓缩氯仿层,得到7.0g 2-氯-5-肼基肉桂酸乙酯。
制备实施例33(制备化合物1-637)
首先,将1.1g(2.9mmol)乙酯基亚乙基三苯基磷烷和1.0g(2.9mmol)2-氯-5-(3,3,3-三氟-2-氧代亚丙基肼基)肉桂酸乙酯在10ml THF中加热回流3小时。反应完成后,浓缩反应混合物,并柱层析所得残留物(洗脱剂:己烷∶乙酸乙酯=5∶1),得到0.66g(1.7mmol)化合物1-637。
Figure C9619770000901
制备实施例34(制备化合物1-367)
首先,将0.5g(1.6mmol)化合物1-353溶于1.5ml吡啶中,向其中滴加入0.2g(1.7mmol)甲磺酰氯,接着搅拌2小时。将反应混合物倒入冰水中,用乙酸乙酯提取。乙酸乙酯层用稀盐酸洗涤,干燥,并浓缩。柱层析所得残留物(洗脱剂,己烷∶乙酸乙酯=3∶1),得到0.42g(1.1mmol)化合物1-367。
Figure C9619770000902
制备实施例35(制备化合物1-369)
该实施例按照制备实施例34的方法进行,只是其中用0.23g(1.6mmol)氯甲基磺酰氯代替甲磺酰氯,得到0.38g(0.91mmol)化合物1-369。
Figure C9619770000903
制备实施例36(制备化合物1-391)
首先,混合32.3g 5-氨基-2-氯-4-氟苯酚和150ml浓盐酸,并将混合物在50℃下搅拌30分钟,然后在0℃下,于10分钟内滴加入15g亚硝酸钠的水(40ml)溶液。在0℃搅拌1小时后,冷却混合物至-50℃。然后,在-50℃下迅速滴加入132g氯化锡(II)的浓硫酸(132g)溶液,并将混合物逐渐温热至室温并搅拌1小时。过滤收集所形成的固体,并在80℃下减压干燥,得到75g粗制2-氟-4-氯-5-羟基苯肼盐酸盐结晶。
    1H-NMR(DMSO-d6,TMSδ(ppm))3-5(2H,br),6.73(1H,d),7.22(1H,
d),8.20(1H,s),9-11(2H,br)
然后,将49.2g乙酸钠和40.5g 1,1-二溴-3,3,3三氟丙酮溶于400ml水,并将此溶液在80-90℃下搅拌40分钟,然后冷却溶液至0℃,加入75g上面所制得的粗制2-氟-4-氯-5-羟基苯肼盐酸盐结晶,并将混合物在室温下搅拌70分钟。过滤收集沉淀结晶并减压干燥,得到35.4g 3,3,3-三氟-2-氧代丙醛1-(4-氯-2-氟-5-羟基苯腙)。
    1H-NMR(300MHz,CDCl3,TMSδ(ppm))5.49(1H,s),7.15(1H,d,J=10.5Hz),7.25(1H,d,J=7.4Hz),7.38(1H,q,J=1.8Hz),8.75(1H,s)
然后,将12.9g 3,3,3-三氟-2-氧代丙醛1-(4-氯-2-氟-5-羟基苯腙)和22.3g乙酯基亚乙基三苯基磷烷溶于110ml四氢呋喃中,并加热回流此溶液3小时。减压蒸除溶剂,所得残留物进行硅胶层析,得到8.8g 2-(2-氟-4-氯-5-羟基苯基)-4-甲基-5-三氟甲基哒嗪-3-酮(化合物1-391)。
Figure C9619770000921
上面所用的5-氨基-2-氯-4-氟苯酚可用欧洲专利申请公开,EP-61741-A中所述的方法制备。
制备实施例37(制备化合物1-332)
首先,将2g 3,3,3-三氟-2-氧代-1-丙醛1-(4-氯苯腙)和2g二乙基磷酰基乙酸乙酯与20ml三乙胺混合,并使反应在50℃进行24小时。减压蒸除溶剂,所得残留物进行柱层析,得到1.16g2-(4-氯苯基)-5-三氟甲基哒嗪-3-酮(化合物1-332)。
参考实施例5
制备实施例19中所制备的3,3,3-三氟-2-氧代丙醛1-(4-氯-2-氟-5-异丙氧基苯腙)也可以用下述方法制备。
Figure C9619770000922
首先,将20.1g 4,4,4-三氟乙酰乙酸乙酯和25g乙酸钠溶于150ml水中,在10℃或更低温度下滴加入重氮盐盐酸溶液[由20.3g 4-氯-2-氟-5-异丙氧基苯胺,20ml浓盐酸,20ml水和7.35g亚硝酸钠制得]。室温搅拌1小时后,过滤收集沉淀出的结晶,水洗,干燥,得到34g所需产物,为橙色晶体(收率,85%)。
然后,将15.9g上面所制得的酯和1.7g氢氧化锂一水合物加到30ml1,4-二噁烷和3ml水中,并加热回流混合物6小时。将反应混合物倒入冰水中,用稀盐酸中和,并用乙酸乙酯提取。干燥并浓缩乙酸乙酯层,并用己烷洗涤沉淀结晶,得到11.3g所需产物,为黄色结晶(收率,76.3%)。
随后,将7.4g上面所得的羧酸溶于42ml N,N-二甲基甲酰胺中,加热反应溶液至100℃,并在此温度下保持30分钟。尔后,冷却反应溶液至室温,倾入水中,用乙酸乙酯提取。将乙酸乙酯层用稀盐酸洗涤,硫酸镁干燥,并浓缩,得到5.9g所需产物,为橙色结晶(收率,90%)。
    1H-NMR(250MHz,CDCl3,TMSδ(ppm))1.39(6H,d,J=6.0Hz),
4.38-4.52(1H,m),7.15(1H,d,J=10.5Hz),7.22(1H,d,J=7.3Hz),7.43(1H,q,
J=1.7Hz),9.18(1H,br)
参考实施例6
采用与参考实施例2所述同样的方法,制备3,3,3-三氟-2-氧代丙醛4-氯苯腙。
Figure C9619770000941
首先,将5.0g酯原料和0.67g氢氧化锂一水合物加到含30ml 1,4-二噁烷和2ml水的混合溶液中,并加热回流混合物1.5小时。将反应混合物倒入冰水中,用稀盐酸中和,并用乙酸乙酯提取。乙酸乙酯层用硫酸镁干燥,浓缩,并用己烷和乙醚(己烷∶乙醚=2∶1)的混合溶剂洗涤沉淀结晶,得到3.3g所需产物,为黄色结晶(收率,73%)。
方法1)将3.3g上步反应制得的羧酸溶于10ml二甲亚砜中,加热此溶液至100℃,并在此温度下保持10分钟,接着冷却至室温。随后硅胶层析反应混合物(洗脱剂,己烷∶乙酸乙酯=7∶1),得到2.55g所需产物(收率,91%)。
方法2)将5.0g上步反应所制得的羧酸,0.5ml喹啉,和0.1g铜粉加到40ml甲苯中制得的反应混合物加热至100℃,并在此温度下保持20分钟。反应完成后,冷却反应混合物至室温,并进行硅胶层析(洗脱剂,己烷∶乙酸乙酯=8∶1),得到3.6g所需产物(收率,86%)。
本发明的一些化合物在表1-5中用它们各自的化合物编号示出。其中符号“n”表示“正-”;“i”表示“异-”;“s”表示“仲-”;和“c”表示“环-”。
                         表1
下式化合物:
Figure C9619770000951
    化合物 X    Y    R3    R1     R2    B编号
    1-1    H    F    H    CF2Cl    H      H1-2    H    Cl   H    CF2Cl    H      H1-3    H    Br   H    CF2Cl    H      H1-4    H    F    H    CF2Cl    CH3   H1-5    H    Cl   H    CF2Cl    CH3   H1-6    H    Br   H    CF2Cl    CH3   H1-7    F    F    H    CF2Cl    H      H1-8    F    Cl   H    CF2Cl    H      H1-9    F    Br   H    CF2Cl    H      H1-10   F    F    H    CF2Cl    CH3   H1-11   F    Cl   H    CF2Cl    CH3   H1-12   F    Br   H    CF2Cl    CH3   H1-13   H    F    H    CF2Cl    CH3   NO2
                             表1(续)
    化合物  X    Y     R3     R1     R2              B编号
    1-14    H    Cl    H    CF2Cl    CH3              NO21-15    H    Br    H    CF2Cl    CH3              NO21-16    F    F     H    CF2Cl    CH3              NO21-17    F    Cl    H    CF2Cl    CH3              NO21-18    F    Br    H    CF2Cl    CH3              NO21-19    H    F     H    CF2Cl    CH3              NH21-20    H    Cl    H    CF2Cl    CH3              NH21-21    H    Br    H    CF2Cl    CH3              NH21-22    F    F     H    CF2Cl    CH3              NH21-23    F    Cl    H    CF2Cl    CH3              NH21-24    F    Br    H    CF2Cl    CH3              NH21-25    H    F     H    CF2Cl    CH3              OH1-26    H    Cl    H    CF2Cl    CH3              OH1-27    H    Br    H    CF2Cl    CH3              OH1-28    F    F     H    CF2Cl    CH3              OH1-29    F    Cl    H    CF2Cl    CH3              OH1-30    F    Br    H    CF2Cl    CH3              OH1-31    H    Cl    H    CF2Cl    CH3    NHCH31-32    H    Cl    H    CF2Cl    CH3    NHC2H51-33    H    Cl    H    CF2Cl    CH3    NHCH2CH=CH21-34    H    Cl    H    CF2Cl    CH3    NHCH2C≡CH1-35    H    Cl    H    CF2Cl    CH3    NHCH(CH3)C≡CH1-36    H    Cl    H    CF2Cl    CH3    NHSO2CH3
                           表1(续)
  化合物  X    Y     R3   R1   R2        B编号
  1-37    H    Cl    H  CF2Cl  CH3    NHSO2C2H51-38    H    Cl    H  CF2Cl  CH3    NHSO2CH2Cl1-39    H    Cl    H  CF2Cl  CH3    NHSO2CF31-40    H    Cl    H  CF2Cl  CH3    N(CH3)SO2CH31-41    H    Cl    H  CF2Cl  CH3    N(CH2C≡CH)SO2CH31-42    H    Cl    H  CF2Cl  CH3    NHCOOCH31-43    H    Cl    H  CF2Cl  CH3    NHCOOC2H51-44    H    Cl    H  CF2Cl  CH3    NHCOOnC3H71-45    H    Cl    H  CF2Cl  CH3    NHCOOiC3H71-46    H    Cl    H  CF2Cl  CH3    NHCOOnC4H91-47    H    Cl    H  CF2Cl  CH3    NHCOOnC5H111-48    H    Cl    H  CF2Cl  CH3    NHCH2COOCH31-49    H    Cl    H  CF2Cl  CH3    NHCH2COOC2H51-50    H    Cl    H  CF2Cl  CH3    NHCH2COOnC3H71-51    H    Cl    H  CF2Cl  CH3    NHCH2COOnC4H91-52    H    Cl    H  CF2Cl  CH3    NHCH2COOnC5H111-53    H    Cl    H  CF2Cl  CH3    NHCH2COOiC3H71-54    H    Cl    H  CF2Cl  CH3    NHCH2COOcC5H91-55    H    Cl    H  CF2Cl  CH3    NHCH2COOcC6H111-56    H    Cl    H  CF2Cl  CH3    NHCH(CH3)COOCH31-57    H    Cl    H  CF2Cl  CH3    NHCH(CH3)COOC2H51-58    H    Cl    H  CF2Cl  CH3    NHCH(CH3)COOnC3H71-59    H    Cl    H  CF2Cl  CH3    NHCH(CH3)COOnC4H9
                            表1(续)
  化合物  X    Y     R3   R1   R2               B编号
  1-60    H    Cl    H  CF2Cl  CH3    NHCH(CH3)COOnC5H111-61    H    Cl    H  CF2Cl  CH3    NHCH(CH3)COOiC3H71-62    H    Cl    H  CF2Cl  CH3    NHCH(CH3)COOcC5H91-63    H    Cl    H  CF2Cl  CH3    NHCH(CH3)COOcC6H111-64    F    Cl    H  CF2Cl  CH3    NHCH31-65    F    Cl    H  CF2Cl  CH3    NHC2H51-66    F    Cl    H  CF2Cl  CH3    NHCH2CH=CH21-67    F    Cl    H  CF2Cl  CH3    NHCH2C≡CH1-68    F    Cl    H  CF2Cl  CH3    NHCH(CH3)C≡CH1-69    F    Cl    H  CF2Cl  CH3    NHSO2CH31-70    F    Cl    H  CF2Cl  CH3    NHSO2C2H51-71    F    Cl    H  CF2Cl  CH3    NHSO2CH2Cl1-72    F    Cl    H  CF2Cl  CH3    NHSO2CF31-73    F    Cl    H  CF2Cl  CH3    N(CH3)SO2CH31-74    F    Cl    H  CF2Cl  CH3    N(CH2C≡CH)SO2CH31-75    F    Cl    H  CF2Cl  CH3    NHCOOCH31-76    F    Cl    H  CF2Cl  CH3    NHCOOC2H51-77    F    Cl    H  CF2Cl  CH3    NHCOOnC3H71-78    F    Cl    H  CF2Cl  CH3    NHCOOiC3H71-79    F    Cl    H  CF2Cl  CH3    NHCOOnC4H91-80    F    Cl    H  CF2Cl  CH3    NHCOOnC5H111-81    F    Cl    H  CF2Cl  CH2    NHCH2COOCH31-82    F    Cl    H  CF2Cl  CH3    NHCH2COOC2H5
                               表1(续)
    化合物   X    X     R3   R1    R2           B编号
    1-83     F    Cl    H  CF2Cl  CH3    NHCH2COOnC3H71-84     F    Cl    H  CF2Cl  CH3    NHCH2COOnC4H91-85     F    Cl    H  CF2Cl  CH3    NHCH2COOnC5H111-86     F    Cl    H  CF2Cl  CH3    NHCH2COOiC3H71-87     F    Cl    H  CF2Cl  CH3    NHCH2COOcC5H91-88     F    Cl    H  CF2Cl  CH3    NH2CH2COOcC6H111-89     F    Cl    H  CF2Cl  CH3    NHCH(CH3)COOCH31-90     F    Cl    H  CF2Cl  CH3    NHCH(CH3)COOC2H51-91     F    Cl    H  CF2Cl  CH3    NHCH(CH3)COOnC3H71-92     F    Cl    H  CF2Cl  CH3    NHCH(CH3)COOnC4H91-93     F    Cl    H  CF2Cl  CH3    NHCH(CH3)COOnC5H111-94     F    Cl    H  CF2Cl  CH3    NHCH(CH3)COOiC3H71-95     F    Cl    H  CF2Cl  CH3    NHCH(CH3)COOcC5H91-96     F    Cl    H  CF2Cl  CH3    NHCH(CH3)COOcC6H111-97     H    Cl    H  CF2Cl  CH3    OCH31-98     H    Cl    H  CF2Cl  CH3    OC2H51-99     H    Cl    H  CF2Cl  CH3    OiC3H71-100    H    Cl    H  CF2Cl  CH3    OnC3H71-101    H    Cl    H  CF2Cl  CH3    OCH2CH2Cl1-102    H    Cl    H  CF2Cl  CH3    OCF2CF2H1-103    H    Cl    H  CF2Cl  CH3    OcC5H91-104    H    Cl    H  CF2Cl  CH3    OcC6H11
                                 表1(续)
  化合物   X    Y     R3  R1    R2           B编号
  1-105    H    Cl    H  CF2Cl  CH3    OCH2CH=CH21-106    H    Cl    H  CF2Cl  CH3    OCH2CCl=CH21-1O7    H    Cl    H  CF2Cl  CH3    OCH2CCl=CHCl1-108    H    Cl    H  CF2Cl  CH3    OCH(CH3)CH=CH21-109    H    Cl    H  CF2Cl  CH3    OCH2C≡CH1-110    H    Cl    H  CF2Cl  CH3    OCH(CH3)C≡CH1-111    H    Cl    H  CF2Cl  CH3    OCH2C≡CBr1-112    H    Cl    H  CF2Cl  CH3    OCH2C≡CCl1-113    H    Cl    H  CF2Cl  CH3    OCH2C≡CCH2Cl1-114    H    Cl    H  CF2Cl  CH3    OCH2CN1-115    H    Cl    H  CF2Cl  CH3    OCH2OCH31-116    H    Cl    H  CF2Cl  CH3    OCH2OC2H51-117    H    Cl    H  CF2Cl  CH3    OCH2SCH31-118    H    Cl    H  CF2Cl  CH3    OCH2COOCH31-119    H    Cl    H  CF2Cl  CH3    OCH2COOC2H51-120    H    Cl    H  CF2Cl  CH3    OCH2COOnC3H71-121    H    Cl    H  CF2Cl  CH3    OCH2COOnC4H91-122    H    Cl    H  CF2Cl  CH3    OCH2COOnC5H111-123    H    Cl    H  CF2Cl  CH3    OCH2COOiC3H71-124    H    Cl    H  CF2Cl  CH3    OCH2COOcC5H91-125    H    Cl    H  CF2Cl  CH3    OCH2COOcC6H111-126    H    Cl    H  CF2Cl  CH3    OCH(CH3)COOCH21-127    H    Cl    H  CF2Cl  CH3    OCH(CH3)COOC2H5
                             表1(续)
  化合物   X    Y     R3  R1    R2              B编号
  1-128    H    Cl    H  CF2Cl  CH3    OCH(CH3)COOnC3H71-129    H    Cl    H  CF2Cl  CH3    OCH(CH3)COOnC4H91-130    H    Cl    H  CF2Cl  CH3    OCH(CH3)COOnC5H111-131    H    Cl    H  CF2Cl  CH3    OCH(CH3)COOiC3H71-132    H    Cl    H  CF2Cl  CH3    OCH(CH3)COOcC5H91-133    H    Cl    H  CF2Cl  CH3    OCH(CH3)COOcC6H111-134    H    Cl    H  CF2Cl  CH3    OCH2CON(CH3)21-135    H    Cl    H  CF2Cl  CH3    OCH2CON(C2H5)21-136    H    Cl    H  CF2Cl  CH3    OCH2CON(CH3)C2H51-137    H    Cl    H  CF2Cl  CH3    OCH(CH3)CON(CH3)21-138    H    Cl    H  CF2Cl  CH3    OCH(CH3)CON(C2H5)21-139    H    Cl    H  CF2Cl  CH3    OCH(CH3)CON(CH3)C2H51-140    H    Cl    H  CF2Cl  CH3    OCH2COON(CH3)21-141    H    Cl    H  CF2Cl  CH3    OCH2COON(C2H5)21-142    H    Cl    H  CF2Cl  CH3    OCH(CH3)COON(CH3)21-143    H    Cl    H  CF2Cl  CH3    OCH(CH3)COON(C2H5)21-144    F    Cl    H  CF2Cl  CH3    OCH31-145    F    Cl    H  CF2Cl  CH3    OC2H51-146    F    Cl    H  CF2Cl  CH3    OiC3H71-147    F    Cl    H  CF2Cl  CH3    OnC3H71-148    F    Cl    H  CF2Cl  CH3    OCH2CH2Cl1-149    F    Cl    H  CF2Cl  CH3    OCF2CF2H1-150    F    Cl    H  CF2Cl  CH3    OcC6H9
                                     表1(续)
  化合物   X    Y     R3  R1    R2             B编号
  1-151    F    Cl    H  CF2Cl  CH3    OcC6H111-152    F    Cl    H  CF2Cl  CH3    OCH2CH2=CH21-153    F    Cl    H  CF2Cl  CH3    OCH2CCl=CH21-154    F    Cl    H  CF2Cl  CH3    OCH2CCl=CHCl1-155    F    Cl    H  CF2Cl  CH3    OCH(CH3)CH=CH21-156    F    Cl    H  CF2Cl  CH3    OCH2C≡CH1-157    F    Cl    H  CF2Cl  CH3    OCH(CH3)C≡CH1-158    F    Cl    H  CF2Cl  CH3    OCH2C≡CBr1-159    F    Cl    H  CF2Cl  CH3    OCH2C≡CCl1-160    F    Cl    H  CF2Cl  CH3    OCH2C≡CCH2Cl1-161    F    Cl    H  CF2Cl  CH3    OCH2CN1-162    F    Cl    H  CF2Cl  CH3    OCH2OCH31-163    F    Cl    H  CF2Cl  CH3    OCH2OC2H51-164    F    Cl    H  CF2Cl  CH3    OCH2SCH31-165    F    Cl    H  CF2Cl  CH3    OCH2COOCH31-166    F    Cl    H  CF2Cl  CH3    OCH2COOC2H51-167    F    Cl    H  CF2Cl  CH3    OCH2COOnC3H71-168    F    Cl    H  CF2Cl  CH3    OCH2COOnC4H91-169    F    Cl    H  CF2Cl  CH3    OCH2COOnC5H111-170    F    Cl    H  CF2Cl  CH3    OCH2COOiC3H71-171    F    Cl    H  CF2Cl  CH3    OCH2COOcC5H91-172    F    Cl    H  CF2Cl  CH3    OCH2COOcC6H111-173    F    Cl    H  CF2Cl  CH3    OCH(CH3)COOCH3
                                表1(续)
    化合物   X    Y     R3  R1    R2              B编号
    1-174    F    Cl    H  CF2Cl  CH3    OCH(CH3)COOC2H51-175    F    Cl    H  CF2Cl  CH3    OCH(CH3)COOnC3H71-176    F    Cl    H  CF2Cl  CH3    OCH(CH3)COOnC4H91-177    F    Cl    H  CF2Cl  CH3    OCH(CH3)COOnC5H111-178    F    Cl    H  CF2Cl  CH3    OCH(CH3)COOiC3H71-179    F    Cl    H  CF2Cl  CH3    OCH(CH3)COOcC5H91-180    F    Cl    H  CF2Cl  CH3    OCH(CH3)COOcC6H111-181    F    Cl    H  CF2Cl  CH3    OCH2CON(CH3)21-182    F    Cl    H  CF2Cl  CH3    OCH2CON(C2H5)21-183    F    Cl    H  CF2Cl  CH3    OCH2CON(CH3)C2H51-184    F    Cl    H  CF2Cl  CH3    OCH(CH3)CON(CH3)21-185    F    Cl    H  CF2Cl  CH3    OCH(CH3)CON(C2H5)21-186    F    Cl    H  CF2Cl  CH3    OCH(CH3)CON(CH3)C2H51-187    F    Cl    H  CF2Cl  CH3    OCH2COON(CH3)21-188    F    Cl    H  CF2Cl  CH3    OCH2COON(C2H5)21-189    F    Cl    H  CF2Cl  CH3    OCH(CH3)COON(CH3)21-190    F    Cl    H  CF2Cl  CH3    OCH(CH3)COON(C2H5)21-191    H    F     H  CF2Cl  CH3    SH1-192    H    Cl    H  CF2Cl  CH3    SH1-193    H    Br    H  CF2Cl  CH3    SH1-194    F    F     H  CF2Cl  CH3    SH1-195    F    Cl    H  CF2Cl  CH3    SH1-196    F    Br    H  CF2Cl  CH3    SH
                              表1(续)
    化合物   X    Y     R3  R1    R2          B编号
    1-197    H    Cl    H  CF2Cl  CH3    SCH31-198    H    Cl    H  CF2Cl  CH3    SC2H51-199    H    Cl    H  CF2Cl  CH3    SiC3H71-200    H    Cl    H  CF2Cl  CH3    SCH2CH2Cl1-201    H    Cl    H  CF2Cl  CH3    ScC5H91-202    H    Cl    H  CF2Cl  CH3    ScC6H111-203    H    Cl    H  CF2Cl  CH3    SCH2CH=CH21-204    H    Cl    H  CF2Cl  CH3    SCH2CCl=CH21-205    H    Cl    H  CF2Cl  CH3    SCH2CCl=CHCl1-206    H    Cl    H  CF2Cl  CH3    SCH(CH3)CH=CH21-207    H    Cl    H  CF2Cl  CH3    SCH2C≡CH1-208    H    Cl    H  CF2Cl  CH3    SCH(CH3)C≡CH1-209    H    Cl    H  CF2Cl  CH3    SCH2COOCH31-210    H    Cl    H  CF2Cl  CH3    SCH2COOC2H51-211    H    Cl    H  CF2Cl  CH3    SCH2COOnC3H71-212    H    Cl    H  CF2Cl  CH3    SCH2COOnC4H91-213    H    Cl    H  CF2Cl  CH3    SCH2COOnC5H111-214    H    Cl    H  CF2Cl  CH3    SCH2COOiC3H71-215    H    Cl    H  CF2Cl  CH3    SCH2COOcC5H91-216    H    Cl    H  CF2Cl  CH3    SCH2COOcC6H111-217    H    Cl    H  CF2Cl  CH3    SCH(CH3)COOCH31-218    H    Cl    H  CF2Cl  CH3    SCH(CH3)COOC2H5
                             表1(续)
    化合物   X    Y     R3   R1   R2            B编号
    1-219    H    Cl    H  CF2Cl  CH3    SCH(CH3)COOnC3H71-220    H    Cl    H  CF2Cl  CH3    SCH(CH3)COOnC4H91-221    H    Cl    H  CF2Cl  CH3    SCH(CH3)COOnC5H111-222    H    Cl    H  CF2Cl  CH3    SCH(CH3)COOiC3H71-223    H    Cl    H  CF2Cl  CH3    SCH(CH3)COOcC5H91-224    H    Cl    H  CF2Cl  CH3    SCH(CH3)COOcC6H111-225    H    Cl    H  CF2Cl  CH3    SCH2CON(CH3)21-226    H    Cl    H  CF2Cl  CH3    SCH2CON(C2H5)21-227    H    Cl    H  CF2Cl  CH3    SCH2CON(四亚甲基)1-228    H    Cl    H  CF2Cl  CH3    SCH2CON(五亚甲基)1-229    H    Cl    H  CF2Cl  CH3    SCH2CON(3-氧杂-1,5-亚戊基)1-230    H    Cl    H  CF2Cl  CH3    SCH(CH3)CON(CH3)21-231    H    Cl    H  CF2Cl  CH3    SCH(CH3)CON(C2H5)21-232    H    Cl    H  CF2Cl  CH3    SCH(CH3)CON(四亚甲基)1-233    H    Cl    H  CF2Cl  CH3    SCH(CH3)CON(五亚甲基)1-234    F    Cl    H  CF2Cl  CH3    SCH31-235    F    Cl    H  CF2Cl  CH3    SC2H51-236    F    Cl    H  CF2Cl  CH3    SiC3H71-237    F    Cl    H  CF2Cl  CH3    SCH2CH2Cl1-238    F    Cl    H  CF2Cl  CH3    ScC5H9
                               表1(续)
    化合物   X    Y     R3   R1    R2           B编号
    1-239    F    Cl    H  CF2Cl  CH3    ScC6H111-240    F    Cl    H  CF2Cl  CH3    SCH2CH=CH21-241    F    Cl    H  CF2Cl  CH3    SCH2CCl=CH21-242    F    Cl    H  CF2Cl  CH3    SCH2CCl=CHCl1-243    F    Cl    H  CF2Cl  CH3    SCH(CH3)CH=CH21-244    F    Cl    H  CF2Cl  CH3    SCH2C≡CH1-245    F    Cl    H  CF2Cl  CH3    SCH(CH3)C≡CH1-246    F    Cl    H  CF2Cl  CH3    SCH2COOCH3 -1-247    F    Cl    H  CF2Cl  CH3    SCH2COOC2H51-248    F    Cl    H  CF2Cl  CH3    SCH2COOnC3H71-249    F    Cl    H  CF2Cl  CH3    SCH2COOnC4H91-250    F    Cl    H  CF2Cl  CH3    SCH2COOnC5H111-251    F    Cl    H  CF2Cl  CH3    SCH2COOiC3H71-252    F    Cl    H  CF2Cl  CH3    SCH2COOcC5H91-253    F    Cl    H  CF2Cl  CH3    SCH2COOcC6H111-254    F    Cl    H  CF2Cl  CH3    SCH(CH3)COOCH31-255    F    Cl    H  CF2Cl  CH3    SCH(CH3)COOC2H51-256    F    Cl    H  CF2Cl  CH3    SCH(CH3)COOnC3H71-257    F    Cl    H  CF2Cl  CH3    SCH(CH3)COOnC4H91-258    F    Cl    H  CF2Cl  CH3    SCH(CH3)COOnC5H111-259    F    Cl    H  CF2Cl  CH3    SCH(CH3)COOiC3H71-260    F    Cl    H  CF2Cl  CH3    SCH(CH3)COOcC5H91-261    F    Cl    H  CF2Cl  CH3    SCH(CH3)COOcC6H11
                              表1(续)
    化合物    X    Y    R3   R1    R2          B编号
    1-262    F    Cl    H  CF2Cl  CH3    SCH2CON(CH3)21-263    F    Cl    H  CF2Cl  CH3    SCH2CON(C2H5)21-264    F    Cl    H  CF2Cl  CH3    SCH2CON(四亚甲基)1-265    F    Cl    H  CF2Cl  CH3    SCH2CON(五亚甲基)1-266    F    Cl    H  CF2Cl  CH3    SCH2CON(3-氧杂-1,5-亚戊基)1-267    F    Cl    H  CF2Cl  CH3    SCH(CH3)CON(CH3)21-268    F    Cl    H  CF2Cl  CH3    SCH(CH3)CON(C2H5)21-269    F    Cl    H  CF2Cl  CH3    SCH(CH3)CON(四亚甲基)1-270    F    Cl    H  CF2Cl  CH3    SCH(CH3)CON(五亚甲基)1-271    H    F     H  CF2Cl  CH3    SO2Cl1-272    H    Cl    H  CF2Cl  CH3    SO2Cl1-273    H    Br    H  CF2Cl  CH3    SO2Cl1-274    F    F     H  CF2Cl  CH3    SO2Cl1-275    F    Cl    H  CF2Cl  CH3    SO2Cl1-276    F    Br    H  CF2Cl  CH3    SO2Cl1-277    H    Cl    H  CF2Cl  CH3    SO2OCH31-278    H    Cl    H  CF2Cl  CH3    SO2OC2H51-279    H    Cl    H  CF2Cl  CH3    SO2OiC3H71-280    H    Cl    H  CF2Cl  CH3    SO2OCH2CH=CH21-281    F    Cl    H  CF2Cl  CH3    SO2OCH3
                           表1(续)
    化合物   X    Y     R3  R1     R2         B编号
    1-282    F    Cl    H  CF2Cl  CH3    SO2OC2H51-283    F    Cl    H  CF2Cl  CH3    SO2OiC3H71-284    F    Cl    H  CF2Cl  CH3    SO2OCH2CH=CH21-285    H    Cl    H  CF2Cl  CH3    SO2N(CH3)21-286    H    Cl    H  CF2Cl  CH3    SO2N(C2H5)21-287    F    Cl    H  CF2Cl  CH3    SO2N(CH3)21-288    F    Cl    H  CF2Cl  CH3    SO2N(C2H5)21-289    H    Cl    H  CF2Cl  CH3    COOH1-290    H    Cl    H  CF2Cl  CH3    COOCH31-291    H    Cl    H  CF2Cl  CH3    COOC2H51-292    H    Cl    H  CF2Cl  CH3    COOnC3H71-293    H    Cl    H  CF2Cl  CH3    COOnC4H91-294    H    Cl    H  CF2Cl  CH3    COOnC5H111-295    H    Cl    H  CF2Cl  CH3    COOiC5H71-296    H    Cl    H  CF2Cl  CH3    COOCH2CH2Cl1-297    H    Cl    H  CF2Cl  CH3    COOCH2CH2Br1-298    H    Cl    H  CF2Cl  CH3    CON(CH3)21-299    H    Cl    H  CF2Cl  CH3    CONHCH31-300    H    Cl    H  CF2Cl  CH3    CON(C2H5)21-301    H    Cl    H  CF2Cl  CH3    CONHC2H51-302    H    Cl    H  CF2Cl  CH3    COCH31-303    H    Cl    H  CF2Cl  CH3    COC2H51-304    H    Cl    H  CF2Cl  CH3    COCH2Cl
                            表1(续)
    化合物   X    Y     R3  R1    R2             B编号
    1-305    H    Cl    H  CF2Cl  CH3    CHO1-306    H    Cl    H  CF2Cl  CH3    CH=CHCOOCH31-307    H    Cl    H  CF2Cl  CH3    CH=CHCOOC2H51-308    H    Cl    H  CF2Cl  CH3    CH2CH2COOCH31-309    H    Cl    H  CF2Cl  CH3    CH2CH2COOC2H51-310    F    Cl    H  CF2Cl  CH3    COOH1-311    F    Cl    H  CF2Cl  CH3    COOCH31-312    F    Cl    H  CF2Cl  CH3    COOC2H51-313    F    Cl    H  CF2Cl  CH3    COOnC3H71-314    F    Cl    H  CF2Cl  CH3    COOnC4H91-315    F    Cl    H  CF2Cl  CH3    COOnC5H111-316    F    Cl    H  CF2Cl  CH3    COOiC3H71-317    F    Cl    H  CF2Cl  CH3    COOCH2CH2Cl1-318    F    Cl    H  CF2Cl  CH3    COOCH2CH2Br1-319    F    Cl    H  CF2Cl  CH3    CON(CH3)21-320    F    Cl    H  CF2Cl  CH3    CONHCH31-321    F    Cl    H  CF2Cl  CH3    CON(C2H5)21-322    F    Cl    H  CF2Cl  CH3    CONHC2H51-323    F    Cl    H  CF2Cl  CH3    COCH31-324    F    Cl    H  CF2Cl  CH3    COC2H51-325    F    Cl    H  CF2Cl  CH3    COCH2Cl1-326    F    Cl    H  CF2Cl  CH3    CHO
                        表1(续)
    化合物   X    Y     R3    R1    R2          B编号
    1-327    F    Cl    H    CF2Cl  CH3    CH=CHCOOCH31-328    F    Cl    H    CF2Cl  CH3    CH=CHCOOC2H51-329    F    Cl    H    CF2Cl  CH3    CH2CH2COOCH31-330    F    Cl    H    CF2Cl  CH3    CH2CH2COOC2H51-331    H    F     H    CF3    H       H1-332    H    Cl    H    CF3    H       H1-333    H    Br    H    CF3    H       H1-334    H    F     H    CF3    CH3    H1-335    H    Cl    H    CF3    CH3    H1-336    H    Br    H    CF3    CH3    H1-337    F    F     H    CF3    H       H1-338    F    Cl    H    CF3    H       H1-339    F    Br    H    CF3    H       H1-340    F    F     H    CF3    CH3    H1-341    F    Cl    H    CF3    CH3    H1-342    F    Br    H    CF3    CH3    H1-343    H    F     H    CF3    CH3    NO21-344    H    Cl    H    CF3    CH3    NO21-345    H    Br    H    CF3    CH3    NO21-346    F    F     H    CF3    CH3    NO21-347    F    Cl    H    CF3    CH3    NO21-348    F    Br    H    CF3    CH3    NO21-349    H    F     H    CF3    CH3    NH2
                                    表1(续)
  化合物   X     Y    R3    R1    R2      B编号
  1-350    H    Cl    H    CF3    CH3    NH21-351    H    Br    H    CF3    CH3    NH21-352    F    F     H    CF3    CH3    NH21-353    F    Cl    H    CF3    CH3    NH21-354    H    Cl    H    CF3    CH3    NHCH(CH3)COOCH31-355    H    Cl    H    CF3    CH3    NHCH(CH3)COOC2H51-356    H    Cl    H    CF3    CH3    NHCH(CH3)COOnC3H71-357    H    Cl    H    CF3    CH3    NHCH(CH3)COOnC4H91-358    H    Cl    H    CF3    CH3    NHCH(CH3)COOnC5H111-359    H    Cl    H    CF3    CH3    NHCH(CH3)COOiC3H71-360    H    Cl    H    CF3    CH3    NHCH(CH3)COOcC5H91-361    H    Cl    H    CF3    CH3    NHCH(CH3)COOcC6H111-362    F    Cl    H    CF3    CH3    NHCH31-363    F    Cl    H    CF3    CH3    NHC2H51-364    F    Cl    H    CF3    CH3    NHCH2CH=CH21-365    F    Cl    H    CF3    CH3    NHCH2C≡CH1-366    F    Cl    H    CF3    CH3    NHCH(CH3)C≡CH1-367    F    Cl    H    CF3    CH3    NHSO2CH31-368    F    Cl    H    CF3    CH3    NHSO2C2H51-369    F    Cl    H    CF3    CH3    NHSO2CH2Cl1-370    F    C1    H    CF3    CH3    NHSO2CF31-371    F    C1    H    CF3    CH3    N(CH3)SO2CH31-372    F    Cl    H    CF3    CH3    N(CH2C≡CH)SO2CH3
                                 表1(续)
    化合物   X    Y     R3   R1     R2        B编号
    1-373    F    Cl    H    CF3    CH3    NHCOOCH31-374    F    Cl    H    CF3    CH3    NHCOOC2H51-375    F    Cl    H    CF3    CH3    NHCOOnC3H71-376    F    Cl    H    CF3    CH3    NHCOOiC3H71-377    F    Cl    H    CF3    CH3    NHCOOnC4H91-378    F    Cl    H    CF3    CH3    NHCOOnC5H111-379    F    Cl    H    CF3    CH3    NHCH2COOCH31-380    F    Cl    H    CF3    CH3    NHCH2COOC2H51-381    F    Cl    H    CF3    CH3    NHCH2COOnC3H71-382    F    Cl    H    CF3    CH3    NHCH2COOnC4H91-383    F    Cl    H    CF3    CH3    NHCH2COOnC5H111-384    F    Cl    H    CF3    CH3    NHCH2COOiC3H71-385    F    Cl    H    CF3    CH3    NHCH2COOcC5H91-386    F    Br    H    CF3    CH3    NH21-387    H    F     H    CF3    CH3    OH1-388    H    Cl    H    CF3    CH3    OH1-389    H    Br    H    CF3    CH3    OH1-390    F    F     H    CF3    CH3    OH1-391    F    Cl    H    CF3    CH3    OH1-392    F    Br    H    CF3    CH3    OH1-393    H    Cl    H    CF3    CH3    NHCH31-394    H    Cl    H    CF3    CH3    NHC2H51-395    H    Cl    H    CF3    CH3    NHCH2CH=CH2
                                  表1(续)
    化合物   X    Y     R3    R1    R2          B编号
    1-396    H    Cl    H    CF3    CH3    NHCH2C≡CH1-397    H    Cl    H    CF3    CH3    NHCH(CH3)C≡CH1-398    H    Cl    H    CF3    CH3    NHSO2CH31-399    H    Cl    H    CF3    CH3    NHSO2C2H51-400    H    Cl    H    CF3    CH3    NHSO2CH2Cl1-401    H    Cl    H    CF3    CH3    NHSO2CF31-402    H    Cl    H    CF3    CH3    N(CH3)SO2CH31-403    H    Cl    H    CF3    CH3    N(CH2C≡CH)SO2CH31-404    H    Cl    H    CF3    CH3    NHCOOCH31-405    H    Cl    H    CF3    CH3    NHCOOC2H51-406    H    Cl    H    CF3    CH3    NHCOOnC3H71-407    H    Cl    H    CF3    CH3    NHCOOiC3H71-408    H    Cl    H    CF3    CH3    NHCOOnC4H91-409    H    Cl    H    CF3    CH3    NHCOOnC5H111-410    H    Cl    H    CF3    CH3    NHCH2COOCH31-411    H    Cl    H    CF3    CH3    NHCH2COOC2H51-412    H    Cl    H    CF3    CH3    NHCH2COOnC3H71-413    H    Cl    H    CF3    CH3    NHCH2COOnC4H91-414    H    Cl    H    CF3    CH3    NHCH2COOnC5H111-415    H    Cl    H    CF3    CH3    NHCH2COOiC3H71-416    H    Cl    H    CF3    CH3    NHCH2COOcC5H91-417    H    Cl    H    CF3    CH3    NHCH2COOcC6H111-418    F    Cl    H    CF3    CH3    NHCH2COOcC6H11
                          表1(续)
    化合物   X    Y     R3   R1     R2               B编号
    1-419    F    Cl    H    CF3    CH3    NHCH(CH3)COOCH31-420    F    Cl    H    CF3    CH3    NHCH(CH3)COOC2H51-421    F    Cl    H    CF3    CH3    NHCH(CH3)COOnC3H71-422    F    Cl    H    CF3    CH3    NHCH(CH3)COOnC4H91-423    F    Cl    H    CF3    CH3    NHCH(CH3)COOnC5H111-424    F    Cl    H    CF3    CH3    NHCH(CH3)COOiC3H71-425    F    Cl    H    CF3    CH3    NHCH(CH3)COOcC5H91-426    F    Cl    H    CF3    CH3    NHCH(CH3)COOcC6H111-427    H    Cl    H    CF3    CH3    OCH31-428    H    Cl    H    CF3    CH3    OC2H51-429    H    Cl    H    CF3    CH3    OiC3H71-430    H    Cl    H    CF3    CH3    OnC3H71-431    H    Cl    H    CF3    CH3    OCH2CH2Cl1-432    H    Cl    H    CF3    CH3    OCF2CF2H1-433    H    Cl    H    CF3    CH3    OcC5H91-434    H    Cl    H    CF3    CH3    OcC6H111-435    H    Cl    H    CF3    CH3    OCH2CH=CH21-436    H    Cl    H    CF3    CH3    OCH2CCl=CH21-437    H    Cl    H    CF3    CH3    OCH2CCl=CHCl1-438    H    Cl    H    CF3    CH3    OCH(CH3)CH=CH21-439    H    Cl    H    CF3    CH3    OCH2C≡CH1-440    H    Cl    H    CF3    CH3    OCH(CH3)C≡CH
                              表1(续)
    化合物   X    Y     R3   R1     R2         B编号
    1-441    H    Cl    H    CF3    CH3    OCH2C≡CBr1-442    H    Cl    H    CF3    CH3    OCH2C≡CCl1-443    H    Cl    H    CF3    CH3    OCH2C≡CCH2Cl1-444    H    Cl    H    CF3    CH3    OCH2CN1-445    H    Cl    H    CF3    CH3    OCH2OCH31-446    H    Cl    H    CF3    CH3    OCH2OC2H51-447    H    Cl    H    CF3    CH3    OCH2SCH31-448    H    Cl    H    CF3    CH3    OCH2COOCH31-449    H    Cl    H    CF3    CH3    OCH2COOC2H51-450    H    Cl    H    CF3    CH3    OCH2COOnC3H71-451    H    Cl    H    CF3    CH3    OCH2COOnC4H91-452    H    Cl    H    CF3    CH3    OCH2COOnC5H111-453    H    Cl    H    CF3    CH3    OCH2COOiC3H71-454    H    Cl    H    CF3    CH3    OCH2COOcC5H91-455    H    Cl    H    CF3    CH3    OCH2COOcC6H111-456    H    Cl    H    CF3    CH3    OCH(CH3)COOCH31-457    H    Cl    H    CF3    CH3    OCH(CH3)COOC2H51-458    H    Cl    H    CF3    CH3    OCH(CH3)COOnC3H71-459    H    Cl    H    CF3    CH3    OCH(CH3)COOnC4H91-460    H    Cl    H    CF3    CH3    OCH(CH3)COOnC5H111-461    H    Cl    H    CF3    CH3    OCH(CH3)COOiC3H71-462    H    Cl    H    CF3    CH3    OCH(CH3)COOcC5H91-463    H    Cl    H    CF3    CH3    OCH(CH3)COOcC6H11
                           表1(续)
    化合物   X     Y    R3   R1     R2          B编号
    1-464    H    Cl    H    CF3    CH3    OCH2CON(CH3)21-465    H    Cl    H    CF3    CH3    OCH2CON(C2H5)21-466    H    Cl    H    CF3    CH3    OCH2CON(CH3)C2H51-467    H    Cl    H    CF3    CH3    OCH(CH3)CON(CH3)21-468    H    Cl    H    CF3    CH3    OCH(CH3)CON(C2H5)21-469    H    Cl    H    CF3    CH3    OCH(CH3)CON(CH3)C2H51-470    H    Cl    H    CF3    CH3    OCH2COON(CH3)21-471    H    Cl    H    CF3    CH3    OCH2COON(C2H5)21-472    H    Cl    H    CF3    CH3    OCH(CH3)COON(CH3)21-473    H    Cl    H    CF3    CH3    OCH(CH3)COON(C2H5)21-474    F    Cl    H    CF3    CH3    OCH31-475    F    Cl    H    CF3    CH3    OC2H51-476    F    Cl    H    CF3    CH3    OiC3H71-477    F    Cl    H    CF3    CH3    OnC3H71-478    F    Cl    H    CF3    CH3    OCH2CH2Cl1-479    F    Cl    H    CF3    CH3    OCF2CF2H1-480    F    Cl    H    CF3    CH3    OcC5H91-481    F    Cl    H    CF3    CH3    OcC6H111-482    F    Cl    H    CF3    CH3    OCH2CH=CH21-483    F    Cl    H    CF3    CH3    OCH2CCl=CH21-484    F    Cl    H    CF3    CH3    OCH2CCl=CHCl1-485    F    Cl    H    CF3    CH3    OCH(CH3)CH=CH21-486    F    Cl    H    CF2    CH3    OCH2C≡CH
                                 表1(续)
    化合物   X     Y    R3   R1     R2            B编号
    1-487    F    Cl    H    CF3    CH3    OCH(CH3)C≡CH1-488    F    Cl    H    CF3    CH3    OCH2C≡CBr1-489    F    Cl    H    CF3    CH3    OCH2C≡CCl1-490    F    Cl    H    CF3    CH3    OCH2C≡CCH2Cl1-491    F    Cl    H    CF3    CH3    OCH2CN1-492    F    Cl    H    CF3    CH3    OCH2OCH31-493    F    Cl    H    CF3    CH3    OCH2OC2H51-494    F    Cl    H    CF3    CH3    OCH2SCH31-495    F    Cl    H    CF3    CH3    OCH2COOCH31-496    F    Cl    H    CF3    CH3    OCH2COOC2H51-497    F    Cl    H    CF3    CH3    OCH2COOnC3H71-498    F    Cl    H    CF3    CH3    OCH2COOnC4H91-499    F    Cl    H    CF3    CH3    OCH2COOnC5H111-500    F    Cl    H    CF3    CH3    OCH2COOiC3H71-501    F    Cl    H    CF3    CH3    OCH2COOcC5H91-502    F    Cl    H    CF3    CH3    OCH2COOcC6H111-503    F    Cl    H    CF3    CH3    OCH(CH3)COOCH31-504    F    Cl    H    CF3    CH3    OCH(CH3)COOC2H51-505    F    Cl    H    CF3    CH3    OCH(CH3)COOnC3H71-506    F    Cl    H    CF3    CH3    OCH(CH3)COOnC4H91-507    F    Cl    H    CF3    CH3    OCH(CH3)COOnC5H111-508    F    Cl    H    CF3    CH3    OCH(CH3)COOiC3H71-509    F    Cl    H    CF3    CH3    OCH(CH3)COOcC5H9
                                表1(续)
  化合物   X    Y     R3   R1     R2             B编号
  1-510    F    Cl    H    CF3    CH3    OCH(CH3)COOcC6H111-511    F    Cl    H    CF3    CH3    OCH2CON(CH3)21-512    F    Cl    H    CF3    CH3    OCH2CON(C2H5)21-513    F    Cl    H    CF3    CH3    OCH2CON(CH3)C2H51-514    F    Cl    H    CF3    CH3    OCH(CH3)CON(CH3)21-515    F    Cl    H    CF3    CH3    OCH(CH3)CON(C2H5)21-516    F    Cl    H    CF3    CH3    OCH(CH3)CON(CH3)C2H51-517    F    Cl    H    CF3    CH3    OCH2COON(CH3)21-518    F    Cl    H    CF3    CH3    OCH2COON(C2H5)21-519    F    Cl    H    CF3    CH3    OCH(CH3)COON(CH3)21-520    F    Cl    H    CF3    CH3    OCH(CH3)COON(C2H5)21-521    H    F     H    CF3    CH3    SH1-522    H    Cl    H    CF3    CH3    SH1-523    H    Br    H    CF3    CH3    SH1-524    F    F     H    CF3    CH3    SH1-525    F    Cl    H    CF3    CH3    SH1-526    F    Br    H    CF3    CH3    SH1-527    H    Cl    H    CF3    CH3    SCH31-528    H    Cl    H    CF3    CH3    SC2H51-529    H    Cl    H    CF3    CH3    SiC3H71-530    H    Cl    H    CF3    CH3    SCH2CH2Cl1-531    H    Cl    H    CF3    CH3    ScC5H91-532    H    Cl    H    CF3    CH3    ScC6H11
                             表1(续)
    化合物   X    Y     R3   R1     R2            B编号
    1-533    H    Cl    H    CF3    CH3    SCH2CH=CH21-534    H    Cl    H    CF3    CH3    SCH2CCl=CH21-535    H    Cl    H    CF3    CH3    SCH2CCl=CHCl1-536    H    Cl    H    CF3    CH3    SCH(CH3)CH=CH21-537    H    Cl    H    CF3    CH3    SCH2C≡CH1-538    H    Cl    H    CF3    CH3    SCH(CH3)C≡CH1-539    H    Cl    H    CF3    CH3    SCH2COOCH31-540    H    Cl    H    CF3    CH3    SCH2COOC2H51-541    H    Cl    H    CF3    CH3    SCH2COOnC3H71-542    H    Cl    H    CF3    CH3    SCH2COOnC4H91-543    H    Cl    H    CF3    CH3    SCH2COOnC5H111-544    H    Cl    H    CF3    CH3    SCH2COOiC3H71-545    H    Cl    H    CF3    CH3    SCH2COOcC5H91-546    H    Cl    H    CF3    CH3    SCH2COOcC6H111-547    H    Cl    H    CF3    CH3    SCH(CH3)COOCH31-548    H    Cl    H    CF3    CH3    SCH(CH3)COOC2H51-549    H    Cl    H    CF3    CH3    SCH(CH3)COOnC3H71-550    H    Cl    H    CF3    CH3    SCH(CH3)COOnC4H91-551    H    Cl    H    CF3    CH3    SCH(CH3)COOnC5H111-552    H    Cl    H    CF3    CH3    SCH(CH3)COOiC3H71-553    H    Cl    H    CF3    CH3    SCH(CH3)COOcC5H91-554    H    Cl    H    CF3    CH3    SCH(CH3)COOcC6H11
                             表1(续)
    化合物   X    Y     R3    R1    R2             B编号
    1-555    H    Cl    H    CF3    CH3    SCH2CON(CH3)21-556    H    Cl    H    CF3    CH3    SCH2CON(C2H5)21-557    H    Cl    H    CF3    CH3    SCH2CON(四亚甲基)1-558    H    Cl    H    CF3    CH3    SCH2CON(五亚甲基)1-559    H    Cl    H    CF3    CH3    SCH2CON(3-氧杂-1,5-亚戊基)1-560    H    Cl    H    CF3    CH3    SCH(CH3)CON(CH3)21-561    H    Cl    H    CF3    CH3    SCH(CH3)CON(C2H5)21-562    H    Cl    H    CF3    CH3    SCH(CH3)CON(四亚甲基)1-563    H    Cl    H    CF3    CH3    SCH(CH3)CON(五亚甲基)1-564    F    Cl    H    CF3    CH3    SCH31-565    F    Cl    H    CF3    CH3    SC2H51-566    F    Cl    H    CF3    CH3    SiC3H71-567    F    Cl    H    CF3    CH3    SCH2CH2Cl1-568    F    Cl    H    CF3    CH3    ScC5H91-569    F    Cl    H    CF3    CH3    ScC6H111-570    F    Cl    H    CF3    CH3    SCH2CH=CH21-571    F    Cl    H    CF3    CH3    SCH2CCl=CH21-572    F    Cl    H    CF3    CH3    SCH2CCl=CHCl1-573    F    Cl    H    CF3    CH3    SCH(CH3)CH=CH21-574    F    Cl    H    CF3    CH3    SCH2C≡CH
