本发明的新型环丙基肟醚具有式Ⅰ结构:其中X是N或CH;Y是O、S或NR8;
A选自氢、卤素、氰基、(C1-C12)烷基、(C1-C12)烷氧基;
Z是O、N-OR9或N-R10;
R1和R8各自独立地选自氢和(C1-C4)烷基;
R2选自氢、(C1-C12)烷基、卤代(C1-C12)烷基、(C3-C7)环烷基、卤代(C3-C7)环烷基、(C2-C8)链烯基、卤代(C2-C8)链烯基、(C2-C8)炔基、卤代(C2-C8)炔基、氰基、(C1-C4)烷氧羰基、芳基、芳烷基、杂环基和杂环基(C1-C4)烷基;
R3和R7各自独立地选自氢、(C1-C12)烷基、卤代(C1-C12)烷基、(C2-C8)链烯基、卤代(C2-C8)链烯基、(C2-C8)炔基、卤代(C2-C8)炔基、芳基、芳烷基、杂环基和杂环基(C1-C4)烷基,其条件是R3和R7中至少一个是芳基、芳烷基、杂环基或杂环基(C1-C4)烷基;
R4、R5和R6各自独立地是选自氢、(C1-C12)烷基、卤代(C1-C12)烷基、(C3-C7)环烷基、卤代(C3-C7)环烷基、(C2-C8)链烯基、卤代(C2-C8)链烯基、(C2-C8)炔基、卤代(C2-C8)炔基、卤素、氰基、(C1-C4)烷氧羰基、芳基、芳烷基、杂环基和杂环基(C1-C4)烷基;
R9选自氢、(C1-C12)烷基、卤代(C1-C12)烷基、(C3-C7)环烷基、卤代(C3-C7)环烷基、(C2-C8)链烯基、卤代(C2-C8)链烯基、(C2-C8)炔基、卤代(C2-C8)炔基、(C1-C4)烷基羰基、芳基羰基、芳烷基羰基、杂环基羰基、(C1-C4)烷氧羰基、芳基、芳烷基、杂环基和杂环基(C1-C4)烷基;
R10选自氢、(C1-C12)烷基、卤代(C1-C12)烷基、(C2-C8)链烯基、卤代(C2-C8)链烯基、(C2-C8)炔基、卤代(C2-C8)炔基、芳基、芳烷基、杂环基或杂环基(C1-C4)烷基、(C1-C4)烷基羰基和(C1-C4)烷氧羰基、芳基羰基、芳烷基羰基、杂环基羰基、(C1-C4)烷基氨基羰基、芳基氨基羰基、N-R8R9、N=CR11R12、(C1-C4)烷基磺酰基、N=环丙基、N=环丁基、N=环戊基、N=环己基和芳基磺酰基;
R11和R12各自独立地是选自氢、(C1-C12)烷基、卤代(C1-C12)烷基、(C1-C12)烷氧基、卤代(C1-C12)烷氧基、(C3-C7)环烷基、卤代(C3-C7)环烷基、(C2-C8)链烯基、卤代(C2-C8)链烯基、(C2-C8)炔基、卤代(C2-C8)炔基、氰基、(C1-C4)烷氧羰基、(C1-C4)烷基氨基、芳基、芳烷基、杂环基和杂环基(C1-C4)烷基。
上述(C1-C12)烷基、(C2-C8)链烯基、(C2-C8)炔基和(C3-C7)环烷基可任选地被多达3个选自硝基、卤代甲基、(C1-C4)烷氧羰基和氰基的取代基所取代。
除非有另外的说明,本文使用的以下术语具有下述的含义。
术语“烷基”是指1-12个碳原子的直链或支链烷基。有代表性的烷基是甲基、乙基、正丙基、异丙基、正丁基、仲丁基、异丁基、叔丁基、正戊基、异戊基、正己基、正庚基、异辛基、壬基、癸基、十一烷基、十二烷基等。术语卤代烷基是指被1-3个卤原子取代的烷基。
术语“链烯基”是指具有2-8个碳原子链长和1或2个烯键、直链或支链的烯属不饱和烃基。术语“卤代链烯基”是指被1-3个卤原子取代的链烯基。术语“炔基”是指具有2-12个碳原子链长和1或2个炔键、直链或支链的不饱和烃基。
术语“芳基”是指苯基或萘基,其可以被多达3个独立地选自于卤素、氰基、三卤甲基、苯基、苯氧基、(C1-C4)烷基、(C1-C4)烷氧基、(C1-C4)烷硫基、(C1-C4)烷基亚磺酰基、卤代(C1-C4)烷基和卤代(C1-C4)烷氧基的取代基所取代。
有代表性的芳基包括但不限于:2-氯苯基、3-氯苯基、4-氯苯基、2-氟苯基、3-氟苯基、4-氟苯基、4-溴苯基、2-甲基苯基、3-甲基苯基、4-甲基苯基、2,4-二溴苯基、3,5-二氟苯基,2,4,6-三氯苯基、2-氯萘基、3-(三氟甲基)苯基、4-(三氟甲基)苯基和2-碘-4-甲基苯基。
术语“杂环”是指含有一个、两个或三个独立地选自氧、氮和硫的杂原子、取代或未取代的不饱和6-员环,或者含有多至10原子,其中包括一个选自氧、氮和硫的杂原子在内的双环不饱和环系。术语“杂环”还指含有一个、两个或三个独立地选自氧、氮和硫的杂原子、取代或未取代的不饱和5-员环,优选含有一或两个杂原子。杂环的例子包括但不限于:2-,3-或4-吡啶基、吡嗪基、2-,4-或5-嘧啶基、哒嗪基、吡唑、三唑基、眯唑基、2-或3-噻吩基、2-或3-呋喃基、吡咯基、噁唑基、异噁唑基、噻唑基、异噻唑基、噁二唑基、噻二唑基、喹啉基和异喹啉基,如果杂环是取代的,可以有多达两个独立地选自(C1-C4)烷基、卤素、氰基、硝基和三卤甲基的取代基。
术语“芳烷基”是指具有烷基链和芳基部分的基团,其中的烷基链为1-10个碳原子且可以是直链或支链的,优选直链;芳基部分如上文所定义,形成烷基部分的终端。有代表性的芳烷基是任选取代的的苄基、苯乙基、苯丙基和苯丁基。典型的苄基基团是2-氯苄基、3-氯苄基、4-氯苄基、2-氟苄基、3-氟苄基、4-氟苄基、4-三氟甲基苄基、2,4-二氯苄基、2,4-二溴苄基、2-甲基苄基、3-甲基苄基和4-甲基苄基。典型的苯乙基基团是2-(2-氯苯基)乙基、2-(3-氯苯基)乙基、2-(4-氯苯基)乙基、2-(2-氟苯基)乙基、2-(3-氟苯基)乙基、2-(4-氟苯基)乙基、2-(2-甲基苯基)乙基、2-(3-甲基苯基)乙基、2-(4-甲基苯基)乙基、2-(4-三氟甲基苯基)乙基、2-(2,4-二氯苯基)乙基和2-(3,5-二甲氧基苯基)乙基。典型的苯丙基基团是3-苯基丙基、3-(2-氯苯基)丙基、3-(3-氯苯基)丙基、3-(4-氯苯基)丙基、3-(2,4-二氯苯基)丙基、3-(2-氟苯基)丙基、3-(3-氟苯基)丙基、3-(4-氟苯基)丙基、3-(2-甲基苯基)丙基、3-(3-甲基苯基)丙基、3-(4-甲基苯基)丙基、3-(4-三氟甲基苯基)丙基、3-(2,4-二氯苯基)丙基和3-(3,5-二甲基苯基)丙基。典型的苯丁基基团是4-苯基丁基、4-(2-氯苯基)丁基、4-(3-氯苯基)丁基、4-(4-氯苯基)丁基、4-(2-氟苯基)丁基、4-(3-氟苯基)丁基、4-(4-氟苯基)丁基、4-(2-甲基苯基)丁基、4-(3-甲基苯基)丁基、4-(4-甲基苯基)丁基和4-(2,4-二氯苯基)丁基。
卤素或卤代包括碘代、氟代、溴代和氯代基团。
由于存在C=C或C=N双键,新的通式Ⅰ化合物可以Z/E异构体混合物的制备形式获得。这些异构体可以按照常规方法分离为各独立组分。式Ⅰ的环丙烷可以得到顺式和反式异构体混合物的制备形式,该混合物可以按照常规方法分离为各独立组分。单一异构体和它们的混合物两者构成了本发明的主题,可用作杀真菌剂和杀虫剂。
本发明还包括式Ⅰ化合物的对映体、盐和配合物。
本发明的优选实施方案是式Ⅱ化合物、其对映体、盐和配合物,其中A是氢,R
1和R
2是氢或(C
1-C
4)烷基,R
3、R
4、R
5和R
6是氢,R
7是芳基、芳烷基或杂环基,Z是N-OR
9,其中R
9是(C
1-C
4)烷基,以及X和Y如上文所定义。
本发明更优选的实施方案是式Ⅲ化合物、其对映体、盐和配合物,其中(在式Ⅱ中)X是N,Y是NH,R1、R2和R9是甲基,A是氢,R7是芳基。
本发明式Ⅰ所涵盖的典型化合物包括式Ⅳ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=Z=O的式Ⅰ化合物,而且其中的R2、R3和R7如表1所定义。
表1
化合物 |
R2 |
R3 |
R7 |
1.1 |
H |
H |
Ph |
1.2 |
H |
H |
4-Cl(Ph) |
1.3 |
H |
H |
4-Br(Ph) |
1.4 |
H |
H |
4-F(Ph) |
1.5 |
H |
H |
4-OCH3(Ph) |
1.6 |
H |
H |
4-CF3(Ph) |
1.7 |
H |
H |
4-NO2(Ph) |
1.8 |
H |
H |
2,4-Cl(Ph) |
1.9 |
H |
H |
2,4-F(Ph) |
1.10 |
H |
H |
3,4-F(Ph) |
1.11 |
CH3 |
H |
Ph |
1.12 |
CH3 |
H |
2-Cl(Ph) |
1.13 |
CH3 |
H |
3-Cl(Ph) |
1.14 |
CH3 |
H |
4-Cl(Ph) |
1.15 |
CH3 |
H |
2-Br(Ph) |
1.16 |
CH3 |
H |
3-Br(Ph) |
1.17 |
CH3 |
H |
4-Br(Ph) |
1.18 |
CH3 |
H |
2-F(Ph) |
1.19 |
CH3 |
H |
3-F(Ph) |
1.20 |
CH3 |
H |
4-F(Ph) |
1.21 |
CH3 |
H |
2-OCH3(Ph) |
1.22 |
CH3 |
H |
3-OCH3(Ph) |
1.23 |
CH3 |
H |
4-OCH3(Ph) |
1.24 |
CH3 |
H |
2-CH3(Ph) |
1.25 |
CH3 |
H |
3-CH3(Ph) |
1.26 |
CH3 |
H |
4-CH3(Ph) |
1.27 |
CH3 |
H |
2-CF3(Ph) |
1.28 |
CH3 |
H |
3-CF3(Ph) |
1.29 |
CH3 |
H |
4-CF3(Ph) |
1.30 |
CH3 |
H |
2-NO2(Ph) |
1.31 |
CH3 |
H |
3-NO2(Ph) |
1.32 |
CH3 |
H |
4-NO2(Ph) |
1.33 |
CH3 |
H |
2,3-Cl(Ph) |
1.34 |
CH3 |
H |
2,4-Cl(Ph) |
1.35 |
CH3 |
H |
2,5-Cl(Ph) |
1.36 |
CH3 |
H |
2,6-Cl(Ph) |
1.37 |
CH3 |
H |
3,4-Cl(Ph) |
1.38 |
CH3 |
H |
3,5-Cl(Ph) |
1.39 |
CH3 |
H |
2,3-F(PH) |
1.40 |
CH3 |
H |
2,4-F(Ph) |
1.41 |
CH3 |
H |
2,5-F(Ph) |
1.42 |
CH3 |
H |
2,6-F(Ph) |
1.43 |
CH3 |
H |
3,4-F(Ph) |
1.44 |
CH3 |
H |
3,5-F(Ph) |
1.45 |
C2H5 |
H |
Ph |
1.46 |
C2H5 |
H |
2-Cl(Ph) |
1.47 |
C2H5 |
H |
3-Cl(Ph) |
1.48 |
C2H5 |
H |
4-Cl(Ph) |
1.49 |
C2H5 |
H |
4-Br(Ph) |
1.50 |
C2H5 |
H |
4-F(Ph) |
1.51 |
C2H5 |
H |
4-OCH3(Ph) |
1.52 |
C2H5 |
H |
4-CH3(Ph) |
1.53 |
C2H5 |
H |
4-NO2(Ph) |
1.54 |
C2H5 |
H |
2,4-Cl(Ph) |
1.55 |
C2H5 |
H |
2,4-F(Ph) |
1.56 |
正-C3H7 |
H |
Ph |
1.57 |
正-C3H7 |
H |
2-Cl(Ph) |
1.58 |
正-C3H7 |
H |
3-Cl(Ph) |
1.59 |
正-C3H7 |
H |
4-Cl(Ph) |
1.60 |
正-C3H7 |
H |
4-F(Ph) |
1.61 |
正-C3H7 |
H |
3-OCH3(Ph) |
1.62 |
正-C3H7 |
H |
4-OCH3(Ph) |
1.63 |
正-C3H7 |
H |
4-CH3(Ph) |
1.64 |
正-C3H7 |
H |
4-NO2(Ph) |
1.65 |
正-C3H7 |
H |
2,4-Cl(Ph) |
1.66 |
正-C3H7 |
H |
2,4-F(Ph) |
1.67 |
异-C3H7 |
H |
Ph |
1.68 |
异-C3H7 |
H |
2-Cl(Ph) |
1.69 |
异-C3H7 |
H |
3-Cl(Ph) |
1.70 |
异-C3H7 |
H |
4-Cl(Ph) |
1.71 |
异-C3H7 |
H |
4-Br(Ph) |
1.72 |
异-C3H7 |
H |
4-F(Ph) |
1.73 |
异-C3H7 |
H |
4-OCH3(Ph) |
1.74 |
异-C3H7 |
H |
4-CH3(Ph) |
1.75 |
异-C3H7 |
H |
4-NO2(Ph) |
1.76 |
异-C3H7 |
H |
2,4-Cl(Ph) |
1.77 |
异-C3H7 |
H |
2,4-F(Ph) |
1.78 |
正-C4H9 |
H |
Ph |
1.79 |
正-C4H9 |
H |
2-Cl(Ph) |
1.80 |
正-C4H9 |
H |
3-Cl(Ph) |
1.81 |
正-C4H9 |
H |
4-Cl(Ph) |
1.82 |
正-C4H9 |
H |
4-Br(Ph) |
1.83 |
正-C4H9 |
H |
4-F(Ph) |
1.84 |
正-C4H9 |
H |
4-OCH3(Ph) |
1.85 |
正-C4H9 |
H |
4-CH3(Ph) |
1.86 |
正-C4H9 |
H |
4-NO2(Ph) |
1.87 |
正-C4H9 |
H |
2,4-Cl(Ph) |
1.88 |
正-C4H9 |
H |
2,4-F(Ph) |
1.89 |
异-C4H9 |
H |
Ph |
1.90 |
异-C4H9 |
H |
2-Cl(Ph) |
1.91 |
异-C4H9 |
H |
3-Cl(Ph) |
1.92 |
异-C4H9 |
H |
4-Cl(Ph) |
1.93 |
异-C4H9 |
H |
4-F(Ph) |
1.94 |
异-C4H9 |
H |
3-OCH3(Ph) |
1.95 |
异-C4H9 |
H |
4-OCH3(Ph) |
1.96 |
异-C4H9 |
H |
4-CH3(Ph) |
1.97 |
异-C4H9 |
H |
4-NO2(Ph) |
1.98 |
异-C4H9 |
H |
2,4-Cl(Ph) |
1.99 |
异-C4H9 |
H |
2,4-F(Ph) |
1.100 |
C(CH3)3 |
H |
Ph |
1.101 |
C(CH3)3 |
H |
2-Cl(Ph) |
1.102 |
C(CH3)3 |
H |
3-Cl(Ph) |
1.103 |
C(CH3)3 |
H |
4-Cl(Ph) |
1.104 |
C(CH3)3 |
H |
4-F(Ph) |
1.105 |
C(CH3)3 |
H |
3-OCH3(Ph) |
1.106 |
C(CH3)3 |
H |
4-OCH3(Ph) |
1.107 |
C(CH3)3 |
H |
4-CH3(Ph) |
1.108 |
C(CH3)3 |
H |
4-NO2(Ph) |
1.109 |
C(CH3)3 |
H |
2,4-Cl(Ph) |
1.110 |
C(CH3)3 |
H |
2,4-F(Ph) |
1.111 |
环丙基 |
H |
Ph |
1.112 |
环丙基 |
H |
2-Cl(Ph) |
1.113 |
环丙基 |
H |
3-Cl(Ph) |
1.114 |
环丙基 |
H |
4-Cl(Ph) |
1.115 |
环丙基 |
H |
4-Br(Ph) |
1.116 |
环丙基 |
H |
3-OCH3(Ph) |
1.117 |
环丙基 |
H |
4-OCH3(Ph) |
1.118 |
环丙基 |
H |
4-CH3(Ph) |
1.119 |
环丙基 |
H |
4-NO2(Ph) |
1.120 |
环丙基 |
H |
2,4-Cl(Ph) |
1.121 |
环丙基 |
H |
2,4-F(Ph) |
1.122 |
1-CH3-环丙基 |
H |
Ph |
1.123 |
1-CH3-环丙基 |
H |
2-Cl(Ph) |
1.124 |
1-CH3-环丙基 |
H |
3-Cl(Ph) |
1.125 |
1-CH3-环丙基 |
H |
4-Cl(Ph) |
1.126 |
1-CH3-环丙基 |
H |
4-Br(Ph) |
1.127 |
1-CH3-环丙基 |
H |
4-F(Ph) |
1.128 |
1-CH3-环丙基 |
H |
4-OCH3(Ph) |
1.129 |
1-CH3-环丙基 |
H |
4-CH3(Ph) |
1.130 |
1-CH3-环丙基 |
H |
4-NO2(Ph) |
1.131 |
1-CH3-环丙基 |
H |
2,4-Cl(Ph) |
1.132 |
1-CH3-环丙基 |
H |
2,4-F(Ph) |
1.133 |
CH3 |
CH3 |
Ph |
1.134 |
CH3 |
CH3 |
2-Cl(Ph) |
1.135 |
CH3 |
CH3 |
3-Cl(Ph) |
1.136 |
CH3 |
CH3 |
4-Cl(Ph) |
1.137 |
CH3 |
CH3 |
4-Br(Ph) |
1.138 |
CH3 |
CH3 |
4-F(Ph) |
1.139 |
CH3 |
CH3 |
4-OCH3(Ph) |
1.140 |
CH3 |
CH3 |
4-CH3(Ph) |
1.141 |
CH3 |
CH3 |
4-NO2(Ph) |
1.142 |
CH3 |
CH3 |
2,4-Cl(Ph) |
1.143 |
CH3 |
CH3 |
2,4-F(Ph) |
1.144 |
C2H5 |
CH3 |
Ph |
1.145 |
C2H5 |
CH3 |
2-Cl(Ph) |
1.146 |
C2H5 |
CH3 |
3-Cl(Ph) |
1.147 |
C2H5 |
CH3 |
4-Cl(Ph) |
1.148 |
C2H5 |
CH3 |
4-Br(Ph) |
1.149 |
C2H5 |
CH3 |
4-F(Ph) |
1.150 |
C2H5 |
CH3 |
4-OCH3(Ph) |
1.151 |
C2H5 |
CH3 |
4-CH3(Ph) |
1.152 |
C2H5 |
CH3 |
4-NO2(Ph) |
1.153 |
C2H5 |
CH3 |
2,4-Cl(Ph) |
1.154 |
C2H5 |
CH3 |
2,4-F(Ph) |
1.155 |
正-C3H7 |
CH3 |
Ph |
1.156 |
正-C3H7 |
CH3 |
2-Cl(Ph) |
1.157 |
正-C3H7 |
CH3 |
3-Cl(Ph) |
1.158 |
正-C3H7 |
CH3 |
4-Cl(Ph) |
1.159 |
正-C3H7 |
CH3 |
4-Br(Ph) |
1.160 |
正-C3H7 |
CH3 |
4-F(Ph) |
1.161 |
正-C3H7 |
CH3 |
4-OCH3(Ph) |
1.162 |
正-C3H7 |
CH3 |
4-CH3(Ph) |
1.163 |
正-C3H7 |
CH3 |
4-NO2(Ph) |
1.164 |
正-C3H7 |
CH3 |
2,4-Cl(Ph) |
1.165 |
正-C3H7 |
CH3 |
2,4-F(Ph) |
1.166 |
异-C3H7 |
CH3 |
Ph |
1.167 |
异-C3H7 |
CH3 |
2-Cl(Ph) |
1.168 |
异-C3H7 |
CH3 |
3-Cl(Ph) |
1.169 |
异-C3H7 |
CH3 |
4-Cl(Ph) |
1.170 |
异-C3H7 |
CH3 |
4-Br(Ph) |
1.171 |
异-C3H7 |
CH3 |
4-F(Ph) |
1.172 |
异-C3H7 |
CH3 |
4-OCH3(Ph) |
1.173 |
异-C3H7 |
CH3 |
4-CH3(Ph) |
1.174 |
异-C3H7 |
CH3 |
4-NO2(Ph) |
1.175 |
异-C3H7 |
CH3 |
2,4-Cl(Ph) |
1.176 |
异-C3H7 |
CH3 |
2,4-F(Ph) |
1.177 |
正-C4H9 |
CH3 |
Ph |
1.178 |
正-C4H9 |
CH3 |
2-Cl(Ph) |
1.179 |
正-C4H9 |
CH3 |
3-Cl(Ph) |
1.180 |
正-C4H9 |
CH3 |
4-Cl(Ph) |
1.181 |
正-C4H9 |
CH3 |
4-Br(Ph) |
1.182 |
正-C4H9 |
CH3 |
4-F(Ph) |
1.183 |
正-C4H9 |
CH3 |
4-OCH3(Ph) |
1.184 |
正-C4H9 |
CH3 |
4-CH3(Ph) |
1.185 |
正-C4H9 |
CH3 |
4-NO2(Ph) |
1.186 |
正-C4H9 |
CH3 |
2,4-Cl(Ph) |
1.187 |
正-C4H9 |
CH3 |
2,4-F(Ph) |
1.188 |
正-C4H9 |
CH3 |
4-CF3(Ph) |
1.189 |
Ph |
H |
Ph |
1.190 |
Ph |
H |
2-Cl(Ph) |
1.191 |
Ph |
H |
3-Cl(Ph) |
1.192 |
Ph |
H |
4-Cl(Ph) |
1.193 |
Ph |
H |
4-Br(Ph) |
1.194 |
Ph |
H |
4-F(Ph) |
1.195 |
Ph |
H |
4-OCH3(Ph) |
1.196 |
Ph |
H |
4-CH3(Ph) |
1.197 |
Ph |
H |
4-NO2(Ph) |
1.198 |
Ph |
H |
2,4-Cl(Ph) |
1.199 |
Ph |
H |
2,4-F(Ph) |
1.200 |
Ph |
CH3 |
Ph |
1.201 |
Ph |
CH3 |
2-Cl(Ph) |
1.202 |
Ph |
CH3 |
3-Cl(Ph) |
1.203 |
Ph |
CH3 |
4-Cl(Ph) |
1.204 |
Ph |
CH3 |
4-Br(Ph) |
1.205 |
Ph |
CH3 |
4-F(Ph) |
1.206 |
Ph |
CH3 |
4-OCH3(Ph) |
1.207 |
Ph |
CH3 |
4-CH3(Ph) |
1.208 |
Ph |
CH3 |
4-NO2(Ph) |
1.209 |
Ph |
CH3 |
2,4-Cl(Ph) |
1.210 |
Ph |
CH3 |
2,4-F(Ph) |
1.211 |
CN |
H |
Ph |
1.212 |
CN |
H |
2-Cl(Ph) |
1.213 |
CN |
H |
3-Cl(Ph) |
1.214 |
CN |
H |
4-Cl(Ph) |
1.215 |
CN |
H |
4-Br(Ph) |
1.216 |
CN |
H |
4-F(Ph) |
1.217 |
CN |
H |
4-OCH3(Ph) |
1.218 |
CN |
H |
4-CH3(Ph) |
1.219 |
CN |
H |
4-NO2(Ph) |
1.220 |
CN |
H |
2,4-Cl(Ph) |
1.221 |
CN |
H |
2,4-F(Ph) |
1.222 |
CN |
CH3 |
Ph |
1.223 |
CN |
CH3 |
2-Cl(Ph) |
1.224 |
CN |
CH3 |
3-Cl(Ph) |
1.225 |
CN |
CH3 |
4-Cl(Ph) |
1.226 |
CN |
CH3 |
4-Br(Ph) |
1.227 |
CN |
CH3 |
4-F(Ph) |
1.228 |
CN |
CH3 |
4-OCH3(Ph) |
1.229 |
CN |
CH3 |
4-CH3(Ph) |
1.230 |
CN |
CH3 |
4-NO2(Ph) |
1.231 |
CN |
CH3 |
2,4-Cl(Ph) |
1.232 |
CN |
CH3 |
2,4-F(Ph) |
1.233 |
H |
H |
1-萘基 |
1.234 |
CH3 |
H |
1-萘基 |
1.235 |
C2H5 |
H |
1-萘基 |
1.236 |
正-C3H7 |
H |
1-萘基 |
1.237 |
异-C3H7 |
H |
1-萘基 |
1.238 |
正-C4H9 |
H |
1-萘基 |
1.239 |
异-C4H9 |
H |
1-萘基 |
1.240 |
环丙基 |
H |
1-萘基 |
1.241 |
1-CH3-环丙基 |
H |
1-萘基 |
1.242 |
CN |
H |
1-萘基 |
1.243 |
Ph |
CH3 |
1-萘基 |
1.244 |
H |
CH3 |
1-萘基 |
1.245 |
CH3 |
CH3 |
1-萘基 |
1.246 |
C2H5 |
CH3 |
1-萘基 |
1.247 |
正-C3H7 |
CH3 |
1-萘基 |
1.248 |
异-C3H7 |
CH3 |
1-萘基 |
1.249 |
正-C4H9 |
CH3 |
1-萘基 |
1.250 |
异-C4H9 |
CH3 |
1-萘基 |
1.251 |
环丙基 |
CH3 |
1-萘基 |
1.252 |
1-CH3-环丙基 |
CH3 |
1-萘基 |
1.253 |
CN |
CH3 |
1-萘基 |
1.254 |
Ph |
CH3 |
1-萘基 |
1.255 |
H |
H |
2-萘基 |
1.256 |
CH3 |
H |
2-萘基 |
1.257 |
C2H5 |
H |
2-萘基 |
1.258 |
正-C3H7 |
H |
2-萘基 |
1.259 |
异-C3H7 |
H |
2-萘基 |
1.260 |
正-C4H9 |
H |
2-萘基 |
1.261 |
异-C4H9 |
H |
2-萘基 |
1.262 |
环丙基 |
H |
2-萘基 |
1.263 |
1-CH3-环丙基 |
H |
2-萘基 |
1.264 |
CN |
H |
2-萘基 |
1.265 |
Ph |
H |
2-萘基 |
1.266 |
H |
CH3 |
2-萘基 |
1.267 |
CH3 |
CH3 |
2-萘基 |
1.268 |
C2H5 |
CH3 |
2-萘基 |
1.269 |
正-C3H7 |
CH3 |
2-萘基 |
1.270 |
异-C3H7 |
CH3 |
2-萘基 |
1.271 |
正-C4H9 |
CH3 |
2-萘基 |
1.272 |
异-C4H9 |
CH3 |
2-萘基 |
1.273 |
环丙基 |
CH3 |
2-萘基 |
1.274 |
1-CH3-环丙基 |
CH3 |
2-萘基 |
1.275 |
CN |
CH3 |
2-萘基 |
1.276 |
Ph |
CH3 |
2-萘基 |
1.277 |
2-Cl(Ph) |
CH3 |
2-萘基 |
1.278 |
3-Cl(Ph) |
CH3 |
2-萘基 |
1.279 |
4-Cl(Ph) |
CH3 |
2-萘基 |
1.280 |
4-Br(Ph) |
CH3 |
2-萘基 |
1.281 |
4-F(Ph) |
CH3 |
2-萘基 |
1.282 |
4-OCH3(Ph) |
CH3 |
2-萘基 |
1.283 |
4-CH3(Ph) |
CH3 |
2-萘基 |
1.284 |
3-CF3(Ph) |
CH3 |
2-萘基 |
1.285 |
CH3 |
C2H5 |
Ph |
1.286 |
CH3 |
C2H5 |
2-Cl(Ph) |
1.287 |
CH3 |
C2H5 |
3-Cl(Ph) |
1.288 |
CH3 |
C2H5 |
4-Cl(Ph) |
1.289 |
CH3 |
C2H5 |
4-Br(Ph) |
1.290 |
CH3 |
C2H5 |
4-F(Ph) |
1.291 |
CH3 |
C2H5 |
4-OCH3(Ph) |
1.292 |
CH3 |
C2H5 |
4-CH3(Ph) |
1.293 |
CH3 |
C2H5 |
4-NO2(Ph) |
1.294 |
CH3 |
C2H5 |
2,4-Cl(Ph) |
1.295 |
CH3 |
C2H5 |
2,4-F(Ph) |
1.296 |
CH3 |
正-C3H7 |
Ph |
1.297 |
CH3 |
正-C3H7 |
2-Cl(Ph) |
1.298 |
CH3 |
正-C3H7 |
3-Cl(Ph) |
1.299 |
CH3 |
正-C3H7 |
4-Cl(Ph) |
1.300 |
CH3 |
正-C3H7 |
4-Br(Ph) |
1.301 |
CH3 |
正-C3H7 |
4-F(Ph) |
1.302 |
CH3 |
正-C3H7 |
4-OCH3(Ph) |
1.303 |
CH3 |
正-C3H7 |
4-CH3(Ph) |
1.304 |
CH3 |
正-C3H7 |
4-NO2(Ph) |
1.305 |
CH3 |
正-C3H7 |
2,4-Cl(Ph) |
1.306 |
CH3 |
正-C3H7 |
2,4-F(Ph) |
1.307 |
CH3 |
异-C3H7 |
Ph |
1.308 |
CH3 |
异-C3H7 |
2-Cl(Ph) |
1.309 |
CH3 |
异-C3H7 |
3-Cl(Ph) |
1.310 |
CH3 |
异-C3H7 |
4-Cl(Ph) |
1.311 |
CH3 |
异-C3H7 |
4-Br(Ph) |
1.312 |
CH3 |
异-C3H7 |
4-F(Ph) |
1.313 |
CH3 |
异-C3H7 |
4-OCH3(Ph) |
1.314 |
CH3 |
异-C3H7 |
4-CH3(Ph) |
1.315 |
CH3 |
异-C3H7 |
4-NO2(Ph) |
1.316 |
CH3 |
异-C3H7 |
2,4-Cl(Ph) |
1.317 |
CH3 |
异-C3H7 |
2,4-F(Ph) |
1.318 |
CH3 |
正-C4H9 |
Ph |
1.319 |
CH3 |
正-C4H9 |
2-Cl(Ph) |
1.320 |
CH3 |
正-C4H9 |
3-Cl(Ph) |
1.321 |
CH3 |
正-C4H9 |
4-Cl(Ph) |
1.322 |
CH3 |
正-C4H9 |
4-Br(Ph) |
1.323 |
CH3 |
正-C4H9 |
4-F(Ph) |
1.324 |
CH3 |
正-C4H9 |
4-OCH3(Ph) |
1.325 |
CH3 |
正-C4H9 |
4-CH3(Ph) |
1.326 |
CH3 |
正-C4H9 |
4-NO2(Ph) |
1.327 |
CH3 |
正-C4H9 |
2,4-Cl(Ph) |
1.328 |
CH3 |
正-C4H9 |
2,4-F(Ph) |
1.329 |
CH3 |
环丙基 |
Ph |
1.330 |
CH3 |
环丙基 |
2-Cl(Ph) |
本发明式Ⅰ所涵盖的典型化合物包括式V化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=N,Y=Z=O的式Ⅰ化合物,而且其中的R
2、R
3和R
7如表2所定义。
化合物 |
R2 |
R3 |
R7 |
2.1 |
H |
H |
Ph |
2.2 |
H |
H |
4-Cl(Ph) |
2.3 |
H |
H |
4-Br(Ph) |
2.4 |
H |
H |
4-F(Ph) |
2.5 |
H |
H |
4-OCH3(Ph) |
2.6 |
H |
H |
4-CF3(Ph) |
2.7 |
H |
H |
4-NO2(Ph) |
2.8 |
H |
H |
2,4-Cl(Ph) |
2.9 |
H |
H |
2,4-F(Ph) |
2.10 |
H |
H |
3,4-F(Ph) |
2.11 |
CH3 |
H |
Ph |
2.12 |
CH3 |
H |
2-Cl(Ph) |
2.13 |
CH3 |
H |
3-Cl(Ph) |
2.14 |
CH3 |
H |
4-Cl(Ph) |
2.15 |
CH3 |
H |
2-Br(Ph) |
2.16 |
CH3 |
H |
3-Br(Ph) |
2.17 |
CH3 |
H |
4-Br(Ph) |
2.18 |
CH3 |
H |
2-F(Ph) |
2.19 |
CH3 |
H |
3-F(Ph) |
2.20 |
CH3 |
H |
4-F(Ph) |
2.21 |
CH3 |
H |
2-OCH3(Ph) |
2.22 |
CH3 |
H |
3-OCH3(Ph) |
2.23 |
CH3 |
H |
4-OCH3(Ph) |
2.24 |
CH3 |
H |
2-CH3(Ph) |
2.25 |
CH3 |
H |
3-CH3(Ph) |
2.26 |
CH3 |
H |
4-CH3(Ph) |
2.27 |
CH3 |
H |
2-CF3(Ph) |
2.28 |
CH3 |
H |
3-CF3(Ph) |
2.29 |
CH3 |
H |
4-CF3(Ph) |
2.30 |
CH3 |
H |
2-NO2(Ph) |
2.31 |
CH3 |
H |
3-NO2(Ph) |
2.32 |
CH3 |
H |
4-NO2(Ph) |
2.33 |
CH3 |
H |
2,3-Cl(Ph) |
2.34 |
CH3 |
H |
2,4-Cl(Ph) |
2.35 |
CH3 |
H |
2,5-Cl(Ph) |
2.36 |
CH3 |
H |
2,6-Cl(Ph) |
2.37 |
CH3 |
H |
3,4-Cl(Ph) |
2.38 |
CH3 |
H |
3,5-Cl(Ph) |
2.39 |
CH3 |
H |
2,3-F(Ph) |
2.40 |
CH3 |
H |
2,4-F(Ph) |
2.41 |
CH3 |
H |
2,5-F(Ph) |
2.42 |
CH3 |
H |
2,6-F(Ph) |
2.43 |
CH3 |
H |
3,4-F(Ph) |
2.44 |
CH3 |
H |
3,5-FPh) |
2.45 |
C2H5 |
H |
Ph |
2.46 |
C2H5 |
H |
2-Cl(Ph) |
2.47 |
C2H5 |
H |
3-Cl(Ph) |
2.48 |
C2H5 |
H |
4-Cl(Ph) |
2.49 |
C2H5 |
H |
4-Br(Ph) |
2.50 |
C2H5 |
H |
4-F(Ph) |
2.51 |
C2H5 |
H |
4-OCH3(Ph) |
2.52 |
C2H5 |
H |
4-CH3(Ph) |
2.53 |
C2H5 |
H |
4-NO2(Ph) |
2.54 |
C2H5 |
H |
2,4-Cl(Ph) |
2.55 |
C2H5 |
H |
2,4-F(Ph) |
2.56 |
正-C3H7 |
H |
Ph |
2.57 |
正-C3H7 |
H |
2-Cl(Ph) |
2.58 |
正-C3H7 |
H |
3-Cl(Ph) |
2.59 |
正-C3H7 |
H |
4-Cl(Ph) |
2.60 |
正-C3H7 |
H |
4-F(Ph) |
2.61 |
正-C3H7 |
H |
3-OCH3(Ph) |
2.62 |
正-C3H7 |
H |
4-OCH3(Ph) |
2.63 |
正-C3H7 |
H |
4-CH3(Ph) |
2.64 |
正-C3H7 |
H |
4-NO2(Ph) |
2.65 |
正-C3H7 |
H |
2,4-Cl(Ph) |
2.66 |
正-C3H7 |
H |
2,4-F(Ph) |
2.67 |
异-C3H7 |
H |
Ph |
2.68 |
异-C3H7 |
H |
2-Cl(Ph) |
2.69 |
异-C3H7 |
H |
3-Cl(Ph) |
2.70 |
异-C3H7 |
H |
4-Cl(Ph) |
2.71 |
异-C3H7 |
H |
4-Br(Ph) |
2.72 |
异-C3H7 |
H |
4-F(Ph) |
2.73 |
异-C3H7 |
H |
4-OCH3(Ph) |
2.74 |
异-C3H7 |
H |
4-CH3(Ph) |
2.75 |
异-C3H7 |
H |
4-NO2(Ph) |
2.76 |
异-C3H7 |
H |
2,4-Cl(Ph) |
2.77 |
异-C3H7 |
H |
2,4-F(Ph) |
2.78 |
正-C4H9 |
H |
Ph |
2.79 |
正-C4H9 |
H |
2-Cl(Ph) |
2.80 |
正-C4H9 |
H |
3-Cl(Ph) |
2.81 |
正-C4H9 |
H |
4-Cl(Ph) |
2.82 |
正-C4H9 |
H |
4-Br(Ph) |
2.83 |
正-C4H9 |
H |
4-F(Ph) |
2.84 |
正-C4H9 |
H |
4-OCH3(Ph) |
2.85 |
正-C4H9 |
H |
4-CH3(Ph) |
2.86 |
正-C4H9 |
H |
4-NO2(Ph) |
2.87 |
正-C4H9 |
H |
2,4-Cl(Ph) |
2.88 |
正-C4H9 |
H |
2,4-F(Ph) |
2.89 |
异-C4H9 |
H |
Ph |
2.90 |
异-C4H9 |
H |
2-Cl(Ph) |
2.91 |
异-C4H9 |
H |
3-Cl(Ph) |
2.92 |
异-C4H9 |
H |
4-Cl(Ph) |
2.93 |
异-C4H9 |
H |
4-F(Ph) |
2.94 |
异-C4H9 |
H |
3-OCH3(Ph) |
2.95 |
异-C4H9 |
H |
4-OCH3(Ph) |
2.96 |
异-C4H9 |
H |
4-CH3(Ph) |
2.97 |
异-C4H9 |
H |
4-NO2(Ph) |
2.98 |
异-C4H9 |
H |
2,4-Cl(Ph) |
2.99 |
异-C4H9 |
H |
2,4-F(Ph) |
2.100 |
C(CH3)3 |
H |
Ph |
2.101 |
C(CH3)3 |
H |
2-Cl(Ph) |
2.102 |
C(CH3)3 |
H |
3-Cl(Ph) |
2.103 |
C(CH3)3 |
H |
4-Cl(Ph) |
2.104 |
C(CH3)3 |
H |
4-F(Ph) |
2.105 |
C(CH3)3 |
H |
3-OCH3(Ph) |
2.106 |
C(CH3)3 |
H |
4-OCH3(Ph) |
2.107 |
C(CH3)3 |
H |
4-CH3(Ph) |
2.108 |
C(CH3)3 |
H |
4-NO2(Ph) |
2.109 |
C(CH3)3 |
H |
2,4-Cl(Ph) |
2.110 |
C(CH3)3 |
H |
2,4-F(Ph) |
2.111 |
环丙基 |
H |
Ph |
2.112 |
环丙基 |
H |
2-Cl(Ph) |
2.113 |
环丙基 |
H |
3-Cl(Ph) |
2.114 |
环丙基 |
H |
4-Cl(Ph) |
2.115 |
环丙基 |
H |
4-Br(Ph) |
2.116 |
环丙基 |
H |
3-OCH3(Ph) |
2.117 |
环丙基 |
H |
4-OCH3(Ph) |
2.118 |
环丙基 |
H |
4-CH3(Ph) |
2.119 |
环丙基 |
H |
4-NO2(Ph) |
2.120 |
环丙基 |
H |
2,4-Cl(Ph) |
2.121 |
环丙基 |
H |
2,4-F(Ph) |
2.122 |
1-CH3-环丙基 |
H |
Ph |
2.123 |
1-CH3-环丙基 |
H |
2-Cl(Ph) |
2.124 |
1-CH3-环丙基 |
H |
3-Cl(Ph) |
2.125 |
1-CH3-环丙基 |
H |
4-Cl(Ph) |
2.126 |
1-CH3-环丙基 |
H |
4-Br(Ph) |
2.127 |
1-CH3-环丙基 |
H |
4-F(Ph) |
2.128 |
1-CH3-环丙基 |
H |
4-OCH3(Ph) |
2.129 |
1-CH3-环丙基 |
H |
4-CH3(Ph) |
2.130 |
1-CH3-环丙基 |
H |
4-NO2(Ph) |
2.131 |
1-CH3-环丙基 |
H |
2,4-Cl(Ph) |
2.132 |
1-CH3-环丙基 |
H |
2,4-F(Ph) |
2.133 |
CH3 |
CH3 |
Ph |
2.134 |
CH3 |
CH3 |
2-Cl(Ph) |
2.135 |
CH3 |
CH3 |
3-Cl(Ph) |
2.136 |
CH3 |
CH3 |
4-Cl(Ph) |
2.137 |
CH3 |
CH3 |
4-Br(Ph) |
2.138 |
CH3 |
CH3 |
4-F(Ph) |
2.139 |
CH3 |
CH3 |
4-OCH3(Ph) |
2.140 |
CH3 |
CH3 |
4-CH3(Ph) |
2.141 |
CH3 |
CH3 |
4-NO2(Ph) |
2.142 |
CH3 |
CH3 |
2,4-Cl(Ph) |
2.143 |
CH3 |
CH3 |
2,4-F(Ph) |
2.144 |
C2H5 |
CH3 |
Ph |
2.145 |
C2H5 |
CH3 |
2-Cl(Ph) |
2.146 |
C2H5 |
CH3 |
3-Cl(Ph) |
2.147 |
C2H5 |
CH3 |
4-Cl(Ph) |
2.148 |
C2H5 |
CH3 |
4-Br(Ph) |
2.149 |
C2H5 |
CH3 |
4-F(Ph) |
2.150 |
C2H5 |
CH3 |
4-OCH3(Ph) |
2.151 |
C2H5 |
CH3 |
4-CH3(Ph) |
2.152 |
C2H5 |
CH3 |
4-NO2(Ph) |
2.153 |
C2H5 |
CH3 |
2,4-Cl(Ph) |
2.154 |
C2H5 |
CH3 |
2,4-F(Ph) |
2.155 |
正-C3H7 |
CH3 |
Ph |
2.156 |
正-C3H7 |
CH3 |
2-Cl(Ph) |
2.157 |
正-C3H7 |
CH3 |
3-Cl(Ph) |
2.158 |
正-C3H7 |
CH3 |
4-Cl(Ph) |
2.159 |
正-C3H7 |
CH3 |
4-Br(Ph) |
2.160 |
正-C3H7 |
CH3 |
4-F(Ph) |
2.161 |
正-C3H7 |
CH3 |
4-OCH3(Ph) |
2.162 |
正-C3H7 |
CH3 |
4-CH3(Ph) |
2.163 |
正-C3H7 |
CH3 |
4-NO2(Ph) |
2.164 |
正-C3H7 |
CH3 |
2,4-Cl(Ph) |
2.165 |
正-C3H7 |
CH3 |
2,4-F(Ph) |
2.166 |
异-C3H7 |
CH3 |
Ph |
2.167 |
异-C3H7 |
CH3 |
2-Cl(Ph) |
2.168 |
异-C3H7 |
CH3 |
3-Cl(Ph) |
2.169 |
异-C3H7 |
CH3 |
4-Cl(Ph) |
2.170 |
异-C3H7 |
CH3 |
4-Br(Ph) |
2.171 |
异-C3H7 |
CH3 |
4-F(Ph) |
2.172 |
异-C3H7 |
CH3 |
4-OCH3(Ph) |
2.173 |
异-C3H7 |
CH3 |
4-CH3(Ph) |
2.174 |
异-C3H7 |
CH3 |
4-NO2(Ph) |
2.175 |
异-C3H7 |
CH3 |
2,4-Cl(Ph) |
2.176 |
异-C3H7 |
CH3 |
2,4-F(Ph) |
2.177 |
正-C4H9 |
CH3 |
Ph |
2.178 |
正-C4H9 |
CH3 |
2-Cl(Ph) |
2.179 |
正-C4H9 |
CH3 |
3-Cl(Ph) |
2.180 |
正-C4H9 |
CH3 |
4-Cl(Ph) |
2.181 |
正-C4H9 |
CH3 |
4-Br(Ph) |
2.182 |
正-C4H9 |
CH3 |
4-F(Ph) |
2.183 |
正-C4H9 |
CH3 |
4-OCH3(Ph) |
2.184 |
正-C4H9 |
CH3 |
4-CH3(Ph) |
2.185 |
正-C4H9 |
CH3 |
4-NO2(Ph) |
2.186 |
正-C4H9 |
CH3 |
2,4-Cl(Ph) |
2.187 |
正-C4H9 |
CH3 |
2,4-F(Ph) |
2.188 |
正-C4H9 |
CH3 |
4-CF3(Ph) |
2.189 |
Ph |
H |
Ph |
2.190 |
Ph |
H |
2-Cl(Ph) |
2.191 |
Ph |
H |
3-Cl(Ph) |
2.192 |
Ph |
H |
4-Cl(Ph) |
2.193 |
Ph |
H |
4-Br(Ph) |
2.194 |
Ph |
H |
4-F(Ph) |
2.195 |
Ph |
H |
4-OCH3(Ph) |
2.196 |
Ph |
H |
4-CH3(Ph) |
2.197 |
Ph |
H |
4-NO2(Ph) |
2.198 |
Ph |
H |
2,4-Cl(Ph) |
2.199 |
Ph |
H |
2,4-F(Ph) |
2.200 |
Ph |
CH3 |
Ph |
2.201 |
Ph |
CH3 |
2-Cl(Ph) |
2.202 |
Ph |
CH3 |
3-Cl(Ph) |
2.203 |
Ph |
CH3 |
4-Cl(Ph) |
2.204 |
Ph |
CH3 |
4-Br(Ph) |
2.205 |
Ph |
CH3 |
4-F(Ph) |
2.206 |
Ph |
CH3 |
4-OCH3(Ph) |
2.207 |
Ph |
CH3 |
4-CH3(Ph) |
2.208 |
Ph |
CH3 |
4-NO2(Ph) |
2.209 |
Ph |
CH3 |
2,4-Cl(Ph) |
2.210 |
Ph |
CH3 |
2,4-F(Ph) |
2.211 |
CN |
H |
Ph |
2.212 |
CN |
H |
2-Cl(Ph) |
2.213 |
CN |
H |
3-Cl(Ph) |
2.214 |
CN |
H |
4-Cl(Ph) |
2.215 |
CN |
H |
4-Br(Ph) |
2.216 |
CN |
H |
4-F(Ph) |
2.217 |
CN |
H |
4-OCH3(Ph) |
2.218 |
CN |
H |
4-CH3(Ph) |
2.219 |
CN |
H |
4-NO2(Ph) |
2.220 |
CN |
H |
2,4-Cl(Ph) |
2.221 |
CN |
H |
2,4-F(Ph) |
2.222 |
CN |
CH3 |
Ph |
2.223 |
CN |
CH3 |
2-Cl(Ph) |
2.224 |
CN |
CH3 |
3-Cl(Ph) |
2.225 |
CN |
CH3 |
4-Cl(Ph) |
2.226 |
CN |
CH3 |
4-Br(Ph) |
2.227 |
CN |
CH3 |
4-F(Ph) |
2.228 |
CN |
CH3 |
4-OCH3(Ph) |
2.229 |
CN |
CH3 |
4-CH3(Ph) |
2.230 |
CN |
CH3 |
4-NO2(Ph) |
2.231 |
CN |
CH3 |
2,4-Cl(Ph) |
2.232 |
CN |
CH3 |
2,4-F(Ph) |
2.233 |
H |
H |
1-萘基 |
2.234 |
CH3 |
H |
1-萘基 |
2.235 |
C2H5 |
H |
1-萘基 |
2.236 |
正-C3H7 |
H |
1-萘基 |
2.237 |
异-C3H7 |
H |
1-萘基 |
2.238 |
正-C4H9 |
H |
1-萘基 |
2.239 |
异-C4H9 |
H |
1-萘基 |
2.240 |
环丙基 |
H |
1-萘基 |
2.241 |
1-CH3-环丙基 |
H |
1-萘基 |
2.242 |
CN |
H |
1-萘基 |
2.243 |
Ph |
H |
1-萘基 |
2.244 |
H |
CH3 |
1-萘基 |
2.245 |
CH3 |
CH3 |
1-萘基 |
2.246 |
C2H5 |
CH3 |
1-萘基 |
2.247 |
正-C3H7 |
CH3 |
1-萘基 |
2.248 |
异-C3H7 |
CH3 |
1-萘基 |
2.249 |
正-C4H9 |
CH3 |
1-萘基 |
2.250 |
异-C4H9 |
CH3 |
1-萘基 |
2.251 |
环丙基 |
CH3 |
1-萘基 |
2.252 |
1-CH3-环丙基 |
CH3 |
1-萘基 |
2.253 |
CN |
CH3 |
1-萘基 |
2.254 |
Ph |
CH3 |
1-萘基 |
2.255 |
H |
H |
2-萘基 |
2.256 |
CH3 |
H |
2-萘基 |
2.257 |
C2H5 |
H |
2-萘基 |
2.258 |
正-C3H7 |
H |
2-萘基 |
2.259 |
异-C3H7 |
H |
2-萘基 |
2.260 |
正-C4H9 |
H |
2-萘基 |
2.261 |
异-C4H9 |
H |
2-萘基 |
2.262 |
环丙基 |
H |
2-萘基 |
2.263 |
1-CH3-环丙基 |
H |
2-萘基 |
2.264 |
CN |
H |
2-萘基 |
2.265 |
Ph |
H |
2-萘基 |
2.266 |
H |
CH3 |
2-萘基 |
2.267 |
CH3 |
CH3 |
2-萘基 |
2.268 |
C2H5 |
CH3 |
2-萘基 |
2.269 |
正-C3H7 |
CH3 |
2-萘基 |
2.270 |
异-C3H7 |
CH3 |
2-萘基 |
2.271 |
正-C4H9 |
CH3 |
2-萘基 |
2.272 |
异-C4H9 |
CH3 |
2-萘基 |
2.273 |
环丙基 |
CH3 |
2-萘基 |
2.274 |
1-CH3-环丙基 |
CH3 |
2-萘基 |
2.275 |
CN |
CH3 |
2-萘基 |
2.276 |
Ph |
CH3 |
2-萘基 |
2.277 |
2-Cl(Ph) |
CH3 |
2-萘基 |
2.278 |
3-Cl(Ph) |
CH3 |
2-萘基 |
2.279 |
4-Cl(Ph) |
CH3 |
2-萘基 |
2.280 |
4-Br(Ph) |
CH3 |
2-萘基 |
2.281 |
4-F(Ph) |
CH3 |
2-萘基 |
2.282 |
4-OCH3(Ph) |
CH3 |
2-萘基 |
2.283 |
4-CH3(Ph) |
CH3 |
2-萘基 |
2.284 |
3-CF3(Ph) |
CH3 |
2-萘基 |
2.285 |
CH3 |
C2H5 |
Ph |
2.286 |
CH3 |
C2H5 |
2-Cl(Ph) |
2.287 |
CH3 |
C2H5 |
3-Cl(Ph) |
2.288 |
CH3 |
C2H5 |
4-Cl(Ph) |
2.289 |
CH3 |
C2H5 |
4-Br(Ph) |
2.290 |
CH3 |
C2H5 |
4-F(Ph) |
2.291 |
CH3 |
C2H5 |
4-OCH3(Ph) |
2.292 |
CH3 |
C2H5 |
4-CH3(Ph) |
2.293 |
CH3 |
C2H5 |
4-NO2(Ph) |
2.294 |
CH3 |
C2H5 |
2,4-Cl(Ph) |
2.295 |
CH3 |
C2H5 |
2,4-F(Ph) |
2.296 |
CH3 |
n-C3H7 |
Ph |
2.297 |
CH3 |
n-C3H7 |
2-Cl(Ph) |
2.298 |
CH3 |
n-C3H7 |
3-Cl(Ph) |
2.299 |
CH3 |
正-C3H7 |
4-Cl(Ph) |
2.300 |
CH3 |
正-C3H7 |
4-Br(Ph) |
2.301 |
CH3 |
正-C3H7 |
4-F(Ph) |
2.302 |
CH3 |
正-C3H7 |
4-OCH3(Ph) |
2.303 |
CH3 |
正-C3H7 |
4-CH3(Ph) |
2.304 |
CH3 |
正-C3H7 |
4-NO2(Ph) |
2.305 |
CH3 |
正-C3H7 |
2,4-Cl(Ph) |
2.306 |
CH3 |
正-C3H7 |
2,4-F(Ph) |
2.307 |
CH3 |
异-C3H7 |
Ph |
2.308 |
CH3 |
异-C3H7 |
2-Cl(Ph) |
2.309 |
CH3 |
异-C3H7 |
3-Cl(Ph) |
2.310 |
CH3 |
异-C3H7 |
4-Cl(Ph) |
2.311 |
CH3 |
异-C3H7 |
4-Br(Ph) |
2.312 |
CH3 |
异-C3H7 |
4-F(Ph) |
2.313 |
CH3 |
异-C3H7 |
4-OCH3(Ph) |
2.314 |
CH3 |
异-C3H7 |
4-CH3(Ph) |
2.315 |
CH3 |
异-C3H7 |
4-NO2(Ph) |
2.316 |
CH3 |
异-C3H7 |
2,4-Cl(Ph) |
2.317 |
CH3 |
异-C3H7 |
2,4-F(Ph) |
2.318 |
CH3 |
正-C4H9 |
Ph |
2.319 |
CH3 |
正-C4H9 |
2-Cl(Ph) |
2.320 |
CH3 |
正-C4H9 |
3-Cl(Ph) |
2.321 |
CH3 |
正-C4H9 |
4-Cl(Ph) |
2.322 |
CH3 |
正-C4H9 |
4-Br(Ph) |
2.323 |
CH3 |
正-C4H9 |
4-F(Ph) |
2.324 |
CH3 |
正-C4H9 |
4-OCH3(Ph) |
2.325 |
CH3 |
正-C4H9 |
4-CH3(Ph) |
2.326 |
CH3 |
正-C4H9 |
4-NO2(Ph) |
2.327 |
CH3 |
正-C4H9 |
2,4-Cl(Ph) |
2.328 |
CH3 |
正-C4H9 |
2,4-F(Ph) |
2.329 |
CH3 |
环丙基 |
Ph |
2.330 |
CH3 |
环丙基 |
2-Cl(Ph) |
本发明式Ⅰ所涵盖的典型化合物包括式Ⅵ化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=N,Y=NH及Z=O的式Ⅰ化合物,而且其中的R
2、R
3和R
7如表3所定义。
表3
3.1 |
H |
H |
Ph |
3.2 |
H |
H |
4-Cl(Ph) |
3.3 |
H |
H |
4-Br(Ph) |
3.4 |
H |
H |
4-F(Ph) |
3.5 |
H |
H |
4-OCH3(Ph) |
3.6 |
H |
H |
4-CF3(Ph) |
3.7 |
H |
H |
4-NO2(Ph) |
3.8 |
H |
H |
2,4-Cl(Ph) |
3.9 |
H |
H |
2,4-F(Ph) |
3.10 |
H |
H |
3,4-F(Ph) |
3.11 |
CH3 |
H |
Ph |
3.12 |
CH3 |
H |
2-Cl(Ph) |
3.13 |
CH3 |
H |
3-Cl(Ph) |
3.14 |
CH3 |
H |
4-Cl(Ph) |
3.15 |
CH3 |
H |
2-Br(Ph) |
3.16 |
CH3 |
H |
3-Br(Ph) |
3.17 |
CH3 |
H |
4-Br(Ph) |
3.18 |
CH3 |
H |
2-F(Ph) |
3.19 |
CH3 |
H |
3-F(Ph) |
3.20 |
CH3 |
H |
4-F(Ph) |
3.21 |
CH3 |
H |
2-OCH3(Ph) |
3.22 |
CH3 |
H |
3-OCH3(Ph) |
3.23 |
CH3 |
H |
4-OCH3(Ph) |
3.24 |
CH3 |
H |
2-CH3(Ph) |
3.25 |
CH3 |
H |
3-CH3(Ph) |
3.26 |
CH3 |
H |
4-CH3(Ph) |
3.27 |
CH3 |
H |
2-CF3(Ph) |
3.28 |
CH3 |
H |
3-CF3(Ph) |
3.29 |
CH3 |
H |
4-CF3(Ph) |
3.30 |
CH3 |
H |
2-NO2(Ph) |
3.31 |
CH3 |
H |
3-NO2(Ph) |
3.32 |
CH3 |
H |
4-NO2(Ph) |
3.33 |
CH3 |
H |
2,3-Cl(Ph) |
3.34 |
CH3 |
H |
2,4-Cl(Ph) |
3.35 |
CH3 |
H |
2,5-Cl(Ph) |
3.36 |
CH3 |
H |
2,6-Cl(Ph) |
3.37 |
CH3 |
H |
3,4-Cl(Ph) |
3.38 |
CH3 |
H |
3,5-Cl(Ph) |
3.39 |
CH3 |
H |
2,3-F(Ph) |
3.40 |
CH3 |
H |
2,4-F(Ph) |
3.41 |
CH3 |
H |
2,5-F(Ph) |
3.42 |
CH3 |
H |
2,6-F(Ph) |
3.43 |
CH3 |
H |
3,4-F(Ph) |
3.44 |
CH3 |
H |
3,5-F(Ph) |
3.45 |
C2H5 |
H |
Ph |
3.46 |
C2H5 |
H |
2-Cl(Ph) |
3.47 |
C2H5 |
H |
3-Cl(Ph) |
3.48 |
C2H5 |
H |
4-Cl(Ph) |
3.49 |
C2H5 |
H |
4-Br(Ph) |
3.50 |
C2H5 |
H |
4-F(Ph) |
3.51 |
C2H5 |
H |
4-OCH3(Ph) |
3.52 |
C2H5 |
H |
4-CH3(Ph) |
3.53 |
C2H5 |
H |
4-NO2(Ph) |
3.54 |
C2H5 |
H |
2,4-Cl(Ph) |
3.55 |
C2H5 |
H |
2,4-F(Ph) |
3.56 |
正-C3H7 |
H |
Ph |
3.57 |
正-C3H7 |
H |
2-Cl(Ph) |
3.58 |
正-C3H7 |
H |
3-Cl(Ph) |
3.59 |
正-C3H7 |
H |
4-Cl(Ph) |
3.60 |
正-C3H7 |
H |
4-F(Ph) |
3.61 |
正-C3H7 |
H |
3-OCH3(Ph) |
3.62 |
正-C3H7 |
H |
4-OCH3(Ph) |
3.63 |
正-C3H7 |
H |
4-CH3(Ph) |
3.64 |
正-C3H7 |
H |
4-NO2(Ph) |
3.65 |
正-C3H7 |
H |
2,4-Cl(Ph) |
3.66 |
正-C3H7 |
H |
2,4-F(Ph) |
3.67 |
异-C3H7 |
H |
Ph |
3.68 |
异-C3H7 |
H |
2-Cl(Ph) |
3.69 |
异-C3H7 |
H |
3-Cl(Ph) |
3.70 |
异-C3H7 |
H |
4-Cl(Ph) |
3.71 |
异-C3H7 |
H |
4-Br(Ph) |
3.72 |
异-C3H7 |
H |
4-F(Ph) |
3.73 |
异-C3H7 |
H |
4-OCH3(Ph) |
3.74 |
异-C3H7 |
H |
4-CH3(Ph) |
3.75 |
异-C3H7 |
H |
4-NO2(Ph) |
3.76 |
异-C3H7 |
H |
2,4-Cl(Ph) |
3.77 |
异-C3H7 |
H |
2,4-F(Ph) |
3.78 |
正-C4H9 |
H |
Ph |
3.79 |
正-C4H9 |
H |
2-Cl(Ph) |
3.80 |
正-C4H9 |
H |
3-Cl(Ph) |
3.81 |
正-C4H9 |
H |
4-Cl(Ph) |
3.82 |
正-C4H9 |
H |
4-Br(Ph) |
3.83 |
正-C4H9 |
H |
4-F(Ph) |
3.84 |
正-C4H9 |
H |
4-OCH3(Ph) |
3.85 |
正-C4H9 |
H |
4-CH3(Ph) |
3.86 |
正-C4H9 |
H |
4-NO2(Ph) |
3.87 |
正-C4H9 |
H |
2,4-Cl(Ph) |
3.88 |
正-C4H9 |
H |
2,4-F(Ph) |
3.89 |
异-C4H9 |
H |
Ph |
3.90 |
异-C4H9 |
H |
2-Cl(Ph) |
3.91 |
异-C4H9 |
H |
3-Cl(Ph) |
3.92 |
异-C4H9 |
H |
4-Cl(Ph) |
3.93 |
异-C4H9 |
H |
4-F(Ph) |
3.94 |
异-C4H9 |
H |
3-OCH3(Ph) |
3.95 |
异-C4H9 |
H |
4-OCH3(Ph) |
3.96 |
异-C4H9 |
H |
4-CH3(Ph) |
3.97 |
异-C4H9 |
H |
4-NO2(Ph) |
3.98 |
异-C4H9 |
H |
2,4-Cl(Ph) |
3.99 |