                             表1(续)
    化合物   X     Y    R3   R1     R2            B编号
    1-575    F    Cl    H    CF3    CH3    SCH(CH3)C≡CH1-576    F    Cl    H    CF3    CH3    SCH2COOCH31-577    F    Cl    H    CF3    CH3    SCH2COOC2H51-578    F    Cl    H    CF3    CH3    SCH2COOnC3H71-579    F    Cl    H    CF3    CH3    SCH2COOnC4H91-580    F    Cl    H    CF3    CH3    SCH2COOnC5H111-581    F    Cl    H    CF3    CH3    SCH2COOiC3H71-582    F    Cl    H    CF3    CH3    SCH2COOcC5H91-583    F    Cl    H    CF3    CH3    SCH2COOcC6H111-584    F    Cl    H    CF3    CH3    SCH(CH3)COOCH31-585    F    Cl    H    CF3    CH3    SCH(CH3)COOC2H51-586    F    Cl    H    CF3    CH3    SCH(CH3)COOnC3H71-587    F    Cl    H    CF3    CH3    SCH(CH3)COOnC4H91-588    F    Cl    H    CF3    CH3    SCH(CH3)COOnC5H111-589    F    Cl    H    CF3    CH3    SCH(CH3)COOiC3H71-590    F    Cl    H    CF3    CH3    SCH(CH3)COOcC5H91-591    F    Cl    H    CF3    CH3    SCH(CH3)COOcC6H111-592    F    Cl    H    CF3    CH3    SCH2CON(CH3)21-593    F    Cl    H    CF3    CH3    SCH2CON(C2H5)21-594    F    Cl    H    CF3    CH3    SCH2CON(四亚甲基)1-595    F    Cl    H    CF3    CH3    SCH2CON(五亚甲基)1-596    F    Cl    H    CF3    CH3    SCH2CON(3-氧杂-1,5-亚戊基)
                            表1(续)
    化合物   X    Y     R3    R1    R2            B编号
    1-597    F    Cl    H    CF3    CH3    SCH(CH3)CON(CH3)21-598    F    Cl    H    CF3    CH3    SCH(CH3)CON(C2H5)21-599    F    Cl    H    CF3    CH3    SCH(CH3)CON(四亚甲基)1-600    F    Cl    H    CF3    CH3    SCH(CH3)CON(五亚甲基)1-601    H    F     H    CF3    CH3    SO2Cl1-602    H    Cl    H    CF3    CH3    SO2Cl1-603    H    Br    H    CF3    CH3    SO2Cl1-604    F    F     H    CF3    CH3    SO2Cl1-605    F    Cl    H    CF3    CH3    SO2Cl1-606    F    Br    H    CF3    CH3    SO2Cl1-607    H    Cl    H    CF3    CH3    SO2OCH31-608    H    Cl    H    CF3    CH3    SO2OC2H51-609    H    Cl    H    CF3    CH3    SO2OiC3H71-610    H    Cl    H    CF3    CH3    SO2OCH2CH=CH21-611    F    Cl    H    CF3    CH3    SO2OCH31-612    F    Cl    H    CF3    CH3    SO2OC2H51-613    F    Cl    H    CF3    CH3    SO2OiC3H71-614    F    Cl    H    CF3    CH3    SO2OCH2CH=CH21-615    H    Cl    H    CF3    CH3    SO2N(CH3)21-616    H    Cl    H    CF3    CH3    SO2N(C2H5)21-617    F    Cl    H    CF3    CH3    SO2N(CH3)2
                                    表1(续)
    化合物   X    Y     R3   R1     R2          B编号
    1-618    F    Cl    H    CF2    CH3    SO2N(C2H5)21-619    H    Cl    H    CF3    CH3    COOH1-620    H    Cl    H    CF3    CH3    COOCH31-621    H    Cl    H    CF3    CH3    COOC2H51-622    H    Cl    H    CF3    CH3    COOnC3H71-623    H    Cl    H    CF3    CH3    COOnC4H91-624    H    Cl    H    CF3    CH3    COOnC5H111-625    H    Cl    H    CF3    CH3    COOiC3 -H71-626    H    Cl    H    CF3    CH3    COOCH2CH2Cl1-627    H    Cl    H    CF3    CH3    COOCH2CH2Br1-628    H    Cl    H    CF3    CH3    CON(CH3)21-629    H    Cl    H    CF3    CH3    CONHCH31-630    H    Cl    H    CF3    CH3    CON(C2H5)21-631    H    Cl    H    CF3    CH3    CONHC2H51-632    H    Cl    H    CF3    CH3    COCH31-633    H    Cl    H    CF3    CH3    COC2H51-634    H    Cl    H    CF3    CH3    COCH2Cl1-635    H    Cl    H    CF3    CH3    CHO1-636    H    Cl    H    CF3    CH3    CH=CHCOOCH31-637    H    Cl    H    CF3    CH3    CH=CHCOOC2H51-638    H    Cl    H    CF3    CH3    CH2CH2COOCH31-639    H    Cl    H    CF3    CH3    CH2CH2COOC2H51-640    F    Cl    H    CF3    CH3    COOH
                               表1(续)
    化合物   X    Y     R3    R1    R2       B编号
    1-641    F    Cl    H    CF3    CH3    COOCH31-642    F    Cl    H    CF3    CH3    COOC2H51-643    F    Cl    H    CF3    CH3    COOnC3H71-644    F    Cl    H    CF3    CH3    COOnC4H91-645    F    Cl    H    CF3    CH3    COOnC5H111-646    F    Cl    H    CF3    CH3    COOiC3H71-647    F    Cl    H    CF3    CH3    COOCH2CH2Cl1-648    F    Cl    H    CF3    CH3    COOCH2CH2Br1-649    F    Cl    H    CF3    CH3    CON(CH3)21-650    F    Cl    H    CF3    CH3    CONHCH31-651    F    Cl    H    CF3    CH3    CON(C2H5)21-652    F    Cl    H    CF3    CH3    CONHC2H51-653    F    Cl    H    CF3    CH3    COCH31-654    F    Cl    H    CF3    CH3    COC2H51-655    F    Cl    H    CF3    CH3    COCH2Cl1-656    F    Cl    H    CF3    CH3    CHO1-657    F    Cl    H    CF3    CH3    CH=CHCOOCH31-658    F    Cl    H    CF3    CH3    CH=CHCOOC2H51-659    F    Cl    H    CF3    CH3    CH2CH2COOCH31-660    F    Cl    H    CF2Cl  CH3    CH2CH2COOC2H51-661    Cl   Cl    H    CF2Cl  H       H1-662    H    F     H    CF2Cl  H       NO2
                             表1(续)
  化合物    X    Y    R3  R1     R2    B编号
  1-663    H    Cl    H  CF2Cl    H    NO21-664    H    Br    H  CF2Cl    H    NO21-665    F    F     H  CF2Cl    H    NO21-666    F    Cl    H  CF2Cl    H    NO21-667    F    Br    H  CF2Cl    H    NO21-668    H    F     H  CF2Cl    H    NH21-669    H    Cl    H  CF2Cl    H    NH21-670    H    Br    H  CF2Cl    H    NH21-671    F    F     H  CF2Cl    H    NH21-672    F    Cl    H  CF2Cl    H    NH21-673    F    Br    H  CF2Cl    H    NH21-674    H    F     H  CF2Cl    H    OH1-675    H    Cl    H  CF2Cl    H    OH1-676    H    Br    H  CF2Cl    H    OH1-677    F    F     H  CF2Cl    H    OH1-678    F    Cl    H  CF2Cl    H    OH1-679    F    Br    H  CF2Cl    H    OH1-680    H    Cl    H  CF2Cl    H    NHCH31-681    H    Cl    H  CF2Cl    H    NHC2H51-682    H    Cl    H  CF2Cl    H    NHCH2CH=CH21-683    H    Cl    H  CF2Cl    H    NHCH2C≡CH1-684    H    Cl    H  CF2Cl    H    NHCH(CH3)C≡CH1-685    H    Cl    H  CF2Cl    H    NHSO2CH3
                          表1(续)
    化合物   X    Y     R3    R1   R2      B编号
    1-686    H    Cl    H  CF2Cl    H    NHSO2C2H51-687    H    Cl    H  CF2Cl    H    NHSO2CH2Cl1-688    H    Cl    H  CF2Cl    H    NHSO2CF31-689    H    Cl    H  CF2Cl    H    N(CH3)SO2CH31-690    H    Cl    H  CF2Cl    H    N(CH2C≡CH)SO2CH31-691    H    Cl    H  CF2Cl    H    NHCOOCH31-692    H    Cl    H  CF2Cl    H    NHCOOC2H51-693    H    Cl    H  CF2Cl    H    NHCOOnC- 3H71-694    H    Cl    H  CF2Cl    H    NHCOOiC3H71-695    H    Cl    H  CF2Cl    H    NHCOOnC4H91-696    H    Cl    H  CF2Cl    H    NHCOOnC5H111-697    H    Cl    H  CF2Cl    H    NHCH2COOCH31-698    H    Cl    H  CF2Cl    H    NHCH2COOC2H51-699    H    Cl    H  CF2Cl    H    NHCH2COOnC3H71-700    H    Cl    H  CF2Cl    H    NHCH2COOnC4H91-701    H    Cl    H  CF2Cl    H    NHCH2COOnC5H111-702    H    Cl    H  CF2Cl    H    NHCH2COOiC3H71-703    H    Cl    H  CF2Cl    H    NHCH2COOcC5H91-704    H    Cl    H  CF2Cl    H    NHCH2COOcC6H111-705    H    Cl    H  CF2Cl    H    NHCH(CH3)COOCH31-706    H    Cl    H  CF2Cl    H    NHCH(CH3)COOC2H51-707    H    Cl    H  CF2Cl    H    NHCH(CH3)COOnC3H71-708    H    Cl    H  CF2Cl    H    NHCH(CH3)COOnC4H9
                             表1(续)
    化合物   X    Y     R3   R1   R2              B编号
    1-709    H    Cl    H  CF2Cl    H    NHCH(CH3)COOnC5H111-710    H    Cl    H  CF2Cl    H    NHCH(CH3)COOiC3H71-711    H    Cl    H  CF2Cl    H    NHCH(CH3)COOcC5H91-712    H    Cl    H  CF2Cl    H    NHCH(CH3)COOcC6H111-713    F    Cl    H  CF2Cl    H    NHCH31-714    F    Cl    H  CF2Cl    H    NHC2H51-715    F    Cl    H  CF2Cl    H    NHCH2CH=CH21-716    F    Cl    H  CF2Cl    H    NHCH2C≡CH1-717    F    Cl    H  CF2Cl    H    NHCH(CH3)C≡CH1-718    F    Cl    H  CF2Cl    H    NHSO2CH31-719    F    Cl    H  CF2Cl    H    NHSO2C2H51-720    F    Cl    H  CF2Cl    H    NHSO2CH2Cl1-721    F    Cl    H  CF2Cl    H    NHSO2CF31-722    F    Cl    H  CF2Cl    H    N(CH3)SO2CH31-723    F    Cl    H  CF2Cl    H    N(CH2C≡CH)SO2CH31-724    F    Cl    H  CF2Cl    H    NHCOOCH31-725    F    Cl    H  CF2Cl    H    NHCOOC2H51-726    F    Cl    H  CF2Cl    H    NHCOOnC3H71-727    F    Cl    H  CF2Cl    H    NHCOOiC3H71-728    F    Cl    H  CF2Cl    H    NHCOOnC4H91-729    F    Cl    H  CF2Cl    H    NHCOOnC5H111-730    F    Cl    H  CF2Cl    H    NHCH2COOCH31-731    F    Cl    H  CF2Cl    H    NHCH2COOC2H5
                             表1(续)
  化合物   X    Y     R3    R1   R2        B编号
  1-732    F    Cl    H  CF2Cl    H    NHCH2COOnC3H71-733    F    Cl    H  CF2Cl    H    NHCH2COOnC4H91-734    F    Cl    H  CF2Cl    H    NHCH2COOnC5H111-735    F    Cl    H  CF2Cl    H    NHCH2COOiC3H71-736    F    Cl    H  CF2Cl    H    NHCH2COOcC5H91-737    F    Cl    H  CF2Cl    H    NH2CH2COOcC6H111-738    F    Cl    H  CF2Cl    H    NHCH(CH3)COOCH31-739    F    Cl    H  CF2Cl    H    NHCH(CH3)COOC2H51-740    F    Cl    H  CF2Cl    H    NHCH(CH3)COOnC3H71-741    F    Cl    H  CF2Cl    H    NHCH(CH3)COOnC4H91-742    F    Cl    H  CF2Cl    H    NHCH(CH3)COOnC5H111-743    F    Cl    H  CF2Cl    H    NHCH(CH3)COOiC3H71-744    F    Cl    H  CF2Cl    H    NHCH(CH3)COOcC5H91-745    F    Cl    H  CF2Cl    H    NHCH(CH3)COOcC5H111-746    H    Cl    H  CF2Cl    H    OCH31-747    H    Cl    H  CF2Cl    H    OC2H51-748    H    Cl    H  CF2Cl    H    OiC3H71-749    H    Cl    H  CF2Cl    H    OnC3H71-750    H    Cl    H  CF2Cl    H    OCH2CH2Cl1-751    H    Cl    H  CF2Cl    H    OCF2CF2H1-752    H    Cl    H  CF2Cl    H    OcC5H91-753    H    Cl    H  CF2Cl    H    OcC6H111-754    H    Cl    H  CF2Cl    H    OCH2CH=CH2
                           表1(续)
    化合物   X     Y    R3    R1   R2       B编号
    1-755    H    Cl    H  CF2Cl    H    OCH2CCl=CH21-756    H    Cl    H  CF2Cl    H    OCH2CCl=CHCl1-757    H    Cl    H  CF2Cl    H    OCH(CH3)CH=CH21-758    H    Cl    H  CF2Cl    H    OCH2C≡CH1-759    H    Cl    H  CF2Cl    H    OCH(CH3)C≡CH1-760    H    Cl    H  CF2Cl    H    OCH2C≡CBr1-761    H    Cl    H  CF2Cl    H    OCH2C≡CCl1-762    H    Cl    H  CF2Cl    H    OCH2C≡CCH2Cl1-763    H    Cl    H  CF2Cl    H    OCH2CN1-764    H    Cl    H  CF2Cl    H    OCH2OCH31-765    H    Cl    H  CF2Cl    H    OCH2OC2H51-766    H    Cl    H  CF2Cl    H    OCH2SCH31-767    H    Cl    H  CF2Cl    H    OCH2COOCH31-768    H    Cl    H  CF2Cl    H    OCH2COOC2H51-769    H    Cl    H  CF2Cl    H    OCH2COOnC3H71-770    H    Cl    H  CF2Cl    H    OCH2COOnC4H91-771    H    Cl    H  CF2Cl    H    OCH2COOnC5H111-772    H    Cl    H  CF2Cl    H    OCH2COOiC3H71-773    H    Cl    H  CF2Cl    H    OCH2COOcC5H91-774    H    Cl    H  CF2Cl    H    OCH2COOcC5H111-775    H    Cl    H  CF2Cl    H    OCH(CH3)COOCH21-776    H    Cl    H  CF2Cl    H    OCH(CH3)COOC2H5
                              表1(续)
    化合物   X    Y     R3    R1   R2    B编号
    1-777    H    Cl    H  CF2Cl  H    OCH(CH3)COOnC3H71-778    H    Cl    H  CF2Cl  H    OCH(CH3)COOnC4H91-779    H    Cl    H  CF2Cl  H    OCH(CH3)COOnC5H111-780    H    Cl    H  CF2Cl  H    OCH(CH3)COOiC3H71-781    H    Cl    H  CF2Cl  H    OCH(CH3)COOcC5H91-782    H    Cl    H  CF2Cl  H    OCH(CH3)COOcC6H111-783    H    Cl    H  CF2Cl  H    OCH2CON(CH3)21-784    H    Cl    H  CF2Cl  H    OCH2CON(C2 -H5)21-785    H    Cl    H  CF2Cl  H    OCH2CON(CH3)C2H51-786    H    Cl    H  CF2Cl  H    OCH(CH3)CON(CH3)21-787    H    Cl    H  CF2Cl  H    OCH(CH3)CON(C2H5)21-788    H    Cl    H  CF2Cl  H    OCH(CH3)CON(CH3)C2H51-789    H    Cl    H  CF2Cl  H    OCH2COON(CH3)21-790    H    Cl    H  CF2Cl  H    OCH2COON(C2H5)21-791    H    Cl    H  CF2Cl  H    OCH(CH3)COON(CH3)2l-792    H    Cl    H  CF2Cl  H    OCH(CH3)COON(C2H5)21-793    F    Cl    H  CF2Cl  H    OCH31-794    F    Cl    H  CF2Cl  H    OC2H51-795    F    Cl    H  CF2Cl  H    OiC3H71-796    F    Cl    H  CF2Cl  H    OnC3H71-797    F    Cl    H  CF2Cl  H    OCH2CH2Cl1-798    F    Cl    H  CF2Cl  H    OCF2CF2H1-799    F    Cl    H  CF2Cl  H    OcC5H9
                            表1(续)
    化合物   X    Y     R3    R1   R2      B编号
    1-800    F    Cl    H  CF2Cl    H    OcC6H111-801    F    Cl    H  CF2Cl    H    OCH2CH=CH21-802    F    Cl    H  CF2Cl    H    OCH2CCl=CH21-803    F    Cl    H  CF2Cl    H    OCH2CCl=CHCl1-804    F    Cl    H  CF2Cl    H    OCH(CH3)CH=CH21-805    F    Cl    H  CF2Cl    H    OCH2C≡CH1-806    F    Cl    H  CF2Cl    H    OCH(CH3)C≡CH1-807    F    Cl    H  CF2Cl    H    OCH2C≡CBr1-808    F    Cl    H  CF2Cl    H    OCH2C≡CCl1-809    F    Cl    H  CF2Cl    H    OCH2C≡CCH2Cl1-810    F    Cl    H  CF2Cl    H    OCH2CN1-811    F    Cl    H  CF2Cl    H    OCH2OCH31-812    F    Cl    H  CF2Cl    H    OCH2OC2H51-813    F    Cl    H  CF2Cl    H    OCH2SCH31-814    F    Cl    H  CF2Cl    H    OCH2COOCH31-815    F    Cl    H  CF2Cl    H    OCH2COOC2H51-816    F    Cl    H  CF2Cl    H    OCH2COOnC3H71-817    F    Cl    H  CF2Cl    H    OCH2COOnC4H91-818    F    Cl    H  CF2Cl    H    OCH2COOnC5H111-819    F    Cl    H  CF2Cl    H    OCH2COOiC3H71-820    F    Cl    H  CF2Cl    H    OCH2COOcC5H91-821    F    Cl    H  CF2Cl    H    OCH2COOcC6H111-822    F    Cl    H  CF2Cl    H    OCH(CH3)COOCH3
                        表1(续)
    化合物   X     Y    R3    R1   R2          B编号
    1-823    F    Cl    H  CF2Cl    H    OCH(CH3)COOC2H51-824    F    Cl    H  CF2Cl    H    OCH(CH3)COOnC3H71-825    F    Cl    H  CF2Cl    H    OCH(CH3)COOnC4H91-826    F    Cl    H  CF2Cl    H    OCH(CH3)COOnC5H111-827    F    Cl    H  CF2Cl    H    OCH(CH3)COOiC3H71-828    F    Cl    H  CF2Cl    H    OCH(CH3)COOcC5H91-829    F    Cl    H  CF2Cl    H    OCH(CH3)COOcC6H111-830    F    Cl    H  CF2Cl    H    OCH2CON(CH3)21-831    F    Cl    H  CF2Cl    H    OCH2CON(C2H5)21-832    F    Cl    H  CF2Cl    H    OCH2CON(CH3)C2H51-833    F    Cl    H  CF2Cl    H    OCH(CH3)CON(CH3)21-834    F    Cl    H  CF2Cl    H    OCH(CH3)CON(C2H5)21-835    F    Cl    H  CF2Cl    H    OCH(CH3)CON(CH3)C2H51-836    F    Cl    H  CF2Cl    H    OCH2COON(CH3)21-837    F    Cl    H  CF2Cl    H    OCH2COON(C2H5)21-838    F    Cl    H  CF2Cl    H    OCH(CH3)COON(CH3)21-839    F    Cl    H  CF2Cl    H    OCH(CH3)COON(C2H5)21-840    H    F     H  CF2Cl    H    SH1-841    H    Cl    H  CF2Cl    H    SH1-842    H    Br    H  CF2Cl    H    SH1-843    F    F     H  CF2Cl    H    SH1-844    F    Cl    H  CF2Cl    H    SH1-845    F    Br    H  CF2Cl    H    SH
                              表1(续)
    化合物   X    Y     R3   R1    R2     B编号
    1-846    H    Cl    H  CF2Cl    H    SCH31-847    H    Cl    H  CF2Cl    H    SC2H51-848    H    Cl    H  CF2Cl    H    SiC3H71-849    H    Cl    H  CF2Cl    H    SCH2CH2Cl1-850    H    Cl    H  CF2Cl    H    ScC5H91-851    H    Cl    H  CF2Cl    H    ScC6H111-852    H    Cl    H  CF2Cl    H    SCH2CH=CH21-853    H    Cl    H  CF2Cl    H    SCH2CCl=CH21-854    H    Cl    H  CF2Cl    H    SCH2CCl=CHCl1-855    H    Cl    H  CF2Cl    H    SCH(CH3)CH=CH21-856    H    Cl    H  CF2Cl    H    SCH2C≡CH1-857    H    Cl    H  CF2Cl    H    SCH(CH3)C≡CH1-858    H    Cl    H  CF2Cl    H    SCH2COOCH31-859    H    Cl    H  CF2Cl    H    SCH2COOC2H51-860    H    Cl    H  CF2Cl    H    SCH2COOnC3H71-861    H    Cl    H  CF2Cl    H    SCH2COOnC4H91-862    H    Cl    H  CF2Cl    H    SCH2COOnC5H111-863    H    Cl    H  CF2Cl    H    SCH2COOiC3H71-864    H    Cl    H  CF2Cl    H    SCH2COOcC5H91-865    H    Cl    H  CF2Cl    H    SCH2COOcC6H111-866    H    Cl    H  CF2Cl    H    SCH(CH3)COOCH31-867    H    Cl    H  CF2Cl    H    SCH(CH3)COOC2H51-868    H    Cl    H  CF2Cl    H    SCH(CH3)COOnC3H7
                              表1(续)
    化合物   X     Y    R3    R1 R2        B编号
    1-869    H    Cl    H  CF2Cl  H    SCH(CH3)COOnC4H91-870    H    Cl    H  CF2Cl  H    SCH(CH3)COOnC5H111-871    H    Cl    H  CF2Cl  H    SCH(CH3)COOiC3H71-872    H    Cl    H  CF2Cl  H    SCH(CH3)COOcC5H91-873    H    Cl    H  CF2Cl  H    SCH(CH3)COOcC6H111-874    H    Cl    H  CF2Cl  H    SCH2CON(CH3)21-875    H    Cl    H  CF2Cl  H    SCH2CON(C2H5)21-876    H    Cl    H  CF2Cl  H    SCH2CON(四亚甲基)1-877    H    Cl    H  CF2Cl  H    SCH2CON(五亚甲基)1-878    H    Cl    H  CF2Cl  H    SCH2CON(3-氧杂-1,5-亚戊基)1-879    H    Cl    H  CF2Cl  H    SCH(CH3)CON(CH3)21-880    H    Cl    H  CF2Cl  H    SCH(CH3)CON(C2H5)21-881    H    Cl    H  CF2Cl  H    SCH(CH3)CON(四亚甲基)1-882    H    Cl    H  CF2Cl  H    SCH(CH3)CON(五亚甲基)1-883    F    Cl    H  CF2Cl  H    SCH31-884    F    Cl    H  CF2Cl  H    SC2H51-885    F    Cl    H  CF2Cl  H    SiC3H71-886    F    Cl    H  CF2Cl  H    SCH2CH2Cl
                                表1(续)
    化合物   X    Y     R3  R1     R2     B编号
    1-887    F    Cl    H  CF2Cl    H    ScC5H91-888    F    Cl    H  CF2Cl    H    ScC6H111-889    F    Cl    H  CF2Cl    H    SCH2CH=CH21-890    F    Cl    H  CF2Cl    H    SCH2CCl=CH21-891    F    Cl    H  CF2Cl    H    SCH2CCl=CHCl1-892    F    Cl    H  CF2Cl    H    SCH(CH3)CH=CH21-893    F    Cl    H  CF2Cl    H    SCH2C≡CH1-894    F    Cl    H  CF2Cl    H    SCH(CH3)C≡CH1-895    F    Cl    H  CF2Cl    H    SCH2COOCH31-896    F    Cl    H  CF2Cl    H    SCH2COOC2H51-897    F    Cl    H  CF2Cl    H    SCH2COOnC3H71-898    F    Cl    H  CF2Cl    H    SCH2COOnC4H91-899    F    Cl    H  CF2Cl    H    SCH2COOnC5H111-900    F    Cl    H  CF2Cl    H    SCH2COOiC3H71-901    F    Cl    H  CF2Cl    H    SCH2COOcC5H91-902    F    Cl    H  CF2Cl    H    SCH2COOcC6H111-903    F    Cl    H  CF2Cl    H    SCH(CH3)COOCH31-904    F    Cl    H  CF2Cl    H    SCH(CH3)COOC2H51-905    F    Cl    H  CF2Cl    H    SCH(CH3)COOnC3H71-906    F    Cl    H  CF2Cl    H    SCH(CH3)COOnC4H91-907    F    Cl    H  CF2Cl    H    SCH(CH3)COOnC5H111-908    F    Cl    H  CF2Cl    H    SCH(CH3)COOiC3H71-909    F    Cl    H  CF2Cl    H    SCH(CH3)COOcC5H9
                                 表1(续)
    化合物   X    Y     R3    R1   R2    B编号
    1-910    F    Cl    H  CF2Cl  H    SCH(CH3)COOcC6H111-911    F    Cl    H  CF2Cl  H    SCH2CON(CH3)21-912    F    Cl    H  CF2Cl  H    SCH2CON(C2H5)21-913    F    Cl    H  CF2Cl  H    SCH2CON(四亚甲基)1-914    F    Cl    H  CF2Cl  H    SCH2CON(五亚甲基)1-915    F    Cl    H  CF2Cl  H    SCH2CON(3-氧杂-1,5-亚戊基)1-916    F    Cl    H  CF2Cl  H    SCH(CH3)CON(CH3)21-917    F    Cl    H  CF2Cl  H    SCH(CH3)CON(C2H5)21-918    F    Cl    H  CF2Cl  H    SCH(CH3)CON(四亚甲基)1-919    F    Cl    H  CF2Cl  H    SCH(CH3)CON(五亚甲基)1-920    H    F     H  CF2Cl  H    SO2Cl1-921    H    Cl    H  CF2Cl  H    SO2Cl1-922    H    Br    H  CF2Cl  H    SO2Cl1-923    F    F     H  CF2Cl  H    SO2Cl1-924    F    Cl    H  CF2Cl  H    SO2Cl1-925    F    Br    H  CF2Cl  H    SO2Cl1-926    H    Cl    H  CF2Cl  H    SO2OCH31-927    H    Cl    H  CF2Cl  H    SO2OC2H51-928    H    Cl    H  CF2Cl  H    SO2OiC3H71-929    H    Cl    H  CF2Cl  H    SO2OCH2CH=CH2
                                 表1(续)
  化合物   X    Y     R3   R1    R2       B编号
  1-930    F    Cl    H  CF2Cl    H    SO2OCH31-931    F    Cl    H  CF2Cl    H    SO2OC2H51-932    F    Cl    H  CF2Cl    H    SO2OiC3H71-933    F    Cl    H  CF2Cl    H    SO2OCH2CH=CH21-934    H    Cl    H  CF2Cl    H    SO2N(CH3)21-935    H    Cl    H  CF2Cl    H    SO2N(C2H5)21-936    F    Cl    H  CF2Cl    H    SO2N(CH3)21-937    F    Cl    H  CF2Cl    H    SO2N(C2H5)21-938    H    Cl    H  CF2Cl    H    COOH1-939    H    Cl    H  CF2Cl    H    COOCH31-940    H    Cl    H  CF2Cl    H    COOC2H51-941    H    Cl    H  CF2Cl    H    COOnC3H71-942    H    Cl    H  CF2Cl    H    COOnC4H91-943    H    Cl    H  CF2Cl    H    COOnC5H111-944    H    Cl    H  CF2Cl    H    COOiC3H71-945    H    Cl    H  CF2Cl    H    COOCH2CH2Cl1-946    H    Cl    H  CF2Cl    H    COOCH2CH2Br1-947    H    Cl    H  CF2Cl    H    CON(CH3)21-948    H    Cl    H  CF2Cl    H    CONHCH31-949    H    Cl    H  CF2Cl    H    CON(C2H5)21-950    H    Cl    H  CF2Cl    H    CONHC2H51-951    H    Cl    H  CF2Cl    H    COCH31-952    H    Cl    H  CF2Cl    H    COC2H5
                                  表1(续)
  化合物   X    Y     R3   R1    R2    B编号
  1-953    H    Cl    H  CF2Cl    H    COCH2Cl1-954    H    Cl    H  CF2Cl    H    CHO1-955    H    Cl    H  CF2Cl    H    CH=CHCOOCH31-956    H    Cl    H  CF2Cl    H    CH=CHCOOC2H51-957    H    Cl    H  CF2Cl    H    CH2CH2COOCH31-958    H    Cl    H  CF2Cl    H    CH2CH2COOC2H51-959    F    Cl    H  CF2Cl    H    COOH1-960    F    Cl    H  CF2Cl    H    COOCH31-961    F    Cl    H  CF2Cl    H    COOC2H51-962    F    Cl    H  CF2Cl    H    COOnC3H71-963    F    Cl    H  CF2Cl    H    COOnC4H91-964    F    Cl    H  CF2Cl    H    COOnC5H111-965    F    Cl    H  CF2Cl    H    COOiC3H71-966    F    Cl    H  CF2Cl    H    COOCH2CH2Cl1-967    F    Cl    H  CF2Cl    H    COOCH2CH2Br1-968    F    Cl    H  CF2Cl    H    CON(CH3)21-969    F    Cl    H  CF2Cl    H    CONHCH31-970    F    Cl    H  CF2Cl    H    CON(C2H5)21-971    F    Cl    H  CF2Cl    H    CONHC2H51-972    F    Cl    H  CF2Cl    H    COCH31-973    F    Cl    H  CF2Cl    H    COC2H51-974    F    Cl    H  CF2Cl    H    COCH2Cl1-975    F    Cl    H  CF2Cl    H    CHO
                                  表1(续)
    化合物   X    Y     R3    R1   R2      B编号
    1-976    F    Cl    H    CF2Cl  H    CH=CHCOOCH31-977    F    Cl    H    CF2Cl  H    CH=CHCOOC2H51-978    F    Cl    H    CF2Cl  H    CH2CH2COOCH31-979    F    Cl    H    CF2Cl  H    CH2CH2COOC2H51-980    H    F     H    CF3    H    NO21-981    H    Cl    H    CF3    H    NO21-982    H    Br    H    CF3    H    NO21-983    F    F     H    CF3    H    NO21-984    F    Cl    H    CF3    H    NO21-985    F    Br    H    CF3    H    NO21-986    H    F     H    CF3    H    NH21-987    H    Cl    H    CF3    H    NH21-988    H    Br    H    CF3    H    NH21-989    F    F     H    CF3    H    NH21-990    F    Cl    H    CF3    H    NH21-991    H    Cl    H    CF3    H    NHCH(CH3)COOCH31-992    H    Cl    H    CF3    H    NHCH(CH3)COOC2H51-993    H    Cl    H    CF3    H    NHCH(CH3)COOnC3H71-994    H    Cl    H    CF3    H    NHCH(CH3)COOnC4H91-995    H    Cl    H    CF3    H    NHCH(CH3)COOnC5H111-996    H    Cl    H    CF3    H    NHCH(CH3)COOiC3H71-997    H    Cl    H    CF3    H    NHCH(CH3)COOcC5H9
                                    表1(续)
  化合物    X    Y     R3    R1   R2          B编号
  1-998     H    Cl    H    CF3    H    NHCH(CH3)COOcC6H111-999     F    Cl    H    CF3    H    NHCH31-1000    F    Cl    H    CF3    H    NHC2H51-1001    F    Cl    H    CF3    H    NHCH2CH=CH21-1002    F    Cl    H    CF3    H    NHCH2C≡CH1-1003    F    Cl    H    CF3    H    NHCH(CH3)C≡CH1-1004    F    Cl    H    CF3    H    NHSO2CH31-1005    F    Cl    H    CF3    H    NHSO2C2H51-1006    F    Cl    H    CF3    H    NHSO2CH2Cl1-1007    F    Cl    H    CF3    H    NHSO2CF31-1008    F    Cl    H    CF3    H    N(CH3)SO2CH31-1009    F    Cl    H    CF3    H    N(CH2C≡CH)SO2CH31-1010    F    Cl    H    CF3    H    NHCOOCH31-1011    F    Cl    H    CF3    H    NHCOOC2H51-1012    F    Cl    H    CF3    H    NHCOOnC3H71-1013    F    Cl    H    CF3    H    NHCOOiC3H71-1014    F    Cl    H    CF3    H    NHCOOnC4H91-1015    F    Cl    H    CF3    H    NHCOOnC5H111-1016    F    Cl    H    CF3    H    NHCH2COOCH31-1017    F    Cl    H    CF3    H    NHCH2COOC2H51-1018    F    Cl    H    CF3    H    NHCH2COOnC3H71-1019    F    Cl    H    CF3    H    NHCH2COOnC4H91-1020    F    Cl    H    CF3    H    NHCH2COOnC5H11
                               表1(续)
  化合物    X    Y     R3   R1    R2      B编号
  1-1021    F    Cl    H    CF3    H    NHCH2COOiC3H71-1022    F    Cl    H    CF3    H    NHCH2COOcC5H91-1023    F    Br    H    CF3    H    NH21-1024    H    F     H    CF3    H    OH1-1025    H    Cl    H    CF3    H    OH1-1026    H    Br    H    CF3    H    OH1-1027    F    F     H    CF3    H    OH1-1028    F    Cl    H    CF3    H    OH1-1029    F    Br    H    CF3    H    OH1-1030    H    Cl    H    CF3    H    NHCH31-1031    H    Cl    H    CF3    H    NHC2H51-1032    H    Cl    H    CF3    H    NHCH2CH=CH21-1033    H    Cl    H    CF3    H    NHCH2C≡CH1-1034    H    Cl    H    CF3    H    NHCH(CH3)C≡CH1-1035    H    Cl    H    CF3    H    NHSO2CH31-1036    H    Cl    H    CF3    H    NHSO2C2H51-1037    H    Cl    H    CF3    H    NHSO2CH2Cl1-1038    H    Cl    H    CF3    H    NHSO2CF31-1039    H    Cl    H    CF3    H    N(CH3)SO2CH31-1040    H    Cl    H    CF3    H    N(CH2C≡CH)SO2CH31-1041    H    Cl    H    CF3    H    NHCOOCH31-1042    H    Cl    H    CF3    H    NHCOOC2H51-1043    H    Cl    H    CF3    H    NHCOOnC3H7
                            表1(续)
    化合物    X    Y     R3   R1    R2      B编号
    1-1044    H    Cl    H    CF3    H    NHCOOiC3H71-1045    H    Cl    H    CF3    H    NHCOOnC4H91-1046    H    Cl    H    CF3    H    NHCOOnC5H111-1047    H    Cl    H    CF3    H    NHCH2COOCH31-1048    H    Cl    H    CF3    H    NHCH2COOC2H51-1049    H    Cl    H    CF3    H    NHCH2COOnC3H71-1050    H    Cl    H    CF3    H    NHCH2COOnC4H91-1051    H    Cl    H    CF3    H    NHCH2COO-nC5H11l-1052    H    Cl    H    CF3    H    NHCH2COOiC3H71-1053    H    Cl    H    CF3    H    NHCH2COOcC5H61-1054    H    Cl    H    CF3    H    NHCH2COOcC6H111-1055    F    Cl    H    CF3    H    NHCH2COOcC6H111-1056    F    Cl    H    CF3    H    NHCH(CH3)COOCH31-1057    F    Cl    H    CF3    H    NHCH(CH3)COOC2H51-1058    F    Cl    H    CF3    H    NHCH(CH3)COOnC3H71-1059    F    Cl    H    CF3    H    NHCH(CH3)COOnC4H91-1060    F    Cl    H    CF3    H    NHCH(CH3)COOnC5H111-1061    F    Cl    H    CF3    H    NHCH(CH3)COOiC3H71-1062    F    Cl    H    CF3    H    NHCH(CH3)COOcC5H91-1063    F    Cl    H    CF3    H    NHCH(CH3)COOcC5H111-1064    H    Cl    H    CF3    H    OCH31-1065    H    Cl    H    CF3    H    OC2H51-1066    H    Cl    H    CF3    H    OiC3H7
                               表1(续)
    化合物    X    Y     R3    R1   R2     B编号
    1-1067    H    Cl    H    CF3    H    OnC3H71-1068    H    Cl    H    CF3    H    OCH2CH2Cl1-1069    H    Cl    H    CF3    H    OCF2CF2H1-1070    H    Cl    H    CF3    H    OcC5H91-1071    H    Cl    H    CF3    H    OcC5H111-1072    H    Cl    H    CF3    H    OCH2CH=CH21-1073    H    Cl    H    CF3    H    OCH2CCl=CH21-1074    H    Cl    H    CF3    H    OCH2CCl=CHCl1-1075    H    Cl    H    CF3    H    OCH(CH3)CH=CH21-1076    H    Cl    H    CF3    H    OCH2C≡CH1-1077    H    Cl    H    CF3    H    OCH(CH3)C≡CH1-1078    H    Cl    H    CF3    H    OCH2C≡CBr1-1079    H    Cl    H    CF3    H    OCH2C≡CCl1-1080    H    Cl    H    CF3    H    OCH2C≡CCH2Cl1-1081    H    Cl    H    CF3    H    OCH2CN1-1082    H    Cl    H    CF3    H    OCH2OCH31-1083    H    Cl    H    CF3    H    OCH2OC2H51-1084    H    Cl    H    CF3    H    OCH2SCH31-1085    H    Cl    H    CF3    H    OCH2COOCH31-1086    H    Cl    H    CF3    H    OCH2COOC2H51-1087    H    Cl    H    CF3    H    OCH2COOnC3H7l-1088    H    Cl    H    CF3    H    OCH2COOnC4H91-1089    H    Cl    H    CF3    H    OCH2COOnC5H11
                              表1(续)
  化合物    X    Y     R3   R1    R2          B编号
  1-1090    H    Cl    H    CF3    H    OCH2COOiC3H71-1091    H    Cl    H    CF3    H    OCH2COOcC5H91-1092    H    Cl    H    CF3    H    OCH2COOcC6H111-1093    H    Cl    H    CF3    H    OCH(CH3)COOCH31-1094    H    Cl    H    CF3    H    OCH(CH3)COOC2H51-1095    H    Cl    H    CF3    H    OCH(CH3)COOnC3H71-1096    H    Cl    H    CF3    H    OCH(CH3)COOnC4H91-1097    H    Cl    H    CF3    H    OCH(CH3)COOnC5H111-1098    H    Cl    H    CF3    H    OCH(CH3)COOiC3H71-1099    H    Cl    H    CF3    H    OCH(CH3)COOcC5H91-1100    H    Cl    H    CF3    H    OCH(CH3)COOcC6H111-1101    H    Cl    H    CF3    H    OCH2CON(CH3)21-1102    H    Cl    H    CF3    H    OCH2CON(C2H5)21-1103    H    Cl    H    CF3    H    OCH2CON(CH3)C2H51-1104    H    Cl    H    CF3    H    OCH(CH3)CON(CH3)21-1105    H    Cl    H    CF3    H    OCH(CH3)CON(C2H5)21-1106    H    Cl    H    CF3    H    OCH(CH3)CON(CH3)C2H51-1107    H    Cl    H    CF3    H    OCH2COON(CH3)21-1108    H    Cl    H    CF3    H    OCH2COON(C2H5)21-1109    H    Cl    H    CF3    H    OCH(CH3)COON(CH3)21-1110    H    Cl    H    CF3    H    OCH(CH3)COON(C2H5)21-1111    F    Cl    H    CF2    H    OCH3
                          表1(续)
    化合物    X    Y     R3   R1   R2      B编号
    1-1112    F    Cl    H    CF3    H    OC2H51-1113    F    Cl    H    CF3    H    OiC3H71-1114    F    Cl    H    CF3    H    OnC3H71-1115    F    Cl    H    CF3    H    OCH2CH2Cl1-1116    F    Cl    H    CF3    H    OCF2CF2H1-1117    F    Cl    H    CF3    H    OcC5H91-1118    F    Cl    H    CF3    H    OcC5H111-1119    F    Cl    H    CF3    H    OCH2CH=CH21-1120    F    Cl    H    CF3    H    OCH2CCl=CH21-1121    F    Cl    H    CF3    H    OCH2CCl=CHCl1-1122    F    Cl    H    CF3    H    OCH(CH3)CH=CH21-1123    F    Cl    H    CF3    H    OCH2C≡CH1-1124    F    Cl    H    CF3    H    OCH(CH3)C≡CH1-1125    F    Cl    H    CF3    H    OCH2C≡CBr1-1126    F    Cl    H    CF3    H    OCH2C≡CCl1-1127    F    Cl    H    CF3    H    OCH2C≡CCH2Cl1-1128    F    Cl    H    CF3    H    OCH2CN1-1129    F    Cl    H    CF3    H    OCH2OCH31-1130    F    Cl    H    CF3    H    OCH2OC2H51-1131    F    Cl    H    CF3    H    OCH2SCH31-1132    F    Cl    H    CF3    H    OCH2COOCH31-1133    F    Cl    H    CF3    H    OCH2COOC2H51-1134    F    Cl    H    CF3    H    OCH2COOnC3H7
                              表1(续)
  化合物    X    Y     R3    R1  R2       B编号
  1-1135    F    Cl    H    CF3    H    OCH2COOnC4H91-1136    F    Cl    H    CF3    H    OCH2COOnC5H111-1137    F    Cl    H    CF3    H    OCH2COOiC3H71-1138    F    Cl    H    CF3    H    OCH2COOcC5H91-1139    F    Cl    H    CF3    H    OCH2COOcC6H111-1140    F    Cl    H    CF3    H    OCH(CH3)COOCH31-1141    F    Cl    H    CF3    H    OCH(CH3)COOC2H51-1142    F    Cl    H    CF3    H    OCH(CH3)COOnC3H71-1143    F    Cl    H    CF3    H    OCH(CH3)COOnC4H91-1144    F    Cl    H    CF3    H    OCH(CH3)COOnC5H111-1145    F    Cl    H    CF3    H    OCH(CH3)COOiC3H71-1146    F    Cl    H    CF3    H    OCH(CH3)COOcC5H91-1147    F    Cl    H    CF3    H    OCH(CH3)COOcC6H111-1148    F    Cl    H    CF3    H    OCH2CON(CH3)21-1149    F    Cl    H    CF3    H    OCH2CON(C2H5)21-1150    F    Cl    H    CF3    H    OCH2CON(CH3)C2H51-1151    F    Cl    H    CF3    H    OCH(CH3)CON(CH3)21-1152    F    Cl    H    CF3    H    OCH(CH3)CON(C2H5)21-1153    F    Cl    H    CF3    H    OCH(CH3)CON(CH3)C2H51-1154    F    Cl    H    CF3    H    OCH2COON(CH3)21-1155    F    Cl    H    CF3    H    OCH2COON(C2H5)21-1156    F    Cl    H    CF3    H    OCH(CH3)COON(CH3)21-1157    F    Cl    H    CF3    H    OCH(CH3)COON(C2H5)2
                            表1(续)
    化合物    X    Y     R3   R1   R2    B编号
    1-1158    H    F     H    CF3    H    SH1-1159    H    Cl    H    CF3    H    SH1-1160    H    Br    H    CF3    H    SH1-1161    F    F     H    CF3    H    SH1-1162    F    Cl    H    CF3    H    SH1-1163    F    Br    H    CF3    H    SH1-1164    H    Cl    H    CF3    H    SCH31-1165    H    Cl    H    CF3    H    SC2H51-1166    H    Cl    H    CF3    H    SiC3H71-1167    H    Cl    H    CF3    H    SCH2CH2Cl1-1168    H    Cl    H    CF3    H    ScC5H91-1169    H    Cl    H    CF3    H    ScC6H111-1170    H    Cl    H    CF3    H    SCH2CH=CH21-1171    H    Cl    H    CF3    H    SCH2CCl=CH21-1172    H    Cl    H    CF3    H    SCH2CCl=CHCl1-1173    H    Cl    H    CF3    H    SCH(CH3)CH=CH21-1174    H    Cl    H    CF3    H    SCH2C≡CH1-1175    H    Cl    H    CF3    H    SCH(CH3)C≡CH1-1176    H    Cl    H    CF3    H    SCH2COOCH31-1177    H    Cl    H    CF3    H    SCH2COOC2H51-1178    H    Cl    H    CF3    H    SCH2COOnC3H71-1179    H    Cl    H    CF3    H    SCH2COOnC4H91-1180    H    Cl    H    CF3    H    SCH2COOnC5H11
                               表1(续)
    化合物    X    Y     R3   R1    R2            B编号
    1-1181    H    Cl    H    CF3    H    SCH2COOiC3H71-1182    H    Cl    H    CF3    H    SCH2COOcC5H91-1183    H    Cl    H    CF3    H    SCH2COOcC6H111-1184    H    Cl    H    CF3    H    SCH(CH3)COOCH31-1185    H    Cl    H    CF3    H    SCH(CH3)COOC2H51-1186    H    Cl    H    CF3    H    SCH(CH3)COOnC3H71-1187    H    Cl    H    CF3    H    SCH(CH3)COOnC4H91-1188    H    Cl    H    CF3    H    SCH(CH3)COOnC5H111-1189    H    Cl    H    CF3    H    SCH(CH3)COOiC3H71-1190    H    Cl    H    CF3    H    SCH(CH3)COOcC5H91-1191    H    Cl    H    CF3    H    SCH(CH3)COOcC6H111-1192    H    Cl    H    CF3    H    SCH2CON(CH3)51-1193    H    Cl    H    CF3    H    SCH2CON(C2H5)21-1194    H    Cl    H    CF3    H    SCH2CON(四亚甲基)1-1195    H    Cl    H    CF3    H    SCH2CON(五亚甲基)1-1196    H    Cl    H    CF3    H    SCH2CON(3-氧杂-1,5-亚戊基)1-1197    H    Cl    H    CF3    H    SCH(CH3)CON(CH3)51-1198    H    Cl    H    CF3    H    SCH(CH3)CON(C2H5)21-1199    H    Cl    H    CF3    H    SCH(CH3)CON1-1200    H    Cl    H    CF3    H    SCH(CH3)CON(五亚甲基)
                                    表1(续)
    化合物    X    Y     R3   R1   R2    B编号
    1-1201    F    Cl    H    CF3    H    SCH31-1202    F    Cl    H    CF3    H    SC2H51-1203    F    Cl    H    CF3    H    SiC3H71-1204    F    Cl    H    CF3    H    SCH2CH2Cl1-1205    F    Cl    H    CF3    H    ScC5H91-1206    F    Cl    H    CF3    H    ScC6H111-1207    F    Cl    H    CF3    H    SCH2CH=CH21-1208    F    Cl    H    CF3    H    SCH2CCl=CH21-1209    F    Cl    H    CF3    H    SCH5CCl=CHCl1-1210    F    Cl    H    CF3    H    SCH(CH3)CH=CH21-1211    F    Cl    H    CF3    H    SCH2C≡CH1-1212    F    Cl    H    CF3    H    SCH(CH3)C≡CH1-1213    F    Cl    H    CF3    H    SCH2COOCH31-1214    F    Cl    H    CF3    H    SCH2COOC2H51-1215    F    Cl    H    CF3    H    SCH2COOnC3H71-1216    F    Cl    H    CF3    H    SCH2COOnC4H91-1217    F    Cl    H    CF3    H    SCH2COOnC5H111-1218    F    Cl    H    CF3    H    SCH2COOiC3H71-1219    F    Cl    H    CF3    H    SCH2COOcC5H91-1220    F    Cl    H    CF3    H    SCH2COOcC6H111-1221    F    Cl    H    CF3    H    SCH(CH3)COOCH31-1222    F    Cl    H    CF3    H    SCH(CH3)COOC2H6
                                   表1(续)
    化合物    X    Y     R3    R1   R2         B编号
    1-1223    F    Cl    H    CF3    H    SCH(CH3)COOnC3H71-1224    F    Cl    H    CF3    H    SCH(CH3)COOnC4H91-1225    F    Cl    H    CF3    H    SCH(CH3)COOnC5H111-1226    F    Cl    H    CF3    H    SCH(CH3)COOiC3H71-1227    F    Cl    H    CF3    H    SCH(CH3)COOcC5H91-1228    F    Cl    H    CF3    H    SCH(CH3)COOcC6H111-1229    F    Cl    H    CF3    H    SCH2CON(CH3)21-1230    F    Cl    H    CF3    H    SCH2CON(C2H5)21-1231    F    Cl    H    CF3    H    SCH2CON(四亚甲基)1-1232    F    Cl    H    CF3    H    SCH2CON(五亚甲基)1-1233    F    Cl    H    CF3    H    SCH2CON(3-氧杂-1,5-亚戊基)1-1234    F    Cl    H    CF3    H    SCH(CH3)CON(CH3)21-1235    F    Cl    H    CF3    H    SCH(CH3)CON(C2H5)21-1236    F    Cl    H    CF3    H    SCH(CH3)CON(四亚甲基)1-1237    F    Cl    H    CF3    H    SCH(CH3)CON(五亚甲基)1-1238    H    F    H     CF3    H    SO2Cl1-1239    H    Cl    H    CF3    H    SO2Cl1-1240    H    Br    H    CF3    H    SO2Cl1-1241    F    F    H     CF3    H    SO2Cl1-1242    F    Cl    H    CF3    H    SO2Cl
                           表1(续)
    化合物    X    Y     R3   R1    R2    B编号
    1-1243    F    Br    H    CF3    H    SO2Cl1-1244    H    Cl    H    CF3    H    SO2OCH31-1245    H    Cl    H    CF3    H    SO2OC2H51-1246    H    Cl    H    CF3    H    SO2OiC3H71-1247    H    Cl    H    CF3    H    SO2OCH2CH=CH21-1248    F    Cl    H    CF3    H    SO2OCH31-1249    F    Cl    H    CF3    H    SO2OC2H51-1250    F    Cl    H    CF3    H    SO2OiC3 -H71-1251    F    Cl    H    CF3    H    SO2OCH2CH=CH21-1252    H    Cl    H    CF3    H    SO2N(CH3)21-1253    H    Cl    H    CF3    H    SO2N(C2H5)21-1254    F    Cl    H    CF3    H    SO2N(CH3)21-1255    F    Cl    H    CF3    H    SO2N(C2H5)21-1256    H    Cl    H    CF3    H    COOH1-1257    H    Cl    H    CF3    H    COOCH31-1258    H    Cl    H    CF3    H    COOC2H51-1259    H    Cl    H    CF3    H    COOnC3H71-1260    H    Cl    H    CF3    H    COOnC4H91-1261    H    Cl    H    CF3    H    COOnC5H111-1262    H    Cl    H    CF3    H    COOiC3H71-1263    H    Cl    H    CF3    H    COOCH2CH2Cl1-1264    H    Cl    H    CF3    H    COOCH2CH2Br1-1265    H    Cl    H    CF3    H    CON(CH3)2
                                 表1(续)
    化合物    X    Y     R3   R1    R2     B编号
    1-1266    H    Cl    H    CF3    H    CONHCH31-1267    H    Cl    H    CF3    H    CON(C2H5)21-1268    H    Cl    H    CF3    H    CONHC2H51-1269    H    Cl    H    CF3    H    COCH31-1270    H    Cl    H    CF3    H    COC2H51-1271    H    Cl    H    CF3    H    COCH2Cl1-1272    H    Cl    H    CF3    H    CHO1-1273    H    Cl    H    CF3    H    CH=CHCOOCH31-1274    H    Cl    H    CF3    H    CH=CHCOOC2H51-1275    H    Cl    H    CF3    H    CH2CH2COOCH31-1276    H    Cl    H    CF3    H    CH2CH2COOC2H51-1277    F    Cl    H    CF3    H    COOH1-1278    F    Cl    H    CF3    H    COOCH31-1279    F    Cl    H    CF3    H    COOC2H51-1280    F    Cl    H    CF3    H    COOnC3H71-1281    F    Cl    H    CF3    H    COOnC4H91-1282    F    Cl    H    CF3    H    COOnC5H111-1283    F    Cl    H    CF3    H    COOiC3H71-1284    F    Cl    H    CF3    H    COOCH2CH2Cl1-1285    F    Cl    H    CF3    H    COOCH2CH2Br1-1286    F    Cl    H    CF3    H    CON(CH3)21-1287    F    Cl    H    CF3    H    CONHCH31-1288    F    Cl    H    CF3    H    CON(C2H5)2
                                 表1(续)
    化合物    X    Y     R3    R1    R2     B编号
    1-1289    F    Cl    H     CF3    H    CONHC2H51-1290    F    Cl    H     CF3    H    COCH31-1291    F    Cl    H     CF3    H    COC2H51-1292    F    Cl    H     CF3    H    COCH2Cl1-1293    F    Cl    H     CF3    H    CHO1-1294    F    Cl    H     CF3    H    CH=CHCOOCH31-1295    F    Cl    H     CF3    H    CH=CHCOOC2H51-1296    F    Cl    H     CF3    H    CH2CH2COOCH31-1297    F    Cl    H     CF3    H    CH2CH2COOC2H51-1298    H    F     CH3  CF3    H    NO21-1299    H    C     CH3  CF3    H    NO21-1300    H    Br    CH3  CF3    H    NO21-1301    F    F     CH3  CF3    H    NO21-1302    F    Cl    CH3  CF3    H    NO21-1303    F    Br    CH3  CF3    H    NO21-1304    H    F     CH3  CF3    H    NH21-1305    H    Cl    CH3  CF3    H    NH21-1306    H    Br    CH3  CF3    H    NH21-1307    F    F     CH3  CF3    H    NH21-1308    F    Cl    CH3  CF3    H    NH21-1309    H    Cl    CH3  CF3    H    NHCH(CH3)COOCH31-1310    H    Cl    CH3  CF3    H    NHCH(CH3)COOC2H51-1311    H    Cl    CH3  CF3    H    NHCH(CH3)COOnC3H7
                                  表1(续)
    化合物    X    Y     R3     R1    R2          B编号
    1-1312    H    Cl    CH3    CF3    H    NHCH(CH3)COOnC4H91-1313    H    Cl    CH3    CF3    H    NHCH(CH3)COOnC5H111-1314    H    Cl    CH3    CF3    H    NHCH(CH3)COOiC3H71-1315    H    Cl    CH3    CF3    H    NHCH(CH3)COOcC5H91-1316    H    Cl    CH3    CF3    H    NHCH(CH3)COOcC6H111-1317    F    Cl    CH3    CF3    H    NHCH31-1318    F    Cl    CH3    CF3    H    NHC2H51-1319    F    Cl    CH3    CF3    H    NHCH2CH=CH21-1320    F    Cl    CH3    CF3    H    NHCH2C≡CH1-1321    F    Cl    CH3    CF3    H    NHCH(CH3)C≡CH1-1322    F    Cl    CH3    CF3    H    NHSO2CH31-1323    F    Cl    CH3    CF3    H    NHSO2C2H51-1324    F    Cl    CH3    CF3    H    NHSO2CH2Cl1-1325    F    Cl    CH3    CF3    H    NHSO2CF31-1326    F    Cl    CH3    CF3    H    N(CH3)SO2CH31-1327    F    Cl    CH3    CF3    H    N(CH2C≡CH)SO2CH31-1328    F    Cl    CH3    CF3    H    NHCOOCH31-1329    F    Cl    CH3    CF3    H    NHCOOC2H51-1330    F    Cl    CH3    CF3    H    NHCOOnC3H71-1331    F    Cl    CH3    CF3    H    NHCOOiC3H71-1332    F    Cl    CH3    CF3    H    NHCOOnC4H91-1333    F    Cl    CH3    CF3    H    NHCOOnC5H11
                            表1(续)
  化合物    X    Y     R3     R1     R2      B编号
  1-1334    F    Cl    CH3    CF3    H    NHCH2COOCH31-1335    F    Cl    CH3    CF3    H    NHCH2COOC2H51-1336    F    Cl    CH3    CF3    H    NHCH2COOnC3H71-1337    F    Cl    CH3    CF3    H    NHCH2COOnC4H91-1338    F    Cl    CH3    CF3    H    NHCH2COOnC5H111-1339    F    Cl    CH3    CF3    H    NHCH2COOiC3H71-1340    F    Cl    CH3    CF3    H    NHCH2COOcC5H91-1341    F    Br    CH3    CF3    H    NH2 -1-1342    H    F     CH3    CF3    H    OH1-1343    H    Cl    CH3    CF3    H    OH1-1344    H    Br    CH3    CF3    H    OH1-1345    F    F     CH3    CF3    H    OH1-1346    F    Cl    CH3    CF3    H    OH1-1347    F    Br    CH3    CF3    H    OH1-1348    H    Cl    CH3    CF3    H    NHCH31-1349    H    Cl    CH3    CF3    H    NHC2H51-1350    H    Cl    CH3    CF3    H    NHCH2CH=CH21-1351    H    Cl    CH3    CF3    H    NHCH2C≡CH1-1352    H    Cl    CH3    CF3    H    NHCH(CH3)C≡CH1-1353    H    Cl    CH3    CF3    H    NHSO2CH31-1354    H    Cl    CH3    CF3    H    NHSO2C2H51-1355    H    Cl    CH3    CF3    H    NHSO2CH2Cl1-1356    H    Cl    CH3    CF3    H    NHSO2CF3
                              表1(续)
    化合物    X    Y     R3     R1     R2       B编号
    1-1357    H    Cl    CH3    CF3    H    N(CH3)SO2CH31-1358    H    Cl    CH3    CF3    H    N(CH2C≡CH)SO2CH31-1359    H    Cl    CH3    CF3    H    NHCOOCH31-1360    H    Cl    CH3    CF3    H    NHCOOC2H51-1361    H    Cl    CH3    CF3    H    NHCOOnC3H71-1362    H    Cl    CH3    CF3    H    NHCOOiC3H71-1363    H    Cl    CH3    CF3    H    NHCOOnC4H91-1364    H    Cl    CH3    CF3    H    NHCOOnC- 5H111-1365    H    Cl    CH3    CF3    H    NHCH2COOCH31-1366    H    Cl    CH3    CF3    H    NHCH2COOC2H51-1367    H    Cl    CH3    CF3    H    NHCH2COOnC3H71-1368    H    Cl    CH3    CF3    H    NHCH2COOnC4H91-1369    H    Cl    CH3    CF3    H    NHCH2COOnC5H111-1370    H    Cl    CH3    CF3    H    NHCH2COOiC3H71-1371    H    Cl    CH3    CF3    H    NHCH2COOcC5H91-1372    H    Cl    CH3    CF3    H    NHCH2COOcC6H111-1373    F    Cl    CH3    CF3    H    NHCH2COOcC6H111-1374    F    Cl    CH3    CF3    H    NHCH(CH3)COOCH31-1375    F    Cl    CH3    CF3    H    NHCH(CH3)COOC2H51-1376    F    Cl    CH3    CF3    H    NHCH(CH3)COOnC3H71-1377    F    Cl    CH3    CF3    H    NHCH(CH3)COOnC4H91-1378    F    Cl    CH3    CF3    H    NHCH(CH3)COOnC5H111-1379    F    Cl    CH3    CF3    H    NHCH(CH3)COOiC3H7
                              表1(续)
    化合物    X    Y     R3     R1     R2       B编号
    1-1380    F    Cl    CH3    CF3    H    NHCH(CH3)COOcC5H91-1381    F    Cl    CH3    CF3    H    NHCH(CH3)COOcC6H111-1382    H    Cl    CH3    CF3    H    OCH31-1383    H    Cl    CH3    CF3    H    OC2H51-1384    H    Cl    CH3    CF3    H    OiC3H71-1385    H    Cl    CH3    CF3    H    OnC3H71-1386    H    Cl    CH3    CF3    H    OCH2CH2Cl1-1387    H    Cl    CH3    CF3    H    OCF2CF2H1-1388    H    Cl    CH3    CF3    H    OcC5H91-1389    H    Cl    CH3    CF3    H    OcC6H111-1390    H    Cl    CH3    CF3    H    OCH2CH=CH21-1391    H    Cl    CH3    CF3    H    OCH2CCl=CH21-1392    H    Cl    CH3    CF3    H    OCH2CCl=CHCl1-1393    H    Cl    CH3    CF3    H    OCH(CH3)CH=CH21-1394    H    Cl    CH3    CF3    H    OCH2C≡CH1-1395    H    Cl    CH3    CF3    H    OCH(CH3)C≡CH1-1396    H    Cl    CH3    CF3    H    OCH2C≡CBr1-1397    H    Cl    CH3    CF3    H    OCH2C≡CCl1-1398    H    Cl    CH3    CF3    H    OCH2C≡CCH2Cl1-1399    H    Cl    CH3    CF3    H    OCH2CN1-1400    H    Cl    CH3    CF3    H    OCH2OCH31-1401    H    Cl    CH3    CF3    H    OCH2OC2H51-1402    H    Cl    CH3    CF3    H    OCH2SCH3
                              表1(续)
    化合物    X    Y     R3     R1     R2     B编号
    1-1403    H    Cl    CH3    CF3    H    OCH2COOCH31-1404    H    Cl    CH3    CF3    H    OCH2COOC2H51-1405    H    Cl    CH3    CF3    H    OCH2COOnC3H71-1406    H    Cl    CH3    CF3    H    OCH2COOnC4H91-1407    H    Cl    CH3    CF3    H    OCH2COOnC5H111-1408    H    Cl    CH3    CF3    H    OCH2COOiC3H71-1409    H    Cl    CH3    CF3    H    OCH2COOcC5H91-1410    H    Cl    CH3    CF3    H    OCH2COOcC6H111-1411    H    Cl    CH3    CF3    H    OCH(CH3)COOCH31-1412    H    Cl    CH3    CF3    H    OCH(CH3)COOC2H51-1413    H    Cl    CH3    CF3    H    OCH(CH3)COOnC3H71-1414    H    Cl    CH3    CF3    H    OCH(CH3)COOnC4H91-1415    H    Cl    CH3    CF3    H    OCH(CH3)COOnC5H111-1416    H    Cl    CH3    CF3    H    OCH(CH3)COOiC3H71-1417    H    Cl    CH3    CF3    H    OCH(CH3)COOcC5H91-1418    H    Cl    CH3    CF3    H    OCH(CH3)COOcC5H111-1419    H    Cl    CH3    CF3    H    OCH2CON(CH3)21-1420    H    Cl    CH3    CF3    H    OCH2CON(C2H5)21-1421    H    Cl    CH3    CF3    H    OCH2CON(CH3)C2H51-1422    H    Cl    CH3    CF3    H    OCH(CH3)CON(CH3)21-1423    H    Cl    CH3    CF3    H    OCH(CH3)CON(C2H5)21-1424    H    Cl    CH3    CF3    H    OCH(CH3)CON(CH3)C2H51-1425    H    Cl    CH3    CF3    H    OCH2COON(CH3)2
                              表1(续)
    化合物    X    Y     R3     R1     R2          B编号
    1-1426    H    Cl    CH3    CF3    H    OCH2COON(C2H5)21-1427    H    Cl    CH3    CF3    H    OCH(CH3)COON(CH3)21-1428    H    Cl    CH3    CF3    H    OCH(CH3)COON(C2H5)21-1429    F    Cl    CH3    CF3    H    OCH31-1430    F    Cl    CH3    CF3    H    OC2H51-1431    F    Cl    CH3    CF3    H    OiC3H71-1432    F    Cl    CH3    CF3    H    OnC3H71-1433    F    Cl    CH3    CF3    H    OCH2CH2Cl1-1434    F    Cl    CH3    CF3    H    OCF2CF2H1-1435    F    Cl    CH3    CF3    H    OcC5H91-1436    F    Cl    CH3    CF3    H    OcC6H111-1437    F    Cl    CH3    CF3    H    OCH2CH=CH21-1438    F    Cl    CH3    CF3    H    OCH2CCl=CH21-1439    F    Cl    CH3    CF3    H    OCH2CCl=CHCl1-1440    F    Cl    CH3    CF3    H    OCH(CH3)CH=CH21-1441    F    Cl    CH3    CF3    H    OCH2C≡CH1-1442    F    Cl    CH3    CF3    H    OCH(CH3)C≡CH1-1443    F    Cl    CH3    CF3    H    OCH2C≡CBr1-1444    F    Cl    CH3    CF3    H    OCH2C≡CCl1-1445    F    Cl    CH3    CF3    H    OCH2C≡CCH2Cl1-1446    F    Cl    CH3    CF3    H    OCH2CN1-1447    F    Cl    CH3    CF3    H    OCH2OCH3
                               表1(续)
    化合物    X    Y     R3     R1     R2      B编号
    1-1448    F    Cl    CH3    CF3    H    OCH2OC2H51-1449    F    Cl    CH3    CF3    H    OCH2SCH31-1450    F    Cl    CH3    CF3    H    OCH2COOCH31-1451    F    Cl    CH3    CF3    H    OCH2COOC2H51-1452    F    Cl    CH3    CF3    H    OCH2COOnC3H71-1453    F    Cl    CH3    CF3    H    OCH2COOnC4H91-1454    F    Cl    CH3    CF3    H    OCH2COOnC5H111-1455    F    Cl    CH3    CF3    H    OCH2COOiC3H71-1456    F    Cl    CH3    CF3    H    OCH2COOcC5H91-1457    F    Cl    CH3    CF3    H    OCH2COOcC6H111-1458    F    Cl    CH3    CF3    H    OCH(CH3)COOCH31-1459    F    Cl    CH3    CF3    H    OCH(CH3)COOC2H51-1460    F    Cl    CH3    CF3    H    OCH(CH3)COOnC3H71-1461    F    Cl    CH3    CF3    H    OCH(CH3)COOnC4H91-1462    F    Cl    CH3    CF3    H    OCH(CH3)COOnC5H111-1463    F    Cl    CH3    CF3    H    OCH(CH3)COOiC3H71-1464    F    Cl    CH3    CF3    H    OCH(CH3)COOcC5H91-1465    F    Cl    CH3    CF3    H    OCH(CH3)COOcC6H111-1466    F    Cl    CH3    CF3    H    OCH2CON(CH3)21-1467    F    Cl    CH3    CF3    H    OCH2CON(C2H5)21-1468    F    Cl    CH3    CF3    H    OCH2CON(CH3)C2H51-1469    F    Cl    CH3    CF3    H    OCH(CH3)CON(CH3)21-1470    F    Cl    CH3    CF3    H    OCH(CH3)CON(C2H5)2
                             表1(续)
    化合物    X    Y     R3     R1     R2       B编号
    1-1471    F    Cl    CH3    CF3    H    OCH(CH3)CON(CH3)C2H51-1472    F    Cl    CH3    CF3    H    OCH2COON(CH3)21-1473    F    Cl    CH3    CF3    H    OCH2COON(C2H5)21-1474    F    Cl    CH3    CF3    H    OCH(CH3)COON(CH3)21-1475    F    Cl    CH3    CF3    H    OCH(CH3)COON(C2H5)21-1476    H    F     CH3    CF3    H    SH1-1477    H    Cl    CH3    CF3    H    SH1-1478    H    Br    CH3    CF3    H    SH1-1479    F    F     CH3    CF3    H    SH1-1480    F    Cl    CH3    CF3    H    SH1-1481    F    Br    CH3    CF3    H    SH1-1482    H    Cl    CH3    CF3    H    SCH31-1483    H    Cl    CH3    CF3    H    SC2H51-1484    H    Cl    CH3    CF3    H    SiC3H71-1485    H    Cl    CH3    CF3    H    SCH2CH2Cl1-1486    H    Cl    CH3    CF3    H    ScC5H91-1487    H    Cl    CH3    CF3    H    ScC6H111-1488    H    Cl    CH3    CF3    H    SCH2CH=CH21-1489    H    Cl    CH3    CF3    H    SCH2CCl=CH21-1490    H    Cl    CH3    CF3    H    SCH2CCl=CHCl1-1491    H    Cl    CH3    CF3    H    SCH(CH3)CH=CH21-1492    H    Cl    CH3    CF3    H    SCH2C≡CH1-1493    H    Cl    CH3    CF3    H    SCH(CH3)C≡CH
                      表1(续)
  化合物    X    Y     R3     R1     R2       B编号
  1-1494    H    Cl    CH3    CF3    H    SCH2COOCH31-1495    H    Cl    CH3    CF3    H    SCH2COOC2H51-1496    H    Cl    CH3    CF3    H    SCH2COOnC3H71-1497    H    Cl    CH3    CF3    H    SCH2COOnC4H91-1498    H    Cl    CH3    CF3    H    SCH2COOnC5H111-1499    H    Cl    CH3    CF3    H    SCH2COOiC3H71-1500    H    Cl    CH3    CF3    H    SCH2COOcC5H91-1501    H    Cl    CH3    CF3    H    SCH2COOcC6H111-1502    H    Cl    CH3    CF3    H    SCH(CH3)COOCH31-1503    H    Cl    CH3    CF3    H    SCH(CH3)COOC2H51-1504    H    Cl    CH3    CF3    H    SCH(CH3)COOnC3H71-1505    H    Cl    CH3    CF3    H    SCH(CH3)COOnC4H91-1506    H    Cl    CH3    CF3    H    SCH(CH3)COOnC5H111-1507    H    Cl    CH3    CF3    H    SCH(CH3)COOiC3H71-1508    H    Cl    CH3    CF3    H    SCH(CH3)COOcC5H91-1509    H    Cl    CH3    CF3    H    SCH(CH3)COOcC6H111-1510    H    Cl    CH3    CF3    H    SCH2CON(CH3)21-1511    H    Cl    CH3    CF3    H    SCH2CON(C2H5)21-1512    H    Cl    CH3    CF3    H    SCH2CON(四亚甲基)1-1513    H    Cl    CH3    CF3    H    SCH2CON(五亚甲基)1-1514    H    Cl    CH3    CF3    H    SCH2CON(3-氧杂-1,5-亚戊基)1-1515    H    Cl    CH3    CF3    H    SCH(CH3)CON(CH3)2
                                  表1(续)
    化合物    X    Y     R3     R1     R2    B编号
    1-1516    H    Cl    CH3    CF3    H  SCH(CH3)CON(C2H5)21-1517    H    Cl    CH3    CF3    H  SCH(CH3)CON(四亚甲基)1-1518    H    Cl    CH3    CF3    H  SCH(CH3)CON(五亚甲基)1-1519    F    Cl    CH3    CF3    H  SCH31-1520    F    Cl    CH3    CF3    H  SC2H51-1521    F    Cl    CH3    CF3    H  SiC3H71-1522    F    Cl    CH3    CF3    H  SCH2CH2Cl1-1523    F    Cl    CH3    CF3    H  ScC5H91-1524    F    Cl    CH3    CF3    H  ScC6H111-1525    F    Cl    CH3    CF3    H  SCH2CH=CH21-1526    F    Cl    CH3    CF3    H  SCH2CCl=CH21-1527    F    Cl    CH3    CF3    H  SCH2CCl=CHCl1-1528    F    Cl    CH3    CF3    H  SCH(CH3)CH=CH21-1529    F    Cl    CH3    CF3    H  SCH2C≡CH1-1530    F    Cl    CH3    CF3    H  SCH(CH3)C≡CH1-1531    F    Cl    CH3    CF3    H  SCH2COOCH31-1532    F    Cl    CH3    CF3    H  SCH2COOC2H51-1533    F    Cl    CH3    CF3    H  SCH2COOnC3H71-1534    F    Cl    CH3    CF3    H  SCH2COOnC4H91-1535    F    Cl    CH3    CF3    H  SCH2COOnC5H111-1536    F    Cl    CH3    CF3    H  SCH2COOiC3H7
                             表1(续)
    化合物    X    Y     R3     R1     R2       B编号
    1-1537    F    Cl    CH3    CF3    H    SCH2COOcC5H91-1538    F    Cl    CH3    CF3    H    SCH2COOcC6H111-1539    F    Cl    CH3    CF3    H    SCH(CH3)COOCH31-1540    F    Cl    CH3    CF3    H    SCH(CH3)COOC2H51-1541    F    Cl    CH3    CF3    H    SCH(CH3)COOnC3H71-1542    F    Cl    CH3    CF3    H    SCH(CH3)COOnC4H91-1543    F    Cl    CH3    CF3    H    SCH(CH3)COOnC5H111-1544    F    Cl    CH3    CF3    H    SCH(CH3)COOiC3H71-1545    F    Cl    CH3    CF3    H    SCH(CH3)COOcC5H91-1546    F    Cl    CH3    CF3    H    SCH(CH3)COOcC6H111-1547    F    Cl    CH3    CF3    H    SCH2CON(CH3)21-1548    F    Cl    CH3    CF3    H    SCH2CON(C2H5)21-1549    F    Cl    CH3    CF3    H    SCH2CON(四亚甲基)1-1550    F    Cl    CH3    CF3    H    SCH2CON(五亚甲基)1-1551    F    Cl    CH3    CF3    H    SCH2CON(3-氧杂-1,5-亚戊基)1-1552    F    Cl    CH3    CF3    H    SCH(CH3)CON(CH3)21-1553    F    Cl    CH3    CF3    H    SCH(CH3)CON(C2H5)21-1554    F    Cl    CH3    CF3    H    SCH(CH3)CON(四亚甲基)1-1555    F    Cl    CH3    CF3    H    SCH(CH3)CON(五亚甲基)
                               表1(续)
    化合物    X    Y     R3     R1     R2    B编号
    1-1556    H    F     CH3    CF3    H    SO2Cl1-1557    H    Cl    CH3    CF3    H    SO2Cl1-1558    H    Br    CH3    CF3    H    SO2Cl1-1559    F    F     CH3    CF3    H    SO2Cl1-1560    F    Cl    CH3    CF3    H    SO2Cl1-1561    F    Br    CH3    CF3    H    SO2Cl1-1562    H    Cl    CH3    CF3    H    SO2OCH31-1563    H    Cl    CH3    CF3    H    SO2OC2H51-1564    H    Cl    CH3    CF3    H    SO2OiC3H71-1565    H    Cl    CH3    CF3    H    SO2OCH2CH=CH21-1566    F    Cl    CH3    CF3    H    SO2OCH31-1567    F    Cl    CH3    CF3    H    SO2OC2H51-1568    F    Cl    CH3    CF3    H    SO2OiC3H71-1569    F    Cl    CH3    CF3    H    SO2OCH2CH=CH21-1570    H    Cl    CH3    CF3    H    SO2N(CH3)21-1571    H    Cl    CH3    CF3    H    SO2N(C2H5)21-1572    F    Cl    CH3    CF3    H    SO2N(CH3)21-1573    F    Cl    CH3    CF3    H    SO2N(C2H5)21-1574    H    Cl    CH3    CF3    H    COOH1-1575    H    Cl    CH3    CF3    H    COOCH31-1576    H    Cl    CH3    CF3    H    COOC2H61-1577    H    Cl    CH3    CF3    H    COOnC3H71-1578    H    Cl    CH3    CF3    H    COOnC4H9
                              表1(续)
    化合物    X    Y     R3     R1     R2    B编号
    1-1579    H    Cl    CH3    CF3    H    COOnC5H111-1580    H    Cl    CH3    CF3    H    COOiC3H71-1581    H    Cl    CH3    CF3    H    COOCH2CH2Cl1-1582    H    Cl    CH3    CF3    H    COOCH2CH2Br1-1583    H    Cl    CH3    CF3    H    CON(CH3)21-1584    H    Cl    CH3    CF3    H    CONHCH31-1585    H    Cl    CH3    CF3    H    CON(C2H5)21-1586    H    Cl    CH3    CF3    H    CONHC2H51-1587    H    Cl    CH3    CF3    H    COCH31-1588    H    Cl    CH3    CF3    H    COC2H51-1589    H    Cl    CH3    CF3    H    COCH2Cl1-1590    H    Cl    CH3    CF3    H    CHO1-1591    H    Cl    CH3    CF3    H    CH=CHCOOCH31-1592    H    Cl    CH3    CF3    H    CH=CHCOOC2H51-1593    H    Cl    CH3    CF3    H    CH2CH2COOCH31-1594    H    Cl    CH3    CF3    H    CH2CH2COOC2H51-1595    F    Cl    CH3    CF3    H    COOH1-1596    F    Cl    CH3    CF3    H    COOCH31-1597    F    Cl    CH3    CF3    H    COOC2H51-1598    F    Cl    CH3    CF3    H    COOnC3H7l-1599    F    Cl    CH3    CF3    H    COOnC4H91-1600    F    Cl    CH3    CF3    H    COOnC5H111-1601    F    Cl    CH3    CF3    H    COOiC3H7
                              表1(续)
    化合物    X    Y     R3     R1     R2       B编号
    1-1602    F    Cl    CH3    CF3    H    COOCH2CH2Cl1-1603    F    Cl    CH3    CF3    H    COOCH2CH2Br1-1604    F    Cl    CH3    CF3    H    CON(CH3)21-1605    F    Cl    CH3    CF3    H    CONHCH31-1606    F    Cl    CH3    CF3    H    CON(C2H5)21-1607    F    Cl    CH3    CF3    H    CONHC2H51-1608    F    Cl    CH3    CF3    H    COCH31-1609    F    Cl    CH3    CF3    H    COC2H51-1610    F    Cl    CH3    CF3    H    COCH2Cl1-1611    F    Cl    CH3    CF3    H    CHO1-1612    F    Cl    CH3    CF3    H    CH=CHCOOCH31-1613    F    Cl    CH3    CF3    H    CH=CHCOOC2H51-1614    F    Cl    CH3    CF3    H    CH2CH2COOCH31-1615    F    Cl    CH3    CF3    H    CH2CH2COOC2H51-1616    H    F     CH3    CF3    H    H1-1617    H    Cl    CH3    CF3    H    H1-1618    H    Br    CH3    CF3    H    H1-1619    F    F     CH3    CF3    H    H1-1620    F    Cl    CH3    CF3    H    H1-1621    F    Br    CH3    CF3    H    H1-1622    F    Cl    H       CF3    CH3 CH2CHClCO2C2H51-1623    F    Cl    H       CF2    H    CH2CHClCO2C2H51-1624    F    Cl    H       CF3    CH3 CH2CHClCO2CH3
                               表1(续)
    化合物    X    Y     R3   R1     R2     B编号
    1-1625    F    Cl    H     CF3    H    CH2CHClCO2CH31-1626    F    Cl    H     CF3    H    OCH2CO2H1-1627    F    Cl    H     CF3    CH3 OCH2CO2H1-1628    F    Cl    CH3  CF3    H    OCH2CO2H1-1629    F    Cl    H     CF3    H    OCH(CH3)CO2H1-1630    F    Cl    H     CF3    CH3 OCH(CH3)CO2H1-1631    F    Cl    CH3  CF3    H    OCH(CH3)CO2H1-1632    H    Cl    H     CF3    H    OCH2CO2H1-1633    H    Cl    H     CF3    CH3 OCH2CO2H1-1634    H    Cl    CH3  CF3    H    OCH2CO2H1-1635    H    Cl    H     CF3    H    OCH(CH3)CO2H1-1636    H    Cl    H     CF3    CH3 OCH(CH3)CO2H1-1637    H    Cl    CH3  CF3    H    OCH(CH3)CO2H1-1638    F    Cl    H     CF3    H    SCH2CO2H1-1639    F    Cl    H     CF3    CH3 SCH2CO2H1-1640    F    Cl    CH3  CF3    H    SCH2CO2H1-1641    F    Cl    H     CF3    H    SCH(CH3)CO2H1-1642    F    Cl    H     CF3    CH3 SCH(CH3)CO2H1-1643    F    Cl    CH3  CF3    H    SCH(CH3)CO2H1-1644    H    Cl    H     CF3    H    SCH2CO2H1-1645    H    Cl    H     CF3    CH3 SCH2CO2H1-1646    H    Cl    CH3  CF3    H    SCH2CO2H1-1647    H    Cl    H     CF3    H    SCH(CH3)CO2H
                               表1(续)
    化合物    X     Y     R3  R1     R2          B编号
    1-1648    H     Cl    H    CF3    CH3   SCH(CH3)CO2H1-1649    H     Cl    CH3 CF3    H      SCH(CH3)CO2H1-1650    F     Cl    H    CF3    CH3   OCH(C2H5)CO2CH31-1651    Cl    Cl    H    CF3    H      OCH2CO2CH31-1652    Cl    Cl    H    CF3    H      OCH2CO2C2H51-1653    Cl    Cl    H    CF3    H      OCH2CO2 iC3H71-1654    Cl    Cl    H    CF3    CH3   OCH2CO2CH31-1655    Cl    Cl    H    CF3    CH3   OCH2CO2C2H51-1656    Cl    Cl    H    CF3    CH3   OCH2CO2 iC3H71-1657    Cl    Cl    CH3 CF3    H      OCH2CO2CH31-1658    Cl    Cl    CH3 CF3    H      OCH2CO2C2H51-1659    Cl    Cl    CH3 CF3    H      OCH2CO2 iC3H71-1660    Cl    Cl    H    CF3    H      OCH2C≡CH1-1661    Cl    Cl    H    CF3    H      OCH(CH3)C≡CH1-1662    Cl    Cl    H    CF3    H      OCH(CH3)CO2C2H51-1663    Cl    Cl    H    CF3    CH3   OCH2C≡CH1-1664    Cl    Cl    H    CF3    CH3   OCH(CH3)C≡CH1-1665    Cl    Cl    H    CF3    CH3   OCH(CH3)CO2C2H51-1666    Cl    Cl    CH3 CF3    H      OCH2C≡CH1-1667    Cl    Cl    CH3 CF3    H      OCH(CH3)C≡CH1-1668    Cl    Cl    CH3 CF3    H      OCH(CH3)CO2C2H51-1669    F     Br    H    CF3    H      OCH2CO2CH3
                               表1(续)
    化合物    X    Y     R3  R1     R2      B编号
    1-1670    F    Br    H    CF3    H    OCH2CO2C2H51-1671    F    Br    H    CF3    H    OCH2CO2 iC3H71-1672    F    Br    H    CF3    CH3 OCH2CO2CH31-1673    F    Br    H    CF3    CH3 OCH2CO2C2H51-1674    F    Br    H    CF3    CH3 OCH2CO2 iC3H71-1675    F    Br    CH3 CF3    H    OCH2CO2CH31-1676    F    Br    CH3 CF3    H    OCH2CO2C2H51-1677    F    Br    CH3 CF3    H    OCH2CO2 iC3H71-1678    F    Br    H    CF3    H    OCH2C≡CH1-1679    F    Br    H    CF3    H    OCH(CH3)C≡CH1-1680    F    Br    H    CF3    H    OCH(CH3)CO2C2H51-1681    F    Br    H    CF3    CH3 OCH2C≡CH1-1682    F    Br    H    CF3    CH3 OCH(CH3)C≡CH1-1683    F    Br    H    CF3    CH3 OCH(CH3)CO2C2H51-1684    F    Br    CH3 CF3    H    OCH2C≡CH1-1685    F    Br    CH3 CF3    H    OCH(CH3)C≡CH1-1686    F    Br    CH3 CF3    H    OCH(CH3)CO2C2H5
                        表1(续)
  化合物    X     Y  R3  R1  R2  B编号
  1-1687    Cl    Cl H    CF3 H    H1-1688    Cl    Cl H    CF3 H    OH1-1689    Cl    Cl H    CF3 H    NO21-1690    Cl    Cl H    CF3 H    NH21-1691    Cl    Cl H    CF3 H    NHSO2CH31-1692    Cl    Cl H    CF3 H    NHSO2CH2Cl1-1693    Cl    Cl H    CF3 H    NHCH2CO2CH31-1694    Cl    Cl H    CF3 H    NHCH2CO2C2H51-1695    Cl    Cl H    CF3 H    NHCH2CO2 iC3H71-1696    Cl    Cl H    CF3 H    NHCH(CH3)CO2CH31-1697    Cl    Cl H    CF3 H    NHCH(CH3)CO2C2H51-1698    Cl    Cl H    CF3 H    NHCH(CH3)CO2 iC3H71-1699    Cl    Cl H    CF3 H    CO2H1-1700    Cl    Cl H    CF3 H    CO2CH31-1701    Cl    Cl H    CF3 H    CO2C2H51-1702    Cl    Cl H    CF3 H    CO2 nC3H71-1703    Cl    Cl H    CF3 H    CO2 nC4H91-1704    Cl    Cl H    CF3 H    CO2 nC5H111-1705    Cl    Cl H    CF3 H    CO2 iC3H71-1706    Cl    Cl H    CF3 H    CO2CH2CH2Cl1-1707    Cl    Cl H    CF3 H    CO2CH2CH2Br1-1708    Cl    Cl H    CF3 H    CON(CH3)21-1709    Cl    Cl H    CF3 H    CONHCH31-1710    Cl    Cl H    CF3 H    CON(C2H5)21-1711    Cl    Cl H    CF3 H    CONHC2H51-1712    Cl    Cl H    CF3 H    COCH31-1713    Cl    Cl H    CF3 H    COC2H51-1714    Cl    Cl H    CF3 H    COCH2Cl1-1715    Cl    Cl H    CF3 H    CHO1-1716    Cl    Cl H    CF3 H    CH=CHCO2CH31-1717    Cl    Cl H    CF3 H    OiC3H71-1718    Cl    Cl H    CF3 CH3 H1-1719    Cl    Cl H    CF3 CH3 OH
                             表1(续)
   化合物编号 X     Y     R3  R1     R2     B
    1-1720    Cl    Cl    H    CF3    CH3    NO21-1721    Cl    Cl    H    CF3    CH3    NH21-1722    Cl    Cl    H    CF3    CH3    NHSO2CH31-1723    Cl    Cl    H    CF3    CH3    NHSO2CH2Cll-l724    Cl    Cl    H    CF3    CH3    NHCH2CO2CH31-1725    Cl    Cl    H    CF3    CH3    NHCH2CO2C2H51-1726    Cl    Cl    H    CF3    CH3    NHCH2CO2 iC3H71-1727    Cl    Cl    H    CF3    CH3    NHCH(CH3)CO2CH31-1728    Cl    Cl    H    CF3    CH3    NHCH(CH3)CO2C2H51-1729    Cl    Cl    H    CF3    CH3    NHCH(CH3)CO2 iC3H71-1730    Cl    Cl    H    CF3    CH3    CO2H1-1731    Cl    Cl    H    CF3    CH3    CO2CH31-1732    Cl    Cl    H    CF3    CH3    CO2C2H51-1733    Cl    Cl    H    CF3    CH3    CO2 nC3H71-1734    Cl    Cl    H    CF3    CH3    CO2 nC4H91-1735    Cl    Cl    H    CF3    CH3    CO2 nC5H111-1736    Cl    Cl    H    CF3    CH3    CO2 iC3H71-1737    Cl    Cl    H    CF3    CH3    CO2CH2CH2Cl1-1738    Cl    Cl    H    CF3    CH3    CO2CH2CH2Br1-1739    Cl    Cl    H    CF3    CH3    CON(CH3)21-1740    Cl    Cl    H    CF3    CH3    CONHCH31-1741    Cl    Cl    H    CF3    CH3    CON(C2H5)21-1742    Cl    Cl    H    CF3    CH3    CONHC2H51-1743    Cl    Cl    H    CF3    CH3    COCH31-1744    Cl    Cl    H    CF3    CH3    COC2H51-1745    Cl    Cl    H    CF3    CH3    COCH2Cl1-1746    Cl    Cl    H    CF3    CH3    CHO1-1747    Cl    Cl    H    CF3    CH3    CH=CHCO2CH31-1748    Cl    Cl    H    CF3    CH3    OiC3H71-1749    Cl    Cl    CH3 CF3    H       H1-1750    Cl    Cl    CH3 CF3    H       OH1-1751    Cl    Cl    CH3 CF3    H       NO21-1752    Cl    Cl    CH3 CF3    H       NH2
                         表1(续)
   化合物编号 X     Y     R3     R1     R2         B
    1-1753    Cl    Cl    CH3    CF3    H    NHSO2CH31-1754    Cl    Cl    CH3    CF3    H    NHSO2CH2Cl1-1755    Cl    Cl    CH3    CF3    H    NHCH2CO2CH31-1756    Cl    Cl    CH3    CF3    H    NHCH2CO2C2H51-1757    Cl    Cl    CH3    CF3    H    NHCH2CO2 iC3H71-1758    Cl    Cl    CH3    CF3    H    NHCH(CH3)CO2CH31-1759    Cl    Cl    CH3    CF3    H    NHCH(CH3)CO2C2H51-1760    Cl    Cl    CH3    CF3    H    NHCH(CH3)CO2 iC3H71-1761    Cl    Cl    CH3    CF3    H    CO2H1-1762    Cl    Cl    CH3    CF3    H    CO2CH31-1763    Cl    Cl    CH3    CF3    H    CO2C2H51-1764    Cl    Cl    CH3    CF3    H    CO2 nC3H71-1765    Cl    Cl    CH3    CF3    H    CO2 nC4H91-1766    Cl    Cl    CH3    CF3    H    CO2 nC5H111-1767    Cl    Cl    CH3    CF3    H    CO2 iC3H71-1768    Cl    Cl    CH3    CF3    H    CO2CH2CH2Cl1-1769    Cl    Cl    CH3    CF3    H    CO2CH2CH2Br1-1770    Cl    Cl    CH3    CF3    H    CON(CH3)21-1771    Cl    Cl    CH3    CF3    H    CONHCH31-1772    Cl    Cl    CH3    CF3    H    CON(C2H5)21-1773    Cl    Cl    CH3    CF3    H    CONHC2H51-1774    Cl    Cl    CH3    CF3    H    COCH31-1775    Cl    Cl    CH3    CF3    H    COC2H51-1776    Cl    Cl    CH3    CF3    H    COCH2Cl1-1777    Cl    Cl    CH3    CF3    H    CHO1-1778    Cl    Cl    CH3    CF3    H    CH=CHCO2CH31-1779    Cl    Cl    CH3    CF3    H    OiC3H71-1780    F     Br    H       CF3    H    OiC3H71-1781    F     Br    H       CF3    H    N(SO2CH3)21-1782    F     Br    H       CF3    H    NHSO2CH31-1783    F     Br    H       CF3    CH3 OiC3H7
                       表1(续)
                     表1(续)
Figure C9619770001751
                        表1(续)
Figure C9619770001761
                      表1(续)
Figure C9619770001771
                       表1(续)
                       表1(续)
Figure C9619770001791
                           表1(续)
                        表1(续)
                         表1(续)
                       表1(续)
Figure C9619770001831
                            表1(续)
Figure C9619770001841
                               表1(续)
化合物编号  X    Y   R3  R1     R2         B
  1-2056    F    Cl  H    CF3    CH3 OCH(CH3)COOCH2COOC31-2057    F    Cl  H    CF3    CH3 OCH(CH3)COOCH2COOC2H51-2058    F    Cl  H    CF3    CH3 OCH(CH3)COOCH2COOiC3H71-2059    F    Cl  H    CF3    CH3 OCH(CH3)COOCH(CH3)COOCH31-2060    F    Cl  H    CF3    CH3 OCH(CH3)COOCH(CH3)COOC2H51-2061    F    Cl  H    CF3    CH3 OCH(CH3)COOCH(CH3)COOiC3H71-2062    F    Cl  H    CF3    H    OCH2COOCH2COOCH31-2063    F    Cl  H    CF3    H    OCH2COOCH2COOC2H51-2064    F    Cl  H    CF3    H    OCH2COOCH2COOiC3H71-2065    F    Cl  H    CF3    H    OCH2COOCH(CH3)COOCH31-2066    F    Cl  H    CF3    H    OCH2COOCH(CH3)COOC2H51-2067    F    Cl  H    CF3    H    OCH2COOCH(CH3)COOiC3H71-2068    F    Cl  H    CF3    H    OCH(CH3)COOCH2COOCH31-2069    F    Cl  H    CF3    H    OCH(CH3)COOCH2COOC2H51-2070    F    Cl  H    CF3    H    OCH(CH3)COOCH2COOiC3H71-2071    F    Cl  H    CF3    H    OCH(CH3)COOCH(CH3)COOCH31-2072    F    Cl  H    CF3    H    OCH(CH3)COOCH(CH3)COOC2H51-2073    F    Cl  H    CF3    H    OCH(CH3)COOCH(CH3)COOiC3H71-2074    F    Cl  CH3 CF3    H    OCH2COOCH2COOCH31-2075    F    Cl  CH3 CF3    H    OCH2COOCH2COOC2H51-2076    F    Cl  CH3 CF3    H    OCH2COOCH2COOiC3H71-2077    F    Cl  CH3 CF3    H    OCH2COOCH(CH3)COOCH31-2078    F    Cl  CH3 CF3    H    OCH2COOCH(CH3)COOC2H51-2079    F    Cl  CH3 CF3    H    OCH2COOCH(CH3)COOiC3H71-2080    F    Cl  CH3 CF3    H    OCH(CH3)COOCH2COOCH31-2081    F    Cl  CH3 CF3    H    OCH(CH3)COOCH2COOC2H51-2082    F    Cl  CH3 CF3    H    OCH(CH3)COOCH2COOiC3H71-2083    F    Cl  CH3 CF3    H    OCH(CH3)COOCH(CH3)COOCH31-2084    F    Cl  CH3 CF3    H    OCH(CH3)COOCH(CH3)COOC2H51-2085    F    Cl  CH3 CF3    H    OCH(CH3)COOCH(CH3)COOiC3H7
                             表1(续)
  化合物编号  X    Y     R3  R1     R2          B