异-C4H9 |
H |
2,4-F(Ph) |
3.100 |
C(CH3)3 |
H |
Ph |
3.101 |
C(CH3)3 |
H |
2-Cl(Ph) |
3.102 |
C(CH3)3 |
H |
3-Cl(Ph) |
3.103 |
C(CH3)3 |
H |
4-Cl(Ph) |
3.104 |
C(CH3)3 |
H |
4-F(Ph) |
3.105 |
C(CH3)3 |
H |
3-OCH3(Ph) |
3.106 |
C(CH3)3 |
H |
4-OCH3(Ph) |
3.107 |
C(CH3)3 |
H |
4-CH3(Ph) |
3.108 |
C(CH3)3 |
H |
4-NO2(Ph) |
3.109 |
C(CH3)3 |
H |
2,4-Cl(Ph) |
3.110 |
C(CH3)3 |
H |
2,4-F(Ph) |
3.111 |
环丙基 |
H |
Ph |
3.112 |
环丙基 |
H |
2-Cl(Ph) |
3.113 |
环丙基 |
H |
3-Cl(Ph) |
3.114 |
环丙基 |
H |
4-Cl(Ph) |
3.115 |
环丙基 |
H |
4-Br(Ph) |
3.116 |
环丙基 |
H |
3-OCH3(Ph) |
3.117 |
环丙基 |
H |
4-OCH3(Ph) |
3.118 |
环丙基 |
H |
4-CH3(Ph) |
3.119 |
环丙基 |
H |
4-NO2(Ph) |
3.120 |
环丙基 |
H |
2,4-Cl(Ph) |
3.121 |
环丙基 |
H |
2,4-F(Ph) |
3.122 |
1-CH3-环丙基 |
H |
Ph |
3.123 |
1-CH3-环丙基 |
H |
2-Cl(Ph) |
3.124 |
1-CH3-环丙基 |
H |
3-Cl(Ph) |
3.125 |
1-CH3-环丙基 |
H |
4-Cl(Ph) |
3.126 |
1-CH3-环丙基 |
H |
4-Br(Ph) |
3.127 |
1-CH3-环丙基 |
H |
4-F(Ph) |
3.128 |
1-CH3-环丙基 |
H |
4-OCH3(Ph) |
3.129 |
1-CH3-环丙基 |
H |
4-CH3(Ph) |
3.130 |
1-CH3-环丙基 |
H |
4-NO2(Ph) |
3.131 |
1-CH3-环丙基 |
H |
2,4-Cl(Ph) |
3.132 |
1-CH3-环丙基 |
H |
2,4-F(Ph) |
3.133 |
CH3 |
CH3 |
Ph |
3.134 |
CH3 |
CH3 |
2-Cl(Ph) |
3.135 |
CH3 |
CH3 |
3-Cl(Ph) |
3.136 |
CH3 |
CH3 |
4-Cl(Ph) |
3.137 |
CH3 |
CH3 |
4-Br(Ph) |
3.138 |
CH3 |
CH3 |
4-F(Ph) |
3.139 |
CH3 |
CH3 |
4-OCH3(Ph) |
3.140 |
CH3 |
CH3 |
4-CH3(Ph) |
3.141 |
CH3 |
CH3 |
4-NO2(Ph) |
3.142 |
CH3 |
CH3 |
2,4-Cl(Ph) |
3.143 |
CH3 |
CH3 |
2,4-F(Ph) |
3.144 |
C2H5 |
CH3 |
Ph |
3.145 |
C2H5 |
CH3 |
2-Cl(Ph) |
3.146 |
C2H5 |
CH3 |
3-Cl(Ph) |
3.147 |
C2H5 |
CH3 |
4-Cl(Ph) |
3.148 |
C2H5 |
CH3 |
4-Br(Ph) |
3.149 |
C2H5 |
CH3 |
4-F(Ph) |
3.150 |
C2H5 |
CH3 |
4-OCH3(Ph) |
3.151 |
C2H5 |
CH3 |
4-CH3(Ph) |
3.152 |
C2H5 |
CH3 |
4-NO2(Ph) |
3.153 |
C2H5 |
CH3 |
2,4-Cl(Ph) |
3.154 |
C2H5 |
CH3 |
2,4-F(Ph) |
3.155 |
正-C3H7 |
CH3 |
Ph |
3.156 |
正-C3H7 |
CH3 |
2-Cl(Ph) |
3.157 |
正-C3H7 |
CH3 |
3-Cl(Ph) |
3.158 |
正-C3H7 |
CH3 |
4-Cl(Ph) |
3.159 |
正-C3H7 |
CH3 |
4-Br(Ph) |
3.160 |
正-C3H7 |
CH3 |
4-F(Ph) |
3.161 |
正-C3H7 |
CH3 |
4-OCH3(Ph) |
3.162 |
正-C3H7 |
CH3 |
4-CH3(Ph) |
3.163 |
正-C3H7 |
CH3 |
4-NO2(Ph) |
3.164 |
正-C3H7 |
CH3 |
2,4-Cl(Ph) |
3.165 |
正-C3H7 |
CH3 |
2,4-F(Ph) |
3.166 |
异-C3H7 |
CH3 |
Ph |
3.167 |
异-C3H7 |
CH3 |
2-Cl(Ph) |
3.168 |
异-C3H7 |
CH3 |
3-Cl(Ph) |
3.169 |
异-C3H7 |
CH3 |
4-Cl(Ph) |
3.170 |
异-C3H7 |
CH3 |
4-Br(Ph) |
3.171 |
异-C3H7 |
CH3 |
4-F(Ph) |
3.172 |
异-C3H7 |
CH3 |
4-OCH3(Ph) |
3.173 |
异-C3H7 |
CH3 |
4-CH3(Ph) |
3.174 |
异-C3H7 |
CH3 |
4-NO2(Ph) |
3.175 |
异-C3H7 |
CH3 |
2,4-Cl(Ph) |
3.176 |
异-C3H7 |
CH3 |
2,4-F(Ph) |
3.177 |
正-C4H9 |
CH3 |
Ph |
3.178 |
正-C4H9 |
CH3 |
2-Cl(Ph) |
3.179 |
正-C4H9 |
CH3 |
3-Cl(Ph) |
3.180 |
正-C4H9 |
CH3 |
4-Cl(Ph) |
3.181 |
正-C4H9 |
CH3 |
4-Br(Ph) |
3.182 |
正-C4H9 |
CH3 |
4-F(Ph) |
3.183 |
正-C4H9 |
CH3 |
4-OCH3(Ph) |
3.184 |
正-C4H9 |
CH3 |
4-CH3(Ph) |
3.185 |
正-C4H9 |
CH3 |
4-NO2(Ph) |
3.186 |
正-C4H9 |
CH3 |
2,4-Cl(Ph) |
3.187 |
正-C4H9 |
CH3 |
2,4-F(Ph) |
3.188 |
正-C4H9 |
CH3 |
4-CF3(Ph) |
3.189 |
Ph |
H |
Ph |
3.190 |
Ph |
H |
2-Cl(Ph) |
3.191 |
Ph |
H |
3-Cl(Ph) |
3.192 |
Ph |
H |
4-Cl(Ph) |
3.193 |
Ph |
H |
4-Br(Ph) |
3.194 |
Ph |
H |
4-F(Ph) |
3.195 |
Ph |
H |
4-OCH3(Ph) |
3.196 |
Ph |
H |
4-CH3(Ph) |
3.197 |
Ph |
H |
4-NO2(Ph) |
3.198 |
Ph |
H |
2,4-Cl(Ph) |
3.199 |
Ph |
H |
2,4-F(Ph) |
3.200 |
Ph |
CH3 |
Ph |
3.201 |
Ph |
CH3 |
2-Cl(Ph) |
3.202 |
Ph |
CH3 |
3-Cl(Ph) |
3.203 |
Ph |
CH3 |
4-Cl(Ph) |
3.204 |
Ph |
CH3 |
4-Br(Ph) |
3.205 |
Ph |
CH3 |
4-F(Ph) |
3.206 |
Ph |
CH3 |
4-OCH3(Ph) |
3.207 |
Ph |
CH3 |
4-CH3(Ph) |
3.208 |
Ph |
CH3 |
4-NO2(Ph) |
3.209 |
Ph |
CH3 |
2,4-Cl(Ph) |
3.210 |
Ph |
CH3 |
2,4-F(Ph) |
3.211 |
CN |
H |
Ph |
3.212 |
CN |
H |
2-Cl(Ph) |
3.213 |
CN |
H |
3-Cl(Ph) |
3.214 |
CN |
H |
4-Cl(Ph) |
3.215 |
CN |
H |
4-Br(Ph) |
3.216 |
CN |
H |
4-F(Ph) |
3.217 |
CN |
H |
4-OCH3(Ph) |
3.218 |
CN |
H |
4-CH3(Ph) |
3.219 |
CN |
H |
4-NO2(Ph) |
3.220 |
CN |
H |
2,4-Cl(Ph) |
3.221 |
CN |
H |
2,4-F(Ph) |
3.222 |
CN |
CH3 |
Ph |
3.223 |
CN |
CH3 |
2-Cl(Ph) |
3.224 |
CN |
CH3 |
3-Cl(Ph) |
3.225 |
CN |
CH3 |
4-Cl(Ph) |
3.226 |
CN |
CH3 |
4-Br(Ph) |
3.227 |
CN |
CH3 |
4-F(Ph) |
3.228 |
CN |
CH3 |
4-OCH3(Ph) |
3.229 |
CN |
CH3 |
4-CH3(Ph) |
3.230 |
CN |
CH3 |
4-NO2(Ph) |
3.231 |
CN |
CH3 |
2,4-Cl(Ph) |
3.232 |
CN |
CH3 |
2,4-F(Ph) |
3.233 |
H |
H |
1-萘基 |
3.234 |
CH3 |
H |
1-萘基 |
3.235 |
C2H5 |
H |
1-萘基 |
3.236 |
正-C3H7 |
H |
1-萘基 |
3.237 |
异-C3H7 |
H |
1-萘基 |
3.238 |
正-C4H9 |
H |
1-萘基 |
3.239 |
异-C4H9 |
H |
1-萘基 |
3.240 |
环丙基 |
H |
1-萘基 |
3.241 |
1-CH3-环丙基 |
H |
1-萘基 |
3.242 |
CN |
H |
1-萘基 |
3.243 |
Ph |
H |
1-萘基 |
3.244 |
H |
CH3 |
1-萘基 |
3.245 |
CH3 |
CH3 |
1-萘基 |
3.246 |
C2H5 |
CH3 |
1-萘基 |
3.247 |
正-C3H7 |
CH3 |
1-萘基 |
3.248 |
异-C3H7 |
CH3 |
1-萘基 |
3.249 |
正-C4H9 |
CH3 |
1-萘基 |
3.250 |
异-C4H9 |
CH3 |
1-萘基 |
3.251 |
环丙基 |
CH3 |
1-萘基 |
3.252 |
1-CH3-环丙基 |
CH3 |
1-萘基 |
3.253 |
CN |
CH3 |
1-萘基 |
3.254 |
Ph |
CH3 |
1-萘基 |
3.255 |
H |
H |
2-萘基 |
3.256 |
CH3 |
H |
2-萘基 |
3.257 |
C2H5 |
H |
2-萘基 |
3.258 |
正-C3H7 |
H |
2-萘基 |
3.259 |
异-C3H7 |
H |
2-萘基 |
3.260 |
正-C4H9 |
H |
2-萘基 |
3.261 |
异-C4H9 |
H |
2-萘基 |
3.262 |
环丙基 |
H |
2-萘基 |
3.263 |
1-CH3-环丙基 |
H |
2-萘基 |
3.264 |
CN |
H |
2-萘基 |
3.265 |
Ph |
H |
2-萘基 |
3.266 |
H |
CH3 |
2-萘基 |
3.267 |
CH3 |
CH3 |
2-萘基 |
3.268 |
C2H5 |
CH3 |
2-萘基 |
3.269 |
正-C3H7 |
CH3 |
2-萘基 |
3.270 |
异-C3H7 |
CH3 |
2-萘基 |
3.271 |
正-C4H9 |
CH3 |
2-萘基 |
3.272 |
异-C4H9 |
CH3 |
2-萘基 |
3.273 |
环丙基 |
CH3 |
2-萘基 |
3.274 |
1-CH3-环丙基 |
CH3 |
2-萘基 |
3.275 |
CN |
CH3 |
2-萘基 |
3.276 |
Ph |
CH3 |
2-萘基 |
3.277 |
2-Cl(Ph) |
CH3 |
2-萘基 |
3.278 |
3-Cl(Ph) |
CH3 |
2-萘基 |
3.279 |
4-Cl(Ph) |
CH3 |
2-萘基 |
3.280 |
4-Br(Ph) |
CH3 |
2-萘基 |
3.281 |
4-OCH3(Ph) |
CH3 |
2-萘基 |
3.282 |
4-CH3(Ph) |
CH3 |
2-萘基 |
3.283 |
3-CF3(Ph) |
CH3 |
2-萘基 |
3.284 |
CH3 |
C2H5 |
Ph |
3.285 |
CH3 |
C2H5 |
2-Cl(Ph) |
3.286 |
CH3 |
C2H5 |
3-Cl(Ph) |
3.287 |
CH3 |
C2H5 |
4-Cl(Ph) |
3.288 |
CH3 |
C2H5 |
4-Br(Ph) |
3.289 |
CH3 |
C2H5 |
4-F(Ph) |
3.290 |
CH3 |
C2H5 |
4-OCH3(Ph) |
3.291 |
CH3 |
C2H5 |
4-CH3(Ph) |
3.292 |
CH3 |
C2H5 |
4-NO2(Ph) |
3.293 |
CH3 |
C2H5 |
2,4-Cl(Ph) |
3.294 |
CH3 |
C2H5 |
2,4-F(Ph) |
3.295 |
CH3 |
正-C3H7 |
Ph |
3.296 |
CH3 |
正-C3H7 |
2-Cl(Ph) |
3.297 |
CH3 |
正-C3H7 |
3-Cl(Ph) |
3.298 |
CH3 |
正-C3H7 |
4-Cl(Ph) |
3.299 |
CH3 |
正-C3H7 |
4-Br(Ph) |
3.300 |
CH3 |
正-C3H7 |
4-F(Ph) |
3.301 |
CH3 |
正-C3H7 |
4-OCH3(Ph) |
3.302 |
CH3 |
正-C3H7 |
4-CH3(Ph) |
3.303 |
CH3 |
正-C3H7 |
4-NO2(Ph) |
3.304 |
CH3 |
正-C3H7 |
2,4-Cl(Ph) |
3.305 |
CH3 |
正-C3H7 |
2,4-F(Ph) |
3.306 |
CH3 |
异-C3H7 |
Ph |
3.307 |
CH3 |
异-C3H7 |
2-Cl(Ph) |
3.308 |
CH3 |
异-C3H7 |
3-Cl(Ph) |
3.309 |
CH3 |
异-C3H7 |
4-Cl(Ph) |
3.310 |
CH3 |
异-C3H7 |
4-Br(Ph) |
3.311 |
CH3 |
异-C3H7 |
4-F(Ph) |
3.312 |
CH3 |
异-C3H7 |
4-OCH3(Ph) |
3.313 |
CH3 |
异-C3H7 |
4-CH3(Ph) |
3.314 |
CH3 |
异-C3H7 |
4-NO2(Ph) |
3.315 |
CH3 |
异-C3H7 |
2,4-Cl(Ph) |
3.316 |
CH3 |
异-C3H7 |
2,4-F(Ph) |
3.317 |
CH3 |
正-C4H9 |
Ph |
3.318 |
CH3 |
正-C4H9 |
2-Cl(Ph) |
3.319 |
CH3 |
正-C4H9 |
3-Cl(Ph) |
3.320 |
CH3 |
正-C4H9 |
4-Cl(Ph) |
3.321 |
CH3 |
正-C4H9 |
4-Br(Ph) |
3.322 |
CH3 |
正-C4H9 |
4-F(Ph) |
3.323 |
CH3 |
正-C4H9 |
4-OCH3(Ph) |
3.324 |
CH3 |
正-C4H9 |
4-CH3(Ph) |
3.325 |
CH3 |
正-C4H9 |
4-NO2(Ph) |
3.326 |
CH3 |
正-C4H9 |
2,4-Cl(Ph) |
3.327 |
CH3 |
正-C4H9 |
2,4-F(Ph) |
本发明式Ⅰ所涵盖的典型化合物包括式Ⅳ化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=CH,Y=O及Z=O的式Ⅰ化合物,而且其中的R
2、R
3和R
7如表4所定义。
表4
4.1 |
H |
Ph |
Ph |
4.2 |
H |
Ph |
2-Cl(Ph) |
4.3 |
H |
Ph |
3-Cl(Ph) |
4.4 |
H |
Ph |
4-Cl(Ph) |
4.5 |
H |
Ph |
2-Br(Ph) |
4.6 |
H |
Ph |
3-Br(Ph) |
4.7 |
H |
Ph |
4-Br(Ph) |
4.8 |
H |
Ph |
2-F(Ph) |
4.9 |
H |
Ph |
3-F(Ph) |
4.10 |
H |
Ph |
4-F(Ph) |
4.11 |
H |
Ph |
2-OCH3(Ph) |
4.12 |
H |
Ph |
3-OCH3(Ph) |
4.13 |
H |
Ph |
4-OCH3(Ph) |
4.14 |
H |
Ph |
2-OC2H5(Ph) |
4.15 |
H |
Ph |
3-OC2H5(Ph) |
4.16 |
H |
Ph |
4-OC2H5(Ph) |
4.17 |
H |
Ph |
4-OPh(Ph) |
4.18 |
H |
Ph |
2-CH3(Ph) |
4.19 |
H |
Ph |
3-CH3Ph) |
4.20 |
H |
Ph |
4-CH3(Ph) |
4.21 |
H |
Ph |
2-CF3(Ph) |
4.22 |
H |
Ph |
3-CF3(Ph) |
4.23 |
H |
Ph |
4-CF3(Ph) |
4.24 |
H |
Ph |
2-NO2(Ph) |
4.25 |
H |
Ph |
3-NO2(Ph) |
4.26 |
H |
Ph |
4-NO2(Ph) |
4.27 |
H |
Ph |
2,3-Cl(Ph) |
4.28 |
H |
Ph |
2,4-Cl(Ph) |
4.29 |
H |
Ph |
2,5-Cl(ph) |
4.30 |
H |
Ph |
2,6-Cl(Ph) |
4.31 |
H |
Ph |
3,4-Cl(ph) |
4.32 |
H |
Ph |
3,5-Cl(Ph) |
4.33 |
H |
Ph |
2,3-F(Ph) |
4.34 |
H |
Ph |
2,4-F(Ph) |
4.35 |
H |
Ph |
2,5-F(Ph) |
4.36 |
H |
Ph |
2,6-F(Ph) |
4.37 |
H |
Ph |
3,4-F(Ph) |
4.38 |
H |
Ph |
3,5-F(Ph) |
4.39 |
CH3 |
Ph |
Ph |
4.40 |
CH3 |
Ph |
2-Cl(Ph) |
4.41 |
CH3 |
Ph |
3-Cl(Ph) |
4.42 |
CH3 |
Ph |
4-Cl(Ph) |
4.43 |
CH3 |
Ph |
2-Br(Ph) |
4.44 |
CH3 |
Ph |
3-Br(Ph) |
4.45 |
CH3 |
Ph |
4-Br(Ph) |
4.46 |
CH3 |
Ph |
2-F(Ph) |
4.47 |
CH3 |
Ph |
3-F(Ph) |
4.48 |
CH3 |
Ph |
4-F(Ph) |
4.49 |
CH3 |
Ph |
2-OCH3(Ph) |
4.50 |
CH3 |
Ph |
3-OCH3(Ph) |
4.51 |
CH3 |
Ph |
4-OCH3(Ph) |
4.52 |
CH3 |
Ph |
2-OC2H5(Ph) |
4.53 |
CH3 |
Ph |
3-OC2H5(Ph) |
4.54 |
CH3 |
Ph |
4-OC2H5(Ph) |
4.55 |
CH3 |
Ph |
2-OPh(Ph) |
4.56 |
CH3 |
Ph |
3-OPh(Ph) |
4.57 |
CH3 |
Ph |
4-OPh(Ph) |
4.58 |
CH3 |
Ph |
2-CH3(Ph) |
4.59 |
CH3 |
Ph |
3-CH3(Ph) |
4.60 |
CH3 |
Ph |
4-CH3(Ph) |
4.61 |
CH3 |
Ph |
2-CF3(Ph) |
4.62 |
CH3 |
Ph |
3-CF3(Ph) |
4.63 |
CH3 |
Ph |
4-CF3(Ph) |
4.64 |
CH3 |
Ph |
4-OCF3(Ph) |
4.65 |
CH3 |
Ph |
2-NO2(Ph) |
4.66 |
CH3 |
Ph |
3-NO2(Ph) |
4.67 |
CH3 |
Ph |
4-NO2(Ph) |
4.68 |
CH3 |
Ph |
2,3-Cl(Ph) |
4.69 |
CH3 |
Ph |
2,4-Cl(Ph) |
4.70 |
CH3 |
Ph |
2,5-Cl(Ph) |
4.71 |
CH3 |
Ph |
2,6-Cl(Ph) |
4.72 |
CH3 |
Ph |
3,4-Cl(Ph) |
4.73 |
CH3 |
Ph |
3,5-Cl(Ph) |
4.74 |
CH3 |
Ph |
2,3-F(Ph) |
4.75 |
CH3 |
Ph |
2,4-F(Ph) |
4.76 |
CH3 |
Ph |
2,5-F(Ph) |
4.77 |
CH3 |
Ph |
2,6-F(Ph) |
4.78 |
CH3 |
Ph |
3,4-F(Ph) |
4.79 |
CH3 |
Ph |
3,5-F(Ph) |
4.80 |
C2H5 |
Ph |
2-Cl(Ph) |
4.81 |
正-C3H7 |
Ph |
3-Cl(Ph) |
4.82 |
异-C3H7 |
Ph |
4-Cl(Ph) |
4.83 |
正-C4H9 |
Ph |
4-Br(Ph) |
4.84 |
异-C4H9 |
Ph |
4-F(Ph) |
4.85 |
C(CH3)3 |
Ph |
4-OCH3(Ph) |
4.86 |
正-C5H11 |
Ph |
4-CH3(Ph) |
4.87 |
环丙基 |
Ph |
4-NO2(Ph) |
4.88 |
1-CH3-环丙基 |
Ph |
2,4-Cl(Ph) |
4.89 |
CN |
Ph |
2,4-F(Ph) |
4.90 |
Ph |
Ph |
Ph |
4.91 |
Ph |
Ph |
2-Cl(Ph) |
4.92 |
Ph |
Ph |
3-Cl(Ph) |
4.93 |
Ph |
Ph |
4-Cl(Ph) |
4.94 |
4-Cl(Ph) |
Ph |
Ph |
4.95 |
4-Cl(Ph) |
Ph |
4-Cl(Ph) |
4.96 |
4-F(Ph) |
Ph |
Ph |
4.97 |
4-F(Ph) |
Ph |
4-F(Ph) |
4.98 |
4-CF3(Ph) |
Ph |
Ph |
4.99 |
4-CF3(Ph) |
Ph |
4-CF3(Ph) |
4.100 |
2,4-Cl(Ph) |
Ph |
Ph |
4.101 |
2,4-Cl(Ph) |
Ph |
2,4-Cl(Ph) |
4.102 |
2,4-F(Ph) |
Ph |
Ph |
4.103 |
H |
2-Cl(Ph) |
Ph |
4.104 |
CH3 |
2-Cl(Ph) |
Ph |
4.105 |
C2H5 |
2-Cl(Ph) |
2-Cl(Ph) |
4.106 |
正-C3H7 |
2-Cl(Ph) |
3-Cl(Ph) |
4.107 |
异-C3H7 |
2-Cl(Ph) |
4-Cl(Ph) |
4.108 |
正-C4H9 |
2-Cl(Ph) |
4-Br(Ph) |
4.109 |
异-C4H9 |
2-Cl(Ph) |
4-F(Ph) |
4.110 |
C(CH3)3 |
2-Cl(Ph) |
4-OCH3(Ph) |
4.111 |
正-C5H11 |
2-Cl(Ph) |
4-CH3(Ph) |
4.112 |
环丙基 |
2-Cl(Ph) |
4-NO2(Ph) |
4.113 |
1-CH3-环丙基 |
2-Cl(Ph) |
2,4-Cl(Ph) |
4.114 |
CN |
2-Cl(Ph) |
2,4-F(Ph) |
4.115 |
Ph |
2-Cl(Ph) |
2-Cl(Ph) |
4.116 |
Ph |
2-Cl(Ph) |
3-Cl(Ph) |
4.117 |
Ph |
2-Cl(Ph) |
4-Cl(Ph) |
4.118 |
4-Cl(Ph) |
2-Cl(Ph) |
Ph |
4.119 |
4-Cl(Ph) |
2-Cl(Ph) |
4-Cl(Ph) |
4.120 |
4-F(Ph) |
2-Cl(Ph) |
Ph |
4.121 |
4-F(Ph) |
2-Cl(Ph) |
4-F(Ph) |
4.122 |
4-CF3(Ph) |
2-Cl(Ph) |
Ph |
4.123 |
4-CF3(Ph) |
2-Cl(Ph) |
4-CF3(Ph) |
4.124 |
2,4-Cl(Ph) |
2-Cl(Ph) |
Ph |
4.125 |
2,4-Cl(Ph) |
2-Cl(Ph) |
2,4-Cl(Ph) |
4.126 |
2,4-F(Ph) |
2-Cl(Ph) |
Ph |
4.127 |
H |
4-Cl(Ph) |
Ph |
4.128 |
CH3 |
4-Cl(Ph) |
Ph |
4.129 |
C2H5 |
4-Cl(Ph) |
2-Cl(Ph) |
4.130 |
正-C3H7 |
4-Cl(Ph) |
3-Cl(Ph) |
4.131 |
异-C3H7 |
4-Cl(Ph) |
4-Cl(Ph) |
4.132 |
正-C4H9 |
4-Cl(Ph) |
4-Br(Ph) |
4.133 |
异-C4H9 |
4-Cl(Ph) |
4-F(Ph) |
4.134 |
C(CH3)3 |
4-Cl(Ph) |
4-OCH3(Ph) |
4.135 |
正-C5H11 |
4-Cl(Ph) |
4-CH3(Ph) |
4.136 |
环丙基 |
4-Cl(Ph) |
4-NO2(Ph) |
4.137 |
1-CH3-环丙基 |
4-Cl(Ph) |
2,4-Cl(Ph) |
4.138 |
CN |
4-Cl(Ph) |
2,4-F(Ph) |
4.139 |
Ph |
4-Cl(Ph) |
2-Cl(Ph) |
4.140 |
Ph |
4-Cl(Ph) |
3-Cl(Ph) |
4.141 |
Ph |
4-Cl(Ph) |
4-Cl(Ph) |
4.142 |
4-Cl(Ph) |
4-Cl(Ph) |
Ph |
4.143 |
4-Cl(Ph) |
4-Cl(Ph) |
4-Cl(Ph) |
4.144 |
4-F(Ph) |
4-Cl(Ph) |
Ph |
4.145 |
4-F(Ph) |
4-Cl(Ph) |
4-F(Ph) |
4.146 |
4-CF3(Ph) |
4-Cl(Ph) |
Ph |
4.147 |
4-CF3(Ph) |
4-Cl(Ph) |
4-CF3(Ph) |
4.148 |
2,4-Cl(Ph) |
4-Cl(Ph) |
Ph |
4.149 |
2,4-Cl(Ph) |
4-Cl(Ph) |
2,4-Cl(Ph) |
4.150 |
2,4-F(Ph) |
4-Cl(Ph) |
Ph |
4.151 |
H |
4-CF3(Ph) |
Ph |
4.152 |
CH3 |
4-CF3(Ph) |
Ph |
4.153 |
C2H5 |
4-CF3(Ph) |
2-Cl(Ph) |
4.154 |
正-C3H7 |
4-CF3(Ph) |
3-Cl(Ph) |
4.155 |
异-C3H7 |
4-CF3(Ph) |
4-Cl(Ph) |
4.156 |
正-C4H9 |
4-CF3(Ph) |
4-Br(Ph) |
4.157 |
异-C4H9 |
4-CF3(Ph) |
4-F(Ph) |
4.158 |
C(CH3)3 |
4-CF3(Ph) |
4-OCH3(Ph) |
4.159 |
正-C5H11 |
4-CF3(Ph) |
4-CH3(Ph) |
4.160 |
环丙基 |
4-CF3(Ph) |
4-NO2(Ph) |
4.161 |
1-CH3-环丙基 |
4-CF3(Ph) |
2,4-Cl(Ph) |
4.162 |
CN |
4-CF3(Ph) |
2,4-F(Ph) |
4.163 |
Ph |
4-CF3(Ph) |
2-Cl(Ph) |
4.164 |
Ph |
4-CF3(Ph) |
3-Cl(Ph) |
4.165 |
Ph |
4-CF3(Ph) |
4-Cl(Ph) |
4.166 |
4-Cl(Ph) |
4-CF3(Ph) |
Ph |
4.167 |
4-Cl(Ph) |
4-CF3(Ph) |
4-Cl(Ph) |
4.168 |
4-F(Ph) |
4-CF3(Ph) |
Ph |
4.169 |
4-F(Ph) |
4-CF3(Ph) |
4-F(Ph) |
4.170 |
4-CF3(Ph) |
4-CF3(Ph) |
Ph |
4.171 |
4-CF3(Ph) |
4-CF3(Ph) |
4-CF3(Ph) |
4.172 |
2,4-Cl(Ph) |
4-CF3(Ph) |
Ph |
4.173 |
2,4-Cl(Ph) |
4-CF3(Ph) |
2,4-Cl(Ph) |
4.174 |
2,4-F(Ph) |
4-CF3(Ph) |
Ph |
4.175 |
H |
1-萘基 |
Ph |
4.176 |
CH3 |
1-萘基 |
Ph |
4.177 |
C2H5 |
1-萘基 |
2-Cl(Ph) |
4.178 |
正-C3H7 |
1-萘基 |
3-Cl(Ph) |
4.179 |
异-C3H7 |
1-萘基 |
4-Cl(Ph) |
4.180 |
正-C4H9 |
1-萘基 |
4-Br(Ph) |
4.181 |
异-C4H9 |
1-萘基 |
4-F(Ph) |
4.182 |
C(CH3)3 |
1-萘基 |
4-OCH3(Ph) |
4.183 |
正-C5H11 |
1-萘基 |
4-CH3(Ph) |
4.184 |
环丙基 |
1-萘基 |
4-NO2(Ph) |
4.185 |
1-CH3-环丙基 |