    1-2086    H    Cl    H    CF3    CH3 OCH2COOCH2COOCH31-2087    H    Cl    H    CF3    CH3 OCH2COOCH2COOC2H51-2088    H    Cl    H    CF3    CH3 OCH2COOCH2COOiC3H71-2089    H    Cl    H    CF3    CH3 OCH2COOCH(CH3)COOCH31-2090    H    Cl    H    CF3    CH3 OCH2COOCH(CH3)COOC2H51-2091    H    Cl    H    CF3    CH3 OCH2COOCH(CH3)COOiC3H71-2092    H    Cl    H    CF3    CH3 OCH(CH3)COOCH2COOCH31-2093    H    Cl    H    CF3    CH3 OCH(CH3)COOCH2COOC2H51-2094    H    Cl    H    CF3    CH3 OCH(CH3)COOCH2COOiC3H71-2095    H    Cl    H    CF3    CH3 OCH(CH3)COOCH(CH3)COOCH31-2096    H    Cl    H    CF3    CH3 OCH(CH3)COOCH(CH3)COOC2H51-2097    H    Cl    H    CF3    CH3 OCH(CH3)COOCH(CH3)COOiC3H71-2098    H    Cl    H    CF3    H    OCH2COOCH2COOCH31-2099    H    Cl    H    CF3    H    OCH2COOCH2COOC2H51-2100    H    Cl    H    CF3    H    OCH2COOCH2COOiC3H71-2101    H    Cl    H    CF3    H    OCH2COOCH(CH3)COOCH31-2102    H    Cl    H    CF3    H    OCH2COOCH(CH3)COOC2H51-2103    H    Cl    H    CF3    H    OCH2COOCH(CH3)COOiC3H71-2104    H    Cl    H    CF3    H    OCH(CH3)COOCH2COOCH31-2105    H    Cl    H    CF3    H    OCH(CH3)COOCH2COOC2H51-2106    H    Cl    H    CF3    H    OCH(CH3)COOCH2COOiC3H71-2107    H    Cl    H    CF3    H    OCH(CH3)COOCH(CH3)COOCH31-2108    H    Cl    H    CF3    H    OCH(CH3)COOCH(CH3)COOC2H51-2109    H    Cl    H    CF3    H    OCH(CH3)COOCH(CH3)COOiC3H71-2110    H    Cl    CH3 CF3    H    OCH2COOCH2COOCH31-2111    H    Cl    CH3 CF3    H    OCH2COOCH2COOC2H51-2112    H    Cl    CH3 CF3    H    OCH2COOCH2COOiC3H71-2113    H    Cl    CH3 CF3    H    OCH2COOCH(CH3)COOCH31-2114    H    Cl    CH3 CF3    H    OCH2COOCH(CH3)COOC2H51-2115    H    Cl    CH3 CF3    H    OCH2COOCH(CH3)COOiC3H7
                              表1(续)
化合物编号  X     Y     R3  R1   R2           B
  1-2116    H     Cl    CH3 CF3  H    OCH(CH3)COOCH2COOCH31-2117    H     Cl    CH3 CF3  H    OCH(CH3)COOCH2COOC2H51-2118    H     Cl    CH3 CF3  H    OCH(CH3)COOCH2COOiC3H71-2119    H     Cl    CH3 CF3  H    OCH(CH3)COOCH(CH3)COOCH31-2120    H     Cl    CH3 CF3  H    OCH(CH3)COOCH(CH3)COOC2H51-2121    H     Cl    CH3 CF3  H    OCH(CH3)COOCH(CH3)COOiC3H71-2122    Cl    Cl    H    CF3  CH3 OCH2COOCH2COOCH31-2123    Cl    Cl    H    CF3  CH3 OCH2COOCH2COOC2H51-2124    Cl    Cl    H    CF3  CH3 OCH2COOCH2COOiC3H71-2125    Cl    Cl    H    CF3  CH3 OCH2COOCH(CH3)COOCH31-2126    Cl    Cl    H    CF3  CH3 OCH2COOCH(CH3)COOC2H51-2127    Cl    Cl    H    CF3  CH3 OCH2COOCH(CH3)COOiC3H71-2128    Cl    Cl    H    CF3  CH3 OCH(CH3)COOCH2COOCH31-2129    Cl    Cl    H    CF3  CH3 OCH(CH3)COOCH2COOC2H51-2130    Cl    Cl    H    CF3  CH3 OCH(CH3)COOCH2COOiC3H71-2131    Cl    Cl    H    CF3  CH3 OCH(CH3)COOCH(CH3)COOCH31-2132    Cl    Cl    H    CF3  CH3 OCH(CH3)COOCH(CH3)COOC2H51-2133    Cl    Cl    H    CF3  CH3 OCH(CH3)COOCH(CH3)COOiC3H71-2134    Cl    Cl    H    CF3  H    OCH2COOCH2COOCH31-2135    Cl    Cl    H    CF3  H    OCH2COOCH2COOC2H51-2136    Cl    Cl    H    CF3  H    OCH2COOCH2COOiC3H71-2137    Cl    Cl    H    CF3  H    OCH2COOCH(CH3)COOCH31-2138    Cl    Cl    H    CF3  H    OCH2COOCH(CH3)COOC2H51-2139    Cl    Cl    H    CF3  H    OCH2COOCH(CH3)COOiC3H71-2140    Cl    Cl    H    CF3  H    OCH(CH3)COOCH2COOCH31-2141    Cl    Cl    H    CF3  H    OCH(CH3)COOCH2COOC2H51-2142    Cl    Cl    H    CF3  H    OCH(CH3)COOCH2COOiC3H71-2143    Cl    Cl    H    CF3  H    OCH(CH3)COOCH(CH3)COOCH31-2144    Cl    Cl    H    CF3  H    OCH(CH3)COOCH(CH3)COOC2H51-2145    Cl    Cl    H    CF3  H    OCH(CH3)COOCH(CH3)COOiC3H71-2146    Cl    Cl    CH3 CF3  H    OCH2COOCH2COOCH3
                              表1(续)
 化合物编号   X     Y     R3   R1     R2           B
    1-2147    Cl    Cl    CH3  CF3    H  OCH2COOCH2COOC2H51-2148    Cl    Cl    CH3  CF3    H  OCH2COOCH2COOiC3H71-2149    Cl    Cl    CH3  CF3    H  OCH2COOCH(CH3)COOCH31-2150    Cl    Cl    CH3  CF3    H  OCH2COOCH(CH3)COOC2H51-2151    Cl    Cl    CH3  CF3    H  OCH2COOCH(CH3)COOiC3H71-2152    Cl    Cl    CH3  CF3    H  OCH(CH3)COOCH2COOCH31-2153    Cl    Cl    CH3  CF3    H  OCH(CH3)COOCH2COOC2H51-2154    Cl    Cl    CH3  CF3    H  OCH(CH3)COOCH2COOiC3H71-2155    Cl    Cl    CH3  CF3    H  OCH(CH3)COOCH(CH3)COOCH31-2156    Cl    Cl    CH3  CF3    H  OCH(CH3)COOCH(CH3)COOC2H51-2157    Cl    Cl    CH3  CF3    H  OCH(CH3)COOCH(CH3)COOiC3H7
                               表12
下式化合物:
  化合物 X  Z1n  R3  R1   R2     R4   R5编号
  2-1    H  O  1  H  CF2Cl  CH3    H    H2-2    H  O  1  H  CF2Cl  CH3    H    CH32-3    H  O  1  H  CF2Cl  CH3    H    C2H52-4    H  O  1  H  CF2Cl  CH3    H   nC3H72-5    H  O  1  H  CF2Cl  CH3    H   iC3H72-6    H  O  1  H  CF2Cl  CH3    H   iC4H92-7    H  O  1  H  CF2Cl  CH3    H   nC4H92-8    H  O  1  H  CF2Cl  CH3    H    CH2CH2Cl2-9    H  O  1  H  CF2Cl  CH3    H    CH2CH2Br2-10   H  O  1  H  CF2Cl  CH3    H    CH2CH=CH22-11   H  O  1  H  CF2Cl  CH3    H    CH(CH3)CH=CH22-12   H  O  1  H  CF2Cl  CH3    H    CH2CCl=CH22-13   H  O  1  H  CF2Cl  CH3    H    CH2C≡CH2-14   H  O  1  H  CF2Cl  CH3    H    CH(CH2)C≡CH
                                     表2(续)
  化合物  X  Z1n  R3  R1   R2     R4      R5编号
  2-15    H  O  1  H  CF2Cl  CH3    H    CH2CN2-16    H  O  1  H  CF2Cl  CH3    H    CH2OCH32-17    H  O  1  H  CF2Cl  CH3    H    CH2OC2H52-18    H  O  1  H  CF2Cl  CH3    H    CH2COOH2-19    H  O  1  H  CF2Cl  CH3    H    CH2COOCH32-20    H  O  1  H  CF2Cl  CH3    H    CH2COOC2H52-21    H  O  1  H  CF2Cl  CH3    H    CH2COOnC3H72-22    H  O  1  H  CF2Cl  CH3    H    CH2COOnC4H92-23    H  O  1  H  CF2Cl  CH3    H    CH2COOnC5H112-24    H  O  1  H  CF2Cl  CH3    H    CH2COOiC3H72-25    H  O  1  H  CF2Cl  CH3    H    CH2COOcC5H92-26    H  O  1  H  CF2Cl  CH3    H    CH2COOcC6H112-27    H  O  1  H  CF2Cl  CH3    H    CH(CH3)COOH2-28    H  O  1  H  CF2Cl  CH3    H    CH(CH3)COOCH32-29    H  O  1  H  CF2Cl  CH3    H    CH(CH3)COOC2H52-30    H  O  1  H  CF2Cl  CH3    H    CH(CH3)COOnC3H72-31    H  O  1  H  CF2Cl  CH3    H    CH(CH3)COOnC4H92-32    H  O  1  H  CF2Cl  CH3    H    CH(CH3)COOnC5H112-33    H  O  1  H  CF2Cl  CH3    H    CH(CH3)COOiC3H72-34    H  O  1  H  CF2Cl  CH3    H    CH(CH3)COOcC5H92-35    H  O  1  H  CF2Cl  CH3    H    CH(CH3)COOcC6H112-36    H  O  1  H  CF2Cl  CH3    CH3 H2-37    H  O  1  H  CF2Cl  CH3    CH3 CH3
                                  表2(续)
  化合物  X  Z1n  R3  R1   R2     R4    R5编号
  2-38    H  O  1  H  CF2Cl  CH3    CH3  C2H52-39    H  O  1  H  CF2Cl  CH3    CH3 nC3H72-40    H  O  1  H  CF2Cl  CH3    CH3 iC3H72-41    H  O  1  H  CF2Cl  CH3    CH3 iC4H92-42    H  O  1  H  CF2Cl  CH3    CH3 nC4H92-43    H  O  1  H  CF2Cl  CH3    CH3  CH2CH=CH22-44    H  O  1  H  CF2Cl  CH3    CH3  CH(CH3)CH=CH22-45    H  O  1  H  CF2Cl  CH3    CH3  CH2C≡CH2-46    H  O  1  H  CF2Cl  CH3    CH3  CH(CH3)C≡CH2-47    H  O  1  H  CF2Cl  CH3    CH3  CH2OCH32-48    H  O  1  H  CF2Cl  CH3    CH3  CH2OC2H52-49    F  O  1  H  CF2Cl  CH3    H     H2-50    F  O  1  H  CF2Cl  CH3    H     CH32-51    F  O  1  H  CF2Cl  CH3    H     C2H52-52    F  O  1  H  CF2Cl  CH3    H    nuC3H72-53    F  O  1  H  CF2Cl  CH3    H    iC3H72-54    F  O  1  H  CF2Cl  CH3    H    iC4H92-55    F  O  1  H  CF2Cl  CH3    H    nC4H92-56    F  O  1  H  CF2Cl  CH3    H     CH2CH2Cl2-57    F  O  1  H  CF2Cl  CH3    H     CH2CH2Br2-58    F  O  1  H  CF2Cl  CH3    H     CH2CH=CH22-59    F  O  1  H  CF2Cl  CH3    H     CH(CH3)CH=CH22-60    F  O  1  H  CF2Cl  CH3    H     CH2CCl=CH2
                            表2(续)
  化合物  X  Z1n  R3   R1  R2     R4      R5编号
  2-61    F  O  1  H  CF2Cl  CH3    H    CH2C≡CH2-62    F  O  1  H  CF2Cl  CH3    H    CH(CH3)C≡CH2-63    F  O  1  H  CF2Cl  CH3    H    CH2CN2-64    F  O  1  H  CF2Cl  CH3    H    CH2OCH32-65    F  O  1  H  CF2Cl  CH3    H    CH2OC2H52-66    F  O  1  H  CF2Cl  CH3    H    CH2COOH2-67    F  O  1  H  CF2Cl  CH3    H    CH2COOCH32-68    F  O  1  H  CF2Cl  CH3    H    CH2COOC2H52-69    F  O  1  H  CF2Cl  CH3    H    CH2COOnC3H72-70    F  O  1  H  CF2Cl  CH3    H    CH2COOnC4H92-71    F  O  1  H  CF2Cl  CH3    H    CH2COOnC5H112-72    F  O  1  H  CF2Cl  CH3    H    CH2COOiC3H72-73    F  O  1  H  CF2Cl  CH3    H    CH2COOcC5H92-74    F  O  1  H  CF2Cl  CH3    H    CH2COOcC6H112-75    F  O  1  H  CF2Cl  CH3    H    CH(CH3)COOH2-76    F  O  1  H  CF2Cl  CH3    H    CH(CH3)COOCH32-77    F  O  1  H  CF2Cl  CH3    H    CH(CH3)COOC2H52-78    F  O  1  H  CF2Cl  CH3    H    CH(CH3)COOnC3H72-79    F  O  1  H  CF2Cl  CH3    H    CH(CH3)COOnC4H92-80    F  O  1  H  CF2Cl  CH3    H    CH(CH3)COOnC5H112-81    F  O  1  H  CF2Cl  CH3    H    CH(CH3)COOiC3H72-82    F  O  1  H  CF2Cl  CH3    H    CH(CH3)COOcC5H92-83    F  O  1  H  CF2Cl  CH3    H    CH(CH3)COOcC6H11
                                表2(续)
    化合物  X  Z1n  R3   R1   R2    R4    R5编号
    2-84    F  O  1  H  CF2Cl  CH3    CH3    H2-85    F  O  1  H  CF2Cl  CH3    CH3    CH32-86    F  O  1  H  CF2Cl  CH3    CH3    C2H52-87    F  O  1  H  CF2Cl  CH3    CH3   nC3H72-88    F  O  1  H  CF2Cl  CH3    CH3   iC3H72-89    F  O  1  H  CF2Cl  CH3    CH3   iC4H92-90    F  O  1  H  CF2Cl  CH3    CH3   nC4H92-91    F  O  1  H  CF2Cl  CH3    CH3    CH2CH=CH22-92    F  O  1  H  CF2Cl  CH3    CH3    CH(CH3)CH=CH22-93    F  O  1  H  CF2Cl  CH3    CH3    CH2C≡CH2-94    F  O  1  H  CF2Cl  CH3    CH3    CH(CH3)C≡CH2-95    F  O  1  H  CF2Cl  CH3    CH3    CH2OCH32-96    F  O  1  H  CF2Cl  CH3    CH3    CH2OC2H52-97    H  S  0  H  CF2Cl  CH3    -       H2-98    H  S  0  H  CF2Cl  CH3    -       CH32-99    H  S  0  H  CF2Cl  CH3    -       C2H52-100   H  S  0  H  CF2Cl  CH3    -      nC3H72-101   H  S  0  H  CF2Cl  CH3    -      nC4H92-102   H  S  0  H  CF2Cl  CH3    -      iC3H72-103   H  S  0  H  CF2Cl  CH3    -      iC4H92-104   H  S  0  H  CF2Cl  CH3    -       CH2CH2Cl2-105   H  S  0  H  CF2Cl  CH3    -       CH2CH2Br
                               表2(续)
    化合物   X  Z1n  R3   R1   R2   R4      R5编号
    2-106    H  S  0  H  CF2Cl  CH3    -    CH2CH=CH22-107    H  S  0  H  CF2Cl  CH3    -    CH(CH3)CH=CH22-108    H  S  0  H  CF2Cl  CH3    -    CH2CCl=CH22-109    H  S  0  H  CF2Cl  CH3    -    CH2C≡CH2-110    H  S  0  H  CF2Cl  CH3    -    CH(CH3)C≡CH2-111    H  S  0  H  CF2Cl  CH3    -    CH2CN2-112    H  S  0  H  CF2Cl  CH3    -    CH2OCH32-113    H  S  0  H  CF2Cl  CH3    -    CH2OC2 -H52-114    H  S  0  H  CF2Cl  CH3    -    CH2COOH2-115    H  S  0  H  CF2Cl  CH3    -    CH2COOCH32-116    H  S  0  H  CF2Cl  CH3    -    CH2COOC2H52-117    H  S  0  H  CF2Cl  CH3    -    CH2COOnC3H72-118    H  S  0  H  CF2Cl  CH3    -    CH2COOC4H92-119    H  S  0  H  CF2Cl  CH3    -    CH2COOnC5H112-120    H  S  0  H  CF2Cl  CH3    -    CH2COOiC3H72-121    H  S  0  H  CF2Cl  CH3    -    CH2COOcC5H92-122    H  S  0  H  CF2Cl  CH3    -    CH2COOcC6H112-123    H  S  0  H  CF2Cl  CH3    -    CH(CH3)COOH2-124    H  S  0  H  CF2Cl  CH3    -    CH(CH3)COOCH22-125    H  S  0  H  CF2Cl  CH3    -    CH(CH3)COOC2H52-126    H  S  0  H  CF2Cl  CH3    -    CH(CH3)COOnC3H72-127    H  S  0  H  CF2Cl  CH3    -    CH(CH3)COOnC4H92-128    H  S  0  H  CF2Cl  CH3    -    CH(CH3)COOnC6H11
                                 表2(续)
    化合物   X  Z1n  R3   R1   R2    R4     R5编号
    2-129    H  S  0  H  CF2Cl  CH3    -    CH(CH3)COOiC3H72-130    H  S  0  H  CF2Cl  CH3    -    CH(CH3)COOcC5H92-131    H  S  0  H  CF2Cl  CH3    -    CH(CH3)COOcC6H112-132    F  S  0  H  CF2Cl  CH3    -    H2-133    F  S  0  H  CF2Cl  CH3    -    CH32-134    F  S  0  H  CF2Cl  CH3    -    C2H52-135    F  S  0  H  CF2Cl  CH3    -   nC3H72-136    F  S  0  H  CF2Cl  CH3    -   nC4H92-137    F  S  0  H  CF2Cl  CH3    -   iC3H72-138    F  S  0  H  CF2Cl  CH3    -   iC4H92-139    F  S  0  H  CF2Cl  CH3    -    CH2CH2Cl2-140    F  S  0  H  CF2Cl  CH3    -    CH2CH2Br2-141    F  S  0  H  CF2Cl  CH3    -    CH2CH=CH22-142    F  S  0  H  CF2Cl  CH3    -    CH(CH3)CH=CH22-143    F  S  0  H  CF2Cl  CH3    -    CH2CCl=CH22-144    F  S  0  H  CF2Cl  CH3    -    CH2C≡CH2-145    F  S  0  H  CF2Cl  CH3    -    CH(CH3)C≡CH2-146    F  S  0  H  CF2Cl  CH3    -    CH2CN2-147    F  S  0  H  CF2Cl  CH3    -    CH2OCH32-148    F  S  0  H  CF2Cl  CH3    -    CH2OC2H52-149    F  S  0  H  CF2Cl  CH3    -    CH2COOH2-150    F  S  0  H  CF2Cl  CH3    -    CH2COOCH32-151    F  S  0  H  CF2Cl  CH3    -    CH2COOC2H5
                               表2(续)
  化合物   X  Z1n  R3   R1   R2    R4      R5编号
  2-152    F  S  0  H  CF2Cl  CH3    -    CH2COOnC3H72-153    F  S  0  H  CF2Cl  CH3    -    CH2COOnC4H92-154    F  S  0  H  CF2Cl  CH3    -    CH2COOnC5H112-155    F  S  0  H  CF2Cl  CH3    -    CH2COOiC3H72-156    F  S  0  H  CF2Cl  CH3    -    CH2COOcC5H92-157    F  S  0  H  CF2Cl  CH3    -    CH2COOcC6H112-158    F  S  0  H  CF2Cl  CH3    -    CH(CH3)COOH2-159    F  S  0  H  CF2Cl  CH3    -    CH(CH3)COOCH32-160    F  S  0  H  CF2Cl  CH3    -    CH(CH3)COOC2H52-161    F  S  0  H  CF2Cl  CH3    -    CH(CH3)COOnC3H72-162    F  S  0  H  CF2Cl  CH3    -    CH(CH3)COOnC4H92-163    F  S  0  H  CF2Cl  CH3    -    CH(CH3)COOnC5H112-164    F  S  0  H  CF2Cl  CH3    -    CH(CH3)COOiC3H72-165    F  S  0  H  CF2Cl  CH3    -    CH(CH3)COOcC5H92-166    F  S  0  H  CF2Cl  CH3    -    CH(CH3)COOcC6H112-167    H  O  0  H  CF2Cl  CH3    -    H2-168    H  O  0  H  CF2Cl  CH3    -    CH32-169    H  O  0  H  CF2Cl  CH3    -    C2H52-170    H  O  0  H  CF2Cl  CH3    -   nC3H72-171    H  O  0  H  CF2Cl  CH3    -   nC4H92-172    H  O  0  H  CF2Cl  CH3    -   iC3H72-173    H  O  0  H  CF2Cl  CH3    -   iC4H92-174    H  O  0  H  CF2Cl  CH3    -    CH2CH=CH2
                             表2(续)
    化合物   X  Z1n  R3   R1    R2     R4        R5编号
    2-175    H  O  0  H    CF2Cl  CH3    -    CH(CH3)CH=CH22-176    H  O  0  H    CF2Cl  CH3    -    CH2C≡CH2-177    H  O  0  H    CF2Cl  CH3    -    CH(CH3)C≡CH2-178    H  O  0  H    CF2Cl  CH3    -    CH2OCH32-179    H  O  0  H    CF2Cl  CH3    -    CH2OC2H52-180    F  O  0  H    CF2Cl  CH3    -    H2-181    F  O  0  H    CF2Cl  CH3    -    CH32-182    F  O  0  H    CF2Cl  CH3    -    C2H52-183    F  O  0  H    CF2Cl  CH3    -   nC3H72-184    F  O  0  H    CF2Cl  CH3    -   nC4H92-185    F  O  0  H    CF2Cl  CH3    -    CH2CH=CH22-186    F  O  0  H    CF2Cl  CH3    -    CH(CH3)CH=CH22-187    F  O  0  H    CF2Cl  CH3    -    CH2C≡CH2-188    F  O  0  H    CF2Cl  CH3    -    CH(CH3)C≡CH2-189    F  O  0  H    CF2Cl  CH3    -    CH2OCH32-190    F  O  0  H    CF2Cl  CH3    -    CH2OC2H52-191    H  O  1  H    CF3    CH3    -    H2-192    H  O  1  H    CF3    CH3    H    CH32-193    H  O  1  H    CF3    CH3    H    C2H52-194    H  O  1  H    CF3    CH3    H   nC3H72-195    H  O  1  H    CF3    CH3    H   iC3H72-196    H  O  1  H    CF3    CH3    H   iC4H92-197    H  O  1  H    CF3    CH3    H   nC4H9
                             表2(续)
  化合的   X  Z1n  R3   R1   R2     R4   R5编号
  2-198    H  O  1  H    CF3    CH3    H    CH2CH2Cl2-199    H  O  1  H    CF3    CH3    H    CH2CH2Br2-200    H  O  1  H    CF3    CH3    H    CH2CH=CH22-201    H  O  1  H    CF3    CH3    H    CH(CH3)CH=CH22-202    H  O  1  H    CF3    CH3    H    CH2CCl=CH22-203    H  O  1  H    CF3    CH3    H    CH2C≡CH2-204    H  O  1  H    CF3    CH3    H    CH(CH3)C≡CH2-205    H  O  1  H    CF3    CH3    H    CH2CN2-206    H  O  1  H    CF3    CH3    H    CH2OCH32-207    H  O  1  H    CF3    CH3    H    CH2OC2H32-208    H  O  1  H    CF3    CH3    H    CH2COOH2-209    H  O  1  H    CF3    CH3    H    CH2COOCH32-210    H  O  1  H    CF3    CH3    H    CH2COOC2H52-211    H  O  1  H    CF3    CH3    H    CH2COOnC3H72-212    H  O  1  H    CF3    CH3    H    CH2COOnC4H92-213    H  O  1  H    CF3    CH3    H    CH2COOnC5H112-214    H  O  1  H    CF3    CH3    H    CH2COOiC3H72-215    H  O  1  H    CF3    CH3    H    CH2COOcC5H92-216    H  O  1  H    CF3    CH3    H    CH2COOcC6H112-217    H  O  1  H    CF3    CH3    H    CH(CH3)COOH2-218    H  O  1  H    CF3    CH3    H    CH(CH3)COOCH32-219    H  O  1  H    CF3    CH3    H    CH(CH3)COOC2H5
                                表2(续)
    化合物   X  Z1n  R3   R1    R2    R4          R5编号
    2-220    H  O  1  H    CF3    CH3    H       CH(CH3)COOnC3H72-221    H  O  1  H    CF3    CH3    H       CH(CH3)COOnC4H92-222    H  O  1  H    CF3    CH3    H       CH(CH3)COOnC5H112-223    H  O  1  H    CF3    CH3    H       CH(CH3)COOiC3H72-224    H  O  1  H    CF3    CH3    H       CH(CH3)COOcC5H92-225    H  O  1  H    CF3    CH3    H       CH(CH3)COOcC6H112-226    H  O  1  H    CF3    CH3    CH3    H2-227    H  O  1  H    CF3    CH3    CH3    CH32-228    H  O  1  H    CF3    CH3    CH3    C2H52-229    H  O  1  H    CF3    CH3    CH3   nC3H72-230    H  O  1  H    CF3    CH3    CH3   iC3H72-231    H  O  1  H    CF3    CH3    CH3   iC4H92-232    H  O  1  H    CF3    CH3    CH3   nC4H92-233    H  O  1  H    CF3    CH3    CH3    CH2CH=CH22-234    H  O  1  H    CF3    CH3    CH3    CH(CH3)CH=CH22-235    H  O  1  H    CF3    CH3    CH3    CH2C≡CH2-236    H  O  1  H    CF3    CH3    CH3    CH(CH3)C≡CH2-237    H  O  1  H    CF3    CH3    CH3    CH2OCH32-238    H  O  1  H    CF3    CH3    CH3    CH2OC2H52-239    F  O  1  H    CF3    CH3    H       H2-240    F  O  1  H    CF3    CH3    H       CH32-241    F  O  1  H    CF3    CH3    H       C2H52-242    F  O  1  H    CF3    CH3    H      nC3H7
                                  表2(续)
  化合物   X  Z1n  R3  R1     R2    R4    R5编号
  2-243    F  O  1  H    CF3    CH3    H   iC3H72-244    F  O  1  H    CF3    CH3    H   iC4H92-245    F  O  1  H    CF3    CH3    H   nC4H92-246    F  O  1  H    CF3    CH3    H    CH2CH2Cl2-247    F  O  1  H    CF3    CH3    H    CH2CH2Br2-248    F  O  1  H    CF3    CH3    H    CH2CH=CH22-249    F  O  1  H    CF3    CH3    H    CH(CH3)CH=CH22-250    F  O  1  H    CF3    CH3    H    CH2CCl=CH22-251    F  O  1  H    CF3    CH3    H    CH2C≡CH2-252    F  O  1  H    CF3    CH3    H    CH(CH3)C≡CH2-253    F  O  1  H    CF3    CH3    H    CH2CN2-254    F  O  1  H    CF3    CH3    H    CH2OCH32-255    F  O  1  H    CF3    CH3    H    CH2OC2H52-256    F  O  1  H    CF3    CH3    H    CH2COOH2-257    F  O  1  H    CF3    CH3    H    CH2COOCH32-258    F  O  1  H    CF3    CH3    H    CH2COOC2H52-259    F  O  1  H    CF3    CH3    H    CH2COOnC3H72-260    F  O  1  H    CF3    CH3    H    CH2COOnC4H92-261    F  O  1  H    CF3    CH3    H    CH2COOnC5H112-262    F  O  1  H    CF3    CH3    H    CH2COOiC3H72-263    F  O  1  H    CF3    CH3    H    CH2COOcC6H92-264    F  O  1  H    CF3    CH3    H    CH2COOcC6H112-265    F  O  1  H    CF3    CH3    H    CH(CH3)COOH
                               表2(续)
  化合物   X  Z1n  R3   R1    R2     R4       R5编号
  2-266    F  O  1  H    CF3    CH3    H     CH(CH3)COOCH32-267    F  O  1  H    CF3    CH3    H     CH(CH3)COOC2H52-268    F  O  1  H    CF3    CH3    H     CH(CH3)COOnC3H72-269    F  O  1  H    CF3    CH3    H     CH(CH3)COOnC4H92-270    F  O  1  H    CF3    CH3    H     CH(CH3)COOnC5H112-271    F  O  1  H    CF3    CH3    H     CH(CH3)COOiC3H72-272    F  O  1  H    CF3    CH3    H     CH(CH3)COOcC5H92-273    F  O  1  H    CF3    CH3    H     CH(CH3)COOcC6H112-274    F  O  1  H    CF3    CH3    CH3  H2-275    F  O  1  H    CF3    CH3    CH3  CH32-276    F  O  1  H    CF3    CH3    CH3  C2H52-277    F  O  1  H    CF3    CH3    CH3 nC3H72-278    F  O  1  H    CF3    CH3    CH3 iC3H72-279    F  O  1  H    CF3    CH3    CH3 iC4H92-280    F  O  1  H    CF3    CH3    CH3 nC4H92-281    F  O  1  H    CF3    CH3    CH3  CH2CH=CH22-282    F  O  1  H    CF3    CH3    CH3  CH(CH3)CH=CH22-283    F  O  1  H    CF3    CH3    CH3  CH2C≡CH2-284    F  O  1  H    CF3    CH3    CH3  CH(CH3)C≡CH2-285    F  O  1  H    CF3    CH3    CH3  CH2OCH32-286    F  O  1  H    CF3    CH3    CH3  CH2OC2H52-287    H  S  0  H    CF3    CH3    -     H2-288    H  S  0  H    CF3    CH3    -     CH3
                     表2(续)
    化合物   X  Z1n  R3   R1    R2    R4    R5编号
    2-289    H  S  0  H    CF3    CH3    -    C2H52-290    H  S  0  H    CF3    CH3    -   nC3H72-291    H  S  0  H    CF3    CH3    -   nC4H92-292    H  S  0  H    CF3    CH3    -   iC3H72-293    H  S  0  H    CF3    CH3    -   iC4H92-294    H  S  0  H    CF3    CH3    -    CH2CH2Cl2-295    H  S  0  H    CF3    CH3    -    CH2CH2Br2-296    H  S  0  H    CF3    CH3    -    CH2CH=CH22-297    H  S  0  H    CF3    CH3    -    CH(CH3)CH=CH22-298    H  S  0  H    CF3    CH3    -    CH2CCl=CH22-299    H  S  0  H    CF3    CH3    -    CH2C≡CH2-300    H  S  0  H    CF3    CH3    -    CH(CH3)C≡CH2-301    H  S  0  H    CF3    CH3    -    CH2CN2-302    H  S  0  H    CF3    CH3    -    CH2OCH32-303    H  S  0  H    CF3    CH3    -    CH2OC2H52-304    H  S  0  H    CF3    CH3    -    CH2COOH2-305    H  S  0  H    CF3    CH3    -    CH2COOCH32-306    H  S  0  H    CF3    CH3    -    CH2COOC2H52-307    H  S  0  H    CF3    CH3    -    CH2COOnC3H72-308    H  S  0  H    CF3    CH3    -    CH2COOnC4H92-309    H  S  0  H    CF3    CH3    -    CH2COOnC5H112-310    H  S  0  H    CF3    CH3    -    CH2COOiC3H72-311    H  S  0  H    CF3    CH3    -    CH2COOcC5H9
                             表2(续)
  化合物   X  Z1n   R3  R1    R2     R4     R5编号
  2-312    H  S  0  H    CF3    CH3    -    CH2COOcC6H112-313    H  S  0  H    CF3    CH3    -    CH(CH3)COOH2-314    H  S  0  H    CF3    CH3    -    CH(CH3)COOCH32-315    H  S  0  H    CF3    CH3    -    CH(CH3)COOC2H52-316    H  S  0  H    CF3    CH3    -    CH(CH3)COOnC3H72-317    H  S  0  H    CF3    CH3    -    CH(CH3)COOnC4H92-318    H  S  0  H    CF3    CH3    -    CH(CH3)COOnC5H112-319    H  S  0  H    CF3    CH3    -    CH(CH3)COOiC3H72-320    H  S  0  H    CF3    CH3    -    CH(CH3)COOcC5H92-321    H  S  0  H    CF3    CH3    -    CH(CH3)COOcC6H112-322    F  S  0  H    CF3    CH3    -    H2-323    F  S  0  H    CF3    CH3    -    CH32-324    F  S  0  H    CF3    CH3    -    C2H52-325    F  S  0  H    CF3    CH3    -   nC3H72-326    F  S  0  H    CF3    CH3    -   nC4H92-327    F  S  0  H    CF3    CH3    -   iC3H72-328    F  S  0  H    CF3    CH3    -   sC4H92-329    F  S  0  H    CF3    CH3    -    CH2CH2Cl2-330    F  S  0  H    CF3    CH3    -    CH2CH2Br2-331    F  S  0  H    CF3    CH3    -    CH2CH=CH22-332    F  S  0  H    CF3    CH3    -    CH(CH3)CH=CH22-333    F  S  0  H    CF3    CH3    -    CH2CCl=CH2
                          表2(续)
  化合物   X  Z1n  R3   R1    R2     R4    R5编号
  2-334    F  S  0  H    CF3    CH3    -    CH2C≡CH2-335    F  S  0  H    CF3    CH3    -    CH(CH3)C≡CH2-336    F  S  0  H    CF3    CH3    -    CH2CN2-337    F  S  0  H    CF3    CH3    -    CH2OCH32-338    F  S  0  H    CF3    CH3    -    CH2OC2H52-339    F  S  0  H    CF3    CH3    -    CH2COOH2-340    F  S  0  H    CF3    CH3    -    CH2COOCH32-341    F  S  0  H    CF3    CH3    -    CH2COOC2H52-342    F  S  0  H    CF3    CH3    -    CH2COOnC3H72-343    F  S  0  H    CF3    CH3    -    CH2COOnC4H92-344    F  S  0  H    CF3    CH3    -    CH2COOnC5H112-345    F  S  0  H    CF3    CH3    -    CH2COOiC3H72-346    F  S  0  H    CF3    CH3    -    CH2COOcC5H92-347    F  S  0  H    CF3    CH3    -    CH2COOcC6H112-348    F  S  0  H    CF3    CH3    -    CH(CH3)COOH2-349    F  S  0  H    CF3    CH3    -    CH(CH3)COOCH32-350    F  S  0  H    CF3    CH3    -    CH(CH3)COOC2H52-351    F  S  0  H    CF3    CH3    -    CH(CH3)COOnC3H72-352    F  S  0  H    CF3    CH3    -    CH(CH3)COOnC4H92-353    F  S  0  H    CF3    CH3    -    CH(CH3)COOnC5H112-354    F  S  0  H    CF3    CH3    -    CH(CH3)COOiC3H72-355    F  S  0  H    CF3    CH3    -    CH(CH3)COOcC5H92-356    F  S  0  H    CF3    CH3    -    CH(CH3)COOcC8H11
                               表2(续)
    化合物   X  Z1n  R3   R1    R2     R4  R5编号
    2-357    H  O  0  H    CF3    CH3    -    H2-358    H  O  0  H    CF3    CH3    -    CH32-359    H  O  0  H    CF3    CH3    -    C2H52-360    H  O  0  H    CF3    CH3    -   nC3H72-361    H  O  0  H    CF3    CH3    -   nC4H92-362    H  O  0  H    CF3    CH3    -   iC3H72-363    H  O  0  H    CF3    CH3    -   iC4H92-364    H  O  0  H    CF3    CH3    -    CH2CH=CH22-365    H  O  0  H    CF3    CH3    -    CH(CH3)CH=CH22-366    H  O  0  H    CF3    CH3    -    CH2C≡CH2-367    H  O  0  H    CF3    CH3    -    CH(CH3)C≡CH2-368    H  O  0  H    CF3    CH3    -    CH2OCH32-369    H  O  0  H    CF3    CH3    -    CH2OC2H52-370    F  O  0  H    CF3    CH3    -    H2-371    F  O  0  H    CF3    CH3    -    CH32-372    F  O  0  H    CF3    CH3    -    C2H52-373    F  O  0  H    CF3    CH3    -   nC3H72-374    F  O  0  H    CF3    CH3    -   nC4H92-375    F  O  0  H    CF3    CH3    -    CH2CH=CH22-376    F  O  0  H    CF3    CH3    -    CH(CH3)CH=CH22-377    F  O  0  H    CF3    CH3    -    CH2C≡CH2-378    F  O  0  H    CF3    CH3    -    CH(CHa)C≡CH2-379    F  O  0  H    CF3    CH3    -    CH2OCH3
                            表2(续)
    化合物 X  Z1n  R3 R1   R2  R4   R5编号
    2-380  F  O  0  H  CF3    CH3 -    CH2OC2H52-381  H  O  1  H  CF2Cl  H    H    H2-382  H  O  1  H  CF2Cl  H    H    CH32-383  H  O  1  H  CF2Cl  H    H    C2H52-384  H  O  1  H  CF2Cl  H    H   nC3H72-385  H  O  1  H  CF2Cl  H    H   iC3H72-386  H  O  1  H  CF2Cl  H    H   iC4H92-387  H  O  1  H  CF2Cl  H    H   nC4H92-388  H  O  1  H  CF2Cl  H    H    CH2CH2Cl2-389  H  O  1  H  CF2Cl  H    H    CH2CH2Br2-390  H  O  1  H  CF2Cl  H    H    CH2CH=CH22-391  H  O  1  H  CF2Cl  H    H    CH(CH3)CH=CH22-392  H  O  1  H  CF2Cl  H    H    CH2CCl=CH22-393  H  O  1  H  CF2Cl  H    H    CH2C≡CH2-394  H  O  1  H  CF2Cl  H    H    CH(CH3)C≡CH2-395  H  O  1  H  CF2Cl  H    H    CH2CN2-396  H  O  1  H  CF2Cl  H    H    CH2OCH32-397  H  O  1  H  CF2Cl  H    H    CH2OC2H52-398  H  O  1  H  CF2Cl  H    H    CH2COOH2-399  H  O  1  H  CF2Cl  H    H    CH2COOCH32-400  H  O  1  H  CF2Cl  H    H    CH2COOC2H52-401  H  O  1  H  CF2Cl  H    H    CH2COOnC2H72-402  H  O  1  H  CF2Cl  H    H    CH2COOnC4H9
                               表2(续)
    化合物 X  Z1n  R3  R1  R2  R4     R5编号
    2-403  H  O  1  H  CF2Cl  H    H     CH2COOnC5H112-404  H  O  1  H  CF2Cl  H    H     CH2COOiC3H72-405  H  O  1  H  CF2Cl  H    H     CH2COOcC5H92-406  H  O  1  H  CF2Cl  H    H     CH2COOcC6H112-407  H  O  1  H  CF2Cl  H    H     CH(CH3)COOH2-408  H  O  1  H  CF2Cl  H    H     CH(CH3)COOCH32-409  H  O  1  H  CF2Cl  H    H     CH(CH3)COOC2H52-410  H  O  1  H  CF2Cl  H    H     CH(CH3)COOnC3H72-411  H  O  1  H  CF2Cl  H    H     CH(CH3)COOnC4H92-412  H  O  1  H  CF2Cl  H    H     CH(CH3)COOnC5H112-413  H  O  1  H  CF2Cl  H    H     CH(CH3)COOiC3H72-414  H  O  1  H  CF2Cl  H    H     CH(CH3)COOcC5H92-415  H  O  1  H  CF2Cl  H    H     CH(CH3)COOcC6H112-416  H  O  1  H  CF2Cl  H    CH3  H2-417  H  O  1  H  CF2Cl  H    CH3  CH32-418  H  O  1  H  CF2Cl  H    CH3  C2H52-419  H  O  1  H  CF2Cl  H    CH3 nC3H72-420  H  O  1  H  CF2Cl  H    CH3 iC3H72-421  H  O  1  H  CF2Cl  H    CH3 iC4H92-422  H  O  1  H  CF2Cl  H    CH3 nC4H92-423  H  O  1  H  CF2Cl  H    CH3  CH2CH=CH22-424  H  O  1  H  CF2Cl  H    CH3  CH(CH3)CH=CH22-425  H  O  1  H  CF2Cl  H    CH3  CH2C≡CH
                              表2(续)
    化合物   X  Z1n  R3  R1   R2  R4         R5编号
    2-426    H  O  1  H  CF2Cl  H    CH3   CH(CH3)C≡CH2-427    H  O  1  H  CF2Cl  H    CH3   CH2OCH32-428    H  O  1  H  CF2Cl  H    CH3   CH2OC2H52-429    F  O  1  H  CF2Cl  H    H      H2-430    F  O  1  H  CF2Cl  H    H      CH32-431    F  O  1  H  CF2Cl  H    H      C2H52-432    F  O  1  H  CF2Cl  H    H     nC3H72-433    F  O  1  H  CF2Cl  H    H     iC3H72-434    F  O  1  H  CF2Cl  H    H     iC4H92-435    F  O  1  H  CF2Cl  H    H     nC4H92-436    F  O  1  H  CF2Cl  H    H      CH2CH2Cl2-437    F  O  1  H  CF2Cl  H    H      CH2CH2Br2-438    F  O  1  H  CF2Cl  H    H      CH2CH=CH22-439    F  O  1  H  CF2Cl  H    H      CH(CH3)CH=CH22-440    F  O  1  H  CF2Cl  H    H      CH2CCl=CH22-441    F  O  1  H  CF2Cl  H    H      CH2C≡CH2-442    F  O  1  H  CF2Cl  H    H      CH(CH3)C≡CH2-443    F  O  1  H  CF2Cl  H    H      CH2CN2-444    F  O  1  H  CF2Cl  H    H      CH2OCH32-445    F  O  1  H  CF2Cl  H    H      CH2OC2H52-446    F  O  1  H  CF2Cl  H    H      CH2COOH2-447    F  O  1  H  CF2Cl  H    H      CH2COOCH3
                         表2(续)
    化合物   X  Z1n  R3  R1  R2  R4          R5编号
    2-448    F  O  1  H  CF2Cl  H    H      CH2COOC2H52-449    F  O  1  H  CF2Cl  H    H      CH2COOnC3H72-450    F  O  1  H  CF2Cl  H    H      CH2COOnC4H92-451    F  O  1  H  CF2Cl  H    H      CH2COOnC5H112-452    F  O  1  H  CF2Cl  H    H      CH2COOiC3H72-453    F  O  1  H  CF2Cl  H    H      CH2COOcC5H92-454    F  O  1  H  CF2Cl  H    H      CH2COOcC9H112-455    F  O  1  H  CF2Cl  H    H      CH(CH3)COOH2-456    F  O  1  H  CF2Cl  H    H      CH(CH3)COOCH32-457    F  O  1  H  CF2Cl  H    H      CH(CH3)COOC2H52-458    F  O  1  H  CF2Cl  H    H      CH(CH3)COOnC3H72-459    F  O  1  H  CF2Cl  H    H      CH(CH3)COOnC4H92-460    F  O  1  H  CF2Cl  H    H      CH(CH3)COOnC5H112-461    F  O  1  H  CF2Cl  H    H      CH(CH3)COOiC3H72-462    F  O  1  H  CF2Cl  H    H      CH(CH3)COOcC5H92-463    F  O  1  H  CF2Cl  H    H      CH(CH3)COOcC9H112-464    F  O  1  H  CF2Cl  H    CH3   H2-465    F  O  1  H  CF2Cl  H    CH3   CH32-466    F  O  1  H  CF2Cl  H    CH3   C2H52-467    F  O  1  H  CF2Cl  H    CH3  nC3H72-468    F  O  1  H  CF2Cl  H    CH3  iC3H72-469    F  O  1  H  CF2Cl  H    CH3  iC4H92-470    F  O  1  H  CF2Cl  H    CH3  nC4H9
                          表2(续)
  化合物   X  Z1n  R3   R1  R2  R4     R5编号
  2-471    F  O  1  H  CF2Cl  H    CH3 CH2CH=CH22-472    F  O  1  H  CF2Cl  H    CH3 CH(CH3)CH=CH22-473    F  O  1  H  CF2Cl  H    CH3 CH2C≡CH2-474    F  O  1  H  CF2Cl  H    CH3 CH(CH3)C≡CH2-475    F  O  1  H  CF2Cl  H    CH3 CH2OCH32-476    F  O  1  H  CF2Cl  H    CH3 CH2OC2H52-477    H  S  0  H  CF2Cl  H    -    H2-478    H  S  0  H  CF2Cl  H    -    CH32-479    H  S  0  H  CF2Cl  H    -    C2H52-480    H  S  0  H  CF2Cl  H    -   nC3H72-481    H  S  0  H  CF2Cl  H    -   nC4H92-482    H  S  0  H  CF2Cl  H    -   iC3H72-483    H  S  0  H  CF2Cl  H    -   iC4H92-484    H  S  0  H  CF2Cl  H    -    CH2CH2Cl2-485    H  S  0  H  CF2Cl  H    -    CH2CH2Br2-486    H  S  0  H  CF2Cl  H    -    CH2CH=CH22-487    H  S  0  H  CF2Cl  H    -    CH(CH3)CH=CH22-488    H  S  0  H  CF2Cl  H    -    CH2CCl=CH22-489    H  S  0  H  CF2Cl  H    -    CH2C≡CH2-490    H  S  0  H  CF2Cl  H    -    CH(CH3)C≡CH2-491    H  S  0  H  CF2Cl  H    -    CH2CN2-492    H  S  0  H  CF2Cl  H    -    CH2OCH32-493    H  S  0  H  CF2Cl  H    -    CH2OC2H5
                             表2(续)
    化合物   X  Z1n  R3   R1  R2  R4    R5编号
    2-494    H  S  0  H  CF2Cl  H    -    CH2COOH2-495    H  S  0  H  CF2Cl  H    -    CH2COOCH32-496    H  S  0  H  CF2Cl  H    -    CH2COOC2H52-497    H  S  0  H  CF2Cl  H    -    CH2COOnC3H72-498    H  S  0  H  CF2Cl  H    -    CH2COOnC4H92-499    H  S  0  H  CF2Cl  H    -    CH2COOnC5H112-500    H  S  0  H  CF2Cl  H    -    CH2COOiC3H72-501    H  S  0  H  CF2Cl  H    -    CH2COOcC5H92-502    H  S  0  H  CF2Cl  H    -    CH2COOcC6H112-503    H  S  0  H  CF2Cl  H    -    CH(CH3)COOH2-504    H  S  0  H  CF2Cl  H    -    CH(CH3)COOCH32-505    H  S  0  H  CF2Cl  H    -    CH(CH3)COOC2H52-506    H  S  0  H  CF2Cl  H    -    CH(CH3)COOnC3H72-507    H  S  0  H  CF2Cl  H    -    CH(CH3)COOnC4H92-508    H  S  0  H  CF2Cl  H    -    CH(CH3)COOnC5H112-509    H  S  0  H  CF2Cl  H    -    CH(CH3)COOiC3H72-510    H  S  0  H  CF2Cl  H    -    CH(CH3)COOcC5H92-511    H  S  0  H  CF2Cl  H    -    CH(CH3)COOcC5H112-512    F  S  0  H  CF2Cl  H    -    H2-513    F  S  0  H  CF2Cl  H    -    CH32-514    F  S  0  H  CF2Cl  H    -    C2H52-515    F  S  0  H  CF2Cl  H    -   nC3H72-516    F  S  0  H  CF2Cl  H    -   nC4H9
                            表2(续)
    化合物   X  Z1n  R3  R1  R2  R4   R5编号
    2-517    F  S  0  H  CF2Cl  H    -   iC3H72-518    F  S  0  H  CF2Cl  H    -   iC4H92-519    F  S  0  H  CF2Cl  H    -    CH2CH2Cl2-520    F  S  0  H  CF2Cl  H    -    CH2CH2Br2-521    F  S  0  H  CF2Cl  H    -    CH2CH=CH22-522    F  S  0  H  CF2Cl  H    -    CH(CH3)CH=CH22-523    F  S  0  H  CF2Cl  H    -    CH2CCl=CH22-524    F  S  0  H  CF2Cl  H    -    CH2C≡CH2-525    F  S  0  H  CF2Cl  H    -    CH(CH3)C≡CH2-526    F  S  0  H  CF2Cl  H    -    CH2CN2-527    F  S  0  H  CF2Cl  H    -    CH2OCH32-528    F  S  0  H  CF2Cl  H    -    CH2OC2H52-529    F  S  0  H  CF2Cl  H    -    CH2COOH2-530    F  S  0  H  CF2Cl  H    -    CH2COOCH32-531    F  S  0  H  CF2Cl  H    -    CH2COOC2H52-532    F  S  0  H  CF2Cl  H    -    CH2COOnC3H72-533    F  S  0  H  CF2Cl  H    -    CH2COOnC4H92-534    F  S  0  H  CF2Cl  H    -    CH2COOnC5H112-535    F  S  0  H  CF2Cl  H    -    CH2COOiC3H72-536    F  S  0  H  CF2Cl  H    -    CH2COOcC5H92-537    F  S  0  H  CF2Cl  H    -    CH2COOcC6H112-538    F  S  0  H  CF2Cl  H    -    CH(CH3)COOH2-539    F  S  0  H  CF2Cl  H    -    CH(CH3)COOCH3
                               表2(续)
    化合物   X  Z1n  R3 R1    R2  R4   R5编号
    2-540    F  S  0  H  CF2Cl  H    -    CH(CH3)COOC2H52-541    F  S  0  H  CF2Cl  H    -    CH(CH3)COOnC3H72-542    F  S  0  H  CF2Cl  H    -    CH(CH3)COOnC4H92-543    F  S  0  H  CF2Cl  H    -    CH(CH3)COOnC5H112-544    F  S  0  H  CF2Cl  H    -    CH(CH3)COOiC3H72-545    F  S  0  H  CF2Cl  H    -    CH(CH3)COOcC5H92-546    F  S  0  H  CF2Cl  H    -    CH(CH3)COOcC6H112-547    H  O  0  H  CF2Cl  H    -    H2-548    H  O  0  H  CF2Cl  H    -    CH32-549    H  O  0  H  CF2Cl  H    -    C2H52-550    H  O  0  H  CF2Cl  H    -   nC3H72-551    H  O  0  H  CF2Cl  H    -   nC4H92-552    H  O  0  H  CF2Cl  H    -   iC3H72-553    H  O  0  H  CF2Cl  H    -   iC4H92-554    H  O  0  H  CF2Cl  H    -    CH2CH=CH22-555    H  O  0  H  CF2Cl  H    -    CH(CH3)CH=CH22-556    H  O  0  H  CF2Cl  H    -    CH2C≡CH2-557    H  O  0  H  CF2Cl  H    -    CH(CH3)C≡CH2-558    H  O  0  H  CF2Cl  H    -    CH2OCH32-559    H  O  0  H  CF2Cl  H    -    CH2OC2H52-560    F  O  0  H  CF2Cl  H    -    H2-561    F  O  0  H  CF2Cl  H    -    CH3
                          表2(续)
    化合物   X  Z1n  R3   R1   R2  R4   R5编号
    2-562    F  O  0  H    CF2Cl  H    -    C2H52-563    F  O  0  H    CF2Cl  H    -   nC3H72-564    F  O  0  H    CF2Cl  H    -   nC4H92-565    F  O  0  H    CF2Cl  H    -    CH2CH=CH22-566    F  O  0  H    CF2Cl  H    -    CH(CH3)CH=CH22-567    F  O  0  H    CF2Cl  H    -    CH2C≡CH2-568    F  O  0  H    CF2Cl  H    -    CH(CH3)C≡CH2-569    F  O  0  H    CF2Cl  H    -    CH2OCH32-570    F  O  0  H    CF2Cl  H    -    CH2OC2H52-571    H  O  1  H    CF3    H    H    H2-572    H  O  1  H    CF3    H    H    CH32-573    H  O  1  H    CF3    H    H    C2H52-574    H  O  1  H    CF3    H    H   nC3H72-575    H  O  1  H    CF3    H    H   iC3H72-576    H  O  1  H    CF3    H    H   iC4H92-577    H  O  1  H    CF3    H    H   nC4H92-578    H  O  1  H    CF3    H    H    CH2CH2Cl2-579    H  O  1  H    CF3    H    H    CH2CH2Br2-580    H  O  1  H    CF3    H    H    CH2CH=CH22-581    H  O  1  H    CF3    H    H    CH(CH3)CH=CH22-582    H  O  1  H    CF3    H    H    CH2CCl=CH22-583    H  O  1  H    CF3    H    H    CH2C≡CH2-584    H  O  1  H    CF3    H    H    CH(CH3)C≡CH
                          表2(续)
    化合物 X  Z1n  R3  R1    R2  R4   R5编号
    2-585  H  O  1  H    CF3    H    H    CH2CN2-586  H  O  1  H    CF3    H    H    CH2OCH32-587  H  O  1  H    CF3    H    H    CH2OC2H52-588  H  O  1  H    CF3    H    H    CH2COOH2-589  H  O  1  H    CF3    H    H    CH2COOCH32-590  H  O  1  H    CF3    H    H    CH2COOC2H52-591  H  O  1  H    CF3    H    H    CH2COOnC3H72-592  H  O  1  H    CF3    H    H    CH2COOnC4H92-593  H  O  1  H    CF3    H    H    CH2COOnC5H112-594  H  O  1  H    CF3    H    H    CH2COOiC3H72-595  H  O  1  H    CF3    H    H    CH2COOcC5H92-596  H  O  1  H    CF3    H    H    CH2COOcC6H112-597  H  O  1  H    CF3    H    H    CH(CH3)COOH2-598  H  O  1  H    CF3    H    H    CH(CH3)COOCH32-599  H  O  1  H    CF3    H    H    CH(CH3)COOC2H52-600  H  O  1  H    CF3    H    H    CH(CH3)COOnC3H72-601  H  O  1  H    CF3    H    H    CH(CH3)COOnC4H92-602  H  O  1  H    CF3    H    H    CH(CH3)COOnC5H112-603  H  O  1  H    CF3    H    H    CH(CH3)COOiC3H72-604  H  O  1  H    CF3    H    H    CH(CH3)COOcC5H92-605  H  O  1  H    CF3    H    H    CH(CH3)COOcC6H112-606  H  O  1  H    CF3    H    CH3 H2-607  H  O  1  H    CF3    H    CH3 CH3
                             表2(续)
  化合物   X  Z1n  R3  R1    R2    R4   R5编号
  2-608    H  O  1  H    CF3    H    CH3   C2H52-609    H  O  1  H    CF3    H    CH3  nC3H72-610    H  O  1  H    CF3    H    CH3  iC3H72-611    H  O  1  H    CF3    H    CH3  iC4H92-612    H  O  1  H    CF3    H    CH3  nC4H92-613    H  O  1  H    CF3    H    CH3   CH2CH=CH22-614    H  O  1  H    CF3    H    CH3   CH(CH3)CH=CH22-615    H  O  1  H    CF3    H    CH3   CH2C≡CH2-616    H  O  1  H    CF3    H    CH3   CH(CH3)C≡CH2-617    H  O  1  H    CF3    H    CH3   CH2OCH32-618    H  O  1  H    CF3    H    CH3   CH2OC2H52-619    F  O  1  H    CF3    H    H      H2-620    F  O  1  H    CF3    H    H      CH32-621    F  O  1  H    CF3    H    H      C2H52-622    F  O  1  H    CF3    H    H     nC3H72-623    F  O  1  H    CF3    H    H     iC3H72-624    F  O  1  H    CF3    H    H     iC4H92-625    F  O  1  H    CF3    H    H     nC4H92-626    F  O  1  H    CF3    H    H      CH2CH2Cl2-627    F  O  1  H    CF3    H    H      CH2CH2Br2-628    F  O  1  H    CF3    H    H      CH2CH=CH22-629    F  O  1  H    CF3    H    H      CH(CH3)CH=CH22-630    F  O  1  H    CF3    H    H      CH2CCl=CH2
                          表2(续)
    化合物   X  Z1n  R3  R1    R2  R4    R5编号
    2-631    F  O  1  H    CF3    H    H    CH2C≡CH2-632    F  O  1  H    CF3    H    H    CH(CH3)C≡CH2-633    F  O  1  H    CF3    H    H    CH2CN2-634    F  O  1  H    CF3    H    H    CH2OCH32-635    F  O  1  H    CF3    H    H    CH2OC2H52-636    F  O  1  H    CF3    H    H    CH2COOH2-637    F  O  1  H    CF3    H    H    CH2COOCH32-638    F  O  1  H    CF3    H    H    CH2COOC2H52-639    F  O  1  H    CF3    H    H    CH2COOnC3H72-640    F  O  1  H    CF3    H    H    CH2COOnC4H92-641    F  O  1  H    CF3    H    H    CH2COOnC5H112-642    F  O  1  H    CF3    H    H    CH2COOiC3H72-643    F  O  1  H    CF3    H    H    CH2COOcC5H92-644    F  O  1  H    CF3    H    H    CH2COOcC6H112-645    F  O  1  H    CF3    H    H    CH(CH3)COOH2-646    F  O  1  H    CF3    H    H    CH(CH3)COOCH32-647    F  O  1  H    CF3    H    H    CH(CH3)COOC2H52-648    F  O  1  H    CF3    H    H    CH(CH3)COOnC3H72-648    F  O  1  H    CF3    H    H    CH(CH3)COOnC4H92-650    F  O  1  H    CF3    H    H    CH(CH3)COOnC5H112-651    F  O  1  H    CF3    H    H    CH(CH3)COOiC3H72-652    F  O  1  H    CF3    H    H    CH(CH3)COOcC6H92-653    F  O  1  H    CF3    H    H    CH(CH3)COOcC6H11
                           表2(续)
    化合物   X  Z1n  R3   R1   R2  R4   R5编号
    2-654    F  O  1  H    CF3    H    CH3  H2-655    F  O  1  H    CF3    H    CH3  CH32-656    F  O  1  H    CF3    H    CH3  C2H52-657    F  O  1  H    CF3    H    CH3 nC3H72-658    F  O  1  H    CF3    H    CH3 iC3H72-659    F  O  1  H    CF3    H    CH3 iC4H92-660    F  O  1  H    CF3    H    CH3 nC4H92-661    F  O  1  H    CF3    H    CH3  CH2CH=CH22-662    F  O  1  H    CF3    H    CH3  CH(CH3)CH=CH22-663    F  O  1  H    CF3    H    CH3  CH2C≡CH2-664    F  O  1  H    CF3    H    CH3  CH(CH3)C≡CH2-665    F  O  1  H    CF3    H    CH3  CH2OCH32-666    F  O  1  H    CF3    H    CH3  CH2OC2H52-667    H  S  0  H    CF3    H    -     H2-668    H  S  0  H    CF3    H    -     CH32-669    H  S  0  H    CF3    H    -     C2H52-670    H  S  0  H    CF3    H    -    nC3H72-671    H  S  0  H    CF3    H    -    nC4H92-672    H  S  0  H    CF3    H    -    iC3H72-673    H  S  0  H    CF3    H    -    iC4H92-674    H  S  0  H    CF3    H    -     CH2CH2Cl2-675    H  S  0  H    CF3    H    -     CH2CH2Br
                        表2(续)
    化合物   X  Z1n  R3  R1    R2  R4   R5编号
    2-676    H  S  0  H    CF3    H    -    CH2CH=CH22-677    H  S  0  H    CF3    H    -    CH(CH3)CH=CH22-678    H  S  0  H    CF3    H    -    CH2CCl=CH22-679    H  S  0  H    CF3    H    -    CH2C≡CH2-680    H  S  0  H    CF3    H    -    CH(CH3)C≡CH2-681    H  S  0  H    CF3    H    -    CH2CN2-682    H  S  0  H    CF3    H    -    CH2OCH32-683    H  S  0  H    CF3    H    -    CH2OC2H52-684    H  S  0  H    CF3    H    -    CH2COOH2-685    H  S  0  H    CF3    H    -    CH2COOCH32-686    H  S  0  H    CF3    H    -    CH2COOC2H52-687    H  S  0  H    CF3    H    -    CH2COOnC3H72-688    H  S  0  H    CF3    H    -    CH2COOnC4H92-689    H  S  0  H    CF3    H    -    CH2COOnC5H112-690    H  S  0  H    CF3    H    -    CH2COOiC3H72-691    H  S  0  H    CF3    H    -    CH2COOcC5H92-692    H  S  0  H    CF3    H    -    CH2COOcC6H112-693    H  S  0  H    CF3    H    -    CH(CH3)COOH2-694    H  S  0  H    CF3    H    -    CH(CH3)COOCH32-695    H  S  0  H    CF3    H    -    CH(CH3)COOC2H52-696    H  S  0  H    CF3    H    -    CH(CH3)COOnC3H72-697    H  S  0  H    CF3    H    -    CH(CH3)COOnC4H92-698    H  S  0  H    CF3    H    -    CH(CH3)COOnC5H11
                             表2(续)
  化合物   X  Z1n  R3  R1    R2  R4      R5编号
  2-699    H  S  0  H    CF3    H    -    CH(CH3)COOiC3H72-700    H  S  0  H    CF3    H    -    CH(CH3)COOcC5H92-701    H  S  0  H    CF3    H    -    CH(CH3)COOcC6H112-702    F  S  0  H    CF3    H    -    H2-703    F  S  0  H    CF3    H    -    CH32-704    F  S  0  H    CF3    H    -    C2H52-705    F  S  0  H    CF3    H    -   nC3H72-706    F  S  0  H    CF3    H    -   nC4H92-707    F  S  0  H    CF3    H    -   iC3H72-708    F  S  0  H    CF3    H    -   sC4H92-709    F  S  0  H    CF3    H    -    CH2CH2Cl2-710    F  S  0  H    CF3    H    -    CH2CH2Br2-711    F  S  0  H    CF3    H    -    CH2CH=CH22-712    F  S  0  H    CF3    H    -    CH(CH3)CH=CH22-713    F  S  0  H    CF3    H    -    CH2CCl=CH22-714    F  S  0  H    CF3    H    -    CH2C≡CH2-715    F  S  0  H    CF3    H    -    CH(CH3)C≡CH2-716    F  S  0  H    CF3    H    -    CH2CN2-717    F  S  0  H    CF3    H    -    CH2OCH32-718    F  S  0  H    CF3    H    -    CH2OC2H52-719    F  S  0  H    CF3    H    -    CH2COOH2-720    F  S  0  H    CF3    H    -    CH2COOCH32-721    F  S  0  H    CF3    H    -    CH2COOC2H5
                             表2(续)
    化合物 X  Z1n  R3  R1  R2  R4     R5编号
    2-722  F  S  0  H    CF3  H    -    CH2COOnC3H72-723  F  S  0  H    CF3  H    -    CH2COOnC4H92-724  F  S  0  H    CF3  H    -    CH2COOnC5H112-725  F  S  0  H    CF3  H    -    CH2COOiC3H72-726  F  S  0  H    CF3  H    -    CH2COOcC5H92-727  F  S  0  H    CF3  H    -    CH2COOcC6H112-728  F  S  0  H    CF3  H    -    CH(CH3)COOH2-729  F  S  0  H    CF3  H    -    CH(CH3)COOCH32-730  F  S  0  H    CF3  H    -    CH(CH3)COOC2H52-731  F  S  0  H    CF3  H    -    CH(CH3)COOnC3H72-732  F  S  0  H    CF3  H    -    CH(CH3)COOnC4H92-733  F  S  0  H    CF3  H    -    CH(CH3)COOnC5H112-734  F  S  0  H    CF3  H    -    CH(CH3)COOiC3H72-735  F  S  0  H    CF3  H    -    CH(CH3)COOcC5H92-736  F  S  0  H    CF3  H    -    CH(CH3)COOcC6H112-737  H  O  0  H    CF3  H    -    H2-738  H  O  0  H    CF3  H    -    CH32-739  H  O  0  H    CF3  H    -    C2H52-740  H  O  0  H    CF3  H    -   nC3H72-741  H  O  0  H    CF3  H    -   nC4H92-742  H  O  0  H    CF3  H    -   iC3H72-743  H  O  0  H    CF3  H    -   iC4H92-744  H  O  0  H    CF3  H    -    CH2CH=CH2
                               表2(续)
    化合物   X  Z1n  R3  R1    R2  R4   R5编号
    2-745    H  O  0  H    CF3    H    -    CH(CH3)CH=CH22-746    H  O  0  H    CF3    H    -    CH2C≡CH2-747    H  O  0  H    CF3    H    -    CH(CH3)C≡CH2-748    H  O  0  H    CF3    H    -    CH2OCH32-749    H  O  0  H    CF3    H    -    CH2OC2H52-750    F  O  0  H    CF3    H    -    H2-751    F  O  0  H    CF3    H    -    CH32-752    F  O  0  H    CF3    H    -    C2H- 52-753    F  O  0  H    CF3    H    -   nC3H72-754    F  O  0  H    CF3    H    -   nC4H92-755    F  O  0  H    CF3    H    -    CH2CH=CH22-756    F  O  0  H    CF3    H    -    CH(CH3)CH=CH22-757    F  O  0  H    CF3    H    -    CH2C≡CH2-758    F  O  0  H    CF3    H    -    CH(CH3)C≡CH2-759    F  O  0  H    CF3    H    -    CH2OCH32-760    F  O  0  H    CF3    H    -    CH2OC2H52-761    H  O  1  CH3 CF3    H    H    H2-762    H  O  1  CH3 CF3    H    H    CH32-763    H  O  1  CH3 CF3    H    H    C2H52-764    H  O  1  CH3 CF3    H    H   nC3H72-765    H  O  1  CH3 CF3    H    H   iC3H72-766    H  O  1  CH3 CF3    H    H   iC4H92-767    H  O  1  CH3 CF3    H    H   nC4H9
                          表2(续)
    化合物   X  Z1n  R3     R1     R2 R4  R5编号
    2-768    H  O  1  CH3    CF3    H    H    CH2CH2Cl2-769    H  O  1  CH3    CF3    H    H    CH2CH2Br2-770    H  O  1  CH3    CF3    H    H    CH2CH=CH22-771    H  O  1  CH3    CF3    H    H    CH(CH3)CH=CH22-772    H  O  1  CH3    CF3    H    H    CH2CCl=CH22-773    H  O  1  CH3    CF3    H    H    CH2C≡CH2-774    H  O  1  CH3    CF3    H    H    CH(CH3)C≡CH2-775    H  O  1  CH3    CF3    H    H    CH2CN2-776    H  O  1  CH3    CF3    H    H    CH2OCH32-777    H  O  1  CH3    CF3    H    H    CH2OC2H52-778    H  O  1  CH3    CF3    H    H    CH2COOH2-779    H  O  1  CH3    CF3    H    H    CH2COOCH32-780    H  O  1  CH3    CF3    H    H    CH2COOC2H52-781    H  O  1  CH3    CF3    H    H    CH2COOnC3H72-782    H  O  1  CH3    CF3    H    H    CH2COOnC4H92-783    H  O  1  CH3    CF3    H    H    CH2COOnC5H112-784    H  O  1  CH3    CF3    H    H    CH2COOiC3H72-785    H  O  1  CH3    CF3    H    H    CH2COOcC5H92-786    H  O  1  CH3    CF3    H    H    CH2COOcC6H112-787    H  O  1  CH3    CF3    H    H    CH(CH3)COOH2-788    H  O  1  CH3    CF3    H    H    CH(CH3)COOCH32-789    H  O  1  CH3    CF3    H    H    CH(CH3)COOC2H6
                             表2(续)
    化合物   X  Z1n  R3     R1    R2  R4         R5编号
    2-790    H  O  1  CH3    CF3    H    H       CH(CH3)COOnC3H72-791    H  O  1  CH3    CF3    H    H       CH(CH3)COOnC4H92-792    H  O  1  CH3    CF3    H    H       CH(CH3)COOnC5H112-793    H  O  1  CH3    CF3    H    H       CH(CH3)COOiC3H72-794    H  O  1  CH3    CF3    H    H       CH(CH3)COOcC5H92-795    H  O  1  CH3    CF3    H    H       CH(CH3)COOcC6H112-796    H  O  1  CH3    CF3    H    CH3    H2-797    H  O  1  CH3    CF3    H    CH3    CH32-798    H  O  1  CH3    CF3    H    CH3    C2H52-799    H  O  1  CH3    CF3    H    CH3   nC3H72-800    H  O  1  CH3    CF3    H    CH3   iC3H72-801    H  O  1  CH3    CF3    H    CH3   iC4H92-802    H  O  1  CH3    CF3    H    CH3   nC4H92-803    H  O  1  CH3    CF3    H    CH3    CH2CH=CH22-804    H  O  1  CH3    CF3    H    CH3    CH(CH3)CH=CH22-805    H  O  1  CH3    CF3    H    CH3    CH2C≡CH2-806    H  O  1  CH3    CF3    H    CH3    CH(CH3)C≡CH2-807    H  O  1  CH3    CF3    H    CH3    CH2OCH32-808    H  O  1  CH3    CF3    H    CH3    CH2OC2H52-809    F  O  1  CH3    CF3    H    H       H2-810    F  O  1  CH3    CF3    H    H       CH32-811    F  O  1  CH3    CF3    H    H       C2H52-812    F  O  1  CH3    CF3    H    H      nC3H7
                          表2(续)
    化合物   X  Z1n  R3     R1     R2 R4   R5编号
    2-813    F  O  1  CH3    CF3    H    H   iC3H72-814    F  O  1  CH3    CF3    H    H   iC4H92-815    F  O  1  CH3    CF3    H    H   nC4H92-816    F  O  1  CH3    CF3    H    H    CH2CH2Cl2-817    F  O  1  CH3    CF3    H    H    CH2CH2Br2-818    F  O  1  CH3    CF3    H    H    CH2CH=CH22-819    F  O  1  CH3    CF3    H    H    CH(CH3)CH=CH22-820    F  O  1  CH3    CF3    H    H    CH2CCl-=CH22-821    F  O  1  CH3    CF3    H    H    CH2C≡CH2-822    F  O  1  CH3    CF3    H    H    CH(CH3)C≡CH2-823    F  O  1  CH3    CF3    H    H    CH2CN2-824    F  O  1  CH3    CF3    H    H    CH2OCH32-825    F  O  1  CH3    CF3    H    H    CH2OC2H52-826    F  O  1  CH3    CF3    H    H    CH2COOH2-827    F  O  1  CH3    CF3    H    H    CH2COOCH32-828    F  O  1  CH3    CF3    H    H    CH2COOC2H52-829    F  O  1  CH3    CF3    H    H    CH2COOnC3H72-830    F  O  1  CH3    CF3    H    H    CH2COOnC4H92-831    F  O  1  CH3    CF3    H    H    CH2COOnC5H112-832    F  O  1  CH3    CF3    H    H    CH2COOiC3H72-833    F  O  1  CH3    CF3    H    H    CH2COOcC5H92-834    F  O  1  CH3    CF3    H    H    CH2COOcC6H112-835    F  O  1  CH3    CF3    H    H    CH(CH3)COOH
                          表2(续)
    化合物   X  Z1n  R3     R1     R2  R4      R5编号
    2-836    F  O  1  CH3    CF3    H    H     CH(CH3)COOCH32-837    F  O  1  CH3    CF3    H    H     CH(CH3)COOC2H52-838    F  O  1  CH3    CF3    H    H     CH(CH3)COOnC3H72-839    F  O  1  CH3    CF3    H    H     CH(CH3)COOnC4H92-840    F  O  1  CH3    CF3    H    H     CH(CH3)COOnC5H112-841    F  O  1  CH3    CF3    H    H     CH(CH3)COOiC3H72-842    F  O  1  CH3    CF3    H    H     CH(CH3)COOcC5H92-843    F  O  1  CH3    CF3    H    H     CH(CH3)COOcC6H112-843    F  O  1  CH3    CF3    H    CH3  H2-845    F  O  1  CH3    CF3    H    CH3  CH32-846    F  O  1  CH3    CF3    H    CH3  C2H52-847    F  O  1  CH3    CF3    H    CH3 nC3H72-848    F  O  1  CH3    CF3    H    CH3 iC3H72-849    F  O  1  CH3    CF3    H    CH3 iC4H92-850    F  O  1  CH3    CF3    H    CH3 nC4H92-851    F  O  1  CH3    CF3    H    CH3  CH2CH=CH22-852    F  O  1  CH3    CF3    H    CH3  CH(CH3)CH=CH22-853    F  O  1  CH3    CF3    H    CH3  CH2C≡CH2-854    F  O  1  CH3    CF3    H    CH3  CH(CH3)C≡CH2-855    F  O  1  CH3    CF3    H    CH3  CH2OCH32-856    F  O  1  CH3    CF3    H    CH3  CH2OC2H52-857    H  S  0  CH3    CF3    H    -     H2-858    H  S  0  CH3    CF3    H    -     CH3
                        表2(续)
  化合物   X  Z1n  R3     R1    R2  R4   R5编号
  2-859    H  S  0  CH3    CF3    H    -    C2H52-860    H  S  0  CH3    CF3    H    -   nC3H72-861    H  S  0  CH3    CF3    H    -   nC4H92-862    H  S  0  CH3    CF3    H    -   iC3H72-863    H  S  0  CH3    CF3    H    -   iC4H92-864    H  S  0  CH3    CF3    H    -    CH2CH2Cl2-865    H  S  0  CH3    CF3    H    -    CH2CH2Br2-866    H  S  0  CH3    CF3    H    -    CH2CH=CH22-867    H  S  0  CH3    CF3    H    -    CH(CH3)CH=CH22-868    H  S  0  CH3    CF3    H    -    CH2CCl=CH22-869    H  S  0  CH3    CF3    H    -    CH2C≡CH2-870    H  S  0  CH3    CF3    H    -    CH(CH3)C≡CH2-871    H  S  0  CH3    CF3    H    -    CH2CN2-872    H  S  0  CH3    CF3    H    -    CH2OCH32-873    H  S  0  CH3    CF3    H    -    CH2OC2H52-874    H  S  0  CH3    CF3    H    -    CH2COOH2-875    H  S  0  CH3    CF3    H    -    CH2COOCH32-876    H  S  0  CH3    CF3    H    -    CH2COOC2H52-877    H  S  0  CH3    CF3    H    -    CH2COOnC3H72-878    H  S  0  CH3    CF3    H    -    CH2COOnC4H92-879    H  S  0  CH3    CF3    H    -    CH2COOnC6H112-880    H  S  0  CH3    CF3    H    -    CH2COOiC3H72-881    H  S  0  CH3    CF3    H    -    CH2COOcC8H9
                            表2(续)
    化合物   X  Z1n  R3     R1     R2 R4      R5编号
    2-882    H  S  0  CH3    CF3    H    -    CH2COOcC6H112-883    H  S  0  CH3    CF3    H    -    CH(CH3)COOH2-884    H  S  0  CH3    CF3    H    -    CH(CH3)COOCH32-885    H  S  0  CH3    CF3    H    -    CH(CH3)COOC2H52-886    H  S  0  CH3    CF3    H    -    CH(CH3)COOnC3H72-887    H  S  0  CH3    CF3    H    -    CH(CH3)COOnC4H92-888    H  S  0  CH3    CF3    H    -    CH(CH3)COOnC5H112-889    H  S  0  CH3    CF3    H    -    CH(CH3)COOiC3H72-890    H  S  0  CH3    CF3    H    -    CH(CH3)COOcC5H92-891    H  S  0  CH3    CF3    H    -    CH(CH3)COOcC6H112-892    F  S  0  CH3    CF3    H    -    H2-893    F  S  0  CH3    CF3    H    -    CH32-894    F  S  0  CH3    CF3    H    -    C2H52-895    F  S  0  CH3    CF3    H    -   nC3H72-896    F  S  0  CH3    CF3    H    -   nC4H92-897    F  S  0  CH3    CF3    H    -   iC3H72-898    F  S  0  CH3    CF3    H    -   sC4H92-899    F  S  0  CH3    CF3    H    -    CH2CH2Cl2-900    F  S  0  CH3    CF3    H    -    CH2CH2Br2-901    F  S  0  CH3    CF3    H    -    CH2CH=CH22-902    F  S  0  CH3    CF3    H    -    CH(CH3)CH=CH22-903    F  S  0  CH3    CF3    H    -    CH2CCl=CH2
                           表2(续)
    化合物   X  Z1n  R3     R1    R2  R4   R5编号
    2-904    F  S  0  CH3    CF3    H    -    CH2C≡CH2-905    F  S  0  CH3    CF3    H    -    CH(CH3)C≡CH2-906    F  S  0  CH3    CF3    H    -    CH2CN2-907    F  S  0  CH3    CF3    H    -    CH2OCH32-908    F  S  0  CH3    CF3    H    -    CH2OC2H52-909    F  S  0  CH3    CF3    H    -    CH2COOH2-910    F  S  0  CH3    CF3    H    -    CH2COOCH32-911    F  S  0  CH3    CF3    H    -    CH2COOC2H52-912    F  S  0  CH3    CF3    H    -    CH2COOnC3H72-913    F  S  0  CH3    CF3    H    -    CH2COOnC4H92-914    F  S  0  CH3    CF3    H    -    CH2COOnC5H112-915    F  S  0  CH3    CF3    H    -    CH2COO1C3H72-916    F  S  0  CH3    CF3    H    -    CH2COOcC5H92-917    F  S  0  CH3    CF3    H    -    CH2COOcC6H112-918    F  S  0  CH3    CF3    H    -    CH(CH3)COOH2-919    F  S  0  CH3    CF3    H    -    CH(CH3)COOCH32-920    F  S  0  CH3    CF3    H    -    CH(CH3)COOC2H52-921    F  S  0  CH3    CF3    H    -    CH(CH3)COOnC3H72-922    F  S  0  CH3    CF3    H    -    CH(CH3)COOnC4H92-923    F  S  0  CH3    CF3    H    -    CH(CH3)COOnC5H112-924    F  S  0  CH3    CF3    H    -    CH(CH3)COOiC3H72-925    F  S  0  CH3    CF3    H    -    CH(CH3)COOcC5H92-926    F  S  0  CH3    CF3    H    -    CH(CH3)COOcC6H11
                             表2(续)
    化合物   X  Z1n  R3     R1    R2  R4  R5编号
    2-927    H  O  0  CH3    CF3    H    -    H2-928    H  O  0  CH3    CF3    H    -    CH32-929    H  O  0  CH3    CF3    H    -    C2H52-930    H  O  0  CH3    CF3    H    -   nC3H72-931    H  O  0  CH3    CF3    H    -   nC4H92-932    H  O  0  CH3    CF3    H    -   iC3H72-933    H  O  0  CH3    CF3    H    -   iC4H92-934    H  O  0  CH3    CF3    H    -    CH2CH=CH22-935    H  O  0  CH3    CF3    H    -    CH(CH3)CH=CH22-936    H  O  0  CH3    CF3    H    -    CH2C≡CH2-937    H  O  0  CH3    CF3    H    -    CH(CH3)C≡CH2-938    H  O  0  CH3    CF3    H    -    CH2OCH32-939    H  O  0  CH3    CF3    H    -    CH2C2H52-940    F  O  0  CH3    CF3    H    -    H2-941    F  O  0  CH3    CF3    H    -    CH32-942    F  O  0  CH3    CF3    H    -    C2H52-943    F  O  0  CH3    CF3    H    -   nC3H72-944    F  O  0  CH3    CF3    H    -   nC4H92-945    F  O  0  CH3    CF3    H    -    CH2CH=CH22-946    F  O  0  CH3    CF3    H    -    CH(CH3)CH=CH22-947    F  O  0  CH3    CF3    H    -    CH2C≡CH2-948    F  O  0  CH3    CF3    H    -    CH(CH3)C≡CH2-949    F  O  0  CH3    CF3    H    -    CH2OCH3
                           表2(续)
    化合物   X  Z1n  R3     R1     R2  R4   R5编号
    2-950    F  O  0  CH3    CF3    H    -    CH2OC2H5
                           表3下式化合物:
Figure C9619770002321
  化合物 X    Y     Z2  R3   R1   R2   R6编号
  3-1    H    F     O    H  CF2Cl    H    CH33-2    H    Cl    O    H  CF2Cl    H    CH33-3    H    Br    O    H  CF2Cl    H    CH33-4    F    F     O    H  CF2Cl    H    CH33-5    F    Cl    O    H  CF2Cl    H    CH33-6    F    Br    O    H  CF2Cl    H    CH33-7    H    F     O    H  CF2Cl    CH3 CH33-8    H    Cl    O    H  CF2Cl    CH3 CH33-9    H    Br    O    H  CF2Cl    CH3 CH33-10   F    F     O    H  CF2Cl    CH3 CH33-11   F    Cl    O    H  CF2Cl    CH3 CH33-12   F    Br    O    H  CF2Cl    CH3 CH33-13   H    F     O    H  CF2Cl    H    C2H53-14   H    Cl    O    H  CF2Cl    H    C2H5
                            表3(续)
    化合物  X    Y    Z2  R3  R1   R2    R6编号
    3-15    H    Br   O    H  CF2Cl  H       C2H53-16    F    F    O    H  CF2Cl  H       C2H53-17    F    Cl   O    H  CF2Cl  H       C2H53-18    F    Br   O    H  CF2Cl  H       C2H53-19    H    F    O    H  CF2Cl  CH3    C2H53-20    H    Cl   O    H  CF2Cl  CH3    C2H53-21    H    Br   O    H  CF2Cl  CH3    C2H53-22    F    F    O    H  CF2Cl  CH3    C2H53-23    F    Cl   O    H  CF2Cl  CH3    C2H53-24    F    Br   O    H  CF2Cl  CH3    C2H53-25    H    F    O    H  CF2Cl  CH3    CH2Br3-26    H    F    O    H  CF2Cl  CH3    CHBr23-27    H    F    O    H  CF2Cl  CH3    CBr33-28    H    F    O    H  CF2Cl  CH3    CHO3-29    H    F    O    H  CF2Cl  CH3    CN3-30    H    F    O    H  CF2Cl  CH3    COOH3-31    H    F    O    H  CF2Cl  CH3    CH2OH3-32    H    F    O    H  CF2Cl  CH3    CH2OCH33-33    H    F    O    H  CF2Cl  CH3    CH2OC2H53-34    H    F    O    H  CF2Cl  CH3    CH2OiC3H73-35    H    F    O    H  CF2Cl  CH3    CH2OCH2OCH33-36    H    F    O    H  CF2Cl  CH3    CH2OCH2OC2H53-37    H    F    O    H  CF2Cl  CH3    CH2OCOCH3
                                表3(续)
    化合物  X    Y     Z2  R3   R1  R2    R6编号
    3-38    H    F     O    H  CF2Cl  CH3    CH2OCOC2H53-39    H    F     O    H  CF2Cl  CH3    CH2OCOiC3H73-40    H    F     O    H  CF2Cl  CH3    CH2OCOCH2Cl3-41    H    F     O    H  CF2Cl  CH3    CH2OCOCCl33-42    H    F     O    H  CF2Cl  CH3    CH2OCOCF33-43    H    F     O    H  CF2Cl  CH3    COOCH33-44    H    F     O    H  CF2Cl  CH3    COOC2H53-45    H    F     O    H  CF2Cl  CH3    COOnC3H73-46    H    F     O    H  CF2Cl  CH3    COOnC4H93-47    H    F     O    H  CF2Cl  CH3    COOnC5H113-48    H    F     O    H  CF2Cl  CH3    COOiC3H73-49    H    F     O    H  CF2Cl  CH3    COCH33-50    H    F     O    H  CF2Cl  CH3    COC2H53-51    H    Cl    O    H  CF2Cl  CH3    CH2Br3-52    H    Cl    O    H  CF2Cl  CH3    CHBr23-53    H    Cl    O    H  CF2Cl  CH3    CBr33-54    H    Cl    O    H  CF2Cl  CH3    CHO3-55    H    Cl    O    H  CF2Cl  CH3    CN3-56    H    Cl    O    H  CF2Cl  CH3    COOH3-57    H    Cl    O    H  CF2Cl  CH3    CH2OH3-58    H    Cl    O    H  CF2Cl  CH3    CH2OCH33-59    H    Cl    O    H  CF2Cl  CH3    CH2OC2H63-60    H    Cl    O    H  CF2Cl  CH3    CH2OiC3H7
                             表3(续)
    化合物  X    Y     Z2  R3   R1  R2         R6编号
    3-61    H    Cl    O    H  CF2Cl  CH3    CH2OCH2OCH33-62    H    Cl    O    H  CF2Cl  CH3    CH2OCH2OC2H53-63    H    Cl    O    H  CF2Cl  CH3    CH2OCOCH33-64    H    Cl    O    H  CF2Cl  CH3    CH2OCOC2H53-65    H    Cl    O    H  CF2Cl  CH3    CH2OCOiC3H73-66    H    Cl    O    H  CF2Cl  CH3    CH2OCOCH2Cl3-67    H    Cl    O    H  CF2Cl  CH3    CH2OCOCCl33-67    H    Cl    O    H  CF2Cl  CH3    CH2OCOCF33-69    H    Cl    O    H  CF2Cl  CH3    COOCH33-70    H    Cl    O    H  CF2Cl  CH3    COOC2H53-71    H    Cl    O    H  CF2Cl  CH3    COOnC3H73-72    H    Cl    O    H  CF2Cl  CH3    COOnC4H93-73    H    Cl    O    H  CF2Cl  CH3    COOnC5H113-74    H    Cl    O    H  CF2Cl  CH3    COOiC3H73-75    H    Cl    O    H  CF2Cl  CH3    COCH33-76    H    Cl    O    H  CF2Cl  CH3    COC2H53-77    F    F     O    H  CF2Cl  CH3    CH2Br3-78    F    F     O    H  CF2Cl  CH3    CHBr23-79    F    F     O    H  CF2Cl  CH3    CBr33-80    F    F     O    H  CF2Cl  CH3    CHO3-81    F    F     O    H  CF2Cl  CH3    CN3-82    F    F     O    H  CF2Cl  CH3    COOH3-83    F    F     O    H  CF2Cl  CH3    CH2OH
                           表3(续)
    化合物  X    Y    Z2  R3  R1   R2     R5编号
    3-84    F    F    O    H  CF2Cl  CH3    CH2OCH33-85    F    F    O    H  CF2Cl  CH3    CH2OC2H53-86    F    F    O    H  CF2Cl  CH3    CH2OiC3H73-87    F    F    O    H  CF2Cl  CH3    CH2OCH2OCH33-88    F    F    O    H  CF2Cl  CH3    CH2OCH2OC2H53-89    F    F    O    H  CF2Cl  CH3    CH2OCOCH33-90    F    F    O    H  CF2Cl  CH3    CH2OCOC2H53-91    F    F    O    H  CF2Cl  CH3    CH2OCOiC3H73-92    F    F    O    H  CF2Cl  CH3    CH2OCOCH2Cl3-93    F    F    O    H  CF2Cl  CH3    CH2OCOCCl33-94    F    F    O    H  CF2Cl  CH3    CH2OCOCF33-95    F    F    O    H  CF2Cl  CH3    COOCH33-96    F    F    O    H  CF2Cl  CH3    COOC2H53-97    F    F    O    H  CF2Cl  CH3    COOnC3H73-98    F    F    O    H  CF2Cl  CH3    COOnC4H93-99    F    F    O    H  CF2Cl  CH3    COOnC5H113-100   F    F    O    H  CF2Cl  CH3    COOiC3H73-101   F    F    O    H  CF2Cl  CH3    COCH33-102   F    F    O    H  CF2Cl  CH3    COC2H53-103   F    Cl   O    H  CF2Cl  CH3    CH2Br3-104   F    Cl   O    H  CF2Cl  CH3    CHBr23-105   F    Cl   O    H  CF2Cl  CH3    CBr3
                        表3(续)
    化合物   X    Y     Z2  R3  R1   R2     R6编号
    3-106    F    Cl    O    H  CF2Cl  CH3    CHO3-107    F    Cl    O    H  CF2Cl  CH3    CN3-108    F    Cl    O    H  CF2Cl  CH3    COOH3-109    F    Cl    O    H  CF2Cl  CH3    CH2OH3-110    F    Cl    O    H  CF2Cl  CH3    CH2OCH33-111    F    Cl    O    H  CF2Cl  CH3    CH2OC2H53-112    F    Cl    O    H  CF2Cl  CH3    CH2OiC3H73-113    F    Cl    O    H  CF2Cl  CH3    CH2OCH2OCH33-114    F    Cl    O    H  CF2Cl  CH3    CH3OCH2OC2H53-115    F    Cl    O    H  CF2Cl  CH3    CH2OCOCH33-116    F    Cl    O    H  CF2Cl  CH3    CH2OCOC2H53-117    F    Cl    O    H  CF2Cl  CH3    CH2OCOiC3H73-118    F    Cl    O    H  CF2Cl  CH3    CH2OCOCH2Cl3-119    F    Cl    O    H  CF2Cl  CH3    CH2OCOCCl33-120    F    Cl    O    H  CF2Cl  CH3    CH2OCOCF33-121    F    Cl    O    H  CF2Cl  CH3    COOCH33-122    F    Cl    O    H  CF2Cl  CH3    COOC2H53-123    F    Cl    O    H  CF2Cl  CH3    COOnC3H73-124    F    Cl    O    H  CF2Cl  CH3    COOnC4H93-125    F    Cl    O    H  CF2Cl  CH3    COOnC5H113-126    F    Cl    O    H  CF2Cl  CH3    COOiC3H73-127    F    Cl    O    H  CF2Cl  CH3    COCH33-128    F    Cl    O    H  CF2Cl  CH3    COC2H5
                         表3(续)
    化合物   X    Y    Z2  R3  R1    R2    R6编号
    3-129    H    F    O    H    CF3    H      CH33-130    H    Cl   O    H    CF3    H      CH33-131    H    Br   O    H    CF3    H      CH33-132    F    F    O    H    CF3    H      CH33-133    F    Cl   O    H    CF3    H      CH33-134    F    Br   O    H    CF3    H      CH33-135    H    F    O    H    CF3    CH3   CH33-136    H    Cl   O    H    CF3    CH3   CH33-137    H    Br   O    H    CF3    CH3   CH33-138    F    F    O    H    CF3    CH3   CH33-139    F    Cl   O    H    CF3    CH3   CH33-140    F    Br   O    H    CF3    CH3   CH33-141    H    F    O    H    CF3    H      C2H53-142    H    Cl   O    H    CF3    H      C2H53-143    H    Br   O    H    CF3    H      C2H53-144    F    F    O    H    CF3    H      C2H53-145    F    Cl   O    H    CF3    H      C2H53-146    F    Br   O    H    CF3    H      C2H53-147    H    F    O    H    CF3    CH3   C2H53-148    H    Cl   O    H    CF3    CH3   C2H53-149    H    Br   O    H    CF3    CH3   C2H53-150    F    F    O    H    CF3    CH3   C2H53-151    F    Cl   O    H    CF2    CH3   C2H5
                                表3(续)
    化合物   X    Y    Z2  R3  R1     R2     R6编号
    3-152    F    Br   O    H    CF3    CH3    C2H53-153    H    F    O    H    CF3    CH3    CH2Br3-154    H    F    O    H    CF3    CH3    CHBr23-155    H    F    O    H    CF3    CH3    CBr33-156    H    F    O    H    CF3    CH3    CHO3-157    H    F    O    H    CF3    CH3    CN3-158    H    F    O    H    CF3    CH3    COOH3-159    H    F    O    H    CF3    CH3    CH2OH3-160    H    F    O    H    CF3    CH3    CH2OCH33-161    H    F    O    H    CF3    CH3    CH2OC2H53-162    H    F    O    H    CF3    CH3    CH2OiC3H73-163    H    F    O    H    CF3    CH3    CH2OCH2OCH33-164    H    F    O    H    CF3    CH3    CH2OCH2OC2H53-165    H    F    O    H    CF3    CH3    CH2OCOCH33-166    H    F    O    H    CF3    CH3    CH2OCOC2H53-167    H    F    O    H    CF3    CH3    CH2OCOiC3H73-168    H    F    O    H    CF3    CH3    CH2OCOCH2Cl3-169    H    F    O    H    CF3    CH3    CH2OCOCCl33-170    H    F    O    H    CF3    CH3    CH2OCOCF33-171    H    F    O    H    CF3    CH3    COOCH33-172    H    F    O    H    CF3    CH3    COOC2H63-173    H    F    O    H    CF3    CH3    COOnC3H73-174    H    F    O    H    CF3    CH3    COOnC4H9
                           表3(续)
    化合物   X    Y     Z2  R3  R1     R2     R6编号
    3-175    H    F     O    H    CF3    CH3    COOnC5H113-176    H    F     O    H    CF3    CH3    COOiC3H73-177    H    F     O    H    CF3    CH3    COCH33-178    H    F     O    H    CF3    CH3    COC2H53-179    H    Cl    O    H    CF3    CH3    CH2Br3-180    H    Cl    O    H    CF3    CH3    CHBr23-181    H    Cl    O    H    CF3    CH3    CBr33-182    H    Cl    O    H    CF3    CH3    CHO3-183    H    Cl    O    H    CF3    CH3    CN3-184    H    Cl    O    H    CF3    CH3    COOH3-185    H    Cl    O    H    CF3    CH3    CH2OH3-186    H    Cl    O    H    CF3    CH3    CH2OCH33-187    H    Cl    O    H    CF3    CH3    CH2OC2H53-188    H    Cl    O    H    CF3    CH3    CH2OC3H73-189    H    Cl    O    H    CF3    CH3    CH2OCH2OCH33-190    H    Cl    O    H    CF3    CH3    CH2OCH2OC2H53-191    H    Cl    O    H    CF3    CH3    CH2OCOCH33-192    H    Cl    O    H    CF3    CH3    CH2OCOC2H53-193    H    Cl    O    H    CF3    CH3    CH2OCOiC3H73-194    H    Cl    O    H    CF3    CH3    CH2OCOCH2Cl3-195    H    Cl    O    H    CF3    CH3    CH2OCOCCl33-196    H    Cl    O    H    CF3    CH3    CH2OCOCF33-197    H    Cl    O    H    CF3    CH3    COOCH3
                            表3(续)
    化合物   X    Y     Z2  R3  R1     R2     R6编号
    3-198    H    Cl   O    H     CF3    CH3    COOC2H53-199    H    Cl   O    H     CF3    CH3    COOnC3H73-200    H    Cl   O    H     CF3    CH3    COOnC4H93-201    H    Cl   O    H     CF3    CH3    COOnC5H113-202    H    Cl   O    H     CF3    CH3    COOiC3H73-203    H    Cl   O    H     CF3    CH3    COCH33-204    H    Cl   O    H     CF3    CH3    COC2H53-205    F    F    O    H     CF3    CH3    CH2Br3-206    F    F    O    H     CF3    CH3    CHBr23-207    F    F    O    H     CF3    CH3    CBr33-208    F    F    O    H     CF3    CH3    CHO3-209    F    F    O    H     CF3    CH3    CN3-210    F    F    O    H     CF3    CH3    COOH3-211    F    F    O    H     CF3    CH3    CH2OH3-212    F    F    O    H     CF3    CH3    CH2OCH33-213    F    F    O    H     CF3    CH3    CH2OC2H53-214    F    F    O    H     CF3    CH3    CH2OiC3H73-215    F    F    O    H     CF3    CH3    CH2OCH2OCH33-216    F    F    O    H     CF3    CH3    CH2OCH2OC2H53-217    F    F    O    H     CF3    CH3    CH2OCOCH33-218    F    F    O    H     CF3    CH3    CH2OCOC2H53-219    F    F    O    H     CF3    CH3    CH2OCOiC3H7
                               表3(续)
   化合物    X    Y     Z2  R3  R1     R2     R6编号