1-萘基 |
2,4-Cl(Ph) |
4.186 |
CN |
1-萘基 |
2,4-F(Ph) |
4.187 |
Ph |
1-萘基 |
2-Cl(Ph) |
4.188 |
Ph |
1-萘基 |
3-Cl(Ph) |
4.189 |
Ph |
1-萘基 |
4-Cl(Ph) |
4.190 |
4-Cl(Ph) |
1-萘基 |
Ph |
4.191 |
4-Cl(Ph) |
1-萘基 |
4-Cl(Ph) |
4.192 |
4-F(Ph) |
1-萘基 |
Ph |
4.193 |
4-F(Ph) |
1-萘基 |
4-F(Ph) |
4.194 |
4-CF3(Ph) |
1-萘基 |
Ph |
4.195 |
4-CF3(Ph) |
1-萘基 |
4-CF3(Ph) |
4.196 |
2,4-Cl(Ph) |
1-萘基 |
Ph |
4.197 |
2,4-Cl(Ph) |
1-萘基 |
2,4-Cl(Ph) |
4.198 |
2,4-F(Ph) |
1-萘基 |
Ph |
4.199 |
CH3 |
2-吡啶基 |
Ph |
4.200 |
CH3 |
3-吡啶基 |
Ph |
4.201 |
CH3 |
4-吡啶基 |
Ph |
4.202 |
CH3 |
2-噻吩基 |
Ph |
4.203 |
CH3 |
3-噻吩基 |
Ph |
4.204 |
CH3 |
2-呋喃基 |
Ph |
4.205 |
CH3 |
3-呋喃基 |
Ph |
4.206 |
CH3 |
5-嘧啶基 |
Ph |
4.207 |
CH3 |
2-吡啶基 |
4-Cl(Ph) |
4.208 |
CH3 |
3-吡啶基 |
4-Cl(Ph) |
4.209 |
CH3 |
4-吡啶基 |
4-Cl(Ph) |
4.210 |
CH3 |
2-噻吩基 |
4-Cl(Ph) |
4.211 |
CH3 |
3-噻吩基 |
4-Cl(Ph) |
4.212 |
CH3 |
2-呋喃基 |
4-Cl(Ph) |
4.213 |
CH3 |
3-呋喃基 |
4-Cl(Ph) |
4.214 |
CH3 |
5-嘧啶基 |
4-Cl(Ph) |
4.215 |
CH3 |
2-吡啶基 |
3-CF3(Ph) |
4.216 |
CH3 |
3-吡啶基 |
3-CF3(Ph) |
4.217 |
CH3 |
4-吡啶基 |
3-CF3(Ph) |
4.218 |
CH3 |
2-噻吩基 |
3-CF3(Ph) |
4.219 |
CH3 |
3-噻吩基 |
3-CF3(Ph) |
4.220 |
CH3 |
2-呋喃基 |
3-CF3(Ph) |
4.221 |
CH3 |
3-呋喃基 |
3-CF3(Ph) |
4.222 |
CH3 |
5-嘧啶基 |
3-CF3(Ph) |
4.223 |
CH3 |
2-吡啶基 |
4-CF3(Ph) |
4.224 |
CH3 |
3-吡啶基 |
4-CF3(Ph) |
4.225 |
CH3 |
4-吡啶基 |
4-CF3(Ph) |
4.226 |
CH3 |
2-噻吩基 |
4-CF3(Ph) |
表5:化合物5.1-5.226为式V化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=O的式Ⅰ化合物,而且其中的R2、R3和R7如表4所定义。
表6:化合物5.1-5.226为式Ⅵ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=O的式Ⅰ化合物,而且其中的R2、R3和R7如表4所定义。
本发明式Ⅰ所涵盖的典型化合物包括式Ⅳ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=O的式Ⅰ化合物,而且其中的R2、R3和R7如表7所定义。
表7
化合物 |
R2 |
R3 |
R7 |
7.1 |
H |
H |
2-吡啶基 |
7.2 |
H |
H |
3-吡啶基 |
7.3 |
H |
H |
4-吡啶基 |
7.4 |
H |
H |
2-噻吩基 |
7.5 |
H |
H |
3-噻吩基 |
7.6 |
H |
H |
2-呋喃基 |
7.7 |
H |
H |
3-呋喃基 |
7.8 |
H |
H |
4-嘧啶基 |
7.9 |
H |
H |
5-嘧啶基 |
7.10 |
H |
H |
吡嗪基 |
7.11 |
CH3 |
H |
2-吡啶基 |
7.12 |
CH3 |
H |
3-吡啶基 |
7.13 |
CH3 |
H |
4-吡啶基 |
7.14 |
CH3 |
H |
2-噻吩基 |
7.15 |
CH3 |
H |
3-噻吩基 |
7.16 |
CH3 |
H |
2-呋喃基 |
7.17 |
CH3 |
H |
3-呋喃基 |
7.18 |
CH3 |
H |
4-嘧啶基 |
7.19 |
CH3 |
H |
5-嘧啶基 |
7.20 |
CH3 |
H |
吡嗪基 |
7.21 |
C2H5 |
H |
2-吡啶基 |
7.22 |
C2H5 |
H |
3-吡啶基 |
7.23 |
C2H5 |
H |
4-吡啶基 |
7.24 |
C2H5 |
H |
2-噻吩基 |
7.25 |
C2H5 |
H |
3-噻吩基 |
7.26 |
C2H5 |
H |
2-呋喃基 |
7.27 |
C2H5 |
H |
3-呋喃基 |
7.28 |
C2H5 |
H |
4-嘧啶基 |
7.29 |
C2H5 |
H |
5-嘧啶基 |
7.30 |
C2H5 |
H |
吡嗪基 |
7.31 |
正-C3H7 |
H |
2-吡啶基 |
7.32 |
正-C3H7 |
H |
3-吡啶基 |
7.33 |
正-C3H7 |
H |
4-吡啶基 |
7.34 |
正-C3H7 |
H |
2-噻吩基 |
7.35 |
正-C3H7 |
H |
3-噻吩基 |
7.36 |
正-C3H7 |
H |
2-呋喃基 |
7.37 |
正-C3H7 |
H |
3-呋喃基 |
7.38 |
正-C3H7 |
H |
4-嘧啶基 |
7.39 |
正-C3H7 |
H |
5-嘧啶基 |
7.40 |
正-C3H7 |
H |
吡嗪基 |
7.41 |
环丙基 |
H |
2-吡啶基 |
7.42 |
环丙基 |
H |
3-吡啶基 |
7.43 |
环丙基 |
H |
4-吡啶基 |
7.44 |
环丙基 |
H |
2-噻吩基 |
7.45 |
环丙基 |
H |
3-噻吩基 |
7.46 |
环丙基 |
H |
2-呋喃基 |
7.47 |
环丙基 |
H |
3-呋喃基 |
7.48 |
环丙基 |
H |
4-嘧啶基 |
7.49 |
环丙基 |
H |
5-嘧啶基 |
7.50 |
环丙基 |
H |
吡嗪基 |
7.51 |
CN |
H |
2-吡啶基 |
7.52 |
CN |
H |
3-吡啶基 |
7.53 |
CN |
H |
4-吡啶基 |
7.54 |
CN |
H |
2-噻吩基 |
7.55 |
CN |
H |
3-噻吩基 |
7.56 |
CN |
H |
2-呋喃基 |
7.57 |
CN |
H |
3-呋喃基 |
7.58 |
CN |
H |
4-嘧啶基 |
7.59 |
CN |
H |
5-嘧啶基 |
7.60 |
CN |
H |
吡嗪基 |
7.61 |
CH3 |
CH3 |
2-吡啶基 |
7.62 |
CH3 |
CH3 |
3-吡啶基 |
7.63 |
CH3 |
CH3 |
4-吡啶基 |
7.64 |
CH3 |
CH3 |
2-噻吩基 |
7.65 |
CH3 |
CH3 |
3-噻吩基 |
7.66 |
CH3 |
CH3 |
2-呋哺基 |
7.67 |
CH3 |
CH3 |
3-呋喃基 |
7.68 |
CH3 |
CH3 |
4-嘧啶基 |
7.69 |
CH3 |
CH3 |
5-嘧啶基 |
7.70 |
CH3 |
CH3 |
吡嗪基 |
7.71 |
CH3 |
H |
2-吡啶基 CH2- |
7.71 |
CH3 |
H |
3-吡啶基 CH2- |
7.70 |
CH3 |
H |
4-吡啶基 CH2- |
7.71 |
CH3 |
H |
2-噻吩基 CH2- |
7.72 |
CH3 |
H |
3-噻吩基 CH2- |
7.73 |
CH3 |
H |
2-呋喃基 CH2- |
7.74 |
CH3 |
H |
3-呋喃基 CH2- |
7.75 |
CH3 |
CH3 |
2-吡啶基 CH2- |
7.76 |
CH3 |
CH3 |
2-噻吩基 CH2- |
7.77 |
H |
Ph |
2-吡啶基 |
7.78 |
H |
Ph |
3-吡啶基 |
7.79 |
H |
Ph |
4-吡啶基 |
7.80 |
H |
Ph |
2-噻吩基 |
7.81 |
H |
Ph |
3-噻吩基 |
7.82 |
H |
Ph |
2-呋哺基 |
7.83 |
H |
Ph |
3-呋喃基 |
7.84 |
H |
Ph |
4-嘧啶基 |
7.85 |
H |
Ph |
5-嘧啶基 |
7.86 |
H |
Ph |
吡嗪基 |
7.87 |
CH3 |
Ph |
2-吡啶基 |
7.88 |
CH3 |
Ph |
3-吡啶基 |
7.89 |
CH3 |
Ph |
4-吡啶基 |
7.90 |
CH3 |
Ph |
2-噻吩基 |
7.91 |
CH3 |
Ph |
3-噻吩基 |
7.92 |
CH3 |
Ph |
2-呋喃基 |
7.93 |
CH3 |
Ph |
3-呋喃基 |
7.94 |
CH3 |
Ph |
4-嘧啶基 |
7.95 |
CH3 |
Ph |
5-嘧啶基 |
7.96 |
CH3 |
Ph |
吡嗪基 |
7.97 |
CH3 |
2-Cl(Ph) |
2-吡啶基 |
7.98 |
CH3 |
2-Cl(Ph) |
3-吡啶基 |
7.99 |
CH3 |
2-Cl(Ph) |
4-吡啶基 |
7.100 |
CH3 |
2-Cl(Ph) |
2-噻吩基 |
7.101 |
CH3 |
2-Cl(Ph) |
3-噻吩基 |
7.102 |
CH3 |
2-Cl(Ph) |
2-呋喃基 |
7.103 |
CH3 |
2-Cl(Ph) |
3-呋喃基 |
7.104 |
CH3 |
2-Cl(Ph) |
4-嘧啶基 |
7.105 |
CH3 |
2-Cl(Ph) |
5-嘧啶基 |
7.106 |
CH3 |
2-Cl(Ph) |
吡嗪基 |
7.107 |
CH3 |
4-Cl(Ph) |
2-吡啶基 |
7.108 |
CH3 |
4-Cl(Ph) |
3-吡啶基 |
7.109 |
CH3 |
4-Cl(Ph) |
4-吡啶基 |
7.110 |
CH3 |
4-Cl(Ph) |
2-噻吩基 |
7.111 |
CH3 |
4-Cl(Ph) |
3-噻吩基 |
7.112 |
CH3 |
4-Cl(Ph) |
2-呋喃基 |
7.113 |
CH3 |
4-Cl(Ph) |
3-呋喃基 |
7.114 |
CH3 |
4-Cl(Ph) |
4-嘧啶基 |
7.115 |
CH3 |
4-Cl(Ph) |
5-嘧啶基 |
7.116 |
CH3 |
4-Cl(Ph) |
吡嗪基 |
7.117 |
CH3 |
1-萘基 |
2-吡啶基 |
7.118 |
CH3 |
1-萘基 |
3-吡啶基 |
7.119 |
CH3 |
1-萘基 |
4-吡啶基 |
7.120 |
CH3 |
1-萘基 |
2-噻吩基 |
7.121 |
CH3 |
1-萘基 |
3-噻吩基 |
7.122 |
CH3 |
1-萘基 |
2-呋喃基 |
7.123 |
CH3 |
1-萘基 |
3-呋喃基 |
7.124 |
CH3 |
1-萘基 |
4-嘧啶基 |
7.125 |
CH3 |
1-萘基 |
5-嘧啶基 |
7.126 |
CH3 |
1-萘基 |
吡嗪基 |
7.127 |
CN |
Ph |
2-吡啶基 |
7.128 |
CN |
Ph |
3-吡啶基 |
7.129 |
CN |
Ph |
4-吡啶基 |
7.130 |
CN |
Ph |
2-噻吩基 |
7.131 |
CN |
Ph |
3-噻吩基 |
7.132 |
CN |
Ph |
2-呋喃基 |
7.133 |
CN |
Ph |
3-呋喃基 |
7.134 |
CN |
Ph |
4-嘧啶基 |
7.135 |
CN |
Ph |
5-嘧啶基 |
7.136 |
CN |
Ph |
吡嗪基 |
7.127 |
CN |
4-Cl(Ph) |
2-吡啶基 |
7.128 |
CN |
4-Cl(Ph) |
3-吡啶基 |
7.129 |
CN |
4-Cl(Ph) |
4-吡啶基 |
7.130 |
CN |
4-Cl(Ph) |
2-噻吩基 |
7.131 |
CN |
4-Cl(Ph) |
3-噻吩基 |
7.132 |
CN |
4-Cl(Ph) |
2-呋喃基 |
7.133 |
CN |
4-Cl(Ph) |
3-呋喃基 |
7.134 |
CN |
4-Cl(Ph) |
4-嘧啶基 |
7.135 |
CN |
4-Cl(Ph) |
5-嘧啶基 |
7.136 |
CN |
4-Cl(Ph) |
吡嗪基 |
7.127 |
CN |
1-萘基 |
2-吡啶基 |
7.128 |
CN |
1-萘基 |
3-吡啶基 |
7.129 |
CN |
1-萘基 |
4-吡啶基 |
7.130 |
CN |
1-萘基 |
2-噻吩基 |
7.131 |
CN |
1-萘基 |
3-噻吩基 |
7.132 |
CN |
1-萘基 |
2-呋喃基 |
7.133 |
CN |
1-萘基 |
3-呋喃基 |
7.134 |
CN |
1-萘基 |
4-嘧啶基 |
7.135 |
CN |
1-萘基 |
5-嘧啶基 |
7.136 |
CN |
1-萘基 |
吡嗪基 |
7.137 |
H |
2-吡啶基 |
2-吡啶基 |
7.138 |
H |
3-吡啶基 |
2-吡啶基 |
7.139 |
H |
4-吡啶基 |
2-吡啶基 |
7.140 |
H |
2-噻吩基 |
2-吡啶基 |
7.141 |
H |
3-噻吩基 |
2-吡啶基 |
7.142 |
H |
2-呋喃基 |
2-吡啶基 |
7.143 |
H |
3-呋喃基 |
2-吡啶基 |
7.144 |
H |
4-嘧啶基 |
2-吡啶基 |
7.145 |
H |
5-嘧啶基 |
2-吡啶基 |
7.146 |
H |
吡嗪基 |
2-吡啶基 |
7.147 |
H |
2-吡啶基 |
3-吡啶基 |
7.148 |
H |
3-吡啶基 |
3-吡啶基 |
7.149 |
H |
4-吡啶基 |
3-吡啶基 |
7.150 |
H |
2-噻吩基 |
3-吡啶基 |
7.151 |
H |
3-噻吩基 |
3-吡啶基 |
7.152 |
H |
2-呋喃基 |
3-吡啶基 |
7.153 |
H |
3-呋喃基 |
3-吡啶基 |
7.154 |
H |
4-嘧啶基 |
3-吡啶基 |
7.155 |
H |
5-嘧啶基 |
3-吡啶基 |
7.156 |
H |
吡嗪基 |
3-吡啶基 |
7.157 |
H |
2-吡啶基 |
2-噻吩基 |
7.158 |
H |
3-吡啶基 |
2-噻吩基 |
7.159 |
H |
4-吡啶基 |
2-噻吩基 |
7.160 |
H |
2-噻吩基 |
2-噻吩基 |
7.161 |
H |
3-噻吩基 |
2-噻吩基 |
7.162 |
H |
2-呋喃基 |
2-噻吩基 |
7.163 |
H |
3-呋喃基 |
2-噻吩基 |
7.164 |
H |
4-嘧啶基 |
2-噻吩基 |
7.165 |
H |
5-嘧啶基 |
2-噻吩基 |
7.166 |
H |
吡嗪基 |
2-噻吩基 |
7.167 |
CH3 |
2-吡啶基 |
2-吡啶基 |
7.168 |
CH3 |
3-吡啶基 |
2-吡啶基 |
7.169 |
CH3 |
4-吡啶基 |
2-吡啶基 |
7.170 |
CH3 |
2-噻吩基 |
2-吡啶基 |
7.171 |
CH3 |
3-噻吩基 |
2-吡啶基 |
7.172 |
CH3 |
2-呋喃基 |
2-吡啶基 |
7.173 |
CH3 |
3-呋喃基 |
2-吡啶基 |
7.174 |
CH3 |
4-嘧啶基 |
2-吡啶基 |
7.175 |
CH3 |
5-嘧啶基 |
2-吡啶基 |
7.176 |
CH3 |
吡嗪基 |
2-吡啶基 |
7.177 |
CH3 |
2-吡啶基 |
3-吡啶基 |
7.178 |
CH3 |
3-吡啶基 |
3-吡啶基 |
7.179 |
CH3 |
4-吡啶基 |
3-吡啶基 |
7.180 |
CH3 |
2-噻吩基 |
3-吡啶基 |
7.181 |
CH3 |
3-噻吩基 |
3-吡啶基 |
7.182 |
CH3 |
2-呋喃基 |
3-吡啶基 |
7.183 |
CH3 |
3-呋喃基 |
3-吡啶基 |
7.184 |
CH3 |
4-嘧啶基 |
3-吡啶基 |
7.185 |
CH3 |
5-嘧啶基 |
3-吡啶基 |
7.186 |
CH3 |
吡嗪基 |
3-吡啶基 |
7.187 |
CH3 |
2-吡啶基 |
2-噻吩基 |
7.188 |
CH3 |
3-吡啶基 |
2-噻吩基 |
7.190 |
CH3 |
4-吡啶基 |
2-噻吩基 |
7.191 |
CH3 |
2-噻吩基 |
2-噻吩基 |
7.192 |
CH3 |
3-噻吩基 |
2-噻吩基 |
7.193 |
CH3 |
2-呋喃基 |
2-噻吩基 |
7.194 |
CH3 |
3-呋喃基 |
2-噻吩基 |
7.195 |
CH3 |
4-嘧啶基 |
2-噻吩基 |
7.196 |
CH3 |
5-嘧啶基 |
2-噻吩基 |
7.197 |
CH3 |
吡嗪基 |
2-噻吩基 |
7.198 |
CN |
2-吡啶基 |
2-吡啶基 |
7.199 |
CN |
3-吡啶基 |
2-吡啶基 |
7.200 |
CN |
4-吡啶基 |
2-吡啶基 |
7.201 |
CN |
2-噻吩基 |
2-吡啶基 |
7.202 |
CN |
3-噻吩基 |
2-吡啶基 |
7.203 |
CN |
2-呋喃基 |
2-吡啶基 |
7.204 |
CN |
3-呋喃基 |
2-吡啶基 |
7.205 |
CN |
4-嘧啶基 |
2-吡啶基 |
7.206 |
CN |
5-嘧啶基 |
2-吡啶基 |
7.207 |
CN |
吡嗪基 |
2-吡啶基 |
7.208 |
CN |
2-吡啶基 |
3-吡啶基 |
7.209 |
CN |
3-吡啶基 |
3-吡啶基 |
7.210 |
CN |
4-吡啶基 |
3-吡啶基 |
7.211 |
CN |
2-噻吩基 |
3-吡啶基 |
7.212 |
CN |
3-噻吩基 |
3-吡啶基 |
7.213 |
CN |
2-呋喃基 |
3-吡啶基 |
7.214 |
CN |
3-呋喃基 |
3-吡啶基 |
7.215 |
CN |
4-嘧啶基 |
3-吡啶基 |
7.216 |
CN |
5-嘧啶基 |
3-吡啶基 |
7.217 |
CN |
吡嗪基 |
3-吡啶基 |
7.218 |
CN |
2-吡啶基 |
2-噻吩基 |
7.219 |
CN |
3-吡啶基 |
2-噻吩基 |
7.220 |
CN |
4-吡啶基 |
2-噻吩基 |
表8:化合物8.1-8.221为式V化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=O的式Ⅰ化合物,而且其中的R2、R3和R7如表7所定义。
表9:化合物9.1-9.221为式V化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=N-H及Z=O的式Ⅰ化合物,而且其中的R2、R3和R7如表7所定义。
本发明式Ⅰ所涵盖的典型化合物包括式Ⅳ化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=CH,Y=O及Z=O的式Ⅰ化合物,而且其中的R
2、R
3和R
2如表10所定义。
表10
化合物 |
R2 |
R3 |
R7 |
10.1 |
H |
Ph |
H |
10.2 |
H |
Ph |
CH3 |
10.3 |
H |
Ph |
C2H5 |
10.4 |
H |
Ph |
正-C3H7 |
10.5 |
H |
Ph |
异-C3H7 |
10.6 |
H |
Ph |
正-C4H9 |
10.7 |
H |
Ph |
C(CH3)3 |
10.3 |
H |
Ph |
正-C5H11 |
10.9 |
H |
Ph |
环丙基 |
10.10 |
H |
4-Cl(Ph) |
H |
10.11 |
H |
4-Cl(Ph) |
CH3 |
10.12 |
H |
4-Cl(Ph) |
C2H5 |
10.13 |
H |
4-Cl(Ph) |
正-C3H7 |
10.14 |
H |
4-Cl(Ph) |
异-C3H7 |
10.15 |
H |
4-Cl(Ph) |
正-C4H9 |
10.16 |
H |
4-Cl(Ph) |
C(CH3)3 |
10.17 |
H |
4-Cl(Ph) |
正-C5H11 |
10.18 |
H |
4-Cl(Ph) |
环丙基 |
10.19 |
H |
4-Cl(Ph) |
环己基 |
10.20 |
CH3 |
Ph |
H |
10.21 |
CH3 |
Ph |
CH3 |
10.22 |
CH3 |
Ph |
C2H5 |
10.23 |
CH3 |
Ph |
正-C3H7 |
10.24 |
CH3 |
Ph |
异-C3H7 |
10.25 |
CH3 |
Ph |
正-C4H9 |
10.26 |
CH3 |
Ph |
C(CH3)3 |
10.27 |
CH3 |
Ph |
正-C5H11 |
10.28 |
CH3 |
Ph |
环丙基 |
10.29 |
CH3 |
4-Cl(Ph) |
H |
10.30 |
CH3 |
4-Cl(Ph) |
CH3 |
10.31 |
CH3 |
4-Cl(Ph) |
C2H5 |
10.32 |
CH3 |
4-Cl(Ph) |
正-C3H7 |
10.33 |
CH3 |
4-Cl(Ph) |
异-C3H7 |
10.34 |
CH3 |
4-Cl(Ph) |
正-C4H9 |
10.35 |
CH3 |
4-Cl(Ph) |
C(CH3)3 |
10.36 |
CH3 |
4-Cl(Ph) |
正-C5H11 |
10.37 |
CH3 |
4-Cl(Ph) |
环丙基 |
10.38 |
CH3 |
4-Cl(Ph) |
环己基 |
10.39 |
H |
1-萘基 |
H |
10.40 |
H |
1-萘基 |
CH3 |
10.41 |
H |
1-萘基 |
C2H5 |
10.42 |
H |
1-萘基 |
正-C3H7 |
10.43 |
H |
1-萘基 |
异-C3H7 |
10.44 |
H |
1-萘基 |
正-C4H9 |
10.45 |
H |
1-萘基 |
C(CH3)3 |
10.46 |
H |
1-萘基 |
正-C5H11 |
10.47 |
H |
1-萘基 |
环丙基 |
10.48 |
H |
1-萘基 |
环己基 |
10.49 |
CH3 |
1-萘基 |
H |
10.50 |
CH3 |
1-萘基 |
CH3 |
10.51 |
CH3 |
1-萘基 |
C2H5 |
10.52 |
CH3 |
1-萘基 |
正-C3H7 |
10.53 |
CH3 |
1-萘基 |
异-C3H7 |
10.54 |
CH3 |
1-萘基 |
正-C4H9 |
10.55 |
CH3 |
1-萘基 |
C(CH3)3 |
10.56 |
CH3 |
1-萘基 |
正-C5H11 |
10.57 |
CH3 |
1-萘基 |
环丙基 |
10.58 |
CH3 |
1-萘基 |
环己基 |
10.59 |
H |
2-吡啶基 |
H |
10.60 |
H |
2-吡啶基 |
CH3 |
10.61 |
H |
2-吡啶基 |
C2H5 |
10.62 |
H |
2-吡啶基 |
正-C3H7 |
10.63 |
H |
2-吡啶基 |
异-C3H7 |
10.64 |
H |
2-吡啶基 |
正-C4H9 |
10.65 |
H |
2-吡啶基 |
C(CH3)3 |
10.66 |
H |
2-吡啶基 |
正-C5H11 |
10.67 |
H |
2-吡啶基 |
环丙基 |
10.68 |
H |
2-吡啶基 |
环己基 |
10.69 |
H |
3-吡啶基 |
H |
10.70 |
H |
3-吡啶基 |
CH3 |
10.71 |
H |
3-吡啶基 |
C2H5 |
10.72 |
H |
3-吡啶基 |
正-C3H7 |
10.73 |
H |
3-吡啶基 |
正-C4H9 |
10.74 |
H |
3-吡啶基 |
异-C4H9 |
10.75 |
H |
3-吡啶基 |
C(CH3)3 |
10.76 |
H |
3-吡啶基 |
正-C5H11 |
10.77 |
H |
3-吡啶基 |
环丙基 |
10.78 |
H |
3-吡啶基 |
环己基 |
10.79 |
H |
2-噻吩基 |
H |
10.80 |
H |
2-噻吩基 |
CH3 |
10.81 |
H |
2-噻吩基 |
C2H5 |
10.82 |
H |
2-噻吩基 |
正-C3H7 |
10.83 |
H |
2-噻吩基 |
异-C3H7 |
10.84 |
H |
2-噻吩基 |
正-C4H9 |
10.85 |
H |
2-噻吩基 |
C(CH3)3 |
10.86 |
H |
2-噻吩基 |
正-C5H11 |
10.87 |
H |
2-噻吩基 |
环丙基 |
10.88 |
H |
2-噻吩基 |
环己基 |
10.89 |
H |
3-噻吩基 |
H |
10.90 |
H |
3-噻吩基 |
CH3 |
10.91 |
H |
3-噻吩基 |
C2H5 |
10.92 |
H |
3-噻吩基 |
正-C3H7 |
10.93 |
H |
3-噻吩基 |
异-C3H7 |
10.94 |
H |
3-噻吩基 |
正-C4H9 |
10.95 |
H |
3-噻吩基 |
C(CH3)3 |
10.96 |
H |
3-噻吩基 |
正-C5H11 |
10.97 |
H |
3-噻吩基 |
环丙基 |
10.98 |
H |
3-噻吩基 |
环己基 |
10.99 |
H |
2-呋喃基 |
H |
10.90 |
H |
2-呋喃基 |
CH3 |
10.91 |
H |
2-呋喃基 |
C2H5 |
10.92 |
H |
2-呋喃基 |
正-C3H7 |
10.93 |
H |
2-呋喃基 |
异-C3H7 |
10.94 |
H |
2-呋喃基 |
正-C4H9 |
10.95 |
H |
2-呋喃基 |
C(CH3)3 |
10.96 |
H |
2-呋喃基 |
正-C5H11 |
10.97 |
H |
2-呋喃基 |
环丙基 |
10.98 |
H |
2-呋喃基 |
环己基 |
10.99 |
CH3 |
2-吡啶基 |
H |
10.100 |
CH3 |
2-吡啶基 |
CH3 |
10.102 |
CH3 |
2-吡啶基 |
C2H5 |
10.103 |
CH3 |
2-吡啶基 |
正-C3H7 |
10.104 |
CH3 |
2-吡啶基 |
异-C3H7 |
10.105 |
CH3 |
2-吡啶基 |
正-C4H9 |
10.106 |
CH3 |
2-吡啶基 |
C(CH3)3 |
10.107 |
CH3 |
2-吡啶基 |
正-C5H11 |
10.108 |
CH3 |
2-吡啶基 |
环丙基 |
10.109 |
CH3 |
2-吡啶基 |
环己基 |
10.110 |
CH3 |
3-吡啶基 |
H |
10.111 |
CH3 |
3-吡啶基 |
CH3 |
10.112 |
CH3 |
3-吡啶基 |
C2H5 |
10.113 |
CH3 |
3-吡啶基 |
正-C3H7 |
10.114 |
CH3 |
3-吡啶基 |
异-C3H7 |
10.115 |
CH3 |
3-吡啶基 |
正-C4H9 |
10.116 |
CH3 |
3-吡啶基 |
C(CH3)3 |
10.117 |
CH3 |
3-吡啶基 |
正-C5H11 |
10.118 |
CH3 |
3-吡啶基 |
环丙基 |
10.119 |
CH3 |
3-吡啶基 |
环己基 |
10.120 |
CH3 |
2-噻吩基 |
H |
10.121 |
CH3 |
2-噻吩基 |
CH3 |
10.122 |
CH3 |
2-噻吩基 |
C2H5 |
10.123 |
CH3 |
2-噻吩基 |
正-C3H7 |
10.124 |
CH3 |
2-噻吩基 |
异-C3H7 |
10.125 |
CH3 |
2-噻吩基 |
正-C4H9 |
10.126 |
CH3 |
2-噻吩基 |
C(CH3)3 |
10.127 |
CH3 |
2-噻吩基 |
正-C5H11 |
10.128 |
CH3 |
2-噻吩基 |
环丙基 |
10.129 |
CH3 |
2-噻吩基 |
环己基 |
10.130 |
CH3 |
3-噻吩基 |
H |
10.131 |
CH3 |
3-噻吩基 |
CH3 |
10.132 |
CH3 |
3-噻吩基 |
C2H5 |
10.133 |
CH3 |
3-噻吩基 |
正-C3H7 |
10.134 |
CH3 |
3-噻吩基 |
异-C3H7 |
10.135 |
CH3 |
3-噻吩基 |
正-C4H9 |
10.136 |
CH3 |
3-噻吩基 |
C(CH3)3 |
10.137 |
CH3 |
3-噻吩基 |
正-C5H11 |
10.133 |
CH3 |
3-噻吩基 |
环丙基 |
10.139 |
CH3 |
3-噻吩基 |
环己基 |
Table 11:
Compounds 11.1 to 11.139 are compounds of Formula V, which isFormula I with A=R4=R5=P6=H,R1=CH3,X=N,Y=O,and Z=O,and whereR2,R3 and R7 are defined in Table 10.Table 12:
Compounds 12.1 to 12.139 are compounds of Formula Ⅵ,which isFormula I with A=R4=R5=P6=H,R1=CH3,X=N,Y=NH,and Z=O,andwhere R2,R3,and R7 are defined in Table 10.
Typical compounds encompassed by the present invention ofFormula I include those compounds of Formula Ⅶ,which is Formula Iwith A=R4=R5=R6=H,R1=CH3,X=CH,Y=O,and Z=NOR9,and where R2,R3,R7 and R9 are defined in Table 13.
Table 13
化合物 |
R2 |
R3 |
R7 |
R9 |
13.1 |
H |
H |
Ph |
H |
13.2 |
H |
H |
4-Cl(Ph) |
H |
13.3 |
H |
H |
4-Br(Ph) |
H |
13.4 |
H |
H |
4-F(Ph) |
H |
13.5 |
H |
H |
4-OCH3(Ph) |
H |
13.6 |
H |
H |
4-CF3(Ph) |
H |
13.7 |
H |
H |
Ph |
CH3 |
13.8 |
H |
H |
4-Cl(Ph) |
CH3 |
13.9 |
H |
H |
4-Br(Ph) |
CH3 |
13.10 |
H |
H |
4-F(Ph) |
CH3 |
13.11 |
CH3 |
H |
Ph |
H |
13.12 |
CH3 |
H |
2-Cl(Ph) |
H |
13.13 |
CH3 |
H |
3-Cl(Ph) |
H |
13.14 |
CH3 |
H |
4-Cl(Ph) |
H |
13.15 |
CH3 |
H |
2-Br(Ph) |
H |
13.16 |
CH3 |
H |
3-Br(Ph) |
H |
13.17 |
CH3 |
H |
4-Br(Ph) |
H |
13.18 |
CH3 |
H |
Ph |
CH3 |
13.19 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
13.20 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
13.21 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
13.22 |
CH3 |
H |
2-F(Ph) |
CH3 |
13.23 |
CH3 |
H |
3-F(Ph) |
CH3 |
13.24 |
CH3 |
H |
4-F(Ph) |
CH3 |
13.25 |
CH3 |
H |
2-CH3(Ph) |
CH3 |
13.26 |
CH3 |
H |
3-CH3(Ph) |
CH3 |
13.27 |
CH3 |
H |
2-CF3(Ph) |
CH3 |
13.23 |
CH3 |
H |
3-CF3(Ph) |
CH3 |
13.29 |
CH3 |
H |
4-CF3(Ph) |
CH3 |
13.30 |
CH3 |
H |
2-OCH3(Ph) |
CH3 |
13.31 |
CH3 |
H |
3-OCH3(Ph) |
CH3 |
13.32 |
CH3 |
H |
2-OCH3(Ph) |
CH3 |
13.33 |
CH3 |
H |
2,3-Cl(Ph) |
CH3 |
13.34 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
13.35 |
CH3 |
H |
2,5-Cl(Ph) |
CH3 |
13.36 |
CH3 |
H |
2,6-Cl(Ph) |
CH3 |
13.37 |
CH3 |
H |
3,4-Cl(Ph) |
CH3 |
13.38 |
CH3 |
H |
3,5-Cl(Ph) |
CH3 |
13.39 |
CH3 |
H |
Ph |
C2H5 |
13.40 |
CH3 |
H |
Ph |
正-C3H7 |
13.41 |
CH3 |
H |
Ph |
异-C3H7 |
13.42 |
CH3 |
H |
Ph |
正-C4H9 |
13.43 |
CH3 |
H |
Ph |
C(CH3)3 |
13.44 |
CH3 |
H |
Ph |
CH2C≡CH |
13.45 |
C2H5 |
H |
Ph |
CH3 |
13.46 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
13.47 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
13.48 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
13.49 |
C2H5 |
H |
4-Br(Ph) |
CH3 |
13.50 |
C2H5 |
H |
4-F(Ph) |
CH3 |
13.51 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
13.52 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
13.53 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
13.54 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
13.55 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
13.56 |
正-C3H7 |
H |
Ph |
CH3 |
13.57 |
正-C3H7 |
H |
2-Cl(Ph) |
CH3 |
13.58 |
正-C3H7 |
H |
3-Cl(Ph) |
CH3 |
13.59 |
正-C3H7 |
H |
4-Cl(Ph) |
CH3 |
13.60 |
正-C3H7 |
H |
4-F(Ph) |
CH3 |
13.61 |
正-C3H7 |
H |
3-OCH3(Ph) |
CH3 |
13.62 |
正-C3H7 |
H |
4-OCH3(Ph) |
CH3 |
13.63 |
正-C3H7 |
H |
4-CH3(Ph) |
CH3 |
13.64 |
正-C3H7 |
H |
4-NO2(Ph) |
CH3 |
13.65 |
正-C3H7 |
H |
2,4-Cl(Ph) |
CH3 |
13.66 |
正-C3H7 |
H |
2,4-F(Ph) |
CH3 |
13.67 |
异-C3H7 |
H |
Ph |
CH3 |
13.68 |
异-C3H7 |
H |
2-Cl(Ph) |
CH3 |
13.69 |
异-C3H7 |
H |
3-Cl(Ph) |
CH3 |
13.70 |
异-C3H7 |
H |
4-Cl(Ph) |
CH3 |
13.71 |
异-C3H7 |
H |
4-Br(Ph) |
CH3 |
13.72 |
异-C3H7 |
H |
4-F(Ph) |
CH3 |
13.73 |
异-C3H7 |
H |
4-OCH3(Ph) |
CH3 |
13.74 |
异-C3H7 |
H |
4-CH3(Ph) |
CH3 |
13.75 |
异-C3H7 |
H |
4-NO2(Ph) |
CH3 |
13.76 |
异-C3H7 |
H |
2,4-Cl(Ph) |
CH3 |
13.77 |
异-C3H7 |
H |
2,4-F(Ph) |
CH3 |
13.78 |
正-C4H9 |
H |
Ph |
CH3 |
13.79 |
正-C4H9 |
H |
2-Cl(Ph) |
CH3 |
13.80 |
正-C4H9 |
H |
3-Cl(Ph) |
CH3 |
13.81 |
正-C4H9 |
H |
4-Cl(Ph) |
CH3 |
13.82 |
正-C4H9 |
H |
4-Br(Ph) |
CH3 |
13.83 |
正-C4H9 |
H |
4-F(Ph) |
CH3 |
13.84 |
正-C4H9 |
H |
4-OCH3(Ph) |
CH3 |
13.85 |
正-C4H9 |
H |
4-CH3(Ph) |
CH3 |
13.86 |
正-C4H9 |
H |
4-NO2(Ph) |
CH3 |
13.87 |
正-C4H9 |
H |
2,4-Cl(Ph) |
CH3 |
13.88 |
正-C4H9 |
H |
2,4-F(Ph) |
CH3 |
13.89 |
异-C4H9 |
H |
Ph |
CH3 |
13.90 |
异-C4H9 |
H |
2-Cl(Ph) |
CH3 |
13.91 |
异-C4H9 |
H |
3-Cl(Ph) |
CH3 |
13.92 |
异-C4H9 |
H |
4-Cl(Ph) |
CH3 |
13.93 |
异-C4H9 |
H |
4-F(Ph) |
CH3 |
13.94 |
异-C4H9 |
H |
3-OCH3(Ph) |
CH3 |
13.95 |
异-C4H9 |
H |
4-OCH3(Ph) |
CH3 |
13.96 |
异-C4H9 |
H |
4-CH3(Ph) |
CH3 |
13.97 |
异-C4H9 |
H |
4-NO2(Ph) |
CH3 |
13.98 |
异-C4H9 |
H |
2,4-Cl(Ph) |
CH3 |
13.99 |
异-C4H9 |
H |
2,4-F(Ph) |
CH3 |
13.100 |
C(CH3)3 |
H |
Ph |
CH3 |
13.101 |
C(CH3)3 |
H |
2-Cl(Ph) |
CH3 |
13.102 |
C(CH3)3 |
H |
3-Cl(Ph) |
CH3 |
13.103 |
C(CH3)3 |
H |
4-Cl(Ph) |
CH3 |
13.104 |
C(CH3)3 |
H |
4-F(Ph) |
CH3 |
13.105 |
C(CH3)3 |
H |
3-OCH3(Ph) |
CH3 |
13.106 |
C(CH3)3 |
H |
4-OCH3(Ph) |
CH3 |
13.107 |
C(CH3)3 |
H |
4-CH3(Ph) |
CH3 |
13.108 |
C(CH3)3 |
H |
4-NO2(Ph) |
CH3 |
13.109 |
C(CH3)3 |
H |
2,4-Cl(Ph) |
CH3 |
13.110 |
C(CH3)3 |
H |
2,4-F(Ph) |
CH3 |
13.111 |
环丙基 |
H |
Ph |
CH3 |
13.112 |
环丙基 |
H |
2-Cl(Pl) |
CH3 |
13.113 |
环丙基 |
H |
3-Cl(Ph) |
CH3 |
13.114 |
环丙基 |
H |
4-Cl(Ph) |
CH3 |
13.115 |
环丙基 |
H |
4-Br(Ph) |
CH3 |
13.116 |
环丙基 |
H |
3-OCH3(Ph) |
CH3 |
13.117 |
环丙基 |
H |
4-OCH3(Ph) |
CH3 |
13.118 |
环丙基 |
H |
4-CH3(Ph) |
CH3 |
13.119 |
环丙基 |
H |
4-NO2(Ph) |
CH3 |
13.120 |
环丙基 |
H |
2,4-Cl(Ph) |
CH3 |
13.121 |
环丙基 |
H |
2,4-F(Ph) |
CH3 |
13.122 |
1-CH3环丙基 |
H |
Ph |
CH3 |
13.123 |
1-CH3-环丙基 |
H |
2-Cl(Ph) |
CH3 |
13.124 |
1-CH3-环丙基 |
H |
3-Cl(Ph) |
CH3 |
13.125 |
1-CH3-环丙基 |
H |
4-Cl(Ph) |
CH3 |
13.126 |
1-CH3-环丙基 |
H |
4-Br(Ph) |
CH3 |
13.127 |
1-CH3-环丙基 |
H |
4-F(Ph) |
CH3 |
13.128 |
1-CH3-环丙基 |
H |
4-OCH3(Ph) |
CH3 |
13.129 |
1-CH3-环丙基 |
H |
4-CH3(Ph) |
CH3 |
13.130 |
1-CH3-环丙基 |
H |
4-NO2(Ph) |
CH3 |
13.131 |
1-CH3-环丙基 |
H |
2,4-Cl(Ph) |
CH3 |
13.132 |
1-CH3-环丙基 |
H |
2,4-F(Ph) |
CH3 |
13.133 |
CH3 |
CH3 |
Ph |
H |
13.134 |
CH3 |
CH3 |
Ph |
CH3 |
13.135 |
CH3 |
CH3 |
Ph |
C2H5 |
13.136 |
CH3 |
CH3 |
Ph |
正-C3H7 |
13.137 |
CH3 |
CH3 |
Ph |
异-C3H7 |
13.138 |
CH3 |
CH3 |
Ph |
正-C4H9 |
13.139 |
CH3 |
CH3 |
Ph |
异-C4H9 |
13.140 |
CH3 |
CH3 |
Ph |
C(CH3)3 |
13.141 |
CH3 |
CH3 |
Ph |
CH2C≡CH |
13.142 |
CH3 |
CH3 |
2-Cl(Ph) |
CH3 |
13.143 |
CH3 |
CH3 |
3-Cl(Ph) |
CH3 |
13.144 |
C2H5 |
CH3 |
Ph |
CH3 |
13.145 |
C2H5 |
CH3 |
2-Cl(Ph) |
CH3 |
13.146 |
C2H5 |
CH3 |
3-Cl(Ph) |
CH3 |
13.147 |
C2H5 |
CH3 |
4-Cl(Ph) |
CH3 |
13.148 |
C2H5 |
CH3 |
4-Br(Ph) |
CH3 |
13.149 |
C2H5 |
CH3 |
4-F(Ph) |
CH3 |
13.150 |
C2H5 |
CH3 |
4-OCH3(Ph) |
CH3 |
13.151 |
C2H5 |
CH3 |
4-CH3(Ph) |
CH3 |
13.152 |
C2H5 |
CH3 |
4-NO2(Ph) |
CH3 |
13.153 |
C2H5 |
CH3 |
2,4-Cl(Ph) |
CH3 |
13.154 |
C2H5 |
CH3 |
2,4-F(Ph) |
CH3 |
13.155 |
正-C3H7 |
CH3 |
Ph |
CH3 |
13.156 |
正-C3H7 |
CH3 |
2-Cl(Ph) |
CH3 |
13.157 |
正-C3H7 |
CH3 |
3-Cl(Ph) |
CH3 |
13.153 |
正-C3H7 |
CH3 |
4-Cl(Ph) |
CH3 |
13.159 |
正-C3H7 |
CH3 |
4-Br(Ph) |
CH3 |
13.160 |
正-C3H7 |
CH3 |
4-F(Ph) |
CH3 |
13.161 |
正-C3H7 |
CH3 |
4-OCH3(Ph) |
CH3 |
13.162 |
正-C3H7 |
CH3 |
4-CH3(Ph) |
CH3 |
13.163 |
正-C3H7 |
CH3 |
4-NO2(Ph) |
CH3 |
13.164 |
正-C3H7 |
CH3 |
2,4-Cl(Ph) |
CH3 |
13.165 |
正-C3H7 |
CH3 |
2,4-F(Ph) |
CH3 |
13.166 |
异-C3H7 |
CH3 |
Ph |
CH3 |
13.167 |
异-C3H7 |
CH3 |
2-Cl(Ph) |
CH3 |
13.168 |
异-C3H7 |
CH3 |
3-Cl(Ph) |
CH3 |
13.169 |
异-C3H7 |
CH3 |
4-Cl(Ph) |
CH3 |
13.170 |
异-C3H7 |
CH3 |
4-Br(Ph) |
CH3 |
13.17l |
异-C3H7 |
CH3 |
4-F(Ph) |
CH3 |
13.172 |
异-C3H7 |
CH3 |
4-OCH3(Ph) |
CH3 |
13.173 |
异-C3H7 |
CH3 |
4-CH3(Ph) |
CH3 |
13.174 |
异-C3H7 |
CH3 |
4-NO2(Ph) |
CH3 |
13.175 |
异-C3H7 |
CH3 |
2,4-Cl(Ph) |
CH3 |
13.176 |
异-C3H7 |
CH3 |
2,4-F(Ph) |
CH3 |
13.177 |
正-C4H9 |
CH3 |
Ph |
CH3 |
13.178 |
正-C4H9 |
CH3 |
2-Cl(Ph) |
CH3 |
13.179 |
正-C4H9 |
CH3 |
3-Cl(Ph) |
CH3 |
13.180 |
正-C4H9 |
CH3 |
4-Cl(Ph) |
CH3 |
13.181 |
正-C4H9 |
CH3 |
4-Br(Ph) |
CH3 |
13.182 |
正-C4H9 |
CH3 |
4-F(Ph) |
CH3 |
13.183 |
正-C4H9 |
CH3 |
4-OCH3(Ph) |
CH3 |
13.184 |
正-C4H9 |
CH3 |
4-CH3(Ph) |
CH3 |
13.185 |
正-C4H9 |
CH3 |
4-NO2(Ph) |
CH3 |
13.186 |
正-C4H9 |
CH3 |
2,4-Cl(Ph) |
CH3 |
13.187 |
正-C4H9 |
CH3 |
2,4-F(Ph) |
CH3 |
13.188 |
正-C4H9 |
CH3 |
4-CF3(Ph) |
CH3 |
13.189 |
Ph |
H |
Ph |
H |
13.190 |
Ph |
H |
Ph |
CH3 |
13.191 |
Ph |
H |
Ph |
C2H5 |
13.192 |
Ph |
H |
Ph |
正-C3H7 |
13.193 |
Ph |
H |
Ph |
异-C3H7 |
13.194 |
Ph |
H |
Ph |
正-C4H9 |
13.195 |
Ph |
H |
Ph |
异-C4H9 |
13.196 |
Ph |
H |
Ph |
C(CH3)3 |
13.197 |
Ph |
H |
Ph |
CH2C≡CH |
13.198 |
Ph |
H |
2-Cl(Ph) |
CH3 |
13.199 |
Ph |
H |
4-Cl(Ph) |
CH3 |
13.200 |
Ph |
CH3 |
Ph |
CH3 |
13.201 |
Ph |
CH3 |
2-Cl(Ph) |
CH3 |
13.202 |
Ph |
CH3 |
3-Cl(Ph) |
CH3 |
13.203 |
Ph |
CH3 |
4-Cl(Ph) |
CH3 |
13.204 |
Ph |
CH3 |
4-Br(Ph) |
CH3 |
13.205 |
Ph |
CH3 |
4-F(Ph) |
CH3 |
13.206 |
Ph |
CH3 |
4-OCH3(Ph) |
CH3 |
13.207 |
Ph |
CH3 |
4-CH3(Ph) |
CH3 |
13.208 |
Ph |
CH3 |
4-NO2(Ph) |
CH3 |
13.209 |
Ph |
CH3 |
2,4-Cl(Ph) |
CH3 |
13.210 |
Ph |
CH3 |
2,4-F(Ph) |
CH3 |
13.211 |
CN |
H |
Ph |
H |
13.212 |
CN |
H |
Ph |
CH3 |
13.213 |
CN |
H |
Ph |
C2H5 |
13.214 |
CN |
H |
Ph |
正-C3H7 |
13.215 |
CN |
H |
Ph |
异-C3H7 |
13.216 |
CN |
H |
Ph |
正-C4H9 |
13.217 |
CN |
H |
Ph |
异-C4H9 |
13.218 |
CN |
H |
Ph |
C(CH3)3 |
13.219 |
CN |
H |
Ph |
CH2C≡CH |
13.220 |
CN |
H |
2-Cl(Ph) |
CH3 |
13.221 |
CN |
H |
4-Cl(Ph) |
CH3 |
13.222 |
CN |
CH3 |
Ph |
H |
13.223 |
CN |
CH3 |
2-Cl(Ph) |
CH3 |
13.224 |
CN |
CH3 |
3-Cl(Ph) |
CH3 |
13.225 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
13.226 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
13.227 |
CN |
CH3 |
4-F(Ph) |
CH3 |
13.228 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
13.229 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
13.230 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
13.231 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
13.232 |
CN |
CH3 |
2,4-F(Ph) |
CH3 |
13.233 |
H |
H |
1-萘基 |
H |
13.234 |
CH3 |
H |
1-萘基 |
CH3 |
13.235 |
C2H5 |
H |
1-萘基 |
CH3 |
13.236 |
正-C3H7 |
H |
1-萘基 |
CH3 |
13.237 |
异-C3H7 |
H |
1-萘基 |
CH3 |
13.238 |
正-C4H9 |
H |
1-萘基 |
CH3 |
13.239 |
异-C4H9 |
H |
1-萘基 |
CH3 |
13.240 |
环丙基 |
H |
1-萘基 |
CH3 |
13.241 |
1-CH3-环丙基 |
H |
1-萘基 |
CH3 |
13.242 |
CN |
H |
1-萘基 |
CH3 |
13.243 |
Ph |
CH3 |
1-萘基 |
CH3 |
13.244 |
H |
CH3 |
1-萘基 |
CH3 |
13.245 |
CH3 |
CH3 |
1-萘基 |
CH3 |
13.246 |
C2H5 |
CH3 |
1-萘基 |
CH3 |
13.247 |
正-C3H7 |
CH3 |
1-萘基 |
CH3 |
13.249 |
异-C3H7 |
CH3 |
1-萘基 |
CH3 |
13.249 |
正-C4H9 |
CH3 |
1-萘基 |
CH3 |
13.250 |
异-C4H9 |
CH3 |
1-萘基 |
CH3 |
13.251 |
环丙基 |
CH3 |
1-萘基 |
CH3 |
13.252 |
1-CH3-环丙基 |
CH3 |
1-萘基 |
CH3 |
13.253 |
CN |
CH3 |
1-萘基 |
CH3 |
13.254 |
Ph |
CH3 |
1-萘基 |
CH3 |
13.255 |
H |
H |
2-萘基 |
H |
13.256 |
CH3 |
H |
2-萘基 |
CH3 |
13.257 |
C2H5 |
H |
2-萘基 |
C2H5 |
13.258 |
正-C3H7 |
H |
2-萘基 |
正-C3H7 |
13.259 |
异-C3H7 |
H |
2-萘基 |
异-C3H7 |
13.260 |
正-C4H9 |
H |
2-萘基 |
正-C4H9 |
13.261 |
异-C4H9 |
H |
2-萘基 |
异-C4H9 |
13.262 |
环丙基 |
H |
2-萘基 |
C(CH3)3 |
13.263 |
1-CH3-环丙基 |
H |
2-萘基 |
CH2C≡CH |
13.264 |
CN |
H |
2-萘基 |
CH2Ph |
13.265 |
Ph |
H |
2-萘基 |
CH2Ph |
13.266 |
H |
CH3 |
2-萘基 |
CH3 |
13.267 |
CH3 |
CH3 |
2-萘基 |
CH3 |
13.268 |
C2H5 |
CH3 |
2-萘基 |
CH3 |
13.269 |
正-C3H7 |
CH3 |
2-萘基 |
CH3 |
13.270 |
异-C3H7 |
CH3 |
2-萘基 |
CH3 |
13.271 |
正-C4H9 |
CH3 |
2-萘基 |
CH3 |
13.272 |
异-C4H9 |
CH3 |
2-萘基 |
CH3 |
13.273 |
环丙基 |
CH3 |
2-萘基 |
CH3 |
13.274 |
1-CH3-环丙基 |
CH3 |
2-萘基 |
CH3 |
13.275 |
CN |
CH3 |
2-萘基 |
CH3 |
13.276 |
Ph |
CH3 |
2-萘基 |
CH3 |
13.277 |
2-Cl(Ph) |
CH3 |
2-萘基 |
CH3 |
13.278 |
3-Cl(Ph) |
CH3 |
2-萘基 |
CH3 |
13.279 |
4-Cl(Ph) |
CH3 |
2-萘基 |
CH3 |
13.280 |
4-Br(Ph) |
CH3 |
2-萘基 |
CH3 |
13.281 |
4-F(Ph) |
CH3 |
2-萘基 |
CH3 |
13.282 |
4-OCH3(Ph) |
CH3 |
2-萘基 |
CH3 |
13.283 |
4-CH3(Ph) |
CH3 |
2-萘基 |
CH3 |
13.284 |
3-CF3(Ph) |
CH3 |
2-萘基 |
CH3 |
13.285 |
CH3 |
C2H5 |
Ph |
CH3 |
13.286 |
CH3 |
C2H5 |
2-Cl(Ph) |
CH3 |
13.287 |
CH3 |
C2H5 |
3-Cl(Ph) |
CH3 |
13.288 |
CH3 |
C2H5 |
4-Cl(Ph) |
CH3 |
13.289 |
CH3 |
C2H5 |
4-Br(Ph) |
CH3 |
13.290 |
CH3 |
C2H5 |
4-F(Ph) |
CH3 |
13.291 |
CH3 |
C2H5 |
4-OCH3(Ph) |
CH3 |
13.292 |
CH3 |
C2H5 |
4-CH3(Ph) |
CH3 |
13.293 |
CH3 |
C2H5 |
4-NO2(Ph) |
CH3 |
13.294 |
CH3 |
C2H5 |
2,4-Cl(Ph) |
CH3 |
13.295 |
CH3 |
C2H5 |
2,4-F(Ph) |
CH3 |
13.296 |
CH3 |
正-C3H7 |
Ph |
CH3 |
13.297 |
CH3 |
正-C3H7 |
2-Cl(Ph) |
CH3 |
13.298 |
CH3 |
正-C3H7 |
3-Cl(Ph) |
CH3 |
13.299 |
CH3 |
正-C3H7 |
4-Cl(Ph) |
CH3 |
13.300 |
CH3 |
正-C3H7 |
4-Br(Ph) |
CH3 |
13.301 |
CH3 |
正-C3H7 |
4-F(Ph) |
CH3 |
13.302 |
CH3 |
正-C3H7 |
4-OCH3(Ph) |
CH3 |
13.303 |
CH3 |
正-C3H7 |
4-CH3(Ph) |
CH3 |
13.304 |
CH3 |
正-C3H7 |
4-NO2(Ph) |
CH3 |
13.305 |
CH3 |
正-C3H7 |
2,4-Cl(Ph) |
CH3 |
13.306 |
CH3 |
正-C3H7 |
2,4-F(Ph) |
CH3 |
13.307 |
CH3 |
异-C3H7 |
Ph |
CH3 |
13.308 |
CH3 |
异-C3H7 |
2-Cl(Ph) |
CH3 |
13.309 |
CH3 |
异-C3H7 |
3-Cl(Ph) |
CH3 |
13.310 |
CH3 |
异-C3H7 |
4-Cl(Ph) |
CH3 |
13.311 |
CH3 |
异-C3H7 |
4-Br(Ph) |
CH3 |
13.312 |
CH3 |
异-C3H7 |
4-F(Ph) |
CH3 |
13.313 |
CH3 |
异-C3H7 |
4-OCH3(Ph) |
CH3 |
13.314 |
CH3 |
异-C3H7 |
4-CH3(Ph) |
CH3 |
13.315 |
CH3 |
异-C3H7 |
4-NO2(Ph) |
CH3 |
本发明式Ⅰ所涵盖的典型化合物包括式Ⅷ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NOR9的式Ⅰ化合物,而且其中的R2、R3、R7和R9如表14所定义。
表14
化合物 |
R2 |
R3 |
R7 |
R9 |
14.1 |
H |
H |
Ph |
H |
14.2 |
H |
H |
4-Cl(Ph) |
H |
14.3 |
H |
H |
4-Br(Ph) |
H |
14.4 |
H |
H |
4-F(Ph) |
H |
14.5 |
H |
H |
4-OCH3(Ph) |
H |
14.6 |
H |
H |
4-CF3(Ph) |
H |
14.7 |
H |
H |
Ph |
CH3 |
14.8 |
H |
H |
4-Cl(Ph) |
CH3 |
14.9 |
H |
H |
4-Br(Ph) |
CH3 |
14.10 |
H |
H |
4-F(Ph) |
CH3 |
14.11 |
CH3 |
H |
Ph |
H |
14.12 |
CH3 |
H |
2-Cl(Ph) |
H |
14.13 |
CH3 |
H |
3-Cl(Ph) |
H |
14.14 |
CH3 |
H |
4-Cl(Ph) |
H |
14.15 |
CH3 |
H |
2-Br(Ph) |
H |
14.16 |
CH3 |
H |
3-Br(Ph) |
H |
14.17 |
CH3 |
H |
4-Br(Ph) |
H |
14.18 |
CH3 |
H |
Ph |
CH3 |
14.19 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
14.20 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
14.21 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
14.22 |
CH3 |
H |
2-F(Ph) |
CH3 |
14.23 |
CH3 |
H |
3-F(Ph) |
CH3 |
14.24 |
CH3 |
H |
4-F(Ph) |
CH3 |
14.25 |
CH3 |
H |
2-CH3(Ph) |
CH3 |
14.26 |
CH3 |
H |
3-CH3(Ph) |
CH3 |
14.27 |
CH3 |
H |
2-CF3(Ph) |
CH3 |
14.28 |
CH3 |
H |
3-CF3(Ph) |
CH3 |
14.29 |
CH3 |
H |
4-CF3(Ph) |
CH3 |
14.30 |
CH3 |
H |
2-OCH3(Ph) |
CH3 |
14.31 |
CH3 |
H |
3-OCH3(Ph) |
CH3 |
14.32 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
14.33 |
CH3 |
H |
2,3-Cl(Ph) |
CH3 |
14.34 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
14.35 |
CH3 |
H |
2,5-Cl(Ph) |
CH3 |
14.36 |
CH3 |
H |
2,6-Cl(Ph) |
CH3 |
14.37 |
CH3 |
H |
3,4-Cl(Ph) |
CH3 |
14.38 |
CH3 |
H |
3,5-Cl(Ph) |
CH3 |
14.39 |
CH3 |
H |
Ph |
C2H5 |
14.40 |
CH3 |
H |
Ph |
正-C3H7 |
14.41 |
CH3 |
H |
Ph |
异-C3H7 |
14.42 |
CH3 |
H |
Ph |
正-C4H9 |
14.43 |
CH3 |
H |
Ph |
C(CH3)3 |
14.44 |
CH3 |
H |
Ph |
CH2C≡CH |
14.45 |
C2H5 |
H |
Ph |
CH3 |
14.46 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
14.47 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
14.48 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
14.49 |
C2H5 |
H |
4-Br(Ph) |
CH3 |
14.50 |
C2H5 |
H |
4-F(Ph) |
CH3 |
14.51 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
14.52 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
14.53 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
14.54 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
14.55 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
14.56 |
正-C3H7 |
H |
Ph |
CH3 |
14.57 |
正-C3H7 |
H |
2-Cl(Ph) |
CH3 |
14.58 |
正-C3H7 |
H |
3-Cl(Ph) |
CH3 |
14.59 |
正-C3H7 |
H |
4-Cl(Ph) |
CH3 |
14.60 |
正-C3H7 |
H |
4-F(Ph) |
CH3 |
14.61 |
正-C3H7 |
H |
3-OCH3(Ph) |
CH3 |
14.62 |
正-C3H7 |
H |
4-OCH3(Ph) |
CH3 |
14.63 |
正-C3H7 |
H |
4-CH3(Ph) |
CH3 |
14.64 |
正-C3H7 |
H |
4-NO2(Ph) |
CH3 |
14.65 |
正-C3H7 |
H |
2,4-Cl(Ph) |
CH3 |
14.66 |
正-C3H7 |
H |
2,4-F(Ph) |
CH3 |
14.67 |
异-C3H7 |
H |
Ph |
CH3 |
14.68 |
异-C3H7 |
H |
2-Cl(ph) |
CH3 |
14.69 |
异-C3H7 |
H |
3-Cl(Ph) |
CH3 |
14.70 |
异-C3H7 |
H |
4-Cl(Ph) |
CH3 |
14.71 |
异-C3H7 |
H |
4-Br(Ph) |
CH3 |
14.72 |
异-C3H7 |
H |
4-F(Ph) |
CH3 |
14.73 |
异-C3H7 |
H |
4-OCH3(Ph) |
CH3 |
14.74 |
异-C3H7 |
H |
4-CH3(Ph) |
CH3 |
14.75 |
异-C3H7 |
H |
4-NO2(Ph) |
CH3 |
14.76 |
异-C3H7 |
H |
2,4-Cl(Ph) |
CH3 |
14.77 |
异-C3H7 |
H |
2,4-F(Ph) |
CH3 |
14.78 |
正-C4H9 |
H |
Ph |
CH3 |
14.79 |
正-C4H9 |
H |
2-Cl(Ph) |
CH3 |
14.80 |
正-C4H9 |
H |
3-Cl(Ph) |
CH3 |