    3-220    F    F     O    H    CF3    CH3    CH2OCOCH2Cl3-221    F    F     O    H    CF3    CH3    CH2OCOCCl33-222    F    F     O    H    CF3    CH3    CH2OCOCF33-223    F    F     O    H    CF3    CH3    COOCH33-224    F    F     O    H    CF3    CH3    COOC2H53-225    F    F     O    H    CF3    CH3    COOnC3H73-226    F    F     O    H    CF3    CH3    COOnC4H93-227    F    F     O    H    CF3    CH3    COOn-C5H113-228    F    F     O    H    CF3    CH3    COOiC3H73-229    F    F     O    H    CF3    CH3    COCH33-230    F    F     O    H    CF3    CH3    COC2H53-231    F    Cl    O    H    CF3    CH3    CH2Br3-232    F    Cl    O    H    CF3    CH3    CHBr23-233    F    Cl    O    H    CF3    CH3    CBr33-234    F    Cl    O    H    CF3    CH3    CHO3-235    F    Cl    O    H    CF3    CH3    CN3-236    F    Cl    O    H    CF3    CH3    COOH3-237    F    Cl    O    H    CF3    CH3    CH2OH3-238    F    Cl    O    H    CF3    CH3    CH2OCH33-239    F    Cl    O    H    CF3    CH3    CH2OC2H53-240    F    Cl    O    H    CF3    CH3    CH2OiC3H73-241    F    Cl    O    H    CF3    CH3    CH2OCH2OCH33-242    F    Cl    O    H    CF3    CH3    CH2OCH2OC2H5
                               表3(续)
   化合物    X    Y     Z2  R3  R1     R2     R6编号
    3-243    F    Cl    O    H    CF3    CH3    CH2OCOCH33-244    F    Cl    O    H    CF3    CH3    CH2OCOC2H53-245    F    Cl    O    H    CF3    CH3    CH2OCOiC3H73-246    F    Cl    O    H    CF3    CH3    CH2OCOCH2Cl3-247    F    Cl    O    H    CF3    CH3    CH2OCOCCl33-248    F    Cl    O    H    CF3    CH3    CH2OCOCF33-249    F    Cl    O    H    CF3    CH3    COOCH33-250    F    Cl    O    H    CF3    CH3    COOC2 -H53-251    F    Cl    O    H    CF3    CH3    COOnC3H73-252    F    Cl    O    H    CF3    CH3    COOnC4H93-253    F    Cl    O    H    CF3    CH3    COOnC5H113-254    F    Cl    O    H    CF3    CH3    COOiC3H73-255    F    Cl    O    H    CF3    CH3    COCH33-256    F    Cl    O    H    CF3    CH3    COC2H53-257    H    F     O    H    CF2Cl  H       CH2Br3-258    H    F     O    H    CF2Cl  H       CHBr23-259    H    F     O    H    CF2Cl  H       CBr33-260    H    F     O    H    CF2Cl  H       CHO3-261    H    F     O    H    CF2Cl  H       CN3-262    H    F     O    H    CF2Cl  H       COOH3-263    H    F     O    H    CF2Cl  H       CH2OH3-264    H    F     O    H    CF2Cl  H       CH2OCH33-265    H    F     O    H    CF2Cl  H       CH2OC2H5
                      表3(续)
   化合物    X    Y    Z2 R3 R1     R2  R6编号
    3-266    H    F    O    H  CF2Cl  H    CH2OiC3H73-267    H    F    O    H  CF2Cl  H    CH2OCH2OCH33-268    H    F    O    H  CF2Cl  H    CH2OCH2OC2H53-269    H    F    O    H  CF2Cl  H    CH2OCOCH33-270    H    F    O    H  CF2Cl  H    CH2OCOC2H53-271    H    F    O    H  CF2Cl  H    CH2OCOiC3H73-272    H    F    O    H  CF2Cl  H    CH2OCOCH2Cl3-273    H    F    O    H  CF2Cl  H    CH2OCOCCl33-274    H    F    O    H  CF2Cl  H    CH2OCOCF33-275    H    F    O    H  CF2Cl  H    COOCH33-276    H    F    O    H  CF2Cl  H    COOC2H53-277    H    F    O    H  CF2Cl  H    COOnC3H73-278    H    F    O    H  CF2Cl  H    COOnC4H93-279    H    F    O    H  CF2Cl  H    COOnC5H113-280    H    F    O    H  CF2Cl  H    COOiC3H73-281    H    F    O    H  CF2Cl  H    COCH33-282    H    F    O    H  CF2Cl  H    COC2H53-283    H    Cl   O    H  CF2Cl  H    CH2Br3-284    H    Cl   O    H  CF2Cl  H    CHBr23-285    H    Cl   O    H  CF2Cl  H    CBr33-286    H    Cl   O    H  CF2Cl  H    CHO3-287    H    Cl   O    H  CF2Cl  H    CN3-288    H    Cl   O    H  CF2Cl  H    COOH
                            表3(续)
   化合物    X    Y     Z2  R3R1     R2  R6编号
    3-289    H    Cl    O    H  CF2Cl  H    CH2OH3-290    H    Cl    O    H  CF2Cl  H    CH2OCH33-291    H    Cl    O    H  CF2Cl  H    CH2OC2H53-292    H    Cl    O    H  CF2Cl  H    CH2OiC3H73-293    H    Cl    O    H  CF2Cl  H    CH2OCH2OCH33-294    H    Cl    O    H  CF2Cl  H    CH2OCH2OC2H53-295    H    Cl    O    H  CF2Cl  H    CH2OCOCH33-296    H    Cl    O    H  CF2Cl  H    CH2OCOC2H53-297    H    Cl    O    H  CF2Cl  H    CH2OCOiC3H73-298    H    Cl    O    H  CF2Cl  H    CH2OCOCH2Cl3-299    H    Cl    O    H  CF2Cl  H    CH2OCOCCl33-300    H    Cl    O    H  CF2Cl  H    CH2OCOCF33-301    H    Cl    O    H  CF2Cl  H    COOCH33-302    H    Cl    O    H  CF2Cl  H    COOC2H53-303    H    Cl    O    H  CF2Cl  H    COOnC3H73-304    H    Cl    O    H  CF2Cl  H    COOnC4H93-305    H    Cl    O    H  CF2Cl  H    COOnC5H113-306    H    Cl    O    H  CF2Cl  H    COOiC3H73-307    H    Cl    O    H  CF2Cl  H    COCH33-308    H    Cl    O    H  CF2Cl  H    COC2H53-309    F    F     O    H  CF2Cl  H    CH2Br3-310    F    F     O    H  CF2Cl  H    CHBr23-311    F    F     O    H  CF2Cl  H    CBr3
                          表3(续)
   化合物    X    Y    Z2  R3R1     R2  R6编号
    3-312    F    F    O    H  CF2Cl  H    CHO3-313    F    F    O    H  CF2Cl  H    CN3-314    F    F    O    H  CF2Cl  H    COOH3-315    F    F    O    H  CF2Cl  H    CH2OH3-316    F    F    O    H  CF2Cl  H    CH2OCH33-317    F    F    O    H  CF2Cl  H    CH2OC2H53-318    F    F    O    H  CF2Cl  H    CH2OiC3H73-319    F    F    O    H  CF2Cl  H    CH2OCH2OCH33-320    F    F    O    H  CF2Cl  H    CH2OCH2OC2H53-321    F    F    O    H  CF2Cl  H    CH2OCOCH33-322    F    F    O    H  CF2Cl  H    CH2OCOC2H53-323    F    F    O    H  CF2Cl  H    CH2OCOiC3H73-324    F    F    O    H  CF2Cl  H    CH2OCOCH2Cl3-325    F    F    O    H  CF2Cl  H    CH2OCOCCl33-326    F    F    O    H  CF2Cl  H    CH2OCOCF33-327    F    F    O    H  CF2Cl  H    COOCH33-328    F    F    O    H  CF2Cl  H    COOC2H53-329    F    F    O    H  CF2Cl  H    COOnC3H73-330    F    F    O    H  CF2Cl  H    COOnC4H93-331    F    F    O    H  CF2Cl  H    COOnC5H113-332    F    F    O    H  CF2Cl  H    COOiC3H73-333    F    F    O    H  CF2Cl  H    COCH3
                         表3(续)
   化合物    X    Y     Z2  R3R1     R2   R6编号
    3-334    F    F     O    H  CF2Cl  H    COC2H53-335    F    Cl    O    H  CF2Cl  H    CH2Br3-336    F    Cl    O    H  CF2Cl  H    CHBr23-337    F    Cl    O    H  CF2Cl  H    CBr33-338    F    Cl    O    H  CF2Cl  H    CHO3-339    F    Cl    O    H  CF2Cl  H    CN3-340    F    Cl    O    H  CF2Cl  H    COOH3-341    F    Cl    O    H  CF2Cl  H    CH2 -OH3-342    F    Cl    O    H  CF2Cl  H    CH2OCH33-343    F    Cl    O    H  CF2Cl  H    CH2OC2H53-344    F    Cl    O    H  CF2Cl  H    CH2OiC3H73-345    F    Cl    O    H  CF2Cl  H    CH2OCH2OCH33-346    F    Cl    O    H  CF2Cl  H    CH2OCH2OC2H53-347    F    Cl    O    H  CF2Cl  H    CH2OCOCH33-348    F    Cl    O    H  CF2Cl  H    CH2OCOC2H53-349    F    Cl    O    H  CF2Cl  H    CH2OCOiC3H73-350    F    Cl    O    H  CF2Cl  H    CH2OCOCH2Cl3-351    F    Cl    O    H  CF2Cl  H    CH2OCOCCl33-352    F    Cl    O    H  CF2Cl  H    CH2OCOCF33-353    F    Cl    O    H  CF2Cl  H    COOCH33-354    F    Cl    O    H  CF2Cl  H    COOC2H53-355    F    Cl    O    H  CF2Cl  H    COOnC3H73-356    F    Cl    O    H  CF2Cl  H    COOnC4H9
                           表3(续)
   化合物    X    Y     Z2  R3  R1     R2   R6编号
    3-357    F    Cl    O    H    CF2Cl  H    COOnC5H113-358    F    Cl    O    H    CF2Cl  H    COOiC3H73-359    F    Cl    O    H    CF2Cl  H    COCH33-360    F    Cl    O    H    CF2Cl  H    COC2H53-361    F    Br    O    H    CF3    H    C2H53-362    H    F     O    H    CF3    H    CH2Br3-363    H    F     O    H    CF3    H    CHBr23-364    H    F     O    H    CF3    H    CBr33-365    H    F     O    H    CF3    H    CHO3-366    H    F     O    H    CF3    H    CN3-367    H    F     O    H    CF3    H    COOH3-368    H    F     O    H    CF3    H    CH2OH3-369    H    F     O    H    CF3    H    CH2OCH33-370    H    F     O    H    CF3    H    CH2OC2H53-371    H    F     O    H    CF3    H    CH2OC3H73-372    H    F     O    H    CF3    H    CH2OCH2OCH33-373    H    F     O    H    CF3    H    CH2OCH2OC2H53-374    H    F     O    H    CF3    H    CH2OCOCH33-375    H    F     O    H    CF3    H    CH2OCOC2H53-376    H    F     O    H    CF3    H    CH2OCOiC3H73-377    H    F     O    H    CF3    H    CH2OCOCH2Cl3-378    H    F     O    H    CF3    H    CH2OCOCCl33-379    H    F     O    H    CF3    H    CH2OCOCF3
                             表3(续)
   化合物    X    Y    Z2  R3  R1   R2  R6编号
    3-380    H    F    O    H    CF3  H    COOCH33-381    H    F    O    H    CF3  H    COOC2H53-382    H    F    O    H    CF3  H    COOnC3H73-383    H    F    O    H    CF3  H    COOnC4H93-384    H    F    O    H    CF3  H    COOnC5H113-385    H    F    O    H    CF3  H    COOiC3H73-386    H    F    O    H    CF3  H    COCH33-387    H    F    O    H    CF3  H    COC2 -H53-388    H    Cl   O    H    CF3  H    CH2Br3-389    H    Cl   O    H    CF3  H    CHBr23-390    H    Cl   O    H    CF3  H    CBr33-391    H    Cl   O    H    CF3  H    CHO3-392    H    Cl   O    H    CF3  H    CN3-393    H    Cl   O    H    CF3  H    COOH3-394    H    Cl   O    H    CF3  H    CH2OH3-395    H    Cl   O    H    CF3  H    CH2OCH33-396    H    Cl   O    H    CF3  H    CH2OC2H53-397    H    Cl   O    H    CF3  H    CH2OiC3H73-398    H    Cl   O    H    CF3  H    CH2OCH2OCH33-399    H    Cl   O    H    CF3  H    CH2OCH2OC2H53-400    H    Cl   O    H    CF3  H    CH2OCOCH33-401    H    Cl   O    H    CF3  H    CH2OCOC2H53-402    H    Cl   O    H    CF3  H    CH2OCOiC3H7
                                表3(续)
   化合物    X    Y     Z2  R3  R1     R2  R6编号
    3-403    H    Cl    O    H    CF3    H    CH2OCOCH2Cl3-404    H    Cl    O    H    CF3    H    CH2OCOCCl33-405    H    Cl    O    H    CF3    H    CH2OCOCF33-406    H    Cl    O    H    CF3    H    COOCH33-407    H    Cl    O    H    CF3    H    COOC2H53-408    H    Cl    O    H    CF3    H    COOnC3H73-409    H    Cl    O    H    CF3    H    COOnC4H93-410    H    Cl    O    H    CF3    H    COOn-C5H113-411    H    Cl    O    H    CF3    H    COOiC3H73-412    H    Cl    O    H    CF3    H    COCH33-413    H    Cl    O    H    CF3    H    COC2H53-414    F    F     O    H    CF3    H    CH2Br3-415    F    F     O    H    CF3    H    CHBr23-416    F    F     O    H    CF3    H    CBr33-417    F    F     O    H    CF3    H    CHO3-418    F    F     O    H    CF3    H    CN3-419    F    F     O    H    CF3    H    COOH3-420    F    F     O    H    CF3    H    CH2OH3-421    F    F     O    H    CF3    H    CH2OCH33-422    F    F     O    H    CF3    H    CH2OC2H53-423    F    F     O    H    CF3    H    CH2OiC3H73-424    F    F     O    H    CF3    H    CH2OCH2OCH33-425    F    F     O    H    CF3    H    CH2OCH2OC2H6
                                表3(续)
   化合物    X    Y     Z2   R3  R1     R2  R6编号
    3-426    F    F     O     H    CF3    H    CH2OCOCH33-427    F    F     O     H    CF3    H    CH2OCOC2H53-428    F    F     O     H    CF3    H    CH2OCOiC3H73-429    F    F     O     H    CF3    H    CH2OCOCH2Cl3-430    F    F     O     H    CF3    H    CH2OCOCCl33-431    F    F     O     H    CF3    H    CH2OCOCF33-432    F    F     O     H    CF3    H    COOCH33-433    F    F     O     H    CF3    H    COOC2 -H53-434    F    F     O     H    CF3    H    COOnC3H73-435    F    F     O     H    CF3    H    COOnC4H93-436    F    F     O     H    CF3    H    COOnC5H113-437    F    F     O     H    CF3    H    COOiC3H73-438    F    F     O     H    CF3    H    COCH33-439    F    F     O     H    CF3    H    COC2H53-440    F    Cl    O     H    CF3    H    CH2Br3-441    F    Cl    O     H    CF3    H    CHBr23-442    F    Cl    O     H    CF3    H    CBr33-443    F    Cl    O     H    CF3    H    CHO3-444    F    Cl    O     H    CF3    H    CN3-445    F    Cl    O     H    CF3    H    COOH3-446    F    Cl    O     H    CF3    H    CH2OH
                              表3(续)
   化合物    X    Y     Z2  R3    R1    R2   R6编号
    3-447    F    Cl    O    H      CF3    H    CH2OCH33-448    F    Cl    O    H      CF3    H    CH2OC2H53-449    F    Cl    O    H      CF3    H    CH2OiC3H73-450    F    Cl    O    H      CF3    H    CH2OCH2OCH33-451    F    Cl    O    H      CF3    H    CH2OCH2OC2H53-452    F    Cl    O    H      CF3    H    CH2OCOCH33-453    F    Cl    O    H      CF3    H    CH2OCOC2H53-454    F    Cl    O    H      CF3    H    CH2OCO-iC3H73-455    F    Cl    O    H      CF3    H    CH2OCOCH2Cl3-456    F    Cl    O    H      CF3    H    CH2OCOCCl33-457    F    Cl    O    H      CF3    H    CH2OCOCF33-458    F    Cl    O    H      CF3    H    COOCH33-459    F    Cl    O    H      CF3    H    COOC2H53-460    F    Cl    O    H      CF3    H    COOnC3H73-461    F    Cl    O    H      CF3    H    COOnC4H93-462    F    Cl    O    H      CF3    H    COOnC5H113-463    F    Cl    O    H      CF3    H    COOiC3H73-464    F    Cl    O    H      CF3    H    COCH33-465    F    Cl    O    H      CF3    H    COC2H53-466    H    F     O    CH3   CF3    H    CH33-467    H    Cl    O    CH3   CF3    H    CH33-468    H    Br    O    CH3   CF3    H    CH33-469    F    F     O    CH3   CF3    H    CH3
                              表3(续)
   化合物    X    Y     Z2   R3    R1     R2  R6编号
    3-470    F    Cl    O    CH3    CF3    H    CH33-471    F    Br    O    CH3    CF3    H    CH33-472    H    F     O    CH3    CF3    H    C2H53-473    H    Cl    O    CH3    CF3    H    C2H53-474    H    Br    O    CH3    CF3    H    C2H53-475    F    F     O    CH3    CF3    H    C2H53-476    F    Cl    O    CH3    CF3    H    C2H53-477    F    Br    O    CH3    CF3    H    C2H53-478    F    Br    O    CH3    CF3    H    C2H53-479    H    F     O    CH3    CF3    H    CH2Br3-480    H    F     O    CH3    CF3    H    CHBr23-481    H    F     O    CH3    CF3    H    CBr33-482    H    F     O    CH3    CF3    H    CHO3-483    H    F     O    CH3    CF3    H    CN3-484    H    F     O    CH3    CF3    H    COOH3-485    H    F     O    CH3    CF3    H    CH2OH3-486    H    F     O    CH3    CF3    H    CH2OCH33-487    H    F     O    CH3    CF3    H    CH2OC2H53-488    H    F     O    CH3    CF3    H    CH2OiC3H73-489    H    F     O    CH3    CF3    H    CH2OCH2OCH33-490    H    F     O    CH3    CF3    H    CH2OCH2OC2H63-491    H    F     O    CH3    CF3    H    CH2OCOCH33-492    H    F     O    CH3    CF3    H    CH2OCOC2H5
                                 表3(续)
   化合物    X    Y     Z2   R3    R1     R2  R6编号
    3-493    H    F     O    CH3    CF3    H    CH2OCOiC3H73-494    H    F     O    CH3    CF3    H    CH2OCOCH2Cl3-495    H    F     O    CH3    CF3    H    CH2OCOCCl33-496    H    F     O    CH3    CF3    H    CH2OCOCF33-497    H    F     O    CH3    CF3    H    COOCH33-498    H    F     O    CH3    CF3    H    COOC2H53-499    H    F     O    CH3    CF3    H    COOnC3H73-500    H    F     O    CH3    CF3    H    COOn-C4H93-501    H    F     O    CH3    CF3    H    COOnC5H113-502    H    F     O    CH3    CF3    H    COOiC3H73-503    H    F     O    CH3    CF3    H    COCH33-504    H    F     O    CH3    CF3    H    COC2H53-505    H    Cl    O    CH3    CF3    H    CH2Br3-506    H    Cl    O    CH3    CF3    H    CHBr23-507    H    Cl    O    CH3    CF3    H    CBr33-508    H    Cl    O    CH3    CF3    H    CHO3-509    H    Cl    O    CH3    CF3    H    CN3-510    H    Cl    O    CH3    CF3    H    COOH3-511    H    Cl    O    CH3    CF3    H    CH2OH3-512    H    Cl    O    CH3    CF3    H    CH2OCH33-513    H    Cl    O    CH3    CF3    H    CH2OC2H63-514    H    Cl    O    CH3    CF3    H    CH2OiC3H73-515    H    Cl    O    CH3    CF3    H    CH2OCH2OCH8
                               表3(续)
   化合物    X    Y     Z2  R3     R1     R2  R6编号
    3-516    H    Cl    O    CH3    CF3    H    CH2OCH2OC2H53-517    H    Cl    O    CH3    CF3    H    CH2OCOCH33-518    H    Cl    O    CH3    CF3    H    CH2OCOC2H53-519    H    Cl    O    CH3    CF3    H    CH2OCOiC3H73-520    H    Cl    O    CH3    CF3    H    CH2OCOCH2Cl3-521    H    Cl    O    CH3    CF3    H    CH2OCOCCl33-522    H    Cl    O    CH3    CF3    H    CH2OCOCF33-523    H    Cl    O    CH3    CF3    H    COOCH33-524    H    Cl    O    CH3    CF3    H    COOC2H53-525    H    Cl    O    CH3    CF3    H    COOnC3H73-526    H    Cl    O    CH3    CF3    H    COOnC4H93-527    H    Cl    O    CH3    CF3    H    COOnC5H113-528    H    Cl    O    CH3    CF3    H    COOiC3H73-529    H    Cl    O    CH3    CF3    H    COCH33-530    H    Cl    O    CH3    CF3    H    COC2H53-531    F    F     O    CH3    CF3    H    CH2Br3-532    F    F     O    CH3    CF3    H    CHBr23-533    F    F     O    CH3    CF3    H    CBr33-534    F    F     O    CH3    CF3    H    CHO3-535    F    F     O    CH3    CF3    H    CN3-536    F    F     O    CH3    CF3    H    COOH3-537    F    F     O    CH3    CF3    H    CH2OH3-538    F    F     O    CH3    CF3    H    CH2OCH3
                                    表3(续)
   化合物    X    Y     Z2  R3     R1     R2  R6编号
    3-539    F    F     O    CH3    CF3    H    CH2OC2H53-540    F    F     O    CH3    CF3    H    CH2OiC3H73-541    F    F     O    CH3    CF3    H    CH2OCH2OCH33-542    F    F     O    CH3    CF3    H    CH2OCH2OC2H53-543    F    F     O    CH3    CF3    H    CH2OCOCH33-544    F    F     O    CH3    CF3    H    CH2OCOC2H53-545    F    F     O    CH3    CF3    H    CH2OCOiC3H73-546    F    F     O    CH3    CF3    H    CH2OCOCH2Cl3-547    F    F     O    CH3    CF3    H    CH2OCOCCl33-548    F    F     O    CH3    CF3    H    CH2OCOCF33-549    F    F     O    CH3    CF3    H    COOCH33-550    F    F     O    CH3    CF3    H    COOC2H53-551    F    F     O    CH3    CF3    H    COOnC3H73-552    F    F     O    CH3    CF3    H    COOnC4H93-553    F    F     O    CH3    CF3    H    COOnC5H113-554    F    F     O    CH3    CF3    H    COOiC3H73-555    F    F     O    CH3    CF3    H    COCH33-556    F    F     O    CH3    CF3    H    COC2H53-557    F    Cl    O    CH3    CF3    H    CH2Br3-558    F    Cl    O    CH3    CF3    H    CHBr23-559    F    Cl    O    CH3    CF3    H    CBr33-560    F    Cl    O    CH3    CF3    H    CHO
                          表3(续)
   化合物    X    Y     Z2  R3     R1     R2  R6编号
    3-561    F    Cl    O    CH3    CF3    H    CN3-562    F    Cl    O    CH3    CF3    H    COOH3-563    F    Cl    O    CH3    CF3    H    CH2OH3-564    F    Cl    O    CH3    CF3    H    CH2OCH33-565    F    Cl    O    CH3    CF3    H    CH2OC2H53-566    F    Cl    O    CH3    CF3    H    CH2OiC3H73-567    F    Cl    O    CH3    CF3    H    CH2OCH2OCH33-568    F    Cl    O    CH3    CF3    H    CH2OCH2OC2H53-569    F    Cl    O    CH3    CF3    H    CH2OCOCH33-570    F    Cl    O    CH3    CF3    H    CH2OCOC2H53-571    F    Cl    O    CH3    CF3    H    CH2OCOiC3H73-572    F    Cl    O    CH3    CF3    H    CH2OCOCH2Cl3-573    F    Cl    O    CH3    CF3    H    CH2OCOCCl33-574    F    Cl    O    CH3    CF3    H    CH2OCOCF33-575    F    Cl    O    CH3    CF3    H    COOCH33-576    F    Cl    O    CH3    CF3    H    COOC2H63-577    F    Cl    O    CH3    CF3    H    COOnC3H73-578    F    Cl    O    CH3    CF3    H    COOnC4H93-579    F    Cl    O    CH3    CF3    H    COOnC5H113-580    F    Cl    O    CH3    CF3    H    COOiC3H73-581    F    Cl    O    CH3    CF3    H    COCH33-582    F    Cl    O    CH3    CF3    H    COC2H6
                          表4
下式化合物:
 化合物   X  Y   R3 R1      R2     R7  R8编号
  4-1     H  Cl  H  CF2Cl    CH3    H    CH2Cl4-2     H  Cl  H  CF2Cl    CH3    H    CH2Br4-3     H  Cl  H  CF2Cl    CH3    H    CH2OCH34-4     H  Cl  H  CF2Cl    CH3    H    CH2OC2H54-5     H  Cl  H  CF2Cl    CH3    H    CH2OCH2OCH34-6     H  Cl  H  CF2Cl    CH3    H    CH2OCH2OC2H54-7     H  Cl  H  CF2Cl    CH3    H    CH2OCOCH34-8     H  Cl  H  CF2Cl    CH3    H    CH2OCOC2H54-9     H  Cl  H  CF2Cl    CH3    H    CH2OCOiC3H74-10    H  Cl  H  CF2Cl    CH3    H    CH2OCOCH2Cl4-11    H  Cl  H  CF2Cl    CH3    H    CH2OCOCCl34-12    H  Cl  H  CF2Cl    CH3    H    CH2OCOCF34-13    H  Cl  H  CF2Cl    CH3    H    COOH4-14    H  Cl  H  CF2Cl    CH3    H    COOCH34-15    H  Cl  H  CF2Cl    CH3    H    COOC2H5
                              表4(续)
 化合物   X  Y   R3 R1      R2     R7  R8编号
  4-16    H  Cl  H  CF2Cl    CH3    H    COOnC3H74-17    H  Cl  H  CF2Cl    CH3    H    COOnC4H94-18    H  Cl  H  CF2Cl    CH3    H    COOnC5H114-19    H  Cl  H  CF2Cl    CH3    H    COOiC3H74-20    H  Cl  H  CF2Cl    CH3    H    COOcC5H94-21    H  Cl  H  CF2Cl    CH3    H    COOcC6H114-22    H  Cl  H  CF2Cl    CH3    H    COOCH2CH=CH24-23    H  Cl  H  CF2Cl    CH3    H    COOCH2 -C≡CH4-24    H  Cl  H  CF2Cl    CH3    H    CONH24-25    H  Cl  H  CF2Cl    CH3    H    CONHCH34-26    H  Cl  H  CF2Cl    CH3    H    CONHC2H54-27    H  Cl  H  CF2Cl    CH3    H    CON(CH3)24-28    H  Cl  H  CF2Cl    CH3    H    CON(C2H5)24-29    F  Cl  H  CF2Cl    CH3    H    CH2Cl4-30    F  Cl  H  CF2Cl    CH3    H    CH2Br4-31    F  Cl  H  CF2Cl    CH3    H    CH2OCH34-32    F  Cl  H  CF2Cl    CH3    H    CH2OC2H54-33    F  Cl  H  CF2Cl    CH3    H    CH2OCH2OCH34-34    F  Cl  H  CF2Cl    CH3    H    CH2OCH2OC2H54-35    F  Cl  H  CF2Cl    CH3    H    CH2OCOCH34-36    F  Cl  H  CF2Cl    CH3    H    CH2OCOC2H54-37    F  Cl  H  CF2Cl    CH3    H    CH2OCOiC3H74-38    F  Cl  H  CF2Cl    CH3    H    CH2OCOCH2Cl
                         表4(续)
   化合物   X  Y   R3 R1      R2     R7  R8编号
    4-39    F  Cl  H  CF2Cl    CH3    H    CH2OCOCCl34-40    F  Cl  H  CF2Cl    CH3    H    CH2OCOCF34-41    F  Cl  H  CF2Cl    CH3    H    COOH4-42    F  Cl  H  CF2Cl    CH3    H    COOCH34-43    F  Cl  H  CF2Cl    CH3    H    COOC2H54-44    F  Cl  H  CF2Cl    CH3    H    COOnC3H74-45    F  Cl  H  CF2Cl    CH3    H    COOnC4H94-46    F  Cl  H  CF2Cl    CH3    H    COOnC5H114-47    F  Cl  H  CF2Cl    CH3    H    COOiC3H74-48    F  Cl  H  CF2Cl    CH3    H    COOcC5H94-49    F  Cl  H  CF2Cl    CH3    H    COOcC6H114-50    F  Cl  H  CF2Cl    CH3    H    COOCH2CH=CH24-51    F  Cl  H  CF2Cl    CH3    H    COOCH2C≡CH4-52    F  Cl  H  CF2Cl    CH3    H    CONH24-53    F  Cl  H  CF2Cl    CH3    H    CONHCH34-54    F  Cl  H  CF2Cl    CH3    H    CONHC2H54-55    F  Cl  H  CF2Cl    CH3    H    CON(CH3)24-56    F  Cl  H  CF2Cl    CH3    H    CON(C2H5)24-57    H  Cl  H  CF2Cl    CH3    CH3 CH2Cl4-58    H  Cl  H  CF2Cl    CH3    CH3 CH2Br4-59    H  Cl  H  CF2Cl    CH3    CH3 CH2OCH34-60    H  Cl  H  CF2Cl    CH3    CH3 CH2OC2H54-61    H  Cl  H  CF2Cl    CH3    CH3 CH2OCH2OCH3
                             表4(续)
   化合物   X  Y   R3 R1      R2     R7     R8编号
    4-62    H  Cl  H  CF2Cl    CH3    CH3    CH2OCH2OC2H54-63    H  Cl  H  CF2Cl    CH3    CH3    CH2OCOCH34-64    H  Cl  H  CF2Cl    CH3    CH3    CH2OCOC2H54-65    H  Cl  H  CF2Cl    CH3    CH3    CH2OCOiC3H74-66    H  Cl  H  CF2Cl    CH3    CH3    CH2OCOCH2Cl4-67    H  Cl  H  CF2Cl    CH3    CH3    CH2OCOCCl34-68    H  Cl  H  CF2Cl    CH3    CH3    CH2OCOCF34-69    H  Cl  H  CF2Cl    CH3    CH3    COOH-4-70    H  Cl  H  CF2Cl    CH3    CH3    COOCH34-71    H  Cl  H  CF2Cl    CH3    CH3    COOC2H54-72    H  Cl  H  CF2Cl    CH3    CH3    COOnC3H74-73    H  Cl  H  CF2Cl    CH3    CH3    COOnC4H94-74    H  Cl  H  CF2Cl    CH3    CH3    COOnC5H114-75    H  Cl  H  CF2Cl    CH3    CH3    COOiC3H74-76    H  Cl  H  CF2Cl    CH3    CH3    COOcC5H94-77    H  Cl  H  CF2Cl    CH3    CH3    COOcC6H114-78    H  Cl  H  CF2Cl    CH3    CH3    COOCH2CH=CH24-79    H  Cl  H  CF2Cl    CH3    CH3    COOCH2C≡CH4-80    H  Cl  H  CF2Cl    CH3    CH3    CONH24-81    H  Cl  H  CF2Cl    CH3    CH3    CONHCH34-82    H  Cl  H  CF2Cl    CH3    CH3    CONHC2H54-83    H  Cl  H  CF2Cl    CH3    CH3    CON(CH3)24-84    H  Cl  H  CF2Cl    CH3    CH3    CON(C2H6)2
                           表4(续)
   化合物    X  Y   R3 R1      R2     R7     R8编号
    4-85     F  Cl  H  CF2Cl    CH3    CH3    CH2Cl4-86     F  Cl  H  CF2Cl    CH3    CH3    CH2Br4-87     F  Cl  H  CF2Cl    CH3    CH3    CH2OCH34-88     F  Cl  H  CF2Cl    CH3    CH3    CH2OC2H54-89     F  Cl  H  CF2Cl    CH3    CH3    CH2OCH2OCH34-90     F  Cl  H  CF2Cl    CH3    CH3    CH2OCH2OC2H54-91     F  Cl  H  CF2Cl    CH3    CH3    CH2OCOCH34-92     F  Cl  H  CF2Cl    CH3    CH3    CH2OCOC2H54-93     F  Cl  H  CF2Cl    CH3    CH3    CH2OCOiC3H74-94     F  Cl  H  CF2Cl    CH3    CH3    CH2OCOCH2Cl4-95     F  Cl  H  CF2Cl    CH3    CH3    CH2OCOCCl34-96     F  Cl  H  CF2Cl    CH3    CH3    CH2OCOCF34-97     F  Cl  H  CF2Cl    CH3    CH3    COOH4-98     F  Cl  H  CF2Cl    CH3    CH3    COOCH34-99     F  Cl  H  CF2Cl    CH3    CH3    COOC2H54-100    F  Cl  H  CF2Cl    CH3    CH3    COOnC3H74-101    F  Cl  H  CF2Cl    CH3    CH3    COOnC4H94-102    F  Cl  H  CF2Cl    CH3    CH3    COOnC5H114-103    F  Cl  H  CF2Cl    CH3    CH3    COOiC3H74-104    F  Cl  H  CF2Cl    CH3    CH3    COOcC5H94-105    F  Cl  H  CF2Cl    CH3    CH3    COOcC6H114-106    F  Cl  H  CF2Cl    CH3    CH3    COOCH2CH=CH2
                                 表4(续)
   化合物    X  Y   R3   R1      R2     R7    R8编号
    4-107    F  Cl  H    CF2Cl    CH3    CH3   COOCH2C≡CH4-108    F  Cl  H    CF2Cl    CH3    CH3   CONH24-109    F  Cl  H    CF2Cl    CH3    CH3   CONHCH34-110    F  Cl  H    CF2Cl    CH3    CH3   CONHC2H54-111    F  Cl  H    CF2Cl    CH3    CH3   CON(CH3)24-112    F  Cl  H    CF2Cl    CH3    CH3   CON(C2H5)24-113    H  Cl  H    CF3      CH3    H      CH2Cl4-114    H  Cl  H    CF3      CH3    H      CH2Br4-115    H  Cl  H    CF3      CH3    H      CH2OCH34-116    H  Cl  H    CF3      CH3    H      CH2OC2H54-117    H  Cl  H    CF3      CH3    H      CH2OCH2OCH34-118    H  Cl  H    CF3      CH3    H      CH2OCH2OC2H54-119    H  Cl  H    CF3      CH3    H      CH2OCOCH34-120    H  Cl  H    CF3      CH3    H      CH2OCOC2H54-121    H  Cl  H    CF3      CH3    H      CH2OCOiC3H74-122    H  Cl  H    CF3      CH3    H      CH2OCOCH2Cl4-123    H  Cl  H    CF3      CH3    H      CH2OCOCCl34-124    H  Cl  H    CF3      CH3    H      CH2OCOCF34-125    H  Cl  H    CF3      CH3    H      COOH4-126    H  Cl  H    CF3      CH3    H      COOCH34-127    H  Cl  H    CF3      CH3    H      COOC2H54-128    H  Cl  H    CF3      CH3    H      COOnC3H74-129    H  Cl  H    CF3      CH3    H      COOnC4H9
                           表4(续)
   化合物    X  Y   R3   R1    R2     R7  R8编号
    4-130    H  Cl  H    CF3    CH3    H    COOnC5H114-131    H  Cl  H    CF3    CH3    H    COOiC3H74-132    H  Cl  H    CF3    CH3    H    COOcC5H94-133    H  Cl  H    CF3    CH3    H    COOcC6H114-134    H  Cl  H    CF3    CH3    H    COOCH2CH=CH24-135    H  Cl  H    CF3    CH3    H    COOCH2C≡CH4-136    H  Cl  H    CF3    CH3    H    CONH24-137    H  Cl  H    CF3    CH3    H    CONHCH34-138    H  Cl  H    CF3    CH3    H    CONHC2H54-139    H  Cl  H    CF3    CH3    H    CON(CH3)24-140    H  Cl  H    CF3    CH3    H    CON(C2H5)24-141    F  Cl  H    CF3    CH3    H    CH2Cl4-142    F  Cl  H    CF3    CH3    H    CH2Br4-143    F  Cl  H    CF3    CH3    H    CH2OCH34-144    F  Cl  H    CF3    CH3    H    CH2OC2H54-145    F  Cl  H    CF3    CH3    H    CH2OCH2OCH34-146    F  Cl  H    CF3    CH3    H    CH2OCH2OC2H54-147    F  Cl  H    CF3    CH3    H    CH2OCOCH34-148    F  Cl  H    CF3    CH3    H    CH2OCOC2H54-149    F  Cl  H    CF3    CH3    H    CH2OCOiC3H74-150    F  Cl  H    CF3    CH3    H    CH2OCOCH2Cl4-151    F  Cl  H    CF3    CH3    H    CH2OCOCCl34-152    F  Cl  H    CF3    CH3    H    CH2OCOCF3
                          表4(续)
    化合物   X  Y   R3  R1     R2    R7   R8编号
    4-153    F  Cl  H    CF3    CH3    H    COOH4-154    F  Cl  H    CF3    CH3    H    COOCH34-155    F  Cl  H    CF3    CH3    H    COOC2H54-156    F  Cl  H    CF3    CH3    H    COOnC3H74-157    F  Cl  H    CF3    CH3    H    COOnC4H94-158    F  Cl  H    CF3    CH3    H    COOnC5H114-159    F  Cl  H    CF3    CH3    H    COOiC3H74-160    F  Cl  H    CF3    CH3    H    COOc-C5H94-161    F  Cl  H    CF3    CH3    H    COOcC6H114-162    F  Cl  H    CF3    CH3    H    COOCH2CH=CH24-163    F  Cl  H    CF3    CH3    H    COOCH2C≡CH4-164    F  Cl  H    CF3    CH3    H    CONH24-165    F  Cl  H    CF3    CH3    H    CONHCH34-166    F  Cl  H    CF3    CH3    H    CONHC2H54-167    F  Cl  H    CF3    CH3    H    CON(CH3)24-168    F  Cl  H    CF3    CH3    H    CON(C2H5)24-169    H  Cl  H    CF3    CH3    CH3 CH2Cl4-170    H  Cl  H    CF3    CH3    CH3 CH2Br4-171    H  Cl  H    CF3    CH3    CH3 CH2OCH34-172    H  Cl  H    CF3    CH3    CH3 CH2OC2H54-173    H  Cl  H    CF3    CH3    CH3 CH2OCH2OCH34-174    H  Cl  H    CF3    CH3    CH3 CH2OCH2OC2H64-175    H  Cl  H    CF3    CH3    CH3 CH2OCOCH3
                        表4(续)
    化合物   X  Y   R3  R1     R2     R7     R8编号
    4-176    H  Cl  H    CF3    CH3    CH3    CH2OCOC2H54-177    H  Cl  H    CF3    CH3    CH3    CH2OCOiC3H74-178    H  Cl  H    CF3    CH3    CH3    CH2OCOCH2Cl4-179    H  Cl  H    CF3    CH3    CH3    CH2OCOCCl34-180    H  Cl  H    CF3    CH3    CH3    CH2OCOCF34-181    H  Cl  H    CF3    CH3    CH3    COOH4-182    H  Cl  H    CF3    CH3    CH3    COOCH34-183    H  Cl  H    CF3    CH3    CH3    COOC2 -H54-184    H  Cl  H    CF3    CH3    CH3    COOnC3H74-185    H  Cl  H    CF3    CH3    CH3    COOnC4H94-186    H  Cl  H    CF3    CH3    CH3    COOnC5H114-187    H  Cl  H    CF3    CH3    CH3    COOiC3H74-188    H  Cl  H    CF3    CH3    CH3    COOcC5H94-189    H  Cl  H    CF3    CH3    CH3    COOcC6H114-190    H  Cl  H    CF3    CH3    CH3    COOCH2CH=CH24-191    H  Cl  H    CF3    CH3    CH3    COOCH2C≡CH4-192    H  Cl  H    CF3    CH3    CH3    CONH24-193    H  Cl  H    CF3    CH3    CH3    CONHCH34-194    H  Cl  H    CF3    CH3    CH3    CONHC2H54-195    H  Cl  H    CF3    CH3    CH3    CON(CH3)24-196    H  Cl  H    CF3    CH3    CH3    CON(C2H5)24-197    F  Cl  H    CF3    CH3    CH3    CH2Cl4-198    F  Cl  H    CF3    CH3    CH3    CH2Br
                        表4(续)
    化合物   X  Y   R3  R1     R2     R7     R8编号
    4-199    F  Cl  H    CF3    CH3    CH3    CH2OCH34-200    F  Cl  H    CF3    CH3    CH3    CH2OC2H54-201    F  Cl  H    CF3    CH3    CH3    CH2OCH2OCH34-202    F  Cl  H    CF3    CH3    CH3    CH2OCH2OC2H54-203    F  Cl  H    CF3    CH3    CH3    CH2OCOCH34-204    F  Cl  H    CF3    CH3    CH3    CH2OCOC2H54-205    F  Cl  H    CF3    CH3    CH3    CH2OCOiC3H74-206    F  Cl  H    CF3    CH3    CH3    CH2OCOCH2Cl4-207    F  Cl  H    CF3    CH3    CH3    CH2OCOCCl34-208    F  Cl  H    CF3    CH3    CH3    CH2OCOCF34-209    F  Cl  H    CF3    CH3    CH3    COOH4-210    F  Cl  H    CF3    CH3    CH3    COOCH34-211    F  Cl  H    CF3    CH3    CH3    COOC2H54-212    F  Cl  H    CF3    CH3    CH3    COOnC3H74-213    F  Cl  H    CF3    CH3    CH3    COOnC4H94-214    F  Cl  H    CF3    CH3    CH3    COOnC5H114-215    F  Cl  H    CF3    CH3    CH3    COOiC3H74-216    F  Cl  H    CF3    CH3    CH3    COOcC5H94-217    F  Cl  H    CF3    CH3    CH3    COOcC6H114-218    F  Cl  H    CF3    CH3    CH3    COOCH2CH=CH24-219    F  Cl  H    CF3    CH3    CH3    COOCH2C≡CH4-220    F  Cl  H    CF3    CH3    CH3    CONH2
                     表4(续)
    化合物   X  Y   R3  R1       R2     R7    R8编号
    4-221    F  Cl  H    CF3      CH3    CH3   CONHCH34-222    F  Cl  H    CF3      CH3    CH3   CONHC2H54-223    F  Cl  H    CF3      CH3    CH3   CON(CH3)24-224    F  Cl  H    CF3      CH3    CH3   CON(C2H5)24-225    H  Cl  H    CF2Cl    CH3    H      CH2Cl4-226    H  Cl  H    CF2Cl    CH3    H      CH2Br4-227    H  Cl  H    CF2Cl    CH3    H      CH2OCH34-228    H  Cl  H    CF2Cl    CH3    H      CH2OC2H54-229    H  Cl  H    CF2Cl    CH3    H      CH2OCH2OCH34-230    H  Cl  H    CF2Cl    CH3    H      CH2OCH2OC2H54-231    H  Cl  H    CF2Cl    CH3    H      CH2OCOCH34-232    H  Cl  H    CF2Cl    CH3    H      CH2OCOC2H54-233    H  Cl  H    CF2Cl    CH3    H      CH2OCOiC3H74-234    H  Cl  H    CF2Cl    CH3    H      CH2OCOCH2Cl4-235    H  Cl  H    CF2Cl    CH3    H      CH2OCOCCl34-236    H  Cl  H    CF2Cl    CH3    H      CH2OCOCF34-237    H  Cl  H    CF2Cl    CH3    H      COOH4-238    H  Cl  H    CF2Cl    CH3    H      COOCH34-239    H  Cl  H    CF2Cl    CH3    H      COOC2H54-240    H  Cl  H    CF2Cl    CH3    H      COOnC3H74-241    H  Cl  H    CF2Cl    CH3    H      COOnC4H94-242    H  Cl  H    CF2Cl    CH3    H      COOnC5H114-243    H  Cl  H    CF2Cl    CH3    H      COOiC3H7
                      表4(续)
   化合物    X  Y   R3R1       R2     R7  R8编号
    4-244    H  Cl  H  CF2Cl    CH3    H    COOcC5H94-245    H  Cl  H  CF2Cl    CH3    H    COOcC6H114-246    H  Cl  H  CF2Cl    CH3    H    COOCH2CH=CH24-247    H  Cl  H  CF2Cl    CH3    H    COOCH2C≡CH4-248    H  Cl  H  CF2Cl    CH3    H    CONH24-249    H  Cl  H  CF2Cl    CH3    H    CONHCH34-250    H  Cl  H  CF2Cl    CH3    H    CONHC2H54-251    H  Cl  H  CF2Cl    CH3    H    CON(CH3)24-252    H  Cl  H  CF2Cl    CH3    H    CON(C2H5)24-253    F  Cl  H  CF2Cl    CH3    H    CH2Cl4-254    F  Cl  H  CF2Cl    CH3    H    CH2Br4-255    F  Cl  H  CF2Cl    CH3    H    CH2OCH34-256    F  Cl  H  CF2Cl    CH3    H    CH2OC2H54-257    F  Cl  H  CF2Cl    CH3    H    CH2OCH2OCH34-258    F  Cl  H  CF2Cl    CH3    H    CH2OCH2OC2H54-259    F  Cl  H  CF2Cl    CH3    H    CH2OCOCH34-260    F  Cl  H  CF2Cl    CH3    H    CH2OCOC2H54-261    F  Cl  H  CF2Cl    CH3    H    CH2OCOiC3H74-262    F  Cl  H  CF2Cl    CH3    H    CH2OCOCH2Cl4-263    F  Cl  H  CF2Cl    CH3    H    CH2OCOCCl34-264    F  Cl  H  CF2Cl    CH3    H    CH2OCOCF34-265    F  Cl  H  CF2Cl    CH3    H    COOH4-266    F  Cl  H  CF2Cl    CH3    H    COOCH3