14.81 |
正-C4H9 |
H |
4-Cl(Ph) |
CH3 |
14.82 |
正-C4H9 |
H |
4-Br(Ph) |
CH3 |
14.83 |
正-C4H9 |
H |
4-F(Ph) |
CH3 |
14.84 |
正-C4H9 |
H |
4-OCH3(Ph) |
CH3 |
14.85 |
正-C4H9 |
H |
4-CH3(Ph) |
CH3 |
14.86 |
正-C4H9 |
H |
4-NO2(Ph) |
CH3 |
14.87 |
正-C4H9 |
H |
2,4-Cl(Ph) |
CH3 |
14.88 |
正-C4H9 |
H |
2,4-F(Ph) |
CH3 |
14.89 |
异-C4H9 |
H |
Ph |
CH3 |
14.90 |
异-C4H9 |
H |
2-Cl(Ph) |
CH3 |
14.91 |
异-C4H9 |
H |
3-Cl(Ph) |
CH3 |
14.92 |
异-C4H9 |
H |
4-Cl(Ph) |
CH3 |
14.93 |
异-C4H9 |
H |
4-F(Ph) |
CH3 |
14.94 |
异-C4H9 |
H |
3-OCH3(Ph) |
CH3 |
14.95 |
异-C4H9 |
H |
4-OCH3(Ph) |
CH3 |
14.96 |
异-C4H9 |
H |
4-CH3(Ph) |
CH3 |
14.97 |
异-C4H9 |
H |
4-NO2(Ph) |
CH3 |
14.98 |
异-C4H9 |
H |
2,4-Cl(Ph) |
CH3 |
14.99 |
异-C4H9 |
H |
2,4-F(Ph) |
CH3 |
14.100 |
C(CH3)3 |
H |
Ph |
CH3 |
14.101 |
C(CH3)3 |
H |
2-Cl(Ph) |
CH3 |
14.102 |
C(CH3)3 |
H |
3-Cl(Ph) |
CH3 |
14.103 |
C(CH3)3 |
H |
4-Cl(Ph) |
CH3 |
14.104 |
C(CH3)3 |
H |
4-F(Ph) |
CH3 |
14.105 |
C(CH3)3 |
H |
3-OCH3(Ph) |
CH3 |
14.106 |
C(CH3)3 |
H |
4-OCH3(Ph) |
CH3 |
14.107 |
C(CH3)3 |
H |
4-CH3(Ph) |
CH3 |
14.108 |
C(CH3)3 |
H |
4-NO2(Ph) |
CH3 |
14.109 |
C(CH3)3 |
H |
2,4-Cl(Ph) |
CH3 |
14.110 |
C(CH3)3 |
H |
2,4-F(Ph) |
CH3 |
14.111 |
环丙基 |
H |
Ph |
CH3 |
14.112 |
环丙基 |
H |
2-Cl(Ph) |
CH3 |
14.113 |
环丙基 |
H |
3-Cl(Ph) |
CH3 |
14.114 |
环丙基 |
H |
4-Cl(Ph) |
CH3 |
14.115 |
环丙基 |
H |
4-Br(Ph) |
CH3 |
14.116 |
环丙基 |
H |
3-OCH3(Ph) |
CH3 |
14.117 |
环丙基 |
H |
4-OCH3(Ph) |
CH3 |
14.118 |
环丙基 |
H |
4-CH3(Ph) |
CH3 |
14.119 |
环丙基 |
H |
4-NO2(Ph) |
CH3 |
14.120 |
环丙基 |
H |
2,4-Cl(Ph) |
CH3 |
14.121 |
环丙基 |
H |
2,4-F(Ph) |
CH3 |
14.122 |
1-CH3-环丙基 |
H |
Ph |
CH3 |
14.123 |
1-CH3-环丙基 |
H |
2-Cl(Ph) |
CH3 |
14.124 |
1-CH3-环丙基 |
H |
3-Cl(Ph) |
CH3 |
14.125 |
1-CH3-环丙基 |
H |
4-Cl(Ph) |
CH3 |
14.126 |
1-CH3-环丙基 |
H |
4-Br(Ph) |
CH3 |
14.127 |
1-CH3-环丙基 |
H |
4-F(Ph) |
CH3 |
14.128 |
1-CH3-环丙基 |
H |
4-OCH3(Ph) |
CH3 |
14.129 |
1-CH3-环丙基 |
H |
4-CH3(Ph) |
CH3 |
14.130 |
1-CH3-环丙基 |
H |
4-NO2(Ph) |
CH3 |
14.131 |
1-CH3-环丙基 |
H |
2,4-Cl(Ph) |
CH3 |
14.132 |
1-CH3-环丙基 |
H |
2,4-F(Ph) |
CH3 |
14.133 |
CH3 |
CH3 |
Ph |
H |
14.134 |
CH3 |
CH3 |
Ph |
CH3 |
14.135 |
CH3 |
CH3 |
Ph |
C2H5 |
14.136 |
CH3 |
CH3 |
Ph |
正-C3H7 |
14.137 |
CH3 |
CH3 |
Ph |
异-C3H7 |
14.138 |
CH3 |
CH3 |
Ph |
正-C4H9 |
14.139 |
CH3 |
CH3 |
Ph |
异-C4H9 |
14.140 |
CH3 |
CH3 |
Ph |
C(CH3)3 |
14.141 |
CH3 |
CH3 |
Ph |
CH2C≡CH |
14.142 |
CH3 |
CH3 |
2-Cl(Ph) |
CH3 |
14.143 |
CH3 |
CH3 |
3-Cl(Ph) |
CH3 |
14.144 |
C2H5 |
CH3 |
Ph |
CH3 |
14.145 |
C2H5 |
CH3 |
2-Cl(Ph) |
CH3 |
14.146 |
C2H5 |
CH3 |
3-Cl(Ph) |
CH3 |
14.147 |
C2H5 |
CH3 |
4-Cl(Ph) |
CH3 |
14.148 |
C2H5 |
CH3 |
4-Br(Ph) |
CH3 |
14.149 |
C2H5 |
CH3 |
4-F(Ph) |
CH3 |
14.150 |
C2H5 |
CH3 |
4-OCH3(Ph) |
CH3 |
14.151 |
C2H5 |
CH3 |
4-CH3(Ph) |
CH3 |
14.152 |
C2H5 |
CH3 |
4-NO2(Ph) |
CH3 |
14.153 |
C2H5 |
CH3 |
2,4-Cl(Ph) |
CH3 |
14.154 |
C2H5 |
CH3 |
2,4-F(Ph) |
CH3 |
14.155 |
n-C3H7 |
CH3 |
Ph |
CH3 |
14.156 |
n-C3H7 |
CH3 |
2-Cl(Ph) |
CH3 |
14.157 |
n-C3H7 |
CH3 |
3-Cl(Ph) |
CH3 |
14.158 |
n-C3H7 |
CH3 |
4-Cl(Ph) |
CH3 |
14.159 |
正-C3H7 |
CH3 |
4-Br(Ph) |
CH3 |
14.160 |
正-C3H7 |
CH3 |
4-F(Ph) |
CH3 |
14.161 |
正-C3H7 |
CH3 |
4-OCH3(Ph) |
CH3 |
14.162 |
正-C3H7 |
CH3 |
4-CH3(Ph) |
CH3 |
14.163 |
正-C3H7 |
CH3 |
4-NO2(Ph) |
CH3 |
14.164 |
正-C3H7 |
CH3 |
2,4-Cl(Ph) |
CH3 |
14.165 |
正-C3H7 |
CH3 |
2,4-F(Ph) |
CH3 |
14.166 |
异-C3H7 |
CH3 |
Ph |
CH3 |
14.167 |
异-C3H7 |
CH3 |
2-Cl(Ph) |
CH3 |
14.168 |
异-C3H7 |
CH3 |
3-Cl(Ph) |
CH3 |
14.169 |
异-C3H7 |
CH3 |
4-Cl(Ph) |
CH3 |
14.170 |
异-C3H7 |
CH3 |
4-Br(Ph) |
CH3 |
14.171 |
异-C3H7 |
CH3 |
4-F(Ph) |
CH3 |
14.172 |
异-C3H7 |
CH3 |
4-OCH3(Ph) |
CH3 |
14.173 |
异-C3H7 |
CH3 |
4-CH3(Ph) |
CH3 |
14.174 |
异-C3H7 |
CH3 |
4-NO2(Ph) |
CH3 |
14.175 |
异-C3H7 |
CH3 |
2,4-Cl(Ph) |
CH3 |
14.176 |
异-C3H7 |
CH3 |
2,4-F(Ph) |
CH3 |
14.177 |
正-C4H9 |
CH3 |
Ph |
CH3 |
14.178 |
正-C4H9 |
CH3 |
2-Cl(Ph) |
CH3 |
14.179 |
正-C4H9 |
CH3 |
3-Cl(Ph) |
CH3 |
14.180 |
正-C4H9 |
CH3 |
4-Cl(Ph) |
CH3 |
14.181 |
正-C4H9 |
CH3 |
4-Br(Ph) |
CH3 |
14.182 |
正-C4H9 |
CH3 |
4-F(Ph) |
CH3 |
14.183 |
正-C4H9 |
CH3 |
4-OCH3(Ph) |
CH3 |
14.184 |
正-C4H9 |
CH3 |
4-CH3(Ph) |
CH3 |
14.185 |
正-C4H9 |
CH3 |
4-NO2(Ph) |
CH3 |
14.186 |
正-C4H9 |
CH3 |
2,4-Cl(Ph) |
CH3 |
14.187 |
正-C4H9 |
CH3 |
2,4-F(Ph) |
CH3 |
14.188 |
正-C4H9 |
CH3 |
4-CF3(Ph) |
CH3 |
14.189 |
Ph |
H |
Ph |
H |
14.190 |
Ph |
H |
Ph |
CH3 |
14.191 |
Ph |
H |
Ph |
C2H5 |
14.192 |
Ph |
H |
Ph |
正-C3H7 |
14.193 |
Ph |
H |
Ph |
异-C3H7 |
14.194 |
Ph |
H |
Ph |
正-C4H9 |
14.195 |
Ph |
H |
Ph |
异-C4H9 |
14.196 |
Ph |
H |
Ph |
C(CH3)3 |
14.197 |
Ph |
H |
Ph |
CH2C≡CH |
14.198 |
Ph |
H |
2-Cl(Ph) |
CH3 |
14.199 |
Ph |
H |
4-Cl(Ph) |
CH3 |
14.200 |
Ph |
CH3 |
Ph |
CH3 |
14.201 |
Ph |
CH3 |
2-Cl(Ph) |
CH3 |
14.202 |
Ph |
CH3 |
3-Cl(Ph) |
CH3 |
14.203 |
Ph |
CH3 |
4-Cl(Ph) |
CH3 |
14.204 |
Ph |
CH3 |
4-Br(Ph) |
CH3 |
14.205 |
Ph |
CH3 |
4-F(Ph) |
CH3 |
14.206 |
Ph |
CH3 |
4-OCH3(Ph) |
CH3 |
14.207 |
Ph |
CH3 |
4-CH3(Ph) |
CH3 |
14.208 |
Ph |
CH3 |
4-NO2(Ph) |
CH3 |
14.209 |
Ph |
CH3 |
2,4-Cl(Ph) |
CH3 |
14.210 |
Ph |
CH3 |
2,4-F(Ph) |
CH3 |
14.211 |
CN |
H |
Ph |
H |
14.212 |
CN |
H |
Ph |
CH3 |
14.213 |
CN |
H |
Ph |
C2H5 |
14.214 |
CN |
H |
Ph |
正-C3H7 |
14.215 |
CN |
H |
Ph |
异-C3H7 |
14.216 |
CN |
H |
Ph |
正-C4H9 |
14.217 |
CN |
H |
Ph |
异-C4H9 |
14.218 |
CN |
H |
Ph |
C(CH3)3 |
14.219 |
CN |
H |
Ph |
CH2C≡CH |
14.220 |
CN |
H |
2-Cl(Ph) |
CH3 |
14.221 |
CN |
H |
4-Cl(Ph) |
CH3 |
14.222 |
CN |
CH3 |
Ph |
H |
14.223 |
CN |
CH3 |
2-Cl(Ph) |
CH3 |
14.224 |
CN |
CH3 |
3-Cl(Ph) |
CH3 |
14.225 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
14.226 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
14.227 |
CN |
CH3 |
4-F(Ph) |
CH3 |
14.228 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
14.229 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
14.230 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
14.231 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
14.232 |
CN |
CH3 |
2,4-F(Ph) |
CH3 |
14.233 |
H |
H |
1-萘基 |
H |
14.234 |
CH3 |
H |
1-萘基 |
CH3 |
14.235 |
C2H5 |
H |
1-萘基 |
CH3 |
14.236 |
正-C3H7 |
H |
1-萘基 |
CH3 |
14.237 |
异-C3H7 |
H |
1-萘基 |
CH3 |
14.238 |
正-C4H9 |
H |
1-萘基 |
CH3 |
14.239 |
异-C4H9 |
H |
1-萘基 |
CH3 |
14.240 |
环丙基 |
H |
1-萘基 |
CH3 |
14.241 |
1-CH3-环丙基 |
H |
1-萘基 |
CH3 |
14.242 |
CN |
H |
1-萘基 |
CH3 |
14.243 |
Ph |
CH3 |
1-萘基 |
CH3 |
14.244 |
H |
CH3 |
1-萘基 |
CH3 |
14.245 |
CH3 |
CH3 |
1-萘基 |
CH3 |
14.246 |
C2H5 |
CH3 |
1-萘基 |
CH3 |
14.247 |
正-C3H7 |
CH3 |
1-萘基 |
CH3 |
14.248 |
异-C3H7 |
CH3 |
1-萘基 |
CH3 |
14.249 |
正-C4H9 |
CH3 |
1-萘基 |
CH3 |
14.250 |
异-C4H9 |
CH3 |
1-萘基 |
CH3 |
14.251 |
环丙基 |
CH3 |
1-萘基 |
CH3 |
14.252 |
1-CH3-环丙基 |
CH3 |
1-萘基 |
CH3 |
14.253 |
CN |
CH3 |
1-萘基 |
CH3 |
14.254 |
Ph |
CH3 |
1-萘基 |
CH3 |
14.255 |
H |
H |
2-萘基 |
H |
14.256 |
CH3 |
H |
2-萘基 |
CH3 |
14.257 |
C2H5 |
H |
2-萘基 |
C2H5 |
14.258 |
正-C3H7 |
H |
2-萘基 |
正-C3H7 |
14.259 |
异-C3H7 |
H |
2-萘基 |
异-C3H7 |
14.260 |
正-C4H9 |
H |
2-萘基 |
正-C4H9 |
14.261 |
异-C4H9 |
H |
2-萘基 |
异-C4H9 |
14.262 |
环丙基 |
H |
2-萘基 |
C(CH3)3 |
14.263 |
1-CH3-环丙基 |
H |
2-萘基 |
CH2C≡CH |
14.264 |
CN |
H |
2-萘基 |
CH2Ph |
14.265 |
Ph |
H |
2-萘基 |
CH2Ph |
14.266 |
H |
CH3 |
2-萘基 |
CH3 |
14.267 |
CH3 |
CH3 |
2-萘基 |
CH3 |
14.268 |
C2H5 |
CH3 |
2-萘基 |
CH3 |
14.269 |
正-C3H7 |
CH3 |
2-萘基 |
CH3 |
14.270 |
异-C3H7 |
CH3 |
2-萘基 |
CH3 |
14.271 |
正-C4H9 |
CH3 |
2-萘基 |
CH3 |
14.272 |
异-C4H9 |
CH3 |
2-萘基 |
CH3 |
14.273 |
环丙基-C3H5 |
CH3 |
2-萘基 |
CH3 |
14.274 |
1-CH3-环丙基 |
CH3 |
2-萘基 |
CH3 |
14.275 |
CN |
CH3 |
2-萘基 |
CH3 |
14.276 |
Ph |
CH3 |
2-萘基 |
CH3 |
14.277 |
2-Cl(Ph) |
CH3 |
2-萘基 |
CH3 |
14.278 |
3-Cl(Ph) |
CH3 |
2-萘基 |
CH3 |
14.279 |
4-Cl(Ph) |
CH3 |
2-萘基 |
CH3 |
14.280 |
4-Br(Ph) |
CH3 |
2-萘基 |
CH3 |
14.281 |
4-F(Ph) |
CH3 |
2-萘基 |
CH3 |
14.282 |
4-OCH3(Ph) |
CH3 |
2-萘基 |
CH3 |
14.283 |
4-CH3(Ph) |
CH3 |
2-萘基 |
CH3 |
14.284 |
3-CF3(Ph) |
CH3 |
2-萘基 |
CH3 |
14.285 |
CH3 |
C2H5 |
Ph |
CH3 |
14.286 |
CH3 |
C2H5 |
2-Cl(Ph) |
CH3 |
14.287 |
CH3 |
C2H5 |
3-Cl(Ph) |
CH3 |
14.288 |
CH3 |
C2H5 |
4-Cl(Ph) |
CH3 |
14.289 |
CH3 |
C2H5 |
4-Br(Ph) |
CH3 |
14.290 |
CH3 |
C2H5 |
4-F(Ph) |
CH3 |
14.291 |
CH3 |
C2H5 |
4-OCH3(Ph) |
CH3 |
14.292 |
CH3 |
C2H5 |
4-CH3(Ph) |
CH3 |
14.293 |
CH3 |
C2H5 |
4-NO2(Ph) |
CH3 |
14.294 |
CH3 |
C2H5 |
2,4-Cl(Ph) |
CH3 |
14.295 |
CH3 |
C2H5 |
2,4-F(Ph) |
CH3 |
14.296 |
CH3 |
正-C3H7 |
Ph |
CH3 |
14.297 |
CH3 |
正-C3H7 |
2-Cl(Ph) |
CH3 |
14.298 |
CH3 |
正-C3H7 |
3-Cl(Ph) |
CH3 |
14.299 |
CH3 |
正-C3H7 |
4-Cl(Ph) |
CH3 |
14.300 |
CH3 |
正-C3H7 |
4-Br(Ph) |
CH3 |
14.301 |
CH3 |
正-C3H7 |
4-F(Ph) |
CH3 |
14.302 |
CH3 |
正-C3H7 |
4-OCH3(Ph) |
CH3 |
14.303 |
CH3 |
正-C3H7 |
4-CH3(Ph) |
CH3 |
14.304 |
CH3 |
正-C3H7 |
4-NO2(Ph) |
CH3 |
14.305 |
CH3 |
正-C3H7 |
2,4-Cl(Ph) |
CH3 |
14.306 |
CH3 |
正-C3H7 |
2,4-F(Ph) |
CH3 |
14.307 |
CH3 |
异-C3H7 |
Ph |
CH3 |
14.308 |
CH3 |
异-C3H7 |
2-Cl(Ph) |
CH3 |
14.309 |
CH3 |
异-C3H7 |
3-Cl(Ph) |
CH3 |
14.310 |
CH3 |
异-C3H7 |
4-Cl(Ph) |
CH3 |
14.311 |
CH3 |
异-C3H7 |
4-Br(Ph) |
CH3 |
14.312 |
CH3 |
异-C3H7 |
4-F(Ph) |
CH3 |
14.313 |
CH3 |
异-C3H7 |
4-OCH3(Ph) |
CH3 |
14.314 |
CH3 |
异-C3H7 |
4-CH3(Ph) |
CH3 |
14.315 |
CH3 |
异-C3H7 |
4-NO2(Ph) |
CH3 |
本发明式Ⅰ所涵盖的典型化合物包括式Ⅸ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NOR9的式Ⅰ化合物,而且其中的R2、R3、R7和R9如表15所定义。
表15
化合物 |
R2 |
R3 |
R7 |
R9 |
15.1 |
H |
H |
Ph |
H |
15.2 |
H |
H |
4-Cl(Ph) |
H |
15.3 |
H |
H |
4-Br(Ph) |
H |
15.4 |
H |
H |
4-F(Ph) |
H |
15.5 |
H |
H |
4-OCH3(Ph) |
H |
15.6 |
H |
H |
4-CF3(Ph) |
H |
15.7 |
H |
H |
Ph |
CH3 |
15.8 |
H |
H |
4-Cl(Ph) |
CH3 |
15.9 |
H |
H |
4-Br(Ph) |
CH3 |
15.10 |
H |
H |
4-F(Ph) |
CH3 |
15.11 |
CH3 |
H |
Ph |
H |
15.12 |
CH3 |
H |
2-Cl(Ph) |
H |
15.13 |
CH3 |
H |
3-Cl(Ph) |
H |
15.14 |
CH3 |
H |
4-Cl(Ph) |
H |
15.15 |
CH3 |
H |
2-Br(Ph) |
H |
15.16 |
CH3 |
H |
3-Br(Ph) |
H |
15.17 |
CH3 |
H |
4-Br(Ph) |
H |
15.18 |
CH3 |
H |
Ph |
CH3 |
15.19 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
15.20 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
15.21 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
15.22 |
CH3 |
H |
2-F(Ph) |
CH3 |
15.23 |
CH3 |
H |
3-F(Ph) |
CH3 |
15.24 |
CH3 |
H |
4-F(Ph) |
CH3 |
15.25 |
CH3 |
H |
2-CH3(Ph) |
CH3 |
15.26 |
CH3 |
H |
3-CH3(Ph) |
CH3 |
15.27 |
CH3 |
H |
2-CF3(Ph) |
CH3 |
15.28 |
CH3 |
H |
3-CF3(Ph) |
CH3 |
15.29 |
CH3 |
H |
4-CF3(Ph) |
CH3 |
15.30 |
CH3 |
H |
2-OCH3(Ph) |
CH3 |
15.31 |
CH3 |
H |
3-OCH3(Ph) |
CH3 |
15.32 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
15.33 |
CH3 |
H |
2,3-Cl(Ph) |
CH3 |
15.34 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
15.35 |
CH3 |
H |
2,5-Cl(Ph) |
CH3 |
15.36 |
CH3 |
H |
2,6-Cl(Ph) |
CH3 |
15.37 |
CH3 |
H |
3,4-Cl(Ph) |
CH3 |
15.38 |
CH3 |
H |
3,5-Cl(Ph) |
CH3 |
15.39 |
CH3 |
H |
Ph |
C2H5 |
15.40 |
CH3 |
H |
Ph |
正-C3H7 |
15.41 |
CH3 |
H |
Ph |
异-C3H7 |
15.42 |
CH3 |
H |
Ph |
正-C4H9 |
15.43 |
CH3 |
H |
Ph |
C(CH3)3 |
15.44 |
CH3 |
H |
Ph |
CH2C≡CH |
15.45 |
C2H5 |
H |
Ph |
CH3 |
15.46 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
15.47 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
15.48 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
15.49 |
C2H5 |
H |
4-Br(Ph) |
CH3 |
15.50 |
C2H5 |
H |
4-F(Ph) |
CH3 |
15.51 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
15.52 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
15.53 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
15.54 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
15.55 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
15.56 |
正-C3H7 |
H |
Ph |
CH3 |
15.57 |
正-C3H7 |
H |
2-Cl(Ph) |
CH3 |
15.58 |
正-C3H7 |
H |
3-Cl(Ph) |
CH3 |
15.59 |
正-C3H7 |
H |
4-Cl(Ph) |
CH3 |
15.60 |
正-C3H7 |
H |
4-F(Ph) |
CH3 |
15.61 |
正-C3H7 |
H |
3-OCH3(Ph) |
CH3 |
15.62 |
正-C3H7 |
H |
4-OCH3(Ph) |
CH3 |
15.63 |
正-C3H7 |
H |
4-CH3(Ph) |
CH3 |
15.64 |
正-C3H7 |
H |
4-NO2(Ph) |
CH3 |
15.65 |
正-C3H7 |
H |
2,4-Cl(Ph) |
CH3 |
15.66 |
正-C3H7 |
H |
2,4-F(Ph) |
CH3 |
15.67 |
异-C3H7 |
H |
Ph |
CH3 |
15.68 |
异-C3H7 |
H |
2-Cl(Ph) |
CH3 |
15.69 |
异-C3H7 |
H |
3-Cl(Ph) |
CH3 |
15.70 |
异-C3H7 |
H |
4-Cl(Ph) |
CH3 |
15.71 |
异-C3H7 |
H |
4-Br(Ph) |
CH3 |
15.72 |
异-C3H7 |
H |
4-F(Ph) |
CH3 |
15.73 |
异-C3H7 |
H |
4-OCH3(Ph) |
CH3 |
15.74 |
异-C3H7 |
H |
4-CH3(Ph) |
CH3 |
15.75 |
异-C3H7 |
H |
4-NO2(Ph) |
CH3 |
15.76 |
异-C3H7 |
H |
2,4-Cl(Ph) |
CH3 |
15.77 |
异-C3H7 |
H |
2,4-F(Ph) |
CH3 |
15.78 |
正-C4H9 |
H |
Ph |
CH3 |
15.79 |
正-C4H9 |
H |
2-Cl(Ph) |
CH3 |
15.80 |
正-C4H9 |
H |
3-Cl(Ph) |
CH3 |
15.81 |
正-C4H9 |
H |
4-Cl(Ph) |
CH3 |
15.82 |
正-C4H9 |
H |
4-Br(Ph) |
CH3 |
15.83 |
正-C4H9 |
H |
4-F(Ph) |
CH3 |
15.84 |
正-C4H9 |
H |
4-OCH3(Ph) |
CH3 |
15.85 |
正-C4H9 |
H |
4-CH3(Ph) |
CH3 |
15.86 |
正-C4H9 |
H |
4-NO2(Ph) |
CH3 |
15.87 |
正-C4H9 |
H |
2,4-Cl(Ph) |
CH3 |
15.88 |
正-C4H9 |
H |
2,4-F(Ph) |
CH3 |
15.89 |
异-C4H9 |
H |
Ph |
CH3 |
15.90 |
异-C4H9 |
H |
2-Cl(Ph) |
CH3 |
15.91 |
异-C4H9 |
H |
3-Cl(Ph) |
CH3 |
15.92 |
异-C4H9 |
H |
4-Cl(Ph) |
CH3 |
15.93 |
异-C4H9 |
H |
4-F(Ph) |
CH3 |
15.94 |
异-C4H9 |
H |
3-OCH3(Ph) |
CH3 |
15.95 |
异-C4H9 |
H |
4-OCH3(Ph) |
CH3 |
15.96 |
异-C4H9 |
H |
4-CH3(Ph) |
CH3 |
15.97 |
异-C4H9 |
H |
4-NO2(Ph) |
CH3 |
15.98 |
异-C4H9 |
H |
2,4-Cl(Ph) |
CH3 |
15.99 |
异-C4H9 |
H |
2,4-F(Ph) |
CH3 |
15.100 |
C(CH3)3 |
H |
Ph |
CH3 |
15.101 |
C(CH3)3 |
H |
2-Cl(Ph) |
CH3 |
15.102 |
C(CH3)3 |
H |
3-Cl(Ph) |
CH3 |
15.103 |
C(CH3)3 |
H |
4-Cl(Ph) |
CH3 |
15.104 |
C(CH3)3 |
H |
4-F(Ph) |
CH3 |
15.105 |
C(CH3)3 |
H |
3-OCH3(Ph) |
CH3 |
15.106 |
C(CH3)3 |
H |
4-OCH3(Ph) |
CH3 |
15.107 |
C(CH3)3 |
H |
4-CH3(Ph) |
CH3 |
15.108 |
C(CH3)3 |
H |
4-NO2(Ph) |
CH3 |
15.109 |
C(CH3)3 |
H |
2,4-Cl(Ph) |
CH3 |
15.110 |
C(CH3)3 |
H |
2,4-F(Ph) |
CH3 |
15.111 |
环丙基 |
H |
Ph |
CH3 |
15.112 |
环丙基 |
H |
2-Cl(Ph) |
CH3 |
15.113 |
环丙基 |
H |
3-Cl(Ph) |
CH3 |
15.114 |
环丙基 |
H |
4-Cl(Ph) |
CH3 |
15.115 |
环丙基 |
H |
4-Br(Ph) |
CH3 |
15.116 |
环丙基 |
H |
3-OCH3(Ph) |
CH3 |
15.117 |
环丙基 |
H |
4-OCH3(Ph) |
CH3 |
15.113 |
环丙基 |
H |
4-CH3(Ph) |
CH3 |
15.119 |
环丙基 |
H |
4-NO2(Ph) |
CH3 |
15.120 |
环丙基 |
H |
2,4-Cl(Ph) |
CH3 |
15.121 |
环丙基 |
H |
2,4-F(Ph) |
CH3 |
15.122 |
1-CH3-环丙基 |
H |
Ph |
CH3 |
15.123 |
1-CH3-环丙基 |
H |
2-Cl(Ph) |
CH3 |
15.124 |
1-CH3-环丙基 |
H |
3-Cl(Ph) |
CH3 |
15.125 |
1-CH3-环丙基 |
H |
4-Cl(Ph) |
CH3 |
15.126 |
1-CH3-环丙基 |
H |
4-Br(Ph) |
CH3 |
15.127 |
1-CH3-环丙基 |
H |
4-F(Ph) |
CH3 |
15.128 |
1-CH3-环丙基 |
H |
4-OCH3(Ph) |
CH3 |
15.129 |
1-CH3-环丙基 |
H |
4-CH3(Ph) |
CH3 |
15.130 |
1-CH3-环丙基 |
H |
4-NO2(Ph) |
CH3 |
15.131 |
1-CH3-环丙基 |
H |
2,4-Cl(Ph) |
CH3 |
15.132 |
1-CH3-环丙基 |
H |
2,4-F(Ph) |
CH3 |
15.133 |
CH3 |
CH3 |
Ph |
H |
15.134 |
CH3 |
CH3 |
Ph |
CH3 |
15.135 |
CH3 |
CH3 |
Ph |
C2H5 |
15.136 |
CH3 |
CH3 |
Ph |
正-C3H7 |
15.137 |
CH3 |
CH3 |
Ph |
异-C3H7 |
15.138 |
CH3 |
CH3 |
Ph |
正-C4H9 |
15.139 |
CH3 |
CH3 |
Ph |
异-C4H9 |
15.140 |
CH3 |
CH3 |
Ph |
C(CH3)3 |
15.141 |
CH3 |
CH3 |
Ph |
CH2C≡CH |
15.142 |
CH3 |
CH3 |
2-Cl(Ph) |
CH3 |
15.143 |
CH3 |
CH3 |
3-Cl(Ph) |
CH3 |
15.144 |
C2H5 |
CH3 |
Ph |
CH3 |
15.145 |
C2H5 |
CH3 |
2-Cl(Ph) |
CH3 |
15.146 |
C2H5 |
CH3 |
3-Cl(Ph) |
CH3 |
15.147 |
C2H5 |
CH3 |
4-Cl(Ph) |
CH3 |
15.148 |
C2H5 |
CH3 |
4-Br(Ph) |
CH3 |
15.149 |
C2H5 |
CH3 |
4-F(Ph) |
CH3 |
15.150 |
C2H5 |
CH3 |
4-OCH3(Ph) |
CH3 |
15.151 |
C2H5 |
CH3 |
4-CH3(Ph) |
CH3 |
15.152 |
C2H5 |
CH3 |
4-NO2(Ph) |
CH3 |
15.153 |
C2H5 |
CH3 |
2,4-Cl(Ph) |
CH3 |
15.154 |
C2H5 |
CH3 |
2,4-F(Ph) |
CH3 |
15.155 |
正-C3H7 |
CH3 |
Ph |
CH3 |
15.156 |
正-C3H7 |
CH3 |
2-Cl(Ph) |
CH3 |
15.157 |
正-C3H7 |
CH3 |
3-Cl(Ph) |
CH3 |
15.158 |
正-C3H7 |
CH3 |
4-Cl(Ph) |
CH3 |
15.159 |
正-C3H7 |
CH3 |
4-Br(Ph) |
CH3 |
15.160 |
正-C3H7 |
CH3 |
4-F(Ph) |
CH3 |
15.161 |
正-C3H7 |
CH3 |
4-OCH3(Ph) |
CH3 |
15.162 |
正-C3H7 |
CH3 |
4-CH3(Ph) |
CH3 |
15.163 |
正-C3H7 |
CH3 |
4-NO2(Ph) |
CH3 |
15.164 |
正-C3H7 |
CH3 |
2,4-Cl(Ph) |
CH3 |
15.165 |
正-C3H7 |
CH3 |
2,4-F(Ph) |
CH3 |
15.166 |
异-C3H7 |
CH3 |
Ph |
CH3 |
15.167 |
异-C3H7 |
CH3 |
2-Cl(Ph) |
CH3 |
15.168 |
异-C3H7 |
CH3 |
3-Cl(Ph) |
CH3 |
15.169 |
异-C3H7 |
CH3 |
4-Cl(Ph) |
CH3 |
15.170 |
异-C3H7 |
CH3 |
4-Br(Ph) |
CH3 |
15.171 |
异-C3H7 |
CH3 |
4-F(Ph) |
CH3 |
15.172 |
异-C3H7 |
CH3 |
4-OCH3(Ph) |
CH3 |
15.173 |
异-C3H7 |
CH3 |
4-CH3(Ph) |
CH3 |
15.174 |
异-C3H7 |
CH3 |
4-NO2(Ph) |
CH3 |
15.175 |
异-C3H7 |
CH3 |
2,4-Cl(Ph) |
CH3 |
15.176 |
异-C3H7 |
CH3 |
2,4-F(Ph) |
CH3 |
15.177 |
正-C4H9 |
CH3 |
Ph |
CH3 |
15.178 |
正-C4H9 |
CH3 |
2-Cl(Ph) |
CH3 |
15.179 |
正-C4H9 |
CH3 |
3-Cl(Ph) |
CH3 |
15.180 |
正-C4H9 |
CH3 |
4-Cl(Ph) |
CH3 |
15.181 |
正-C4H9 |
CH3 |
4-Br(Ph) |
CH3 |
15.182 |
正-C4H9 |
CH3 |
4-F(Ph) |
CH3 |
15.183 |
正-C4H9 |
CH3 |
4-OCH3(Ph) |
CH3 |
15.184 |
正-C4H9 |
CH3 |
4-CH3(Ph) |
CH3 |
15.185 |
正-C4H9 |
CH3 |
4-NO2(Ph) |
CH3 |
15.186 |
正-C4H9 |
CH3 |
2,4-Cl(Ph) |
CH3 |
15.187 |
正-C4H9 |
CH3 |
2,4-F(Ph) |
CH3 |
15.188 |
正-C4H9 |
CH3 |
4-CF3(Ph) |
CH3 |
15.189 |
Ph |
H |
Ph |
H |
15.190 |
Ph |
H |
Ph |
CH3 |
15.191 |
Ph |
H |
Ph |
C2H5 |
15.192 |
Ph |
H |
Ph |
正-C3H7 |
15.193 |
Ph |
H |
Ph |
异-C3H7 |
15.194 |
Ph |
H |
Ph |
正-C4H9 |
15.195 |
Ph |
H |
Ph |
异-C4H9 |
15.196 |
Ph |
H |
Ph |
C(CH3)3 |
15.197 |
Ph |
H |
Ph |
CH2C≡CH |
15.198 |
Ph |
H |
2-Cl(Ph) |
CH3 |
15.199 |
Ph |
H |
4-Cl(Ph) |
CH3 |
15.200 |
Ph |
CH3 |
Ph |
CH3 |
15.201 |
Ph |
CH3 |
2-Cl(Ph) |
CH3 |
15.202 |
Ph |
CH3 |
3-Cl(Ph) |
CH3 |
15.203 |
Ph |
CH3 |
4-Cl(Ph) |
CH3 |
15.204 |
Ph |
CH3 |
4-Br(Ph) |
CH3 |
15.205 |
Ph |
CH3 |
4-F(Ph) |
CH3 |
15.206 |
Ph |
CH3 |
4-OCH3(Ph) |
CH3 |
15.207 |
Ph |
CH3 |
4-CH3(Ph) |
CH3 |
15.208 |
Ph |
CH3 |
4-NO2(Ph) |
CH3 |
15.209 |
Ph |
CH3 |
2,4-(Cl(Ph) |
CH3 |
15.210 |
Ph |
CH3 |
2,4-F(Ph) |
CH3 |
15.211 |
CN |
H |
Ph |
H |
15.212 |
CN |
H |
Ph |
CH3 |
15.213 |
CN |
H |
Ph |
C2H5 |
15.214 |
CN |
H |
Ph |
正-C3H7 |
15.215 |
CN |
H |
Ph |
异-C3H7 |
15.216 |
CN |
H |
Ph |
正-C4H9 |
15.217 |
CN |
H |
Ph |
异-C4H9 |
15.218 |
CN |
H |
Ph |
C(CH3)3 |
15.219 |
CN |
H |
Ph |
CH2C≡CH |
15.220 |
CN |
H |
2-Cl(Ph) |
CH3 |
15.221 |
CN |
H |
4-Cl(Ph) |
CH3 |
15.222 |
CN |
CH3 |
Ph |
H |
15.223 |
CN |
CH3 |
2-Cl(Ph) |
CH3 |
15.224 |
CN |
CH3 |
3-Cl(Ph) |
CH3 |
15.225 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
15.226 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
15.227 |
CN |
CH3 |
4-F(Ph) |
CH3 |
15.228 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
15.229 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
15.230 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
15.231 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
15.232 |
CN |
CH3 |
2,4-F(Ph) |
CH3 |
15.233 |
H |
H |
1-萘基 |
H |
15.234 |
CH3 |
H |
1-萘基 |
CH3 |
15.235 |
C2H5 |
H |
1-萘基 |
CH3 |
15.236 |
正-C3H7 |
H |
1-萘基 |
CH3 |
15.237 |
异-C3H7 |
H |
1-萘基 |
CH3 |
15.238 |
正-C4H9 |
H |
1-萘基 |
CH3 |
15.239 |
异-C4H9 |
H |
1-萘基 |
CH3 |
15.240 |
环丙基 |
H |
1-萘基 |
CH3 |
15.241 |
1-CH3-环丙基 |
H |
1-萘基 |
CH3 |
15.242 |
CN |
H |
1-萘基 |
CH3 |
15.248 |
Ph |
CH3 |
1-萘基 |
CH3 |
15.244 |
H |
CH3 |
1-萘基 |
CH3 |
15.245 |
CH3 |
CH3 |
1-萘基 |
CH3 |
15.246 |
C2H5 |
CH3 |
1-萘基 |
CH3 |
15.247 |
正-C3H7 |
CH3 |
1-萘基 |
CH3 |
15.248 |
异-C3H7 |
CH3 |
1-萘基 |
CH3 |
15.249 |
正-C4H9 |
CH3 |
1-萘基 |
CH3 |
15.250 |
异-C4H9 |
CH3 |
1-萘基 |
CH3 |
15.251 |
环丙基 |
CH3 |
1-萘基 |
CH3 |
15.252 |
1-CH3-环丙基 |
CH3 |
1-萘基 |
CH3 |
15.253 |
CN |
CH3 |
1-萘基 |
CH3 |
15.254 |
Ph |
CH3 |
1-萘基 |
CH3 |
15.255 |
H |
H |
2-萘基 |
H |
15.256 |
CH3 |
H |
2-萘基 |
CH3 |
15.257 |
C2H5 |
H |
2-萘基 |
C2H5 |
15.258 |
正-C3H7 |
H |
2-萘基 |
正-C3H7 |
15.259 |
异-C3H7 |
H |
2-萘基 |
异-C3H7 |
15.260 |
正-C4H9 |
H |
2-萘基 |
正-C4H9 |
15.261 |
异-C4H9 |
H |
2-萘基 |
异-C4H9 |
15.262 |
环丙基 |
H |
2-萘基 |
C(CH3)3 |
15.263 |
1-CH3-环丙基 |
H |
2-萘基 |
CH2C≡CH |
15.264 |
CN |
H |
2-萘基 |
CH2Ph |
15.265 |
Ph |
H |
2-萘基 |
CH2Ph |
15.266 |
H |
CH3 |
2-萘基 |
CH3 |
15.267 |
CH3 |
CH3 |
2-萘基 |
CH3 |
15.268 |
C2H5 |
CH3 |
2-萘基 |
CH3 |
15.269 |
正-C3H7 |
CH3 |
2-萘基 |
CH3 |
15.270 |
异-C3H7 |
CH3 |
2-萘基 |
CH3 |
15.271 |
正-C4H9 |
CH3 |
2-萘基 |
CH3 |
15.272 |
异-C4H9 |
CH3 |
2-萘基 |
CH3 |
15.273 |
环丙基 |
CH3 |
2-萘基 |
CH3 |
15.274 |
1-CH3-环丙基 |
CH3 |
2-萘基 |
CH3 |
15.275 |
CN |
CH3 |
2-萘基 |
CH3 |
15.276 |
Ph |
CH3 |
2-萘基 |
CH3 |
15.277 |
2-Cl(Ph) |
CH3 |
2-萘基 |
CH3 |
15.273 |
3-Cl(Ph) |
CH3 |
2-萘基 |
CH3 |
15.279 |
4-Cl(Ph) |
CH3 |
2-萘基 |
CH3 |
15.280 |
4-Br(Ph) |
CH3 |
2-萘基 |
CH3 |
15.281 |
4-F(Ph) |
CH3 |
2-萘基 |
CH3 |
15.282 |
4-OCH3(Ph) |
CH3 |
2-萘基 |
CH3 |
15.283 |
4-CH3(Ph) |
CH3 |
2-萘基 |
CH3 |
15.284 |
3-CF3(Ph) |
CH3 |
2-萘基 |
CH3 |
15.285 |
CH3 |
C2H5 |
Ph |
CH3 |
15.286 |
CH3 |
C2H5 |
2-Cl(Ph) |
CH3 |
15.287 |
CH3 |
C2H5 |
3-Cl(Ph) |
CH3 |
15.288 |
CH3 |
C2H5 |
4-Cl(Ph) |
CH3 |
15.289 |
CH3 |
C2H5 |
4-Br(Ph) |
CH3 |
15.290 |
CH3 |
C2H5 |
4-F(Ph) |
CH3 |
15.291 |
CH3 |
C2H5 |
4-OCH3(Ph) |
CH3 |
15.292 |
CH3 |
C2H5 |
4-CH3(Ph) |
CH3 |
15.293 |
CH3 |
C2H5 |
4-NO2(Ph) |
CH3 |
15.294 |
CH3 |
C2H5 |
2.4-Cl(Ph) |
CH3 |
15.295 |
CH3 |
C2H5 |
2,4-F(Ph) |
CH3 |
15.296 |
CH3 |
正-C3H7 |
Ph |
CH3 |
15.297 |
CH3 |
正-C3H7 |
2-Cl(Ph) |
CH3 |
15.298 |
CH3 |
正-C3H7 |
3-Cl(Ph) |
CH3 |
15.299 |
CH3 |
正-C3H7 |
4-Cl(Ph) |
CH3 |
15.300 |
CH3 |
正-C3H7 |
4-Br(Ph) |
CH3 |
15.301 |
CH3 |
正-C3H7 |
4-F(Ph) |
CH3 |
15.302 |
CH3 |
正-C3H7 |
4-OCH3(Ph) |
CH3 |
15.303 |
CH3 |
正-C3H7 |
4-CH3(Ph) |
CH3 |
15.304 |
CH3 |
正-C3H7 |
4-NO2(Ph) |
CH3 |
15.305 |
CH3 |
正-C3H7 |
2,4-Cl(Ph) |
CH3 |
15.306 |
CH3 |
正-C3H7 |
2,4-F(Ph) |
CH3 |
15.307 |
CH3 |
异-C3H7 |
Ph |
CH3 |
15.308 |
CH3 |
异-C3H7 |
2-Cl(Ph) |
CH3 |
15.309 |
CH3 |
异-C3H7 |
3-Cl(Ph) |
CH3 |
15.310 |
CH3 |
异-C3H7 |
4-Cl(Ph) |
CH3 |
15.311 |
CH3 |
异-C3H7 |
4-Br(Ph) |
CH3 |
15.312 |
CH3 |
异-C3H7 |
4-F(Ph) |
CH3 |
15.313 |
CH3 |
异-C3H7 |
4-OCH3(Ph) |
CH3 |
15.314 |
CH3 |
异-C3H7 |
4-CH3(Ph) |
CH3 |
15.315 |
CH3 |
异-C3H7 |
4-NO2(Ph) |
CH3 |
表16:化合物16.1-16.226为式Ⅶ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NOR9的式Ⅰ化合物,其中R9为CH3,R2、R3和R7如表4所定义。
表17:化合物17.1-17.226为式Ⅷ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NOR9的式Ⅰ化合物,其中R9为CH3,R2、R3和R7如表4所定义。
表18:化合物18.1-18.226为式Ⅸ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NOR9的式Ⅰ化合物,其中R9为CH3,R2、R3和R7如表4所定义。
表19:化合物19.1-19.221为式Ⅶ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NOR9的式Ⅰ化合物,其中R9为C2H5,R2、R3和R7如表7所定义。
表20:化合物20.1-20.221为式Ⅷ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NOR9的式Ⅰ化合物,其中R9为C2H5,R2、R3和R7如表7所定义。
表21:化合物21.1-21.221为式Ⅸ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NOR9的式Ⅰ化合物,其中R9为C2H5,R2、R3和R7如表7所定义。
表22:化合物22.1-22.139为式Ⅶ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NOR9的式Ⅰ化合物,其中R9为CH2Ph,R2、R3和R7如表10所定义。
表23:化合物23.1-23.139为式Ⅷ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NOR9的式Ⅰ化合物,其中R9为CH2Ph,R2、R3和R7如表10所定义。
表24:化合物24.1-24.139为式Ⅸ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NOR9的式Ⅰ化合物,其中R9为CH2Ph,R2、R3和R7如表10所定义。
本发明式Ⅰ所涵盖的典型化合物包括式Ⅹ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O,Z=NR10且其中R10为NR8R9的式Ⅰ化合物,其中的R2、R3、R7、R8和R9如表25所定义。
表25
化合物 |
R2 |
R3 |
R7 |
R8 |
R9 |
25.1 |
H |
H |
Ph |
CH3 |
H |
25.2 |
H |
H |
4-Cl(Ph) |
CH3 |
H |
25.3 |
H |
H |
4-Br(Ph) |
CH3 |
H |
25.4 |
H |
H |
4-F(Ph) |
CH3 |
H |
25.5 |
H |
H |
4-OCH3(Ph) |
CH3 |
H |
25.6 |
H |
H |
4-CF3(Ph) |
CH3 |
H |
25.7 |
H |
H |
Ph |
CH3 |
CH3 |
25.8 |
H |
H |
4-Cl(Ph) |
CH3 |
CH3 |
25.9 |
H |
H |
4-Br(Ph) |
CH3 |
CH3 |
25.10 |
H |
H |
4-F(Ph) |
CH3 |
CH3 |
25.11 |
CH3 |
H |
Ph |
CH3 |
H |
25.12 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
H |
25.13 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
H |
25.14 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
H |
25.15 |
CH3 |
H |
2-Br(Ph) |
CH3 |
H |
25.16 |
CH3 |
H |
3-Br(Ph) |
CH3 |
H |
25.17 |
CH3 |
H |
4-Br(Ph) |
CH3 |
H |
25.18 |
CH3 |
H |
Ph |
CH3 |
CH3 |
25.19 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
CH3 |
25.20 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
CH3 |
25.21 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
CH3 |
25.22 |
CH3 |
H |
2-Br(Ph) |
CH3 |
CH3 |
25.23 |
CH3 |
H |
3-Br(Ph) |
CH3 |
CH3 |
25.24 |
CH3 |
H |
4-Br(Ph) |
CH3 |
CH3 |
25.25 |
CH3 |
H |
2-CH3(Ph) |
CH3 |
CH3 |
25.26 |
CH3 |
H |
3-CH3(Ph) |
CH3 |
CH3 |
25.27 |
CH3 |
H |
2-CF3(Ph) |
CH3 |
CH3 |
25.28 |
CH3 |
H |
3-CF3(Ph) |
CH3 |
CH3 |
25.29 |
CH3 |
H |
4-CF3(Ph) |
CH3 |
CH3 |
25.30 |
CH3 |
H |
2-NO2(Ph) |
CH3 |
CH3 |
25.31 |
CH3 |
H |
3-NO2(Ph) |
CH3 |
CH3 |
25.32 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
CH3 |
25.33 |
CH3 |
H |
2,3-Cl(Ph) |
CH3 |
CH3 |
25.34 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
CH3 |
25.35 |
CH3 |
H |
2,5-Cl(Ph) |
CH3 |
CH3 |
25.36 |
CH3 |
H |
2,6-Cl(Ph) |
CH3 |
CH3 |
25.37 |
CH3 |
H |
3,4-Cl(Ph) |
CH3 |
CH3 |
25.38 |
CH3 |
H |
3,5-Cl(Ph) |
CH3 |
CH3 |
25.39 |
CH3 |
H |
Ph |
C2H5 |
CH3 |
25.40 |
CH3 |
H |
Ph |
正-C3H7 |
CH3 |
25.41 |
CH3 |
H |
Ph |
异-C3H7 |
CH3 |
25.42 |
CH3 |
H |
Ph |
正-C4H9 |
CH3 |
25.43 |
CH3 |
H |
Ph |
异-C4H9 |
CH3 |
25.44 |
CH3 |
H |
Ph |
C(CH3)3 |
CH3 |
25.45 |
CH3 |
H |
Ph |
H |
COCH3 |
25.46 |
CH3 |
H |
2-Cl(Ph) |
H |
COCH3 |
25.47 |
CH3 |
H |
3-Cl(Ph) |
H |
COCH3 |
25.48 |
CH3 |
H |
4-Cl(Ph) |
H |
COCH3 |
25.49 |
CH3 |
H |
4-Br(Ph) |
H |
COCH3 |
25.50 |
CH3 |
H |
4-F(Ph) |
H |
COCH3 |
25.51 |
CH3 |
H |
4-OCH3(Ph) |
H |
COCH3 |
25.52 |
CH3 |
H |
4-CH3(Ph) |
H |
COCH3 |
25.53 |
CH3 |
H |
4-NO2(Ph) |
H |
COCH3 |
25.54 |
CH3 |
H |
2,4-Cl(Ph) |
H |
COCH3 |
25.55 |
CH3 |
H |
2,4-F(Ph) |
H |
COCH3 |
25.56 |
CH3 |
H |
Ph |
CH3 |
COCH3 |
25.57 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
COCH3 |
25.58 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
COCH3 |
25.59 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
COCH3 |
25.60 |
CH3 |
H |
4-F(Ph) |
CH3 |
COCH3 |
25.61 |
CH3 |
H |
3-OCH3(Ph) |
CH3 |
COCH3 |
25.62 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
COCH3 |
25.63 |
CH3 |
H |
4-CH3(Ph) |
CH3 |
COCH3 |
25.64 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
COCH3 |
25.65 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
COCH3 |
25.66 |
CH3 |
H |
2,4-F(Ph) |
CH3 |
COCH3 |
25.67 |
CH3 |
H |
Ph |
H |
COPh |
25.68 |
CH3 |
H |
2-Cl(Ph) |
H |
COPh |
25.69 |
CH3 |
H |
3-Cl(Ph) |
H |
COPh |
25.70 |
CH3 |
H |
4-Cl(Ph) |
H |
COPh |
25.71 |
CH3 |
H |
4-Br(Ph) |
H |
COPh |
25.72 |
CH3 |
H |
4-F(Ph) |
H |
COPh |
25.73 |
CH3 |
H |
4-OCH3(Ph) |
H |
COPh |
25.74 |
CH3 |
H |
4-CH3(Ph) |
H |
COPh |
25.75 |
CH3 |
H |
4-NO2(Ph) |
H |
COPh |
25.76 |
CH3 |
H |
2,4-Cl(Ph) |
H |
COPh |
25.77 |
CH3 |
H |
2,4-F(Ph) |
H |
COPh |
25.78 |
CH3 |
H |
Ph |
CH3 |
COPh |
25.79 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
COPh |
25.80 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
COPh |
25.81 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
COPh |
25.82 |
CH3 |
H |
4-Br(Ph) |
CH3 |
COPh |
25.83 |
CH3 |
H |
4-F(Ph) |
CH3 |
COPh |
25.84 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
COPh |
25.85 |
CH3 |
H |
4-CH3(Ph) |
CH3 |
COPh |
25.86 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
COPh |
25.87 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
COPh |
25.88 |
CH3 |
H |
2,4-F(Ph) |
CH3 |
COPh |
25.89 |
C2H5 |
H |
Ph |
H |
COCH3 |
25.90 |
C2H5 |
H |
2-Cl(Ph) |
H |
COCH3 |
25.91 |
C2H5 |
H |
3-Cl(Ph) |
H |
COCH3 |
25.92 |
C2H5 |
H |
4-Cl(Ph) |
H |
COCH3 |
25.93 |
C2H5 |
H |
4-F(Ph) |
H |
COCH3 |
25.94 |
C2H5 |
H |
3-OCH3(Ph) |
H |
COCH3 |
25.95 |
C2H5 |
H |
4-OCH3(Ph) |
H |
COCH3 |
25.96 |
C2H5 |
H |
4-CH3(Ph) |
H |
COCH3 |
25.97 |
C2H5 |
H |
4-NO2(Ph) |
H |
COCH3 |
25.98 |
C2H5 |
H |
2,4-Cl(Ph) |
H |
COCH3 |
25.99 |
C2H5 |
H |
2,4-F(Ph) |
H |
COCH3 |
25.100 |
C2H5 |
H |
Ph |
CH3 |
COCH3 |
25.101 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
COCH3 |
25.102 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
COCH3 |
25.103 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
COCH3 |
25.104 |
C2H5 |
H |
4-F(Ph) |
CH3 |
COCH3 |
25.105 |
C2H5 |
H |
3-OCH3(Ph) |
CH3 |
COCH3 |
25.106 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
COCH3 |
25.107 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
COCH3 |
25.108 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
COCH3 |
25.109 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
COCH3 |
25.110 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
COCH3 |
25.111 |
C2H5 |
H |
Ph |
H |
COPh |
25.112 |
C2H5 |
H |
2-Cl(Ph) |
H |
COPh |
25.113 |
C2H5 |
H |
3-Cl(Ph) |
H |
COPh |
25.114 |
C2H5 |
H |
4-Cl(Ph) |
H |
COPh |
25.115 |
C2H5 |
H |
4-Br(Ph) |
H |
COPh |
25.116 |
C2H5 |
H |
3-OCH3(Ph) |
H |
COPh |
25.117 |
C2H5 |
H |
4-OCH3(Ph) |
H |
COPh |
25.118 |
C2H5 |
H |
4-CH3(Ph) |
H |
COPh |
25.119 |
C2H5 |
H |
4-NO2(Ph) |
H |
COPh |
25.120 |
C2H5 |
H |
2,4-Cl(Ph) |
H |
COPh |
25.121 |
C2H5 |
H |
2,4-F(Ph) |
H |
COPh |
25.122 |
C2H5 |
H |
Ph |
CH3 |
COPh |
25.123 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
COPh |
25.124 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
COPh |
25.125 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
COPh |
25.126 |
C2H5 |
H |
4-Br(Ph) |
CH3 |
COPh |
25.127 |
C2H5 |
H |
4-F(Ph) |
CH3 |
COPh |
25.128 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
COPh |
25.129 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
COPh |
25.130 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
COPh |
25.131 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
COPh |
25.132 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
COPh |
25.133 |
CH3 |
H |
Ph |
C2H5 |
COCH3 |
25.134 |
CH3 |
H |
Ph |
正-C3H7 |
COCH3 |
25.135 |
CH3 |
H |
Ph |
异-C3H7 |
COCH3 |
25.136 |
CH3 |
H |
Ph |
正-C4H9 |
COCH3 |
25.137 |
CH3 |
H |
Ph |
异-C4H9 |
COCH3 |
25.138 |
CH3 |
H |
Ph |
C(CH3)3 |
COCH3 |
25.139 |
CH3 |
H |
4-Cl(Ph) |
C2H5 |
COCH3 |
25.140 |
CH3 |
H |
4-Cl(Ph) |
正-C3H7 |
COCH3 |
25.141 |
CH3 |
H |
4-Cl(Ph) |
异-C3H7 |
COCH3 |
25.142 |
CH3 |
H |
4-Cl(Ph) |
正-C4H9 |
COCH3 |
25.143 |
CH3 |
H |
4-Cl(Ph) |
异-C4H9 |
COCH3 |
25.144 |
CH3 |
H |
4-Cl(Ph) |
C(CH3)3 |
COCH3 |
25.145 |
CH3 |
H |
Ph |
C2H5 |
COPh |
25.146 |
CH3 |
H |
Ph |
正-C3H7 |
COPh |
25.147 |
CH3 |
H |
Ph |
异-C3H7 |
COPh |
25.148 |
CH3 |
H |
Ph |
正-C4H9 |
COPh |
25.149 |
CH3 |
H |
Ph |
C(CH3)3 |
COPh |
25.150 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
COCH2Ph |
25.151 |
CH3 |
H |
4-Br(Ph) |
CH3 |
COCH2Ph |
25.152 |
CH3 |
H |
4-F(Ph) |
CH3 |
COCH2Ph |
25.153 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
COCH2Ph |
25.154 |
CH3 |
H |
4-CH3(Ph) |
CH3 |
COCH2Ph |
25.155 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
COCH2Ph |
25.156 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
COCH2Ph |
25.157 |
CH3 |
H |
2,4-F(Ph) |
CH3 |
COCH2Ph |
25.158 |
CH3 |
H |
4-C(Ph) |
C2H5 |
COCH2Ph |
25.159 |
CH3 |
H |
4-Br(Ph) |
正-C3H7 |
COCH2Ph |
25.160 |
CH3 |
H |
4-F(Ph) |
异-C3H7 |
COCH2Ph |
25.161 |
CH3 |
H |
4-OCH3(Ph) |
正-C4H9 |
COCH2Ph |
25.162 |
CH3 |
H |
4-CH3(Ph) |
异-C4H9 |
COCH2Ph |
25.163 |
CH3 |
H |
4-NO2(Ph) |
C(CH3)3 |
COCH2Ph |
25.164 |
Ph |
H |
Ph |
CH3 |
H |
25.165 |
Ph |
H |
2-Cl(Ph) |
CH3 |
H |
25.166 |
Ph |
H |
3-Cl(Ph) |
CH3 |
H |
25.167 |
Ph |
H |
4-Cl(Ph) |
CH3 |
H |
25.168 |
Ph |
H |
4-Br(Ph) |
CH3 |
H |
25.169 |
Ph |
H |
4-F(Ph) |
CH3 |
H |
25.170 |
Ph |
H |
4-OCH3(Ph) |
CH3 |
H |
25.171 |
Ph |
H |
4-CH3(Ph) |
CH3 |
H |
25.172 |
Ph |
H |
4-NO2(Ph) |
CH3 |
H |
25.173 |
Ph |
H |
2,4-Cl(Ph) |
CH3 |
H |
25.174 |
Ph |
H |
Ph |
CH3 |
CH3 |
25.175 |
Ph |
H |
2-Cl(Ph) |
CH3 |
CH3 |
25.176 |
Ph |
H |
3-Cl(Ph) |
CH3 |
CH3 |
25.177 |
Ph |
H |
4-Cl(Ph) |
CH3 |
CH3 |
25.178 |
Ph |
H |
4-Br(Ph) |
CH3 |
CH3 |
25.179 |
Ph |
H |
4-F(Ph) |
CH3 |
CH3 |
25.180 |
CN |
H |
4-Cl(Ph) |
CH3 |
H |
25.181 |
CN |
H |
4-Br(Ph) |
CH3 |
H |
25.182 |
CN |
H |
4-F(Ph) |
CH3 |
H |
25.183 |
CN |
H |
4-OCH3(Ph) |
CH3 |
H |
25.184 |
CN |
H |
4-CH3(Ph) |
CH3 |
H |
25.185 |
CN |
H |
4-NO2(Ph) |
CH3 |
H |
25.186 |
CN |
H |
2,4-Cl(Ph) |
CH3 |
H |
25.187 |
CN |
H |
2,4-F(Ph) |
CH3 |
H |
25.188 |