                       表4(续)
   化合物    X  Y   R3R1       R2     R7  R8编号
    4-267    F  Cl  H  CF2Cl    CH3    H    COOC2H54-268    F  Cl  H  CF2Cl    CH3    H    COOnC3H74-269    F  Cl  H  CF2Cl    CH3    H    COOnC4H94-270    F  Cl  H  CF2Cl    CH3    H    COOnC5H114-271    F  Cl  H  CF2Cl    CH3    H    COOiC3H74-272    F  Cl  H  CF2Cl    CH3    H    COOcC5H94-273    F  Cl  H  CF2Cl    CH3    H    COOcC5H114-274    F  Cl  H  CF2Cl    CH3    H    COOCH2CH=CH24-275    F  Cl  H  CF2Cl    CH3    H    COOCH2C≡CH4-276    F  Cl  H  CF2Cl    CH3    H    CONH24-277    F  Cl  H  CF2Cl    CH3    H    CONHCH34-278    F  Cl  H  CF2Cl    CH3    H    CONHC2H54-279    F  Cl  H  CF2Cl    CH3    H    CON(CH3)24-280    F  Cl  H  CF2Cl    CH3    H    CON(C2H5)24-281    H  Cl  H  CF2Cl    CH3    CH3 CH2Cl4-282    H  Cl  H  CF2Cl    CH3    CH3 CH2Br4-283    H  Cl  H  CF2Cl    CH3    CH3 CH2OCH34-284    H  Cl  H  CF2Cl    CH3    CH3 CH2OC2H54-285    H  Cl  H  CF2Cl    CH3    CH3 CH2OCH2OCH34-286    H  Cl  H  CF2Cl    CH3    CH3 CH2OCH2OC2H54-287    H  Cl  H  CF2Cl    CH3    CH3 CH2OCOCH34-288    H  Cl  H  CF2Cl    CH3    CH3 CH2OCOC2H54-289    H  Cl  H  CF2Cl    CH3    CH3 CH2OCOiC3H7
                       表4(续)
    化合物   X  Y   R3 R1      R2     R7     R8编号
    4-290    H  Cl  H  CF2Cl    CH3    CH3    CH2OCOCH2Cl4-291    H  Cl  H  CF2Cl    CH3    CH3    CH2OCOCCl34-292    H  Cl  H  CF2Cl    CH3    CH3    CH2OCOCF34-293    H  Cl  H  CF2Cl    CH3    CH3    COOH4-294    H  Cl  H  CF2Cl    CH3    CH3    COOCH34-295    H  Cl  H  CF2Cl    CH3    CH3    COOC2H54-296    H  Cl  H  CF2Cl    CH3    CH3    COOnC3H74-297    H  Cl  H  CF2Cl    CH3    CH3    COOnC4H94-298    H  Cl  H  CF2Cl    CH3    CH3    COOnC5H114-299    H  Cl  H  CF2Cl    CH3    CH3    COOiC3H74-300    H  Cl  H  CF2Cl    CH3    CH3    COOcC5H94-301    H  Cl  H  CF2Cl    CH3    CH3    COOcC6H114-302    H  Cl  H  CF2Cl    CH3    CH3    COOCH2CH=CH24-303    H  Cl  H  CF2Cl    CH3    CH3    COOCH2C≡CH4-304    H  Cl  H  CF2Cl    CH3    CH3    CONH24-305    H  Cl  H  CF2Cl    CH3    CH3    CONHCH34-306    H  Cl  H  CF2Cl    CH3    CH3    CONHC2H54-307    H  Cl  H  CF2Cl    CH3    CH3    CON(CH3)24-308    H  Cl  H  CF2Cl    CH3    CH3    CON(C2H5)24-309    F  Cl  H  CF2Cl    CH3    CH3    CH2Cl4-310    F  Cl  H  CF2Cl    CH3    CH3    CH2Br4-311    F  Cl  H  CF2Cl    CH3    CH3    CH2OCH34-312    F  Cl  H  CF2Cl    CH3    CH3    CH2OC2H6
                       表4(续)
    化合物   X  Y   R3 R1      R2     R7     R8编号
    4-313    F  Cl  H  CF2Cl    CH3    CH3    CH2OCH2OCH34-314    F  Cl  H  CF2Cl    CH3    CH3    CH2OCH2OC2H54-315    F  Cl  H  CF2Cl    CH3    CH3    CH2OCOCH34-316    F  Cl  H  CF2Cl    CH3    CH3    CH2OCOC2H54-317    F  Cl  H  CF2Cl    CH3    CH3    CH2OCOiC3H74-318    F  Cl  H  CF2Cl    CH3    CH3    CH2OCOCH2Cl4-319    F  Cl  H  CF2Cl    CH3    CH3    CH2OCOCCl34-320    F  Cl  H  CF2Cl    CH3    CH3    CH2OCOCF34-321    F  Cl  H  CF2Cl    CH3    CH3    COOH4-322    F  Cl  H  CF2Cl    CH3    CH3    COOCH34-323    F  Cl  H  CF2Cl    CH3    CH3    COOC2H54-324    F  Cl  H  CF2Cl    CH3    CH3    COOnC3H74-325    F  Cl  H  CF2Cl    CH3    CH3    COOnC4H94-326    F  Cl  H  CF2Cl    CH3    CH3    COOnC5H114-327    F  Cl  H  CF2Cl    CH3    CH3    COOiC3H74-328    F  Cl  H  CF2Cl    CH3    CH3    COOcC5H94-329    F  Cl  H  CF2Cl    CH3    CH3    COOcC6H114-330    F  Cl  H  CF2Cl    CH3    CH3    COOCH2CH=CH24-331    F  Cl  H  CF2Cl    CH3    CH3    COOCH2C≡CH4-332    F  Cl  H  CF2Cl    CH3    CH3    CONH24-333    F  Cl  H  CF2Cl    CH3    CH3    CONHCH34-334    F  Cl  H  CF2Cl    CH3    CH3    CONHC2H5
                         表4(续)
   化合物    X  Y   R3  R1       R2     R7  R8编号
    4-335    F  Cl  H    CF2Cl    CH3    CH3 CON(CH3)24-336    F  Cl  H    CF2Cl    CH3    CH3 CON(C2H5)24-337    H  Cl  H    CF3      CH3    H    CH2Cl4-338    H  Cl  H    CF3      CH3    H    CH2Br4-339    H  Cl  H    CF3      CH3    H    CH2OCH34-340    H  Cl  H    CF3      CH3    H    CH2OC2H54-341    H  Cl  H    CF3      CH3    H    CH2OCH2OCH34-342    H  Cl  H    CF3      CH3    H    CH2OCH2OC2H54-343    H  Cl  H    CF3      CH3    H    CH2OCOCH34-344    H  Cl  H    CF3      CH3    H    CH2OCOC2H54-345    H  Cl  H    CF3      CH3    H    CH2OCOiC3H74-346    H  Cl  H    CF3      CH3    H    CH2OCOCH2Cl4-347    H  Cl  H    CF3      CH3    H    CH2OCOCCl34-348    H  Cl  H    CF3      CH3    H    CH2OCOCF34-349    H  Cl  H    CF3      CH3    H    COOH4-350    H  Cl  H    CF3      CH3    H    COOCH34-351    H  Cl  H    CF3      CH3    H    COOC2H54-352    H  Cl  H    CF3      CH3    H    COOnC3H74-353    H  Cl  H    CF3      CH3    H    COOnC4H94-354    H  Cl  H    CF3      CH3    H    COOnC5H114-355    H  Cl  H    CF3      CH3    H    COOiC3H74-356    H  Cl  H    CF3      CH3    H    COOcC5H94-357    H  Cl  H    CF3      CH3    H    COOcC6H11
                           表4(续)
    化合物   X  Y   R3  R1     R2     R7  R8编号
    4-358    H  Cl  H    CF3    CH3    H    COOCH2CH=CH24-359    H  Cl  H    CF3    CH3    H    COOCH2C≡CH4-360    H  Cl  H    CF3    CH3    H    CONH24-361    H  Cl  H    CF3    CH3    H    CONHCH34-362    H  Cl  H    CF3    CH3    H    CONHC2H54-363    H  Cl  H    CF3    CH3    H    CON(CH3)24-364    H  Cl  H    CF3    CH3    H    CON(C2H5)24-365    F  Cl  H    CF3    CH3    H    CH2Cl-4-366    F  Cl  H    CF3    CH3    H    CH2Br4-367    F  Cl  H    CF3    CH3    H    CH2OCH34-368    F  Cl  H    CF3    CH3    H    CH2OC2H54-369    F  Cl  H    CF3    CH3    H    CH2OCH2OCH34-370    F  Cl  H    CF3    CH3    H    CH2OCH2OC2H54-371    F  Cl  H    CF3    CH3    H    CH2OCOCH34-372    F  Cl  H    CF3    CH3    H    CH2OCOC2H54-373    F  Cl  H    CF3    CH3    H    CH2OCOiC3H74-374    F  Cl  H    CF3    CH3    H    CH2OCOCH2Cl4-375    F  Cl  H    CF3    CH3    H    CH2OCOCCl34-376    F  Cl  H    CF3    CH3    H    CH2OCOCF34-377    F  Cl  H    CF3    CH3    H    COOH4-378    F  Cl  H    CF3    CH3    H    COOCH34-379    F  Cl  H    CF3    CH3    H    COOC2H54-380    F  Cl  H    CF3    CH3    H    COOnC3H7
                       表4(续)
    化合物   X  Y   R3  R1     R2     R7     R8编号
    4-381    F  Cl  H    CF3    CH3    H       COOnC4H94-382    F  Cl  H    CF3    CH3    H       COOnC5H114-383    F  Cl  H    CF3    CH3    H       COOiC3H74-384    F  Cl  H    CF3    CH3    H       COOcC5H94-385    F  Cl  H    CF3    CH3    H       COOcC6H114-386    F  Cl  H    CF3    CH3    H       COOCH2CH=CH24-387    F  Cl  H    CF3    CH3    H       COOCH2C≡CH4-388    F  Cl  H    CF3    CH3    H       CONH2 -4-389    F  Cl  H    CF3    CH3    H       CONHCH34-390    F  Cl  H    CF3    CH3    H       CONHC2H54-391    F  Cl  H    CF3    CH3    H       CON(CH3)24-392    F  Cl  H    CF3    CH3    H       CON(C2H5)24-393    H  Cl  H    CF3    CH3    CH3    CH2Cl4-394    H  Cl  H    CF3    CH3    CH3    CH2Br4-395    H  Cl  H    CF3    CH3    CH3    CH2OCH34-396    H  Cl  H    CF3    CH3    CH3    CH2OC2H54-397    H  Cl  H    CF3    CH3    CH3    CH2OCH2OCH34-398    H  Cl  H    CF3    CH3    CH3    CH2OCH2OC2H54-399    H  Cl  H    CF3    CH3    CH3    CH2OCOCH34-400    H  Cl  H    CF3    CH3    CH3    CH2OCOC2H54-401    H  Cl  H    CF3    CH3    CH3    CH2OCOiC3H74-402    H  Cl  H    CF3    CH3    CH3    CH2OCOCH2Cl4-403    H  Cl  H    CF3    CH3    CH3    CH2OCOCCl3
                        表4(续)
    化合物   X  Y   R3  R1     R2     R7     R8编号
    4-404    H  Cl  H    CF3    CH3    CH3    CH2OCOCF34-405    H  Cl  H    CF3    CH3    CH3    COOH4-406    H  Cl  H    CF3    CH3    CH3    COOCH34-407    H  Cl  H    CF3    CH3    CH3    COOC2H54-408    H  Cl  H    CF3    CH3    CH3    COOnC3H74-409    H  Cl  H    CF3    CH3    CH3    COOnC4H94-410    H  Cl  H    CF3    CH3    CH3    COOnC5H114-411    H  Cl  H    CF3    CH3    CH3    COOi-C3H74-412    H  Cl  H    CF3    CH3    CH3    COOcC5H94-413    H  Cl  H    CF3    CH3    CH3    COOcC6H114-414    H  Cl  H    CF3    CH3    CH3    COOCH2CH=CH24-415    H  Cl  H    CF3    CH3    CH3    COOCH2C≡CH4-416    H  Cl  H    CF3    CH3    CH3    CONH24-417    H  Cl  H    CF3    CH3    CH3    CONHCH34-418    H  Cl  H    CF3    CH3    CH3    CONHC2H54-419    H  Cl  H    CF3    CH3    CH3    CON(CH3)24-420    H  Cl  H    CF3    CH3    CH3    CON(C2H5)24-421    F  Cl  H    CF3    CH3    CH3    CH2Cl4-422    F  Cl  H    CF3    CH3    CH3    CH2Br4-423    F  Cl  H    CF3    CH3    CH3    CH2OCH34-424    F  Cl  H    CF3    CH3    CH3    CH2OC2H54-425    F  Cl  H    CF3    CH3    CH3    CH2OCH2OCH34-426    F  Cl  H    CF3    CH3    CH3    CH2OCH2OC2H5
                            表4(续)
    化合物   X  Y   R3  R1     R2     R7     R8编号
    4-427    F  Cl  H    CF3    CH3    CH3    CH2OCOCH34-428    F  Cl  H    CF3    CH3    CH3    CH2OCOC2H54-429    F  Cl  H    CF3    CH3    CH3    CH2OCOiC3H74-430    F  Cl  H    CF3    CH3    CH3    CH2OCOCH2Cl4-431    F  Cl  H    CF3    CH3    CH3    CH2OCOCCl34-432    F  Cl  H    CF3    CH3    CH3    CH2OCOCF34-433    F  Cl  H    CF3    CH3    CH3    COOH4-434    F  Cl  H    CF3    CH3    CH3    COOCH34-435    F  Cl  H    CF3    CH3    CH3    COOC2H54-436    F  Cl  H    CF3    CH3    CH3    COOnC3H74-437    F  Cl  H    CF3    CH3    CH3    COOnC4H94-438    F  Cl  H    CF3    CH3    CH3    COOnC5H114-439    F  Cl  H    CF3    CH3    CH3    COOiC3H74-440    F  Cl  H    CF3    CH3    CH3    COOcC5H94-441    F  Cl  H    CF3    CH3    CH3    COOcC6H114-442    F  Cl  H    CF3    CH3    CH3    COOCH2CH=CH24-443    F  Cl  H    CF3    CH3    CH3    COOCH2C≡CH4-444    F  Cl  H    CF3    CH3    CH3    CONH24-445    F  Cl  H    CF3    CH3    CH3    CONHCH34-446    F  Cl  H    CF3    CH3    CH3    CONHC2H54-447    F  Cl  H    CF3    CH3    CH3    CON(CH3)24-448    F  Cl  H    CF3    CH3    CH3    CON(C2H5)2
                             表4(续)
    化合物   X  Y   R3   R1      R2    R7     R8编号
    4-449    F  Cl  H    CF3      CH3   H      CH34-450    F  Cl  H    CF3      CH3   H      CH2OH4-451    F  Cl  H    CF3      CH3   CH3   CH34-452    F  Cl  H    CF3      CH3   CH3   CH2OH4-453    F  Cl  H    CF3      H      H      CH34-454    F  Cl  H    CF3      H      H      CH2OH4-455    F  Cl  H    CF3      H      CH3   CH34-456    F  Cl  H    CF3      H      CH3   CH2OH4-457    H  Cl  H    CF3      CH3   H      CH34-458    H  Cl  H    CF3      CH3   H      CH2OH4-459    H  Cl  H    CF3      CH3   CH3   CH34-460    H  Cl  H    CF3      CH3   CH3   CH2OH4-461    H  Cl  H    CF3      H      H      CH34-462    H  Cl  H    CF3      H      H      CH2OH4-463    H  Cl  H    CF3      H      CH3   CH34-464    H  Cl  H    CF3      H      CH3   CH2OH4-465    F  Cl  H    CF2Cl    CH3   H      CH34-466    F  Cl  H    CF2Cl    CH3   H      CH2OH4-467    F  Cl  H    CF2Cl    CH3   CH3   CH34-468    F  Cl  H    CF2Cl    CH3   CH3   CH2OH4-469    F  Cl  H    CF2Cl    H      H      CH34-470    F  Cl  H    CF2Cl    H      H      CH2OH4-471    F  Cl  H    CF2Cl    H      CH3   CH3
                         表4(续)
   化合物    X  Y   R3  R1       R2    R7  R8编号
    4-472    F  Cl  H    CF2Cl    H      CH3 CH2OH4-473    H  Cl  H    CF2Cl    CH3   H    CH34-474    H  Cl  H    CF2Cl    CH3   H    CH2OH4-475    H  Cl  H    CF2Cl    CH3   CH3 CH34-476    H  Cl  H    CF2Cl    CH3   CH3 CH2OH4-477    H  Cl  H    CF2Cl    H      H    CH34-478    H  Cl  H    CF2Cl    H      H    CH2OH4-479    H  Cl  H    CF2Cl    H      CH3 CH34-480    H  Cl  H    CF2Cl    H      CH3 CH2OH4-481    H  Cl  H    CF3      H      H    CH2Cl4-482    H  Cl  H    CF3      H      H    CH2Br4-483    H  Cl  H    CF3      H      H    CH2OCH34-484    H  Cl  H    CF3      H      H    CH2OC2H54-485    H  Cl  H    CF3      H      H    CH2OCH2OCH34-486    H  Cl  H    CF3      H      H    CH2OCH2OC2H54-487    H  Cl  H    CF3      H      H    CH2OCOCH34-488    H  Cl  H    CF3      H      H    CH2OCOC2H54-489    H  Cl  H    CF3      H      H    CH2OCOiC3H74-490    H  Cl  H    CF3      H      H    CH2OCOCH2Cl4-491    H  Cl  H    CF3      H      H    CH2OCOCCl34-492    H  Cl  H    CF3      H      H    CH2OCOCF34-493    H  Cl  H    CF3      H      H    COOH4-494    H  Cl  H    CF3      H      H    COOCH3
                       表4(续)
   化合物    X  Y   R3  R1     R2  R7  R8编号
    4-495    H  Cl  H    CF3    H    H    COOC2H54-496    H  Cl  H    CF3    H    H    COOnC3H74-497    H  Cl  H    CF3    H    H    COOnC4H94-498    H  Cl  H    CF3    H    H    COOnC5H114-499    H  Cl  H    CF3    H    H    COOiC3H74-500    H  Cl  H    CF3    H    H    COOcC5H94-501    H  Cl  H    CF3    H    H    COOcC6H114-502    H  Cl  H    CF3    H    H    COOCH2 -CH=CH24-503    H  Cl  H    CF3    H    H    COOCH2C≡CH4-504    H  Cl  H    CF3    H    H    CONH24-505    H  Cl  H    CF3    H    H    CONHCH34-506    H  Cl  H    CF3    H    H    CONHC2H54-507    H  Cl  H    CF3    H    H    CON(CH3)24-508    H  Cl  H    CF3    H    H    CON(C2H5)24-509    F  Cl  H    CF3    H    H    CH2Cl4-510    F  Cl  H    CF3    H    H    CH2Br4-511    F  Cl  H    CF3    H    H    CH2OCH34-512    F  Cl  H    CF3    H    H    CH2OC2H54-513    F  Cl  H    CF3    H    H    CH2OCH2OCH34-514    F  Cl  H    CF3    H    H    CH2OCH2OC2H54-515    F  Cl  H    CF3    H    H    CH2OCOCH34-516    F  Cl  H    CF3    H    H    CH2OCOC2H54-517    F  Cl  H    CF3    H    H    CH2OCOiC3H7
                           表4(续)
    化合物   X  Y   R3  R1     R2  R7    R8编号
    4-518    F  Cl  H    CF3    H    H      CH2OCOCH2Cl4-519    F  Cl  H    CF3    H    H      CH2OCOCCl34-520    F  Cl  H    CF3    H    H      CH2OCOCF34-521    F  Cl  H    CF3    H    H      COOH4-522    F  Cl  H    CF3    H    H      COOCH34-523    F  Cl  H    CF3    H    H      COOC2H54-524    F  Cl  H    CF3    H    H      COOnC3H74-525    F  Cl  H    CF3    H    H      COOn-C4H94-526    F  Cl  H    CF3    H    H      COOnC5H114-527    F  Cl  H    CF3    H    H      COOiC3H74-528    F  Cl  H    CF3    H    H      COOcC5H94-529    F  Cl  H    CF3    H    H      COOcC6H114-530    F  Cl  H    CF3    H    H      COOCH2CH=CH24-531    F  Cl  H    CF3    H    H      COOCH2C≡CH4-532    F  Cl  H    CF3    H    H      CONH24-533    F  Cl  H    CF3    H    H      CONHCH34-534    F  Cl  H    CF3    H    H      CONHC2H54-535    F  Cl  H    CF3    H    H      CON(CH3)24-536    F  Cl  H    CF3    H    H      CON(C2H5)24-537    H  Cl  H    CF3    H    CH3   CH2Cl4-538    H  Cl  H    CF3    H    CH3   CH2Br4-539    H  Cl  H    CF3    H    CH3   CH2OCH34-540    H  Cl  H    CF3    H    CH3   CH2OC2H5
                        表4(续)
    化合物   X  Y   R3  R1     R2  R7     R8编号
    4-541    H  Cl  H    CF3    H    CH3    CH2OCH2OCH34-542    H  Cl  H    CF3    H    CH3    CH2OCH2OC2H54-543    H  Cl  H    CF3    H    CH3    CH2OCOCH34-544    H  Cl  H    CF3    H    CH3    CH2OCOC2H54-545    H  Cl  H    CF3    H    CH3    CH2OCOiC3H74-546    H  Cl  H    CF3    H    CH3    CH2OCOCH2Cl4-547    H  Cl  H    CF3    H    CH3    CH2OCOCCl34-548    H  Cl  H    CF3    H    CH3    CH2OCOCF34-549    H  Cl  H    CF3    H    CH3    COOH4-550    H  Cl  H    CF3    H    CH3    COOCH34-551    H  Cl  H    CF3    H    CH3    COOC2H54-552    H  Cl  H    CF3    H    CH3    COOnC3H74-553    H  Cl  H    CF3    H    CH3    COOnC4H94-554    H  Cl  H    CF3    H    CH3    COOnC5H114-555    H  Cl  H    CF3    H    CH3    COOiC3H74-556    H  Cl  H    CF3    H    CH3    COOcC5H94-557    H  Cl  H    CF3    H    CH3    COOcC6H114-558    H  Cl  H    CF3    H    CH3    COOCH2CH=CH24-559    H  Cl  H    CF3    H    CH3    COOCH2C≡CH4-560    H  Cl  H    CF3    H    CH3    CONH24-561    H  Cl  H    CF3    H    CH3    CONHCH34-562    H  Cl  H    CF3    H    CH3    CONHC2H6
                         表4(续)
    化合物   X  Y   R3  R1     R2  R7     R8编号
    4-563    H  Cl  H    CF3    H    CH3    CON(CH3)24-564    H  Cl  H    CF3    H    CH3    CON(C2H5)24-565    F  Cl  H    CF3    H    CH3    CH2Cl4-566    F  Cl  H    CF3    H    CH3    CH2Br4-567    F  Cl  H    CF3    H    CH3    CH2OCH34-568    F  Cl  H    CF3    H    CH3    CH2OC2H54-569    F  Cl  H    CF3    H    CH3    CH2OCH2OCH34-570    F  Cl  H    CF3    H    CH3    CH2OCH2 -OC2H54-571    F  Cl  H    CF3    H    CH3    CH2OCOCH34-572    F  Cl  H    CF3    H    CH3    CH2OCOC2H54-573    F  Cl  H    CF3    H    CH3    CH2OCOiC3H74-574    F  Cl  H    CF3    H    CH3    CH2OCOCH2Cl4-575    F  Cl  H    CF3    H    CH3    CH2OCOCCl34-576    F  Cl  H    CF3    H    CH3    CH2OCOCF34-577    F  Cl  H    CF3    H    CH3    COOH4-578    F  Cl  H    CF3    H    CH3    COOCH34-579    F  Cl  H    CF3    H    CH3    COOC2H54-580    F  Cl  H    CF3    H    CH3    COOnC3H74-581    F  Cl  H    CF3    H    CH3    COOnC4H94-582    F  Cl  H    CF3    H    CH3    COOnC5H114-583    F  Cl  H    CF3    H    CH3    COOiC3H74-584    F  Cl  H    CF3    H    CH3    COOcC5H94-585    F  Cl  H    CF3    H    CH3    COOcC8H11
                      表4(续)
    化合物   X  Y   R3  R1     R2  R7    R8编号
    4-586    F  Cl  H    CF3    H    CH3    COOCH2CH=CH24-587    F  Cl  H    CF3    H    CH3   COOCH2C≡CH4-588    F  Cl  H    CF3    H    CH3   CONH24-589    F  Cl  H    CF3    H    CH3   CONHCH34-590    F  Cl  H    CF3    H    CH3   CONHC2H54-591    F  Cl  H    CF3    H    CH3   CON(CH3)24-592    F  Cl  H    CF3    H    CH3   CON(C2H5)24-593    H  Cl  H    CF3    H    H      CH2Cl-4-594    H  Cl  H    CF3    H    H      CH2Br4-595    H  Cl  H    CF3    H    H      CH2OCH34-596    H  Cl  H    CF3    H    H      CH2OC2H54-597    H  Cl  H    CF3    H    H      CH2OCH2OCH34-598    H  Cl  H    CF3    H    H      CH2OCH2OC2H54-599    H  Cl  H    CF3    H    H      CH2OCOCH34-600    H  Cl  H    CF3    H    H      CH2OCOC2H54-601    H  Cl  H    CF3    H    H      CH2OCOiC3H74-602    H  Cl  H    CF3    H    H      CH2OCOCH2Cl4-603    H  Cl  H    CF3    H    H      CH2OCOCCl34-604    H  Cl  H    CF3    H    H      CH2OCOCF34-605    H  Cl  H    CF3    H    H      COOH4-606    H  Cl  H    CF3    H    H      COOCH34-607    H  Cl  H    CF3    H    H      COOC2H64-608    H  Cl  H    CF3    H    H      COOnC3H7
                         表4(续)
    化合物   X  Y   R3  R1     R2  R7  R8编号
    4-609    H  Cl  H    CF3    H    H    COOnC4H94-610    H  Cl  H    CF3    H    H    COOnC5H114-611    H  Cl  H    CF3    H    H    COOiC3H74-612    H  Cl  H    CF3    H    H    COOcC5H94-613    H  Cl  H    CF3    H    H    COOcC6H114-614    H  Cl  H    CF3    H    H    COOCH2CH=CH24-615    H  Cl  H    CF3    H    H    COOCH2C≡CH4-616    H  Cl  H    CF3    H    H    CONH2 -4-617    H  Cl  H    CF3    H    H    CONHCH34-618    H  Cl  H    CF3    H    H    CONHC2H54-619    H  Cl  H    CF3    H    H    CON(CH3)24-620    H  Cl  H    CF3    H    H    CON(C2H5)24-621    F  Cl  H    CF3    H    H    CH2Cl4-622    F  Cl  H    CF3    H    H    CH2Br4-623    F  Cl  H    CF3    H    H    CH2OCH34-624    F  Cl  H    CF3    H    H    CH2OC2H54-625    F  Cl  H    CF3    H    H    CH2OCH2OCH34-626    F  Cl  H    CF3    H    H    CH2OCH2OC2H54-627    F  Cl  H    CF3    H    H    CH2OCOCH34-628    F  Cl  H    CF3    H    H    CH2OCOC2H54-629    F  Cl  H    CF3    H    H    CH2OCOiC3H74-630    F  Cl  H    CF3    H    H    CH2OCOCH2Cl4-631    F  Cl  H    CF3    H    H    CH2OCOCCl3
                       表4(续)
    化合物   X  Y   R3  R1     R2  R7    R8编号
    4-632    F  Cl  H    CF3    H    H      CH2OCOCF34-633    F  Cl  H    CF3    H    H      COOH4-634    F  Cl  H    CF3    H    H      COOCH34-635    F  Cl  H    CF3    H    H      COOC2H54-636    F  Cl  H    CF3    H    H      COOnC3H74-637    F  Cl  H    CF3    H    H      COOnC4H94-638    F  Cl  H    CF3    H    H      COOnC5H114-639    F  Cl  H    CF3    H    H      COOi-C3H74-640    F  Cl  H    CF3    H    H      COOcC5H94-641    F  Cl  H    CF3    H    H      COOcC6H114-642    F  Cl  H    CF3    H    H      COOCH2CH=CH24-643    F  Cl  H    CF3    H    H      COOCH2C≡CH4-644    F  Cl  H    CF3    H    H      CONH24-645    F  Cl  H    CF3    H    H      CONHCH34-646    F  Cl  H    CF3    H    H      CONHC2H54-647    F  Cl  H    CF3    H    H      CON(CH3)24-648    F  Cl  H    CF3    H    H      CON(C2H5)24-649    H  Cl  H    CF3    H    CH3   CH2Cl4-650    H  Cl  H    CF3    H    CH3   CH2Br4-651    H  Cl  H    CF3    H    CH3   CH2OCH34-652    H  Cl  H    CF3    H    CH3   CH2OC2H54-653    H  Cl  H    CF3    H    CH3   CH2OCH2OCH34-654    H  Cl  H    CF3    H    CH3   CH2OCH2OC2H5
                         表4(续)
    化合物   X  Y   R3  R1     R2  R7     R8编号
    4-655    H  Cl  H    CF3    H    CH3    CH2OCOCH34-656    H  Cl  H    CF3    H    CH3    CH2OCOC2H54-657    H  Cl  H    CF3    H    CH3    CH2OCOiC3H74-658    H  Cl  H    CF3    H    CH3    CH2OCOCH2Cl4-659    H  Cl  H    CF3    H    CH3    CH2OCOCCl34-660    H  Cl  H    CF3    H    CH3    CH2OCOCF34-661    H  Cl  H    CF3    H    CH3    COOH4-662    H  Cl  H    CF3    H    CH3    COOCH34-663    H  Cl  H    CF3    H    CH3    COOC2H54-664    H  Cl  H    CF3    H    CH3    COOnC3H74-665    H  Cl  H    CF3    H    CH3    COOnC4H94-666    H  Cl  H    CF3    H    CH3    COOnC5H114-667    H  Cl  H    CF3    H    CH3    COOiC3H74-668    H  Cl  H    CF3    H    CH3    COOcC5H94-669    H  Cl  H    CF3    H    CH3    COOcC6H114-670    H  Cl  H    CF3    H    CH3    COOCH2CH=CH24-671    H  Cl  H    CF3    H    CH3    COOCH2C≡CH4-672    H  Cl  H    CF3    H    CH3    CONH24-673    H  Cl  H    CF3    H    CH3    CONHCH34-674    H  Cl  H    CF3    H    CH3    CONHC2H54-675    H  Cl  H    CF3    H    CH3    CON(CH3)24-676    H  Cl  H    CF3    H    CH3    CON(C2H5)2
                         表4(续)
    化合物   X  Y   R3  R1     R2  R7     R8编号
    4-677    F  Cl  H    CF3    H    CH3    CH2Cl4-678    F  Cl  H    CF3    H    CH3    CH2Br4-679    F  Cl  H    CF3    H    CH3    CH2OCH34-680    F  Cl  H    CF3    H    CH3    CH2OC2H54-681    F  Cl  H    CF3    H    CH3    CH2OCH2OCH34-682    F  Cl  H    CF3    H    CH3    CH2OCH2OC2H54-683    F  Cl  H    CF3    H    CH3    CH2OCOCH34-684    F  Cl  H    CF3    H    CH3    CH2OCOC2H54-685    F  Cl  H    CF3    H    CH3    CH2OCOiC3H74-686    F  Cl  H    CF3    H    CH3    CH2OCOCH2Cl4-687    F  Cl  H    CF3    H    CH3    CH2OCOCCl34-688    F  Cl  H    CF3    H    CH3    CH2OCOCF34-689    F  Cl  H    CF3    H    CH3    COOH4-690    F  Cl  H    CF3    H    CH3    COOCH34-691    F  Cl  H    CF3    H    CH3    COOC2H54-692    F  Cl  H    CF3    H    CH3    COOnC3H74-693    F  Cl  H    CF3    H    CH3    COOnC4H94-694    F  Cl  H    CF3    H    CH3    COOnC5H114-695    F  Cl  H    CF3    H    CH3    COOiC3H74-696    F  Cl  H    CF3    H    CH3    COOcC5H94-697    F  Cl  H    CF3    H    CH3    COOcC6H114-698    F  Cl  H    CF3    H    CH3    COOCH2CH=CH24-699    F  Cl  H    CF3    H    CH3    COOCH2C≡CH
                        表4(续)
  化合物   X  Y   R3     R1     R2  R7    R8编号
  4-700    F  Cl  H       CF3    H    CH3   CONH24-701    F  Cl  H       CF3    H    CH3   CONHCH34-702    F  Cl  H       CF3    H    CH3   CONHC2H54-703    F  Cl  H       CF3    H    CH3   CON(CH3)24-704    F  Cl  H       CF3    H    CH3   CON(C2H5)24-705    H  Cl  CH3    CF3    H    H      CH2Cl4-706    H  Cl  CH3    CF3    H    H      CH2Br4-707    H  Cl  CH3    CF3    H    H      CH2OCH34-708    H  Cl  CH3    CF3    H    H      CH2OC2H54-709    H  Cl  CH3    CF3    H    H      CH2OCH2OCH34-710    H  Cl  CH3    CF3    H    H      CH2OCH2OC2H54-711    H  Cl  CH3    CF3    H    H      CH2OCOCH34-712    H  Cl  CH3    CF3    H    H      CH2OCOC2H54-713    H  Cl  CH3    CF3    H    H      CH2OCOiC3H74-714    H  Cl  CH3    CF3    H    H      CH2OCOCH2Cl4-715    H  Cl  CH3    CF3    H    H      CH2OCOCCl34-716    H  Cl  CH3    CF3    H    H      CH2OCOCF34-717    H  Cl  CH3    CF3    H    H      COOH4-718    H  Cl  CH3    CF3    H    H      COOCH34-719    H  Cl  CH3    CF3    H    H      COOC2H54-720    H  Cl  CH3    CF3    H    H      COOnC3H74-721    H  Cl  CH3    CF3    H    H      COOnC4H94-722    H  Cl  CH3    CF3    H    H      COOnC5H11
                          表4(续)
    化合物   X  Y   R3     R1     R2  R7  R8编号
    4-723    H  Cl  CH3    CF3    H    H    COOiC3H74-724    H  Cl  CH3    CF3    H    H    COOcC5H94-725    H  Cl  CH3    CF3    H    H    COOcC6H114-726    H  Cl  CH3    CF3    H    H    COOCH2CH=CH24-727    H  Cl  CH3    CF3    H    H    COOCH2C≡CH4-728    H  Cl  CH3    CF3    H    H    CONH24-729    H  Cl  CH3    CF3    H    H    CONHCH34-730    H  Cl  CH3    CF3    H    H    CONHC2 -H54-731    H  Cl  CH3    CF3    H    H    CON(CH3)24-732    H  Cl  CH3    CF3    H    H    CON(C2H5)24-733    F  Cl  CH3    CF3    H    H    CH2Cl4-734    F  Cl  CH3    CF3    H    H    CH2Br4-735    F  Cl  CH3    CF3    H    H    CH2OCH34-736    F  Cl  CH3    CF3    H    H    CH2OC2H54-737    F  Cl  CH3    CF3    H    H    CH2OCH2OCH34-738    F  Cl  CH3    CF3    H    H    CH2OCHOC2H54-739    F  Cl  CH3    CF3    H    H    CH2OCOCH34-74O    F  Cl  CH3    CF3    H    H    CH2OCOC2H54-741    F  Cl  CH3    CF3    H    H    CH2OCOiC3H74-742    F  Cl  CH3    CF3    H    H    CH2OCOCH2Cl4-743    F  Cl  CH3    CF3    H    H    CH2OCOCCl34-744    F  Cl  CH3    CF3    H    H    CH2OCOCF34-745    F  Cl  CH3    CF3    H    H    COOH
                       表4(续)
  化合物   X  Y   R3     R1     R2  R7  R8编号
  4-746    F  Cl  CH3    CF3    H    H    COOCH34-747    F  Cl  CH3    CF3    H    H    COOC2H54-748    F  Cl  CH3    CF3    H    H    COOnC3H74-749    F  Cl  CH3    CF3    H    H    COOnC4H94-750    F  Cl  CH3    CF3    H    H    COOnC5H114-751    F  Cl  CH3    CF3    H    H    COOiC3H74-752    F  Cl  CH3    CF3    H    H    COOcC5H94-753    F  Cl  CH3    CF3    H    H    COOc-C6H114-754    F  Cl  CH3    CF3    H    H    COOCH2CH=CH24-755    F  Cl  CH3    CF3    H    H    COOCH2C≡CH4-756    F  Cl  CH3    CF3    H    H    CONH24-757    F  Cl  CH3    CF3    H    H    CONHCH34-758    F  Cl  CH3    CF3    H    H    CONHC2H54-759    F  Cl  CH3    CF3    H    H    CON(CH3)24-760    F  Cl  CH3    CF3    H    H    CON(C2H5)24-761    H  Cl  CH3    CF3    H    CH3 CH2Cl4-762    H  Cl  CH3    CF3    H    CH3 CH2Br4-763    H  Cl  CH3    CF3    H    CH3 CH2OCH34-764    H  Cl  CH3    CF3    H    CH3 CH2OC2H54-765    H  Cl  CH3    CF3    H    CH3 CH2OCH2OCH34-766    H  Cl  CH3    CF3    H    CH3 CH2OCH2OC2H64-767    H  Cl  CH3    CF3    H    CH3 CH2OCOCH34-768    H  Cl  CH3    CF3    H    CH3 CH2OCOC2H6
                        表4(续)
   化合物    X  Y   R3     R1     R2  R7     R8编号
    4-769    H  Cl  CH3    CF3    H    CH3    CH2OCOiC3H74-770    H  Cl  CH3    CF3    H    CH3    CH2OCOCH2Cl4-771    H  Cl  CH3    CF3    H    CH3    CH2OCOCCl34-772    H  Cl  CH3    CF3    H    CH3    CH2OCOCF34-773    H  Cl  CH3    CF3    H    CH3    COOH4-774    H  Cl  CH3    CF3    H    CH3    COOCH34-775    H  Cl  CH3    CF3    H    CH3    COOC2H54-776    H  Cl  CH3    CF3    H    CH3    COOn-C3H74-777    H  Cl  CH3    CF3    H    CH3    COOnC4H94-778    H  Cl  CH3    CF3    H    CH3    COOnC5H114-779    H  Cl  CH3    CF3    H    CH3    COOiC3H74-780    H  Cl  CH3    CF3    H    CH3    COOcC5H94-781    H  Cl  CH3    CF3    H    CH3    COOcC6H114-782    H  Cl  CH3    CF3    H    CH3    COOCH2CH=CH24-783    H  Cl  CH3    CF3    H    CH3    COOCH2C≡CH4-784    H  Cl  CH3    CF3    H    CH3    CONH24-785    H  Cl  CH3    CF3    H    CH3    CONHCH34-786    H  Cl  CH3    CF3    H    CH3    CONHC2H54-787    H  Cl  CH3    CF3    H    CH3    CON(CH3)24-788    H  Cl  CH3    CF3    H    CH3    CON(C2H6)24-789    F  Cl  CH3    CF3    H    CH3    CH2Cl4-790    F  Cl  CH3    CF3    H    CH3    CH2Br
                          表4(续)
   化合物    X  Y   R3     R1     R2  R7     R8编号
    4-791    F  Cl  CH3    CF3    H    CH3    CH2OCH34-792    F  Cl  CH3    CF3    H    CH3    CH2OC2H54-793    F  Cl  CH3    CF3    H    CH3    CH2OCH2OCH34-794    F  Cl  CH3    CF3    H    CH3    CH2OCH2OC2H54-795    F  Cl  CH3    CF3    H    CH3    CH2OCOCH34-796    F  Cl  CH3    CF3    H    CH3    CH2OCOC2H54-797    F  Cl  CH3    CF3    H    CH3    CH2OCOiC3H74-798    F  Cl  CH3    CF3    H    CH3    CH2OCOCH2Cl4-799    F  Cl  CH3    CF3    H    CH3    CH2OCOCCl34-800    F  Cl  CH3    CF3    H    CH3    CH2OCOCF34-801    F  Cl  CH3    CF3    H    CH3    COOH4-802    F  Cl  CH3    CF3    H    CH3    COOCH34-803    F  Cl  CH3    CF3    H    CH3    COOC2H54-804    F  Cl  CH3    CF3    H    CH3    COOnC3H74-805    F  Cl  CH3    CF3    H    CH3    COOnC4H94-806    F  Cl  CH3    CF3    H    CH3    COOnC5H114-807    F  Cl  CH3    CF3    H    CH3    COOiC3H74-808    F  Cl  CH3    CF3    H    CH3    CO0cC5H94-809    F  Cl  CH3    CF3    H    CH3    COOcC6H114-810    F  Cl  CH3    CF3    H    CH3    COOCH2CH=CH24-811    F  Cl  CH3    CF3    H    CH3    COOCH2C≡CH4-812    F  Cl  CH3    CF3    H    CH3    CONH24-813    F  Cl  CH3    CF3    H    CH3    CONHCH3
                             表4(续)
   化合物    X  Y   R3     R1     R2  R7    R8编号
    4-814    F  Cl  CH3    CF3    H    CH3   CONHC2H54-815    F  Cl  CH3    CF3    H    CH3   CON(CH3)24-816    F  Cl  CH3    CF3    H    CH3   CON(C2H5)24-817    H  Cl  CH3    CF3    H    H      CH2Cl4-818    H  Cl  CH3    CF3    H    H      CH2Br4-819    H  Cl  CH3    CF3    H    H      CH2OCH34-820    H  Cl  CH3    CF3    H    H      CH2OC2H54-821    H  Cl  CH3    CF3    H    H      CH2OCH- 2OCH34-822    H  Cl  CH3    CF3    H    H      CH2OCH2OC2H54-823    H  Cl  CH3    CF3    H    H      CH2OCOCH34-824    H  Cl  CH3    CF3    H    H      CH2OCOC2H54-825    H  Cl  CH3    CF3    H    H      CH2OCOiC3H74-826    H  Cl  CH3    CF3    H    H      CH2OCOCH2Cl4-827    H  Cl  CH3    CF3    H    H      CH2OCOCCl34-828    H  Cl  CH3    CF3    H    H      CH2OCOCF34-829    H  Cl  CH3    CF3    H    H      COOH4-830    H  Cl  CH3    CF3    H    H      COOCH34-831    H  Cl  CH3    CF3    H    H      COOC2H54-832    H  Cl  CH3    CF3    H    H      COOnC3H74-833    H  Cl  CH3    CF3    H    H      COOnC4H94-834    H  Cl  CH3    CF3    H    H      COOnC5H114-835    H  Cl  CH3    CF3    H    H      COOiC3H74-836    H  Cl  CH3    CF3    H    H      COOcC5H9
                     表4(续)
   化合物    X  Y   R3     R1     R2  R7  R8编号
    4-837    H  Cl  CH3    CF3    H    H    COOcC6H114-838    H  Cl  CH3    CF3    H    H    COOCH2CH=CH24-839    H  Cl  CH3    CF3    H    H    COOCH2C≡CH4-840    H  Cl  CH3    CF3    H    H    CONH24-841    H  Cl  CH3    CF3    H    H    CONHCH34-842    H  Cl  CH3    CF3    H    H    CONHC2H54-843    H  Cl  CH3    CF3    H    H    CON(CH3)24-844    H  Cl  CH3    CF3    H    H    CON(C2 -H5)24-845    F  Cl  CH3    CF3    H    H    CH2Cl4-846    F  Cl  CH3    CF3    H    H    CH2Br4-847    F  Cl  CH3    CF3    H    H    CH2OCH34-848    F  Cl  CH3    CF3    H    H    CH2OC2H54-849    F  Cl  CH3    CF3    H    H    CH2OCH2OCH34-850    F  Cl  CH3    CF3    H    H    CH2OCH2OC2H54-851    F  Cl  CH3    CF3    H    H    CH2OCOCH34-852    F  Cl  CH3    CF3    H    H    CH2OCOC2H54-853    F  Cl  CH3    CF3    H    H    CH2OCOiC3H74-854    F  Cl  CH3    CF3    H    H    CH2OCOCH2Cl4-855    F  Cl  CH3    CF3    H    H    CH2OCOCCl34-856    F  Cl  CH3    CF3    H    H    CH2OCOCF34-857    F  Cl  CH3    CF3    H    H    COOH4-858    F  Cl  CH3    CF3    H    H    COOCH34-859    F  Cl  CH3    CF3    H    H    COOC2H5
                        表4(续)
   化合物    X  Y   R3     R1     R2  R7  R8编号
    4-860    F  Cl  CH3    CF3    H    H    COOnC3H74-861    F  Cl  CH3    CF3    H    H    COOnC4H94-862    F  Cl  CH3    CF3    H    H    COOnC5H114-863    F  Cl  CH3    CF3    H    H    COOiC3H74-864    F  Cl  CH3    CF3    H    H    COOcC5H94-865    F  Cl  CH3    CF3    H    H    COOcC6H114-866    F  Cl  CH3    CF3    H    H    COOCH2CH=CH24-867    F  Cl  CH3    CF3    H    H    COOCH2C≡CH4-868    F  Cl  CH3    CF3    H    H    CONH24-869    F  Cl  CH3    CF3    H    H    CONHCH34-870    F  Cl  CH3    CF3    H    H    CONHC2H54-871    F  Cl  CH3    CF3    H    H    CON(CH3)24-872    F  Cl  CH3    CF3    H    H    CON(C2H5)24-873    H  Cl  CH3    CF3    H    CH3 CH2Cl4-874    H  Cl  CH3    CF3    H    CH3 CH2Br4-875    H  Cl  CH3    CF3    H    CH3 CH2OCH34-876    H  Cl  CH3    CF3    H    CH3 CH2OC2H54-877    H  Cl  CH3    CF3    H    CH3 CH2OCH2OCH34-878    H  Cl  CH3    CF3    H    CH3 CH2OCH2OC2H54-879    H  Cl  CH3    CF3    H    CH3 CH2OCOCH34-880    H  Cl  CH3    CF3    H    CH3 CH2OCOC2H54-881    H  Cl  CH3    CF3    H    CH3 CH2OCOiC3H74-882    H  Cl  CH3    CF3    H    CH3 CH2OCOCH2Cl
                          表4(续)
   化合物    X  Y   R3     R1     R2  R7     R8编号
    4-883    H  Cl  CH3    CF3    H    CH3    CH2OCOCCl34-884    H  Cl  CH3    CF3    H    CH3    CH2OCOCF34-885    H  Cl  CH3    CF3    H    CH3    COOH4-886    H  Cl  CH3    CF3    H    CH3    COOCH34-887    H  Cl  CH3    CF3    H    CH3    COOC2H54-888    H  Cl  CH3    CF3    H    CH3    COOnC3H74-889    H  Cl  CH3    CF3    H    CH3    COOnC4H94-890    H  Cl  CH3    CF3    H    CH3    COOn-C5H114-891    H  Cl  CH3    CF3    H    CH3    COOiC3H74-892    H  Cl  CH3    CF3    H    CH3    COOcC5H94-893    H  Cl  CH3    CF3    H    CH3    COOcC6H114-894    H  Cl  CH3    CF3    H    CH3    COOCH2CH=CH24-895    H  Cl  CH3    CF3    H    CH3    COOCH2C≡CH4-896    H  Cl  CH3    CF3    H    CH3    CONH24-897    H  Cl  CH3    CF3    H    CH3    CONHCH34-898    H  Cl  CH3    CF3    H    CH3    CONHC2H54-899    H  Cl  CH3    CF3    H    CH3    CON(CH3)24-900    H  Cl  CH3    CF3    H    CH3    CON(C2H5)24-901    F  Cl  CH3    CF3    H    CH3    CH2Cl4-902    F  Cl  CH3    CF3    H    CH3    CH2Br4-903    F  Cl  CH3    CF3    H    CH3    CH2OCH34-904    F  Cl  CH3    CF3    H    CH3    CH2OC2H5
                     表4(续)
   化合物    X  Y   R3     R1     R2  R7     R8编号
    4-905    F  Cl  CH3    CF3    H    CH3    CH2OCH2OCH34-906    F  Cl  CH3    CF3    H    CH3    CH2OCH2OC2H54-907    F  Cl  CH3    CF3    H    CH3    CH2OCOCH34-908    F  Cl  CH3    CF3    H    CH3    CH2OCOC2H54-909    F  Cl  CH3    CF3    H    CH3    CH2OCOiC3H74-910    F  Cl  CH3    CF3    H    CH3    CH2OCOCH2Cl4-911    F  Cl  CH3    CF3    H    CH3    CH2OCOCCl34-912    F  Cl  CH3    CF3    H    CH3    CH2OCOCF34-913    F  Cl  CH3    CF3    H    CH3    COOH4-914    F  Cl  CH3    CF3    H    CH3    COOCH34-915    F  Cl  CH3    CF3    H    CH3    COOC2H54-916    F  Cl  CH3    CF3    H    CH3    COOnC3H74-917    F  Cl  CH3    CF3    H    CH3    COOnC4H94-918    F  Cl  CH3    CF3    H    CH3    COOnC5H114-919    F  Cl  CH3    CF3    H    CH3    COOiC3H74-920    F  Cl  CH3    CF3    H    CH3    COOcC5H94-921    F  Cl  CH3    CF3    H    CH3    COOcC6H114-922    F  Cl  CH3    CF3    H    CH3    COOCH2CH=CH24-923    F  Cl  CH3    CF3    H    CH3    COOCH2C≡CH4-924    F  Cl  CH3    CF3    H    CH3    CONH24-925    F  Cl  CH3    CF3    H    CH3    CONHCH34-926    F  Cl  CH3    CF3    H    CH3    CONHC2H54-927    F  Cl  CH3    CF3    H    CH3    CON(CH3)2
                        表4(续)
   化合物    X  Y   R3     R1     R2  R7    R8编号
    4-928    F  Cl  CH3    CF3    H    CH3   CON(C2H5)24-929    F  Cl  CH3    CF3    H    H      CH34-930    F  Cl  CH3    CF3    H    H      CH2OH4-931    F  Cl  CH3    CF3    H    CH3   CH34-932    F  Cl  CH3    CF3    H    CH3   CH2OH4-933    H  Cl  CH3    CF3    H    H      CH34-934    H  Cl  CH3    CF3    H    H      CH2OH4-935    H  Cl  CH3    CF3    H    CH3   CH34-936    H  Cl  CH3    CF3    H    CH3   CH2OH
                     表5
下式化合物:
Figure C9619770003001
   化合物   X    R3  R1       R2     R5编号
    5-1     H    H    CF2Cl    CH3    CH35-2     H    H    CF2Cl    CH3    C2H55-3     H    H    CF2Cl    CH3   iC3H75-4     H    H    CF2Cl    CH3   nC3H75-5     H    H    CF2Cl    CH3   iC4H95-6     H    H    CF2Cl    CH3    CH2CH=CH25-7     H    H    CF2Cl    CH3    CH(CH3)CH=CH25-8     H    H    CF2Cl    CH3    CH2C≡CH5-9     H    H    CF2Cl    CH3    CH(CH3)C≡CH5-10    F    H    CF2Cl    CH3    CH35-11    F    H    CF2Cl    CH3    C2H55-12    F    H    CF2Cl    CH3   iC3H75-13    F    H    CF2Cl    CH3   nC3H75-14    F    H    CF2Cl    CH3   iC4H95-15    F    H    CF2Cl    CH3    CH2CH=CH2
                       表5(续)
   化合物   X    R3  R1       R2     R5编号
    5-16    F    H    CF2Cl    CH3    CH(CH3)CH=CH25-17    F    H    CF2Cl    CH3    CH2C≡CH5-18    F    H    CF2Cl    CH3    CH(CH3)C≡CH5-19    H    H    CF3      CH3    CH35-20    H    H    CF3      CH3    C2H55-21    H    H    CF3      CH3   iC3H75-22    H    H    CF3      CH3   nC3H75-23    H    H    CF3      CH3   iC4 -H95-24    H    H    CF3      CH3    CH2CH=CH25-25    H    H    CF3      CH3    CH(CH3)CH=CH25-26    H    H    CF3      CH3    CH2C≡CH5-27    H    H    CF3      CH3    CH(CH3)C≡CH5-28    F    H    CF3      CH3    CH35-29    F    H    CF3      CH3    C2H55-30    F    H    CF3      CH3   iC3H75-31    F    H    CF3      CH3   iC4H95-32    F    H    CF3      CH3    CH2CH=CH25-33    F    H    CF3      CH3    CH(CH3)CH=CH25-34    F    H    CF3      CH3    CH2C≡CH5-35    F    H    CF3      CH3    CH(CH3)C≡CH5-36    H    H    CF2Cl    H       CH35-37    H    H    CF2Cl    H       C2H55-38    H    H    CF2Cl    H      iC3H7
                    表5(续)
   化合物   X    R3  R1       R2  R5编号
    5-39    H    H    CF2Cl    H   nC3H75-40    H    H    CF2Cl    H   iC4H95-41    H    H    CF2Cl    H    CH2CH=CH25-42    H    H    CF2Cl    H    CH(CH3)CH=CH25-43    H    H    CF2Cl    H    CH2C≡CH5-44    H    H    CF2Cl    H    CH(CH3)C≡CH5-45    F    H    CF2Cl    H    CH35-46    F    H    CF2Cl    H    C2H55-47    F    H    CF2Cl    H   iC3H75-48    F    H    CF2Cl    H   nC3H75-49    F    H    CF2Cl    H   iC4H95-50    F    H    CF2Cl    H    CH2CH=CH25-51    F    H    CF2Cl    H    CH(CH3)CH=CH25-52    F    H    CF2Cl    H    CH2C≡CH5-53    F    H    CF2Cl    H    CH(CH3)C≡CH5-54    H    H    CF3      H    CH35-55    H    H    CF3      H    C2H55-56    H    H    CF3      H   iC3H75-57    H    H    CF3      H   nC3H75-58    H    H    CF3      H   iC4H95-59    H    H    CF3      H    CH2CH=CH25-60    H    H    CF3      H    CH(CH3)CH=CH25-61    H    H    CF3      H    CH2C≡CH
                      表5(续)
   化合物   X    R3     R1     R2  R5编号
    5-62    H    H       CF3    H    CH(CH3)C≡CH5-63    F    H       CF3    H    CH35-64    F    H       CF3    H    C2H55-65    F    H       CF3    H   iC3H75-66    F    H       CF3    H   iC4H95-67    F    H       CF3    H    CH2CH=CH25-68    F    H       CF3    H    CH(CH3)CH=CH25-69    F    H       CF3    H    CH2C-≡CH5-70    F    H       CF3    H    CH(CH3)C≡CH5-71    H    CH3    CF3    H    CH35-72    H    CH3    CF3    H    C2H55-73    H    CH3    CF3    H   iC3H75-74    H    CH3    CF3    H   nC3H75-75    H    CH3    CF3    H   iC4H95-76    H    CH3    CF3    H    CH2CH=CH25-77    H    CH3    CF3    H    CH(CH3)CH=CH25-78    H    CH3    CF3    H    CH2C≡CH5-79    H    CH3    CF3    H    CH(CH3)C≡CH5-80    F    CH3    CF3    H    CH35-81    F    CH3    CF3    H    C2H65-82    F    CH3    CF3    H   iC3H75-83    F    CH3    CF3    H   iC4H95-84    F    CH3    CF3    H    CH2CH=CH2
                   表5(续)
   化合物   X    R3     R1     R2  R5编号
    5-85    F    CH3    CF3    H    CH(CH3)CH=CH25-86    F    CH3    CF3    H    CH2C≡CH5-87    F    CH3    CF3    H    CH(CH3)C≡CH
本发明化合物的物理性质(熔点,m.p)或1H-NMR(250 or 300MHz,CDCl3,TMS,δ(ppm))数据表示如下:
         化合物1-332,m.p.97.0℃
         化合物1-335,m.p.80.8℃
         化合物1-337,m.p.91.5℃
         化合物1-338,m.p.86.1℃
         化合物1-344,m.p.94.2℃
         化合物1-347,m.p.80.7℃
         化合物1-350,2.41(3H,q,J=1.8Hz),4.05-4.35(2H,b),6.87-6.94(1H,m),7.03(1H,d,J=2.4Hz),7.33(1H,d,J=8.5Hz),7.98(1H,s)
         化合物1-353,m.p.124.0℃
         化合物1-367,2.44(3H,q,J=1.9Hz),3.04(3H,s),6.88(1H,s),7.37(1H,d,J=9.0Hz),7.79(1H,d,J=7.0Hz),8.01(1H,s)
         化合物1-369,2.44(3H,q,J=2.0Hz),4.57(2H,s),7.06(1H,s),7.38(1H,d,J=9.0Hz),7.83(1H,d,J=6.9Hz),8.01(1H,s)
         化合物1-391,m.p.177.6℃
         化合物1-392,m.p.172.5℃
         化合物1-398,m.p.133.1℃
         化合物1-420,1.25(3H,t,J=7.5Hz),1.51(3H,d,J=7.0Hz),2.42(3H,q,J=1.8Hz),4.0-4.18(3H,m),4.82(1H,d,J=7.9Hz),6.59(1H,d,J=6.3Hz),7.23(1H,d,J=9.3Hz),7.97(1H,s)
         化合物1-429,1.40(6H,d,J=6.3Hz),2.43(3H,q,J=2.4Hz),4.52-4.63(1H,m),7.14(0.5H,d,J=2.4Hz),7.17(0.5H,d,J=2.4Hz),7.24(1H,d,J=3.6Hz),7.29(1H,s),7.46(1H,d,J=8.4Hz)
         化合物1-439,m.p.110.6℃
         化合物1-449,1.29(3H,t,J=7.5Hz),2.42(3H,q,J=2.4Hz),4.28(2H,q,J=7.5Hz),4.73(2H,s),7.20-7.32(2H,m),7.49(1H,d,J=10.4Hz),8.00(1H,s)
         化合物1-456,1.70(3H,d,J=6.9Hz),2.41(3H,q,J=2.1Hz),3.77(3H,s),4.81(1H,q,J=6.9Hz),7.21-7.28(2H,m),7.47(1H,d,J=8.7Hz),7.99(1H,s)
         化合物1-474,m.p.110.6℃
         化合物1-475,1.46(3H,t,J=5.8Hz),2.44(3H,q,J=1.5Hz),4.07(2H,q,J=5.8Hz),6.94(1H,d,J=5.0Hz),7.29(1H,d,J=7.5Hz),8.01(1H,s)
         化合物1-476,1.38(6H,d,J=6.3Hz),2.43(3H,q,J=2.0Hz),4.47(1H,m),6.99(1H,d,J=5.0Hz),7.29(1H,d,J=9.5Hz),8.00(1H,s)
         化合物1-482,m.p.79.8℃
         化合物1-483,m.p.132.7℃
         化合物1-486,m.p.140.7℃(分解)
         化合物1-487,m.p.114.1℃
         化合物1-491,m.p.82.9℃
         化合物1-495,m.p.80.4℃
         化合物1-496,m.p.102.0℃
         化合物1-497,m.p.82.9℃
         化合物1-498,m.p.75.6℃
         化合物1-499,0.88(3H,t,J=7Hz),1.2-1.4(4H,m),1.55-1.70(2H,m),2.43(3H,q,J=2Hz),4.19(2H,t,J=7Hz),4.68(2H,s),6.98(1H,d,J=7Hz),7.33(1H,d,J=8Hz),7.99(1H,s)
         化合物1-500,1.26(6H,d,J=6.3Hz),2.43(3H,q,J=2Hz),4.65(2H,s),5.05-5.18(1H,m),6.98(1H,d,J=7Hz),7.33(1H,d,J=8Hz),7.98(1H,s)
         化合物1-501,1.5-1.9(8H,m),2.43(3H,q,J=2Hz),4.65(2H,s),5.2-5.4(1H,m),6.97(1H,d,J=7Hz),7.33(1H,d,J=8Hz),7.98(1H,s)
         化合物1-503,1.68(3H,d,J=7Hz),2.43(3H,q,J=2Hz),3.76(3H,s),4.73(1H,q,J=7Hz),6.98(1H,d,J=7Hz),7.32(1H,d,J=8Hz),7.99(1H,s)
         化合物1-504,1.25(3H,t,J=7.3Hz),1.68(3H,d,J=6.8Hz),2.42(3H,q,J=2.0Hz),4.21(2H,q,J=7.3Hz),4.70(1H,q,J=6.8Hz),6.99(1H,d,J=6.8Hz),7.32(1H,d,J=9.3Hz),7.98(1H,s)
         化合物1-511,m.p.110.7℃
         化合物1-518,m.p.131.2℃(分解)
         化合物1-576,2.43(3H,q,J=1.8Hz),3.67(2H,s),3.72(3H,s),7.32(1H,d,J=8.5Hz),7.59(1H,d,J=7.1Hz),8.2(1H,s)
         化合物1-577,1.15(3H,t,J=7.5Hz),2.36(3H,q,J=1.8Hz),3.58(2H,s),4.09(2H,q,J=7.5Hz),7.28(1H,d,J=8.6Hz),7.52(1H,d,J=7.1Hz),7.93(1H,s)
         化合物1-579,m.p.71.6℃
         化合物1-581,m.p.97.5℃
         化合物1-584,1.53(3H,d,J=7.2Hz),2.43(3H,q,J=1.8Hz),3.66(3H,s),3.88(1H,q,J=7.2Hz),7.38(1H,d,J=9.6Hz),7.66(1H,d,J=7.5Hz),7.99(1H,s)
         化合物1-585,1.17(3H,t,J=6.9Hz),1.53(3H,d,J=7.2Hz),2.43(3H,q,J=1.8Hz),3.89(1H,q,J=7.2Hz),4.11(2H,q,J=6.9Hz),7.37(1H,d,J=9.6Hz),7.67(1H,d,J=9.0Hz),7.99(1H,s)
         化合物1-586,0.85(3H,t,J=6.8Hz),1.51-1.62(5H,m),2.43(3H,q,J=1.8Hz),3.89(1H,q,J=7.2Hz),4.02(2H,t,J=6.8Hz),7.33(1H,d.J=9.5Hz),7.66(1H,d,J=7.5Hz),7.98(1H,s)
         化合物1-587,0.88(3H,t,J=7.2Hz),1.30-1.40(2H,m),1.47-1.55(5H,m),2.43(3H,q,J=1.8Hz),3.89(1H,q,J=7.1Hz),4.02-4.08(2H,m),7.36(1H,d,J=9.4Hz),7.66(1H,d,J=7.5Hz),7.99(1H,s)
         化合物1-619,2.45(3H,q,J=1.6Hz),7.60(1H,d,J=8.6Hz),7.80-7.86(1H,m),8.04(1H,s),8 36(1H,d,J=2.5Hz)
         化合物1-621,1.40(3H,t,J=7.1Hz),2.43(3H,q,J=1.8Hz),4.41(2H,q,J=7.1Hz),7.56(1H,d,J=8.6Hz),7.72-7.78(1H,m),8.02(1H,s),8.16(1H,d,J=2.7Hz)
         化合物1-625,1.39(6H,d,J=6.2Hz),2.43(3H,q,J=1.6Hz),5.23-5.28(1H,m),7.54(1H,d,J=8.7Hz),7.70-7.76(1H,m),8.02(1H,s),8.10(1H,d,J=2.6Hz)
         化合物1-632,m.p.761℃
         化合物1-637,m.p.102.8℃
         化合物1-641,2.43(3H,q,J=2.0Hz),3.92(3H,s),7.39(1H,d,J=9.5Hz),8.02(1H,s),8.07(1H,d,J=7.7Hz)
         化合物1-642,1.39(3H,t,J=7.2Hz),2.44(3H,q,J=1.9Hz),4.40(2H,q,J=7.2Hz),7.38(1H,d,J=9.5Hz),8.00-8.06(2H,m)
         化合物1-981,m.p.87.1℃
         化合物1-987,4.0-4.4(2H,b),6.8-6.9(1H,m),7.04(1H,d,J=2.4Hz),7.28(1H,q,J=1.2Hz),7.35(1H,d,J=8.6Hz),8.02(1H,d,J=2.2Hz)
         化合物1-1025,5.92(1H,s),7.16(0.5H,d,J=2.4Hz),7.19(0.5H,d,J=2.4Hz),7.30(1H,q,J=1.1Hz),7.34(1H,d,J=5.7Hz),7.43(1H,d,J=9.0Hz),8.04(1H,q,J=3.0Hz)
         化合物1-1028,m.p.180.2℃,
                       5.65-5.9(1H,br),7.09(1H,d,J=7Hz),7.27-7.30(2H,m),8.10(1H,q,J=2.2Hz)
         化合物1-1029,7.09(1H,d,J=6.4Hz),7.31(1H,q,J=1.1Hz),7.42(1H,d,J=8.8Hz),8.04(1H,q,J=2.2Hz)
         化合物1-1035,m.p.61.1℃
         化合物1-1057,m.p.158℃
         化合物1-1066,m.p.89.1℃
         化合物1-1076,m.p.113.5℃
         化合物1-1086,m.p.83.9℃
         化合物1-1093,m.p.83.1℃
         化合物1-1113,m.p.68.6℃
         化合物1-1123,m.p.147.4℃
         化合物1-1124,m.p.117.2℃
         化合物1-1133,m.p.149.2℃(分解)
         化合物1-1140,m.p.99.1℃
         化合物1-1141,m.p.80.2℃
         化合物1-1213,m.p.85.8℃
         化合物1-1214,m.p.65.1℃
         化合物1-1221,1.54(3H,d,J=7.2Hz),3.66(3H,s),3.90(1H,q,J=7.2Hz),7.31(1H,s),7.39(1H,d,J=9.0Hz),7.67(1H,d,J=8.7Hz),8.04(1H,d,J=3.6Hz)
         化合物1-1222,1.16(3H,t,J=5.1Hz),1.53(3H,d,J=7.2Hz),3.89(1H,q,J=7.2Hz),4.10(2H,q,J=5.1Hz),7.30(1H,q,J=1.1Hz),7.38(1H,d,J=9.0Hz),7 68(1H,d,J=7.5Hz),8.04(1H,q,J=2.2Hz)
         化合物1-1226,1.12(3H,d,J=6.0Hz),1.21(3H,d,J=6.0Hz),1.52(3H,d,J=3.0Hz),3.88(1H,q,J=3.0Hz),4.85-5.03(1H,m),7.30(1H,q,J=1.8Hz),7.37(1H,d,J=9.0Hz),7.67(1H,d,J=7.5Hz),8.02(1H,q,J=2.1Hz)
         化合物1-1256,7.35(1H,q,J=1.1Hz),7.62(1H,d,J=8.7Hz),7.82-7.88(1H,m),8.09(1H,d,J=2.2Hz),8.35(1H,d,J=2.6Hz)
         化合物1-1258,1.41(3H,t,J=7.1Hz),4.42(2H,q,J=7.1Hz),7.31(1H,s),7.57(1H,d,J=8.7Hz),7.74-7.79(1H,m),8.07(1H,q,J=2.1Hz),8.16(1H,d,J=2.6Hz)
         化合物1-1269,m.p.89.7℃
         化合物1-1274,m.p.154.2℃
         化合物1-1278,m.p.128.6℃
         化合物1-1279,1.40(3H,t,J=7.1Hz),4.40(2H,q,J=7.1Hz),7.33(1H,q,J=1.1Hz),7.39(1H,d,J=9.4Hz),8.05(1H,d,J=8.3Hz),8.07(1H,s)
         化合物1-1346,2.48(3H,s),5.66(1H,s),7.08(1H,d,J=7.8Hz),7.28(1H,d,J=9.0Hz),7.32(1H,s)
         化合物1-1431,m.p.74.5℃
         化合物1-1441,m.p.128.2℃
         化合物1-1442,1.73(3H,d,J=6.6Hz),2.49(3H,q,J=1.3Hz),2.54(1H,d,J=2.0Hz),4.84(1H,m),7.22(1H,d,J=6.5Hz),7.28-7.34(2H,m)
         化合物1-1451,1.29(3H,t,J=7.0Hz),2.47(3H,q,J=1.4Hz),4.27(2H,q,J=7.0Hz),4.68(2H,s),6.99(1H,d,J=7.1Hz),7.32(1H,s),7.34(1H,d,J=7.2Hz)
         化合物1-1458,1.69(3H,d,J=6.8Hz),2.48(3H,q,J=1.3Hz),3.76(3H,s),4.74(1H,q,J=6.8Hz),7.01(1H,d,J=6.5Hz),7.29-7.34(2H,m)
         化合物1-1540,1.17(3H,t,J=7.0Hz),1.54(3H,d,J=7.3Hz),2.48(3H,q,J=1.4Hz),3.89(1H,q,J=7.3Hz),4.11(2H,q,J=7.0Hz),7.31(1H,s),7.37(1H,d,J=9.5Hz),7.67(1H,d,J=7.5Hz)
         化合物1-1617,m.p.105.7℃
         化合物1-1622,1.27(3H,t,J=7.0Hz),2.42(3H,q,J=2.0Hz),3.26(0.3H,d,J=7.6Hz),3.32(0.7H,d,J=7.6Hz),3.49(0.7H,d,J=7.6Hz),3.54(0.3H,d,J=7.6Hz),4.23(2H,q,J=7.0Hz),4.54(0.5H,d,J=7.6Hz),4.57(0.5H,d,J=7.6Hz),7.34(1H,d,J=9.3Hz),7.40(1H,d,J=7.5Hz),8.00(1H,s)
         化合物1-1627,m.p.182.2℃
         化合物1-1638,3.66(2H,s),7.31(1H,s),7.34(1H,d,J=9.3Hz),7.62(1H,d,J=7.2Hz),8.08(1H,s)
         化合物1-1639,m.p.158.9℃(分解)
         化合物1-1641,1.55(3H,d,J=7.2Hz),3.88(1H,q,J=7.2Hz),7.32(1H,s),7.37(1H,d,J=9.2Hz),7.69(1H,d,J=7.1Hz),8.03(1H,s)
         化合物1-1650,1.11(3H,t,J=7.5Hz),2.03-2.12(2H,m),2.43(3H,q,J=1.8Hz),3.75(3H,s),4.58(1H,t,J=7.5Hz),6.92(1H,d,J=8.2Hz),7.32(1H,d,J=9.3Hz),8.00(1H,s)
         化合物1-1655,m.p.119.7℃,
                       1.29(3H,t,J=7.1Hz),2.43(3H,q,J=1.8Hz),4.26(2H,q,J=7.1Hz),4.68(2H,s),6.91(1H,s),7.60(1H,s),7.99(1H,s)
         化合物1-1663,m.p.136.2℃,
                       2.44(3H,q,J=1.8Hz),2.58(1H,t,J=2.3Hz),4.78(2H,d,J=2.3Hz),7.12(1H,s),7.59(1H,s),8.01(1H,s)
         化合物1-1665,1.23(3H,t,J=6.9Hz),1.68(3H,d,J=6.8Hz),2.42(3H,q,J=1.8Hz),4.1-4.3(2H,m),4.72(1H,q,J=6.8Hz),6.90(1H,s),7.58(1H,s),7.97(1H,s)
         化合物1-1670,m.p.118.1℃
         化合物1-1673,m.p.107.2℃
         化合物1-1678,m.p.164.7℃
         化合物1-1679,1.73(3H,d,J=6.9Hz),2.54(1H,d,J=2.1Hz),4.73-4.90(1H,m),7.20(1H,d,J=6.3Hz),7.30(1H,s),7.49(1H,d,J=8.7Hz),8.00(1H,s)
         化合物1-1680,m.p.90.1℃
         化合物1-1681,m.p.148.1℃
         化合物1-1682,m.p.107.0℃
         化合物1-1683,1.25(3H,t,J=7.2Hz),1.68(3H,d,J=6.8Hz),2.42(3H,q,J=1.5Hz),4.13-4.26(2H,m),4.70(1H,q,J=6.8Hz),6.96(1H,d,J=6.3Hz),7.48(1H,d,J=9.0Hz),7.97(1H,s)
         化合物1-1687,m.p.200.1℃
         化合物1-1689,m.p.76.3℃
         化合物1-1690,m.p.196.1℃
         化合物1-1691,3.06(3H,s),7.10-7.30(1H,b),7.30(1H,s),7.64(1H,s),7.74(1H,s),8.06(1H,q,J=2.1Hz)
         化合物1-1701,1.39(3H,t,J=7.1Hz),4.40(2H,q,J=7.1Hz),7.33(1H,q,J=1.1Hz),7.69(1H,s),7.97(1H,s),8.06(1H,q,J=2.2Hz)
         化合物1-1718,m.p.63.9℃
         化合物1-1719,m.p.189.5℃
         化合物1-1720,m.p.117.3℃
         化合物1-1721,m.p.156.1℃
         化合物1-1722,2.47(3H,q,J=1.8Hz),3.05(3H,s),7.15-7.30(1H,b),7.66(1H,s),7.78(1H,s),8.03(1H,s)
         化合物1-1732,1.38(3H,t,J=7.1Hz),2.44(3H,q,J=1.8Hz),4.39(2H,q,J=7.1Hz),7.68(1H,s),7.96(1H,s),8.02(1H,s)
         化合物1-1748,1.38(6H,d,J=6.0Hz),2.44(3H,q,J=1.9Hz),4.40-4.59(1H,m),6.95(1H,s),7.55(1H,s),8.00(1H,s)
         化合物1-1780,m.p.76.4℃
         化合物1-1781,3.51(3H,s),3.51(3H,s),7.30(1H,q,J=1.2Hz),7.59(1H,d,J=6.7Hz),7.65(1H,d,J=9.0Hz),8.06(1H,d,J=2.1Hz)
         化合物1-1782,3.03(3H,s),7.09(1H,s),7.32(1H,q,J=1.0Hz),7.53(1H,d,J=8.7Hz),7.77(1H,d,J=6.8Hz),8.07(1H,q,J=2.2Hz)
         化合物1-1783,1.38(6H,d,J=6.1Hz),2.43(3H,q,J=1.7Hz),4.4-4.6(1H,m),6.95(1H,d,J=6.4Hz),7.47(1H,d,J=8.9Hz),8.00(1H,s)
         化合物1-1785,2.43(3H,q,J=1.9Hz),3.03(3H,s),7.03(1H,s),7.52(1H,d,J=8.8Hz),7.76(1H,d,J=6.9Hz),8.02(1H,s)
         化合物1-1789,m.p.78.3℃
         化合物1-1790,m.p.63.2℃
         化合物1-1879,2.42(3H,q,J=1.8Hz),5.38(2H,s),7.28-7.47(5H,m),7.56(1H,d,J=8.7Hz),7.72-7.79(1H,m),8.00(1H,s),8.18(1H,d,J=2.5Hz)
         化合物1-1881,2.20(0.75H,s),2.24(2.25H,s),2.42(3H,q,J=1.9Hz),3.82(0.75H,s),3.98(2.25H,s),7.47-7.68(3H,m),8.00(1H,s)
         化合物1-1901,m.p.99.2℃
        化合物1-1908,m.p.77.6℃
        化合物1-1910,m.p.75.3℃
        化合物1-1930,m.p.139.7℃
        化合物1-2051,1.25(3H,t,J=7.2Hz),2.42(3H,q,J=1.9Hz),4.17(2H,q,J=7.2Hz),4.71(2H,s),4.82(2H,s),7.10(1H,d,J=6.3Hz),7.33(1H,d,J=9.1Hz),7.99(1H,s)
        化合物1-2054,1.24(3H,t,J=7.1Hz),1.51(3H,d,J=7.2Hz),2.42(3H,q,J=1.8Hz),4.15(2H,q,J=7.1Hz),4.78(2H,s),5.19(1H,q,J=7.2Hz),7.08(1H,d,J=6.3Hz),7.32(1H,d,J=9.1Hz),7.98(1H,s)
        化合物2-203,2.3-2.4(1H,m),2.35(3H,q,J=1.9Hz),4.5-4.7(4H,m),7.00(1H,d,J=6.5Hz),7.19(1H,m),7.39(1H,d,J=2.5Hz),7.95(1H,s)
        化合物2-251,m.p.168.3℃
        化合物2-328,0.90(3H,t,J=7.3Hz),1.54(3H,d,J=7.0Hz),1.70-1.90(2H,m),2.46(3H,m),4.50(1H,m),7.18(1H,d,J=5.75Hz),7.35(1H,d,J=8.8Hz),8.04(1H,s)
        化合物2-583,m.p.149.1℃
        化合物2-631,m.p.168.3℃
        化合物2-708,0.90(3H,t,J=7.3Hz),1.55(3H,d,J=7.0Hz),1.75-1.95(2H,m),4.50(1H,m),7.22(1H,d,J=5.8Hz),7.30-7.40(2H,m),8.08(1H,q,J=2.2Hz)
        化合物2-821,m.p.162.7℃
        化合物3-139,m.p.88.2℃
        化合物4434,1.67(3H,s),2.35(3H,q,J=1.7Hz),3.0-3.2(1H,m),3 4-3.7(1H,m),3.71(3H,s),7.03(1H,d,J=5.0Hz),7.97(1H,q,J=3.3Hz)
        化合物4-451,1.53(6H,s),2.43(3H,q,J=1.9Hz),2.96(1H,d,J=16.2Hz),3.08(1H,d,J=16.2Hz),7.07(1H,d,J=9.9Hz),7.99(1H,s)
        化合物4-452,1.4-1.5(3H,m),2.43(3H,q,J=2.0Hz),2.7-3.0(1H,m),3.1-3.5(1H,m),3.5-3.8(2H,m),7.07(1H,d,J=10.0Hz),8.00(1H,q,J=2.5Hz)
下面描述制剂实施例,其中本发明化合物用表1-5中所给出的各化合物编号表示,而且所有份数均按重量计。
制剂实施例1
将50份化合物1-1至1-2157,2-1至2-950,3-1至3-582,4-1至4-936和5-1至5-87中的任一种化合物,3份木质素磺酸钙,2份十二烷基硫酸钠,以及45份合成水合氧化硅均匀粉碎并一同混合,得到各化合物的可湿性粉剂。
制剂实施例2
将10份化合物1-1至1-2157,2-1至2-950,3-1至3-582,4-1至4-936和5-1至5-87中的任一种化合物与14份聚氧乙烯苯乙烯基苯基醚,6份十二烷基苯磺酸钙,35份二甲苯,和35份环己酮充分混合,得到各化合物的的乳油制剂。
制剂实施例3
将2份化合物1-1至1-2157,2-1至2-950,3-1至3-582,4-1至4-936和5-1至5-87中的任一种化合物,2份合成水合二氧化硅,2份木质素磺酸钙,30份膨润土,和64份高岭土充分粉碎并一同混合,向其中加入水,充分捏合混合物,成粒并干燥,得到各化合物的颗粒剂。
制剂实施例4
将25份化合物1-1至1-2157,2-1至2-950,3-1至3-582,4-1至4-936和5-1至5-87中的任一种化合物与50份10%聚乙烯醇水溶液,和25份水一同混合,并粉化混合物至平均粒径小于或等于5μm,得到各化合物的流动剂。
制剂实施例5
将5份化合物1-1650加到40份10%聚乙烯醇水溶液中,并用均化器分散乳液至平均粒径小于或等于10μm,加入55份水,得到浓乳剂。
下述试验实施例将证明本发明化合物可用作除草剂的活性成分。本发明化合物用表1-5中所示的相应的化合物编号表示。
除草活性和植物毒性用指标0-5分6个等级评价,即用数字“0”,“1”,“2”,“3”,“4”或“5”表示,其中“0”是指在试验情况下处理与未处理测试植物之间的发芽或生长程度没有任何差别或只有很小差别,而“5”是指测试植物完全死亡或其发芽或生长被完全抑制。当评定等级为“4”或“5”时,表明除草活性优良,但当评定等级为“3”或更低时,则表示除草活性不足。植物毒性当评定等级为“0”或“1”时,则表示实际应用时是可以耐受的,但当评定等级为“2”或更高级时,则表示不能耐受。
试验实施例1:旱田叶面处理
将直径10cm,深10cm的圆筒性塑料盆中填上土壤,在土壤中播种全叶裂叶牵牛(Ipomoea hederacea var.integriuscula)和苘麻(Abutilon theophrasti)的种子,并将试验植物在温室中生长19天。按照制剂实施例2,将下面所列的每种受试化合物配制成乳油,用含有分散剂的水稀释到预定浓度。利用喷雾器,以每公顷1000升的体积将稀释液均匀喷雾到受试植物的叶面上。喷雾完后,使试验植物在温室中生长19天,测定除草活性。结果示于表6中。
                               表6
     试验化合物 活性成分的施用量(g/ha)            除草活性
全叶裂叶牵牛    苘麻
    1-3321-3351-3381-3471-3501-3531-3671-3691-3911-3921-3981-4201-4291-4391-4491-4561-4741-4751-4761-4821-4831-4861-4871-4911-4951-4961-4971-4981-4991-5001-5011-5031-5041-5111-5761-5771-5791-5811-5841-5851-5861-5871-6191-6211-6251-6371-6411-642     500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500     555555555555555555555555555555555555555555555555     555555555555555555555555555555555555555555555555
                               表6(续)
     试验化合物 活性成分的施用量(g/ha)          除草活性
全叶裂叶牵牛    苘麻
    1-9871-10251-10281-10291-10351-10571-10661-10761-10861-10931-11131-11231-11241-11331-11401-11411-12131-12141-12211-12221-12261-12741-12781-12791-14221-14311-14411-14511-14581-15401-16171-16221-16271-16381-16391-16411-16501-16551-16631-16651-16701-16731-16781-16791-16801-16811-16821-1683     500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500     555555555555555555555555555555555555555555555555     555555555555555555555555555555555555555555555555
                                表6(续)
试验化 活性成分的施用量(g/ha)            除草活性
全叶裂叶牵牛    苘麻
    1-16911-17011-17181-17191-17221-17321-17481-17801-17811-17821-17831-17852-2032-2512-3282-5832-6312-7082-8213-1394-4344-4511-3441-9811-16891-17201-1721     50050050050050050050050050050050050050050050050050050050050050050020002000200020002000     555555555555555555555555555     555555555555555555555555555
试验实施例2:旱田叶面处理
在直径10cm,深10cm的圆筒性塑料盆中填上土壤,在土壤中播种稗草(Echinochloa crus-galli),全叶裂叶牵牛(Ipomoea hederacea var.integriuscula)和苘麻(Abutilon theophrasti)的种子,并将试验植物在温室中生长19天。按照制剂实施例2,将下面所列的每种受试化合物配制成乳油,用含有分散剂的水稀释到预定浓度。利用喷雾器,以每公顷1000升的体积将稀释液均匀喷雾到受试植物的叶面上。喷雾完后,使试验植物在温室中生长19天,测定除草活性。结果示于表7中。
                                  表7
   试验化合物 活性成分的施用量(g/ha)              除草活性
   稗草 全叶裂叶牵牛    苘麻
  1-3691-4201-4391-4821-4861-4871-4911-4951-4961-4991-5031-5761-5771-5791-5811-5841-5851-6251-6411-6421-10571-10761-11231-11241-11401-11411-12131-12141-12211-12221-12261-12791-14221-14311-14411-14581-15401-16651-16701-16731-16781-16791-16801-16811-16821-16831-17011-1732     323232323232323232323232323232323232323232323232323232323232323232323232323232323232323232323232     554545555555555555555445545555555555555555555555     555555555555555555555555555555555555555555555555     555555555555555555555555555555555555555555555555
                                  表7(续)
  试验化合物 活性成分的施用量(g/ha)          除草活性
   稗草 全叶牛裂叶牵    苘麻
    1-17801-17832-2032-2512-5832-6312-8214-434     3232323232323232     55454555     55555555     55555555
试验实施例3:旱田土壤表面处理
将直径10cm,深10cm的圆筒性塑料盆中填上土壤,在土壤中播种全叶裂叶牵牛(Ipomoea hederacea var.integriuscula)和苘麻(Abutilon theophrasti)的种子。按照制剂实施例2,将下面所列的每种受试化合物配制成乳油,用水稀释到预定浓度。利用喷雾器,以每公顷1000升的体积将稀释液均匀喷雾到盆中的土壤表面上。喷雾完后,使试验植物在温室中生长19天,测定除草活性。结果示于表8中。
                       表8
  试验化合物 活性成分的施用量(g/ha)           除草活性
全叶裂叶牵牛    苘麻
    1-3471-3321-3351-3381-3531-3671-3691-3911-392     500500500500500500500500500     555555555     555555555
                               表8(续)
     试验化合物 活性成分的施用量(g/ha)              除草活性
全叶裂叶牵牛    苘麻
    1-3981-4201-4391-4491-4561-4741-4751-4761-4821-4861-4871-4911-4951-4961-4971-4981-4991-5001-5011-5031-5041-5111-5761-5771-5791-5811-5841-5851-5871-6211-6251-6411-6421-10281-10291-10351-10571-10661-10761-10931-11131-11231-11241-11331-11401-11411-12131-1214     500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500     555555555555555555555555555555555555555555555555     555555555555555555555555555555555555555555555555
                               图8(续)
     试验化合物 活性成分的施用量(g/ha)              除草活性
全叶裂叶牵牛    苘麻
    1-12211-12221-12261-12791-14221-14311-14411-14511-14581-15401-16171-16221-16271-16381-16391-16411-16501-16551-16631-16651-16701-16731-16781-16791-16801-16811-16821-16831-16911-17801-17811-17821-17831-17852-2032-2512-3282-5832-6312-7082-8214-434     500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500500     555555555555555555555555555555555555555555     555555555555555555555555555555555555555555
试验实施例4:水田漫灌处理
将直径9cm,深11cm的圆筒性塑料盆中填上土壤,在土壤中播种上稗草(Echinochloa oryzicola)的种子。将这些盆灌上水形成水田,并使受试植物在温室中生长7天。按照制剂实施例2,将下面所列的每种受试化合物配制成乳油,用水稀释到预定浓度。以每公顷50升的体积将稀释液施加到盆中的水表面。施加完之后,使试验植物在温室中生长19天,测定除草活性。结果示于表9中。
                         表9
  试验化合物 活性成分的施用量(g/ha)  除草活性
   稗草
    1-3321-3351-3381-3471-3531-3671-3691-3911-3921-3981-4201-4391-4491-4561-4741-4751-4761-4821-4831-4861-4871-4911-4951-4961-4971-4981-499     250250250250250250250250250250250250250250250250250250250250250250250250250250250     555555555555555555555555555
                     表9(续)
     试验化合物 活性成分的施用量(g/a)  除草活性
   稗草
    1-5001-5011-5031-5041-5111-5761-5771-5791-5811-5841-5851-5861-5871-6211-6251-6411-6421-10251-10281-10291-10351-10571-10661-10761-10861-10931-11131-11231-11241-11331-11401-11411-12131-12141-12211-12221-12261-12741-12781-12791-14221-14311-14411-14511-14581-15401-16171-16221-1627     250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250     5555555555555555555555555555555555555555555555555
                        表9(续)
     试验化合物 活性成分的施用量(g/ha) 除草活性
  稗草
    1-16381-16391-16411-16501-16551-16631-16651-16701-16731-16781-16791-16801-16811-16821-16831-16871-16911-17011-17181-17191-17221-17321-17481-17801-17811-17821-17831-17852-2032-2512-3282-5832-6312-7082-8213-1394-4344-4511-3441-16901-17201-1721     250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250250500500500500     555555555555555555555555555555555555555555
试验实施例5:旱田叶面处理
将面积25×18cm2,深7cm的塑料盆中填上土壤,并在土壤中播种大豆(Glycine max),玉米(Zea mays),全叶裂叶牵牛(Ipomoeahederacea var.integriuscula),宾州苍耳(Xanthium pensylyanicum),美洲豚草(Ambrosia artemisiifolia),和藜(Chenopodium album)的种子,并使受试植物生长16天。按照制剂实施例2,将下面所列的每种受试化合物配制成乳油,用水稀释到预定浓度。以每公顷1000升的体积将稀释液均匀喷雾到受试植物的叶面上。此时,由于它们的生长随杂草植物种类不同而处于不同阶段,因此这些有害杂草和作物为1-至4-叶期,植物高度为5-20cm。施药后18天,测定除草活性和植物毒性。结果示于表10中。此试验的整个周期在温室中进行。
                            表10
试验化合物  活性成分施用量(g/ha)       除草活性和植物毒性
  玉米   大豆 宾州苍耳  全叶裂叶牵牛 美州豚草    藜
  1-4951-4961-4991-5031-577     6363636363    11111    11122     55555     55555     55555     55455
试验实施例6:旱田叶面处理
将面积16×11cm2,深7cm的塑料盆中填上土壤,并在土壤中播种小麦(Triticum aestiyum),酸模叶蓼(Polygonum lapathifolium),猪殃殃(Galium aparine),和繁缕(Stellaria media)的种子,并使受试植物生长29天。按照制剂实施例2,将下面所列的每种受试化合物配制成乳油,用水稀释到预定浓度。以每公顷1000升的体积将稀释液均匀喷雾到受试植物的叶面上。此时,由于它们的生长随植物种类不同而处于不同阶段,因此这些有害杂草和作物为1-至4-叶期,植物高度为5-15cm。施药后25天,测定除草活性和植物毒性。结果示于表11中。此试验的整个周期在温室中进行。
                             表11
试验化合物  活性成分施用量(g/ha)         除草活性和植物毒性
  小麦 酸模叶蓼  猪殃殃   繁缕
  1-4391-4821-4861-4961-10761-11231-1441     63636363636363     1110111     5554555     5555555     5554555
试验实施例7:旱田土壤表面处理
将面积25×18cm2,深7cm的塑料盆中填上土壤,并在土壤中播种大豆(Glycine max),玉米(Zeamays),藜(Chenopodium album),绿苋(Amaranthus gracilis),和酸模叶蓼(Polygonum lapathifolium)的种子。按照制剂实施例2,将下面所列的每种受试化合物配制成乳油,用水稀释到预定浓度。以每公顷1000升的体积将稀释液均匀喷雾到盆中的土壤表面上。喷雾完后,使试验植物在温室中生长19天,测定除草活性和植物毒性。结果示于表12中。
                            表12
试验化合物 活性成分的施用量(g/ha)                除草活性和植物毒性
  大豆   玉米    藜   绿苋   叶蓼酸模
  1-5111-6421-12791-16912-2032-631     636363636363     110021     001123     555555     555555     555555

Claims (50)

1.式[1]化合物:其中R1为C1-C3卤代烷基;R2和R3相同或不同,并且为氢,C1-C3烷基,C1-C3卤代烷基,或C1-C3烷氧基C1-C3烷基;以及Q为下列式[Q-1]:
             [Q-1]其中X为氢或卤素;
Y为卤素,硝基,氰基,或三氟甲基;
Z1为氧,硫或NH;
Z2为氧或硫;
n为0或1;
B为氢,卤素,硝基,氰基,氯磺酰基,OR10,SR10,SO2OR10,N(R11)R12,SO2N(R11)R12,NR11(COR13),NR11(SO2R14),N(SO2R14)(SO2R15)N(SO2R14)(COR13),NHCOOR13,COOR10,CON(R11)R12,CSN(R11)R12,COR16,CR17=CR18COR16,CR17=CR18COOR13,CR17=CR18CON(R11)R12,CH2CHWCOOR13,CH2CHWCON(R11)R12,CR17=NOR33,CR17=NN(R11)R12,CR17(Z2R34)2,OCO2R19,或OCOR19
R4为氢或C1-C3烷基;
R5为氢,C1-C6烷基,C1-C6卤代烷基,C3-C8环烷基烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,氰基C1-C6烷基,C2-C8烷氧基烷基,C3-C8烷氧基烷氧基烷基,羧基C1-C6烷基,(C1-C6烷氧基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基,(C3-C8环烷氧基)羰基C1-C6烷基,CH2CON(R11)R12,CH2COON(R11)R12,CH(C1-C4烷基)CON(R11)R12,CH(C1-C4烷基)COON(R11)R12,C2-C8烷硫基烷基,或羟基C1-C6烷基;
R6为C1-C6烷基,C1-C6卤代烷基,甲酰基,氰基,羧基,羟基C1-C6烷基,C1-C6烷氧基C1-C6烷基,C1-C6烷氧基C1-C6烷氧基C1-C6烷基,(C1-C6烷基)羰氧基C1-C6烷基,(C1-C6卤代烷基)羰氧基C1-C6烷基,(C1-C6烷氧基)羰基,或(C1-C6烷基)羰基;
R7为氢或C1-C6烷基;和
R8为氢,C1-C6烷基,C1-C6卤代烷基,羟基C1-C6烷基,C2-C8烷氧基烷基,C3-C18烷氧基烷氧基烷基,(C1-C5烷基)羰氧基C1-C6烷基,(C1-C6卤代烷基)羰氧基C1-C6烷基,羧基,羧基C1-C6烷基,(C1-C8烷氧基)羰基,(C1-C6卤代烷氧基)羰基,(C3-C10环烷氧基)羰基,(C3-C8链烯氧基)羰基,(C3-C8炔氧基)羰基,氨基羰基,(C1-C6烷基)氨基羰基,二(C1-C6烷基)氨基羰基,(C1-C6烷基)氨基羰氧基C1-C6烷基,或二(C1-C6烷基)氨基羰氧基C1-C6烷基;
其中R10为氢,C1-C6烷基,C1-C6卤代烷基,C3-C8环烷基,苄基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,氰基C1-C6烷基,C2-C8烷氧基烷基,C2-C8烷硫基烷基,羧基C1-C6烷基,(C1-C8烷氧基)羰基C1-C6烷基,(C1-C6卤代烷氧基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基,(C3-C8环烷氧基)羰基C1-C6烷基,(C1-C6烷基)羰基C1-C6烷基,(C1-C6卤代烷基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷基}羰基C1-C6烷基,(C3-C8环烷基)羰基C1-C6烷基,CH2CON(R11)R12,CH2COON(R11)R12,CH(C1-C4烷基)CON(R11)R12,CH(C1-C4烷基)COON(R11)R12,{(C1-C6烷氧基)羰基C1-C6烷基}氧羰基C1-C6烷基,或羟基C1-C6烷基;
R11和R12独立地为氢,C1-C6烷基,C1-C6卤代烷基,C3-C6链烯基,C3-C6炔基,氰基C1-C6烷基,C2-C8烷氧基烷基,C2-C8烷硫基烷基,羧基C1-C6烷基,(C1-C6烷氧基)羰基C1-C6烷基,(C3-C8环烷氧基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基,或者R11和R12一同结合形成四亚甲基,五亚甲基,或3-氧杂-1,5-亚戊基;
R13为氢,C1-C6烷基,C1-C6卤代烷基,C3-C8环烷基,或C3-C6链烯基;
R14和R15独立地为C1-C6烷基,C1-C6卤代烷基,或被甲基或硝基任选取代的苯基;
R16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,C2-C8烷氧基烷基,或羟基C1-C6烷基;
R17和R18独立地为氢或C1-C6烷基;
R19为C1-C6烷基;
R33为氢,C1-C6烷基,C1-C6卤代烷基,C3-C8环烷基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,氰基C1-C6烷基,或(C1-C6烷氧基)羰基C1-C6烷基;
R34为C1-C6烷基,或者两个R34一同结合形成(CH2)2或(CH2)3;和
W为氢,氯,或溴。
2.根据权利要求1的化合物,其中R1为三氟甲基。
3.根据权利要求1的化合物,其中R2为氢或C1-C3烷基,以及R3为氢或C1-C3烷基。
4.根据权利要求1的化合物,其中R1为三氟甲基,R2为氢或C1-C3烷基,以及R3为氢或C1-C3烷基。
5.根据权利要求1,2,3,或4的化合物,其中Q为[Q-1]。
6.根据权利要求5的化合物,其中B为OR10
7.根据权利要求5的化合物,其中B为SR10
8.根据权利要求5的化合物,其中B为N(R11)R12
9.根据权利要求5的化合物,其中B为NR11(SO2R14)。
10.根据权利要求5的化合物,其中B为COOR10
11.根据权利要求5的化合物,其中X为氟且Y为氯。
12.根据权利要求5的化合物,其中X为氟,Y为氯,以及B为OR10
13.根据权利要求1的化合物,所述化合物为2-(4-氯-2-氟-5-异丙氧基苯基)-4-甲基-5-三氟甲基哒嗪-3-酮(化合物1-476)。
14.根据权利要求1的化合物,所述化合物为2-(4-氯-2-氟-5-甲氧基苯基)-4-甲基-5-三氟甲基哒嗪-3-酮(化合物1-474)。
15.根据权利要求1的化合物,所述化合物为2-(4-氯-2-氟-5-乙氧基苯基)-4-甲基-5-三氟甲基哒嗪-3-酮(化合物1-475)。
16.根据权利要求1的化合物,所述化合物为2-(4-氯-2-氟-5-丙炔氧基苯基)-4-甲基-5-三氟甲基哒嗪-3-酮(化合物1-486)。
17.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸甲酯(化合物1-495)。
18.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸乙酯(化合物1-496)。
19.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸丙酯(化合物1-497)。
20.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸异丙酯(化合物1-500)。
21.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸丁酯(化合物1-498)。
22.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸戊酯(化合物1-499)。
23.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯氧基乙酸环戊酯(化合物1-501)。
24.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯氧基}丙酸乙酯(化合物1-504)。
25.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯氧基}丙酸甲酯(化合物1-503)。
26.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)-苯硫基乙酸乙酯(化合物1-577)。
27.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯硫基乙酸甲酯(化合物1-576)。
28.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯硫基}丙酸乙酯(化合物1-585)。
29.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯硫基}丙酸甲酯(化合物1-584)。
30.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)-苯氧基}丙酸甲酯(化合物1-1140)。
31.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)苯氧基}丙酸乙酯(化合物1-1141)。
32.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)苯硫基乙酸乙酯(化合物1-1214)。
33.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)苯硫基乙酸甲酯(化合物1213)。
34.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)苯硫基}丙酸乙酯(化合物1-1222)。
35.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)苯硫基}丙酸甲酯(化合物1-1221)。
36.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)苯硫基}丙酸异丙酯(化合物1-1226)。
37.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯氨基}丙酸乙酯(1-420)。
38.根据权利要求1的化合物,所述化合物为2-{2-氯-4-氟-5-(5-三氟甲基-3-哒嗪酮-2-基)苯氨基}丙酸乙酯(化合物1-1057)。
39.根据权利要求1的化合物,所述化合物为N-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯基}甲磺酰胺(化合物1-367)。
40.根据权利要求1的化合物,所述化合物为N-{2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯基}氯甲磺酰胺(化合物1-369)。
41.根据权利要求1的化合物,所述化合物为N-{2-氯-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯基}甲磺酰胺(化合物1-398)。
42.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯甲酸甲酯(化合物1-641)。
43.根据权利要求1的化合物,所述化合物为2-氯-4-氟-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯甲酸乙酯(化合物1-642)。
44.根据权利要求1的化合物,所述化合物为2-氯-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯甲酸乙酯(化合物1-621)。
45.根据权利要求1的化合物,所述化合物为2-氯-5-(4-甲基-5-三氟甲基-3-哒嗪酮-2-基)苯甲酸异丙酯(化合物1-625)。
46.根据权利要求1的化合物,所述化合物为2-(4-氯-2-氟-5-丙炔氧基苯基)-6-甲基-5-三氟甲基-哒嗪-3-酮(化合物1-1441)。
47.一种除草组合物,其中包括除草有效量权利要求1的化合物,和惰性载体或稀释剂。
48.一种防治有害杂草的方法,该方法包括对生长有或将要生长有害杂草的地区施用除草有效量权利要求1的化合物。
49.权利要求1的化合物作为除草剂的应用。
50.下式化合物:
Figure C9619770000081
其中R3的定义同权利要求1,且Q1为下式[Q1-1]:
             [Q1-1]其中X,Y,Z1,Z2,n,R4,R5,R7和R8的定义同权利要求1;
B1为氢,卤素,硝基,氰基,OR27,SR27,SO2OR27,NR11(R12),SO2NR11(R12),NR11(COR13),NR11(SO2R14),N(SO2R14)(SO2R15),N(SO2R14)(COR13),NHCOOR13,COOR27,CONR11(R12),CSNR11(R12),CR17=CR18COOR13,CR17=CR18CONR11(R12),CH2CHWCOOR13,CH2CHWCONR11(R12),CR17=NOR33,CR17=NNR11(R12),CR17(Z2R34)2,OCO2R19,或OCOR19;和
R9为C1-C6烷基,C1-C6卤代烷基,氰基,羧基,羟基C1-C6烷基,C1-C6烷氧基C1-C6烷基,C1-C6烷氧基C1-C6烷氧基C1-C6烷基,(C1-C6烷基)羰氧基C1-C6烷基,(C1-C6卤代烷基)羰氧基C1-C6烷基,(C1-C6烷氧基)羰基,或(C1-C6烷基)羰基;
其中R27为氢,C1-C6烷基,C1-C6卤代烷基,C3-C8环烷基,苄基,C3-C6链烯基,C3-C6卤代链烯基,C3-C6炔基,C3-C6卤代炔基,氰基C1-C6烷基,C2-C8烷氧基烷基,C2-C8烷硫基烷基,羧基C1-C6烷基,(C1-C8烷氧基)羰基C1-C6烷基,(C1-C6卤代烷氧基)羰基C1-C6烷基,{(C1-C4烷氧基)C1-C4烷氧基}羰基C1-C6烷基,(C3-C8环烷氧基)羰基C1-C6烷基,CH2CON(R11)R12,CH2COON(R11)R12,CH(C1-C4烷基)CON(R11)R12,CH(C1-C4烷基)COON(R11)R12,{(C1-C6烷氧基)羰基C1-C6烷基}氧羰基C1-C6烷基,或羟基C1-C6烷基;以及R11,R12,R13,R14,R15,R17,R18,R19,R33,R34,和Z2的定义同权利要求1。
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TW332202B (en) 1998-05-21
US6703503B2 (en) 2004-03-09
SK22198A3 (en) 1999-04-13
BR9609908A (pt) 1999-03-02
IL123162A0 (en) 1998-09-24
CO4750760A1 (es) 1999-03-31
US6348628B1 (en) 2002-02-19
CA2230199A1 (en) 1997-02-27
TR199800290T2 (xx) 1998-07-21
PL325062A1 (en) 1998-07-06
ATE383344T1 (de) 2008-01-15
HUP9802304A2 (hu) 1999-01-28
EP0850227B1 (en) 2008-01-09
MX9801353A (es) 1998-07-31
KR100510028B1 (ko) 2005-10-25
CZ25698A3 (cs) 1998-06-17
EA000868B1 (ru) 2000-06-26
KR19990044024A (ko) 1999-06-25
BG102326A (bg) 1998-12-30
UA49844C2 (uk) 2002-10-15
US6090753A (en) 2000-07-18
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CA2230199C (en) 2007-09-25
NO980720D0 (no) 1998-02-20
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IL123162A (en) 2003-01-12
US20040005986A1 (en) 2004-01-08
CN1252066C (zh) 2006-04-19
DE69637405T2 (de) 2008-12-24
DE69637405D1 (de) 2008-02-21
CN1202157A (zh) 1998-12-16
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RO117915B1 (ro) 2002-09-30
HUP9802304A3 (en) 1999-04-28

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