CN |
H |
4-CF3(Ph) |
CH3 |
H |
25.189 |
CN |
H |
Ph |
CH3 |
CH3 |
25.190 |
CN |
H |
Ph |
CH3 |
COCH3 |
25.191 |
H |
H |
1-萘基 |
CH3 |
H |
25.192 |
H |
H |
1-萘基 |
CH3 |
CH3 |
25.193 |
H |
H |
1-萘基 |
CH3 |
COCH3 |
25.194 |
H |
H |
1-萘基 |
CH3 |
COPh |
25.195 |
CH3 |
H |
1-萘基 |
CH3 |
H |
25.196 |
CH3 |
H |
1-萘基 |
CH3 |
CH3 |
25.197 |
CH3 |
H |
1-萘基 |
CH3 |
COCH3 |
25.198 |
CH3 |
H |
1-萘基 |
CH3 |
COPh |
25.199 |
CH3 |
H |
1-萘基 |
CH3 |
COCH2Ph |
25.200 |
H |
H |
1-萘基 |
CH3 |
CO2CH3 |
25.201 |
CH3 |
H |
1-萘基 |
CH3 |
CO2CH3 |
25.202 |
H |
H |
2-萘基 |
CH3 |
H |
25.203 |
H |
H |
2-萘基 |
CH3 |
CH3 |
25.204 |
H |
H |
2-萘基 |
CH3 |
COCH3 |
25.205 |
H |
H |
2-萘基 |
CH3 |
COPh |
25.206 |
CH3 |
H |
2-萘基 |
CH3 |
H |
25.207 |
CH3 |
H |
2-萘基 |
CH3 |
CH3 |
25.208 |
CH3 |
H |
2-萘基 |
CH3 |
COCH3 |
25.209 |
CH3 |
H |
2-萘基 |
CH3 |
COPh |
25.210 |
CH3 |
H |
2-萘基 |
CH3 |
COCH2Ph |
25.211 |
H |
H |
2-萘基 |
CH3 |
CO2CH3 |
25.212 |
CH3 |
H |
2-萘基 |
CH3 |
CO2CH3 |
25.213 |
H |
CH3 |
Ph |
CH3 |
H |
25.214 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
H |
25.215 |
H |
CH3 |
4-Br(Ph) |
CH3 |
H |
25.216 |
H |
CH3 |
4-F(Ph) |
CH3 |
H |
25.217 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
H |
25.218 |
H |
CH3 |
4-CF3(Ph) |
CH3 |
H |
25.219 |
H |
CH3 |
Ph |
CH3 |
CH3 |
25.220 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
CH3 |
25.221 |
H |
CH3 |
4-Br(Ph) |
CH3 |
CH3 |
25.222 |
H |
CH3 |
4-F(Ph) |
CH3 |
CH3 |
25.223 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
CH3 |
25.224 |
H |
CH3 |
4-CF3(Ph) |
CH3 |
CH3 |
25.225 |
H |
CH3 |
Ph |
CH3 |
C2H5 |
25.226 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
正-C3H7 |
25.227 |
H |
CH3 |
4-Br(Ph) |
CH3 |
异-C3H7 |
25.228 |
H |
CH3 |
4-F(Ph) |
CH3 |
正-C4H9 |
25.229 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
异-C4H9 |
25.230 |
H |
CH3 |
4-CH3(Ph) |
CH3 |
C(CH3)3 |
25.231 |
H |
CH3 |
4-NO2(Ph) |
CH3 |
CH3 |
25.232 |
H |
CH3 |
2,4-Cl(Ph) |
CH3 |
CH3 |
25.233 |
H |
CH3 |
Ph |
CH3 |
COCH3 |
25.234 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
COCH3 |
25.235 |
H |
CH3 |
4-Br(Ph) |
CH3 |
COCH3 |
25.236 |
H |
CH3 |
4-F(Ph) |
CH3 |
COCH3 |
25.237 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
COCH3 |
25.238 |
H |
CH3 |
4-CH3(Ph) |
CH3 |
COCH3 |
25.239 |
H |
CH3 |
4-NO2(Ph) |
CH3 |
COCH3 |
25.240 |
H |
CH3 |
2,4-Cl(Ph) |
CH3 |
COCH3 |
25.241 |
H |
CH3 |
Ph |
CH3 |
COPh |
25.242 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
COPh |
25.243 |
H |
CH3 |
4-Br(Ph) |
CH3 |
COPh |
25.244 |
H |
CH3 |
4-F(Ph) |
CH3 |
COPh |
25.245 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
COPh |
25.246 |
H |
CH3 |
4-CH3(Ph) |
CH3 |
COPh |
25.247 |
H |
CH3 |
4-NO2(Ph) |
CH3 |
COPh |
25.248 |
H |
CH3 |
2,4-(Cl(Ph) |
CH3 |
COPh |
25.249 |
CH3 |
CH3 |
Ph |
CH3 |
H |
25.250 |
CH3 |
CH3 |
4-Cl(Ph) |
CH3 |
H |
25.251 |
CH3 |
CH3 |
4-Br(Ph) |
CH3 |
H |
25.252 |
CH3 |
CH3 |
4-F(Ph) |
CH3 |
H |
25.253 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH3 |
H |
25.254 |
CH3 |
CH3 |
4-CH3(Ph) |
CH3 |
H |
25.255 |
CH3 |
CH3 |
4-NO2(Ph) |
CH3 |
H |
25.256 |
CH3 |
CH3 |
2,4-Cl(Ph) |
CH3 |
H |
25.257 |
CH3 |
CH3 |
Ph |
CH3 |
COCH3 |
25.258 |
CH3 |
CH3 |
4-Cl(Ph) |
CH3 |
COCH3 |
25.259 |
CH3 |
CH3 |
4-Br(Ph) |
CH3 |
COCH3 |
25.260 |
CH3 |
CH3 |
4-F(Ph) |
CH3 |
COCH3 |
25.261 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH3 |
COCH3 |
25.262 |
CH3 |
CH3 |
4-CH3(Ph) |
CH3 |
COCH3 |
25.263 |
CH3 |
CH3 |
4-NO2(Ph) |
CH3 |
COCH3 |
25.264 |
CH3 |
CH3 |
2,4-Cl(Ph) |
CH3 |
COCH3 |
25.265 |
CN |
CH3 |
Ph |
CH3 |
H |
25.266 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
H |
25.267 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
H |
25.268 |
CN |
CH3 |
4-F(Ph) |
CH3 |
H |
25.269 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
H |
25.270 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
H |
25.271 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
H |
25.272 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
H |
25.273 |
CN |
CH3 |
Ph |
CH3 |
CH3 |
25.274 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
CH3 |
25.275 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
CH3 |
25.276 |
CN |
CH3 |
4-F(Ph) |
CH3 |
CH3 |
25.277 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
CH3 |
25.278 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
CH3 |
25.279 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
CH3 |
25.280 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
CH3 |
25.281 |
CN |
CH3 |
Ph |
CH3 |
COCH3 |
25.282 |
CN |
CH3 |
4-(Cl(Ph) |
CH3 |
COCH3 |
25.283 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
COCH3 |
25.284 |
CN |
CH3 |
4-F(Ph) |
CH3 |
COCH3 |
25.285 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
COCH3 |
25.286 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
COCH3 |
25.287 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
COCH3 |
25.288 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
COCH3 |
25.289 |
CN |
CH3 |
Ph |
CH3 |
COPh |
25.290 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
COPh |
25.291 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
COPh |
25.292 |
CN |
CH3 |
4-F(Ph) |
CH3 |
COPh |
25.293 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
COPh |
25.294 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
COPh |
25.295 |
CN |
CH3 |
2,4-F(Ph) |
CH3 |
COPh |
25.296 |
CN |
H |
Ph |
C2H5 |
H |
25.297 |
CN |
H |
2-Cl(Ph) |
正-C3H7 |
H |
25.298 |
CN |
H |
3-Cl(Ph) |
异-C3H7 |
H |
25.299 |
CN |
H |
4-Cl(Ph) |
正-C4H9 |
H |
25.300 |
CN |
H |
4-Br(Ph) |
异-C4H9 |
H |
25.301 |
CN |
H |
4-F(Ph) |
C(CH3)3 |
H |
25.302 |
CN |
H |
4-OCH3(Ph) |
C2H5 |
COCH3 |
25.303 |
CN |
H |
4-CH3(Ph) |
正-C3H7 |
COCH3 |
25.304 |
CN |
H |
4-NO2(Ph) |
异-C3H7 |
COCH3 |
25.305 |
CN |
H |
2,4-Cl(Ph) |
正-C4H9 |
COCH3 |
25.306 |
CN |
H |
2,4-F(Ph) |
异-C4H9 |
COCH3 |
25.307 |
CN |
H |
Ph |
C(CH3)3 |
COCH3 |
25.308 |
CN |
H |
2-Cl(Ph) |
C2H5 |
COPh |
25.309 |
CN |
H |
3-Cl(Ph) |
正-C3H7 |
COPh |
25.310 |
CN |
H |
4-Cl(Ph) |
异-C3H7 |
COPh |
25.311 |
CH3 |
H |
4-Br(Ph) |
正-C4H9 |
COPh |
25.312 |
CH3 |
H |
4-F(Ph) |
异-C4H9 |
COPh |
25.313 |
CH3 |
H |
4-OCH3(Ph) |
C(CH3)3 |
COPh |
本发明式Ⅰ所涵盖的典型化合物包括式Ⅺ化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=N,Y=O,Z=NR
10且其中R
10为NR
8R
9的式Ⅰ化合物,其中的R
2、R
3、R
7、R
8和R
9如表26所定义。
表26
化合物 |
R2 |
R3 |
R7 |
R8 |
R9 |
26.1 |
H |
H |
Ph |
CH3 |
H |
26.2 |
H |
H |
4-Cl(Ph) |
CH3 |
H |
26.3 |
H |
H |
4-Br(Ph) |
CH3 |
H |
26.4 |
H |
H |
4-F(Ph) |
CH3 |
H |
26.5 |
H |
H |
4-OCH3(Ph) |
CH3 |
H |
26.6 |
H |
H |
4-CF3(Ph) |
CH3 |
H |
26.7 |
H |
H |
Ph |
CH3 |
CH3 |
26.8 |
H |
H |
4-Cl(Ph) |
CH3 |
CH3 |
26.9 |
H |
H |
4-Br(Ph) |
CH3 |
CH3 |
26.10 |
H |
H |
4-F(Ph) |
CH3 |
CH3 |
26.11 |
CH3 |
H |
Ph |
CH3 |
H |
26.12 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
H |
26.13 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
H |
26.14 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
H |
26.15 |
CH3 |
H |
2-Br(Ph) |
CH3 |
H |
26.16 |
CH3 |
H |
3-Br(Ph) |
CH3 |
H |
26.17 |
CH3 |
H |
4-Br(Ph) |
CH3 |
H |
26.18 |
CH3 |
H |
Ph |
CH3 |
CH3 |
26.19 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
CH3 |
26.20 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
CH3 |
26.21 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
CH3 |
26.22 |
CH3 |
H |
2-Br(Ph) |
CH3 |
CH3 |
26.23 |
CH3 |
H |
3-Br(Ph) |
CH3 |
CH3 |
26.24 |
CH3 |
H |
4-Br(Ph) |
CH3 |
CH3 |
26.25 |
CH3 |
H |
2-CH3(Ph) |
CH3 |
CH3 |
26.26 |
CH3 |
H |
3-CH3(Ph) |
CH3 |
CH3 |
26.27 |
CH3 |
H |
2-CF3(Ph) |
CH3 |
CH3 |
26.28 |
CH3 |
H |
3-CF3(Ph) |
CH3 |
CH3 |
26.29 |
CH3 |
H |
4-CF3(Ph) |
CH3 |
CH3 |
26.30 |
CH3 |
H |
2-NO2(Ph) |
CH3 |
CH3 |
26.31 |
CH3 |
H |
3-NO2(Ph) |
CH3 |
CH3 |
26.32 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
CH3 |
26.33 |
CH3 |
H |
2,3-Cl(Ph) |
CH3 |
CH3 |
26.34 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
CH3 |
26.35 |
CH3 |
H |
2,5-Cl(Ph) |
CH3 |
CH3 |
26.36 |
CH3 |
H |
2,6-Cl(Ph) |
CH3 |
CH3 |
26.37 |
CH3 |
H |
3,4-Cl(Ph) |
CH3 |
CH3 |
26.38 |
CH3 |
H |
3,5-Cl(Ph) |
CH3 |
CH3 |
26.39 |
CH3 |
H |
Ph |
C2H5 |
CH3 |
26.40 |
CH3 |
H |
Ph |
正-C3H7 |
CH3 |
26.41 |
CH3 |
H |
Ph |
异-C3H7 |
CH3 |
26.42 |
CH3 |
H |
Ph |
正-C4H9 |
CH3 |
26.43 |
CH3 |
H |
Ph |
异-C4H9 |
CH3 |
26.44 |
CH3 |
H |
Ph |
C(CH3)3 |
CH3 |
26.45 |
CH3 |
H |
Ph |
H |
COCH3 |
26.46 |
CH3 |
H |
2-Cl(Ph) |
H |
COCH3 |
26.47 |
CH3 |
H |
3-Cl(Ph) |
H |
COCH3 |
26.48 |
CH3 |
H |
4-Cl(Ph) |
H |
COCH3 |
26.49 |
CH3 |
H |
4-Br(Ph) |
H |
COCH3 |
26.50 |
CH3 |
H |
4-F(Ph) |
H |
COCH3 |
26.51 |
CH3 |
H |
4-OCH3(Ph) |
H |
COCH3 |
26.52 |
CH3 |
H |
4-CH3(Ph) |
H |
COCH3 |
26.53 |
CH3 |
H |
4-NO2(Ph) |
H |
COCH3 |
26.54 |
CH3 |
H |
2.4-Cl(Ph) |
H |
COCH3 |
26.55 |
CH3 |
H |
2,4-F(Ph) |
H |
COCH3 |
26.56 |
CH3 |
H |
Ph |
CH3 |
COCH3 |
26.57 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
COCH3 |
26.58 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
COCH3 |
26.59 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
COCH3 |
26.60 |
CH3 |
H |
4-F(Ph) |
CH3 |
COCH3 |
26.61 |
CH3 |
H |
3-OCH3(Ph) |
CH3 |
COCH3 |
26.62 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
COCH3 |
26.63 |
CH3 |
H |
4-CH3(Ph) |
CH3 |
COCH3 |
26.64 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
COCH3 |
26.65 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
COCH3 |
26.66 |
CH3 |
H |
2,4-F(Ph) |
CH3 |
COCH3 |
26.67 |
CH3 |
H |
Ph |
H |
COPh |
26.68 |
CH3 |
H |
2-Cl(Ph) |
H |
COPh |
26.69 |
CH3 |
H |
3-Cl(Ph) |
H |
COPh |
26.70 |
CH3 |
H |
4-Cl(Ph) |
H |
COPh |
26.71 |
CH3 |
H |
4-Br(Ph) |
H |
COPh |
26.72 |
CH3 |
H |
4-F(Ph) |
H |
COPh |
26.73 |
CH3 |
H |
4-OCH3(Ph) |
H |
COPh |
26.74 |
CH3 |
H |
4-CH3(Ph) |
H |
COPh |
26.75 |
CH3 |
H |
4-NO2(Ph) |
H |
COPh |
26.76 |
CH3 |
H |
2,4-Cl(Ph) |
H |
COPh |
26.77 |
CH3 |
H |
2,4-F(Ph) |
H |
COPh |
26.78 |
CH3 |
H |
Ph |
CH3 |
COPh |
26.79 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
COPh |
26.80 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
COPh |
26.81 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
COPh |
26.82 |
CH3 |
H |
4-Br(Ph) |
CH3 |
COPh |
26.83 |
CH3 |
H |
4-F(Ph) |
CH3 |
COPh |
26.84 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
COPh |
26.85 |
CH3 |
H |
4-CH3(Ph) |
CH3 |
COPh |
26.86 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
COPh |
26.87 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
COPh |
26.88 |
CH3 |
H |
2,4-F(Ph) |
CH3 |
COPh |
26.89 |
C2H5 |
H |
Ph |
H |
COCH3 |
26.90 |
C2H5 |
H |
2-Cl(Ph) |
H |
COCH3 |
26.91 |
C2H5 |
H |
3-(Cl(Ph) |
H |
COCH3 |
26.92 |
C2H5 |
H |
4-(Cl(Ph) |
H |
COCH3 |
26.93 |
C2H5 |
H |
4-F(Ph) |
H |
COCH3 |
26.94 |
C2H5 |
H |
3-OCH3(Ph) |
H |
COCH3 |
26.95 |
C2H5 |
H |
4-OCH3(Ph) |
H |
COCH3 |
26.96 |
C2H5 |
H |
4-CH3(Ph) |
H |
COCH3 |
26.97 |
C2H5 |
H |
4-NO2(Ph) |
H |
COCH3 |
26.98 |
C2H5 |
H |
2,4-Cl(Ph) |
H |
COCH3 |
26.99 |
C2H5 |
H |
2,4-F(Ph) |
H |
COCH3 |
26.100 |
C2H5 |
H |
Ph |
CH3 |
COCH3 |
26.101 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
COCH3 |
26.102 |
C2H5 |
H |
3-(Cl(Ph) |
CH3 |
COCH3 |
26.103 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
COCH3 |
26.104 |
C2H5 |
H |
4-F(Ph) |
CH3 |
COCH3 |
26.105 |
C2H5 |
H |
3-OCH3(Ph) |
CH3 |
COCH3 |
26.106 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
COCH3 |
26.107 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
COCH3 |
26.108 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
COCH3 |
26.109 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
COCH3 |
26.110 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
COCH3 |
26.111 |
C2H5 |
H |
Ph |
H |
COPh |
26.112 |
C2H5 |
H |
2-(Cl(Ph) |
H |
COPh |
26.113 |
C2H5 |
H |
3-Cl(Ph) |
H |
COPh |
26.114 |
C2H5 |
H |
4-Cl(Ph) |
H |
COPh |
26.115 |
C2H5 |
H |
4-Br(Ph) |
H |
COPh |
26.116 |
C2H5 |
H |
8-OCH3(Ph) |
H |
COPh |
26.117 |
C2H5 |
H |
4-OCH3(Ph) |
H |
COPh |
26.118 |
C2H5 |
H |
4-CH3(Ph) |
H |
COPh |
26.119 |
C2H5 |
H |
4-NO2(Ph) |
H |
COPh |
26.120 |
C2H5 |
H |
2,4-Cl(Ph) |
H |
COPh |
26.121 |
C2H5 |
H |
2,4-F(Ph) |
H |
COPh |
26.122 |
C2H5 |
H |
Ph |
CH3 |
COPh |
26.123 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
COPh |
26.124 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
COPh |
26.125 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
COPh |
26.126 |
C2H5 |
H |
4-Br(Ph) |
CH3 |
COPh |
26.127 |
C2H5 |
H |
4-F(Ph) |
CH3 |
COPh |
26.128 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
COPh |
26.129 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
COPh |
26.130 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
COPh |
26.131 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
COPh |
26.132 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
COPh |
26.133 |
CH3 |
H |
Ph |
C2H5 |
COCH3 |
26.134 |
CH3 |
H |
Ph |
正-C3H7 |
COCH3 |
26.135 |
CH3 |
H |
Ph |
异-C3H7 |
COCH3 |
26.136 |
CH3 |
H |
Ph |
正-C4H9 |
COCH3 |
26.137 |
CH3 |
H |
Ph |
异-C4H9 |
COCH3 |
26.138 |
CH3 |
H |
Ph |
C(CH3)3 |
COCH3 |
26.139 |
CH3 |
H |
4-Cl(Ph) |
C2H5 |
COCH3 |
26.140 |
CH3 |
H |
4-Cl(Ph) |
正-C3H7 |
COCH3 |
26.141 |
CH3 |
H |
4-Cl(Ph) |
异-C3H7 |
COCH3 |
26.142 |
CH3 |
H |
4-Cl(Ph) |
正-C4H9 |
COCH3 |
26.143 |
CH3 |
H |
4-Cl(Ph) |
异-C4H9 |
COCH3 |
26.144 |
CH3 |
H |
4-Cl(Ph) |
C(CH3)3 |
COCH3 |
26.145 |
CH3 |
H |
Ph |
C2H5 |
COPh |
26.146 |
CH3 |
H |
Ph |
正-C3H7 |
COPh |
26.147 |
CH3 |
H |
Ph |
异-C3H7 |
COPh |
26.148 |
CH3 |
H |
Ph |
正-C4H9 |
COPh |
26.149 |
CH3 |
H |
Ph |
C(CH3)3 |
COPh |
26.150 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
COCH2Ph |
26.151 |
CH3 |
H |
4-Br(Ph) |
CH3 |
COCH2Ph |
26.152 |
CH3 |
H |
4-F(Ph) |
CH3 |
COCH2Ph |
26.153 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
COCH2Ph |
26.154 |
CH3 |
H |
4-CH3(Ph) |
CH3 |
COCH2Ph |
26.155 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
COCH2Ph |
26.156 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
COCH2Ph |
26.157 |
CH3 |
H |
2,4-F(Ph) |
CH3 |
COCH2Ph |
26.158 |
CH3 |
H |
4-Cl(Ph) |
C2H5 |
COCH2Ph |
26.159 |
CH3 |
H |
4-Br(Ph) |
正-C3H7 |
COCH2Ph |
26.160 |
CH3 |
H |
4-F(Ph) |
异-C3H7 |
COCH2Ph |
26.16l |
CH3 |
H |
4-OCH3(Ph) |
正-C4H9 |
COCH2Ph |
26.162 |
CH3 |
H |
4-CH3(Ph) |
异-C4H9 |
COCH2Ph |
26.163 |
CH3 |
H |
4-NO2(Ph) |
C(CH3)3 |
COCH2Ph |
26.164 |
Ph |
H |
Ph |
CH3 |
H |
26.165 |
Ph |
H |
2-Cl(Ph) |
CH3 |
H |
26.166 |
Ph |
H |
3-Cl(Ph) |
CH3 |
H |
26.167 |
Ph |
H |
4-Cl(Ph) |
CH3 |
H |
26.168 |
Ph |
H |
4-Br(Ph) |
CH3 |
H |
26.169 |
Ph |
H |
4-F(Ph) |
CH3 |
H |
26.170 |
Ph |
H |
4-OCH3(Ph) |
CH3 |
H |
26.171 |
Ph |
H |
4-CH3(Ph) |
CH3 |
H |
26.172 |
Ph |
H |
4-NO2(Ph) |
CH3 |
H |
26.173 |
Ph |
H |
2,4-Cl(Ph) |
CH3 |
H |
26.174 |
Ph |
H |
Ph |
CH3 |
CH3 |
26.175 |
Ph |
H |
2-Cl(Ph) |
CH3 |
CH3 |
26.176 |
Ph |
H |
3-Cl(Ph) |
CH3 |
CH3 |
26.177 |
Ph |
H |
4-Cl(Ph) |
CH3 |
CH3 |
26.178 |
Ph |
H |
4-Br(Ph) |
CH3 |
CH3 |
26.179 |
Ph |
H |
4-F(Ph) |
CH3 |
CH3 |
26.180 |
CN |
H |
4-Cl(Ph) |
CH3 |
H |
26.181 |
CN |
H |
4-Br(Ph) |
CH3 |
H |
26.182 |
CN |
H |
4-F(Ph) |
CH3 |
H |
26.183 |
CN |
H |
4-OCH3(Ph) |
CH3 |
H |
26.184 |
CN |
H |
4-CH3(Ph) |
CH3 |
H |
26.185 |
CN |
H |
4-NO2(Ph) |
CH3 |
H |
26.186 |
CN |
H |
2,4-Cl(Ph) |
CH3 |
H |
26.187 |
CN |
H |
2,4-F(Ph) |
CH3 |
H |
26.188 |
CN |
H |
4-CF3(Ph) |
CH3 |
H |
26.189 |
CN |
H |
Ph |
CH3 |
CH3 |
26.190 |
CN |
H |
Ph |
CH3 |
COCH3 |
26.191 |
H |
H |
1-萘基 |
CH3 |
H |
26.192 |
H |
H |
1-萘基 |
CH3 |
CH3 |
26.193 |
H |
H |
1-萘基 |
CH3 |
COCH3 |
26.194 |
H |
H |
1-萘基 |
CH3 |
COPh |
26.195 |
CH3 |
H |
1-萘基 |
CH3 |
H |
26.196 |
CH3 |
H |
1-萘基 |
CH3 |
CH3 |
26.197 |
CH3 |
H |
1-萘基 |
CH3 |
COCH3 |
26.198 |
CH3 |
H |
1-萘基 |
CH3 |
COPh |
26.199 |
CH3 |
H |
1-萘基 |
CH3 |
COCH2Ph |
26.200 |
H |
H |
1-萘基 |
CH3 |
CO2CH3 |
26.201 |
CH3 |
H |
1-萘基 |
CH3 |
CO2CH3 |
26.202 |
H |
H |
2-萘基 |
CH3 |
H |
26.203 |
H |
H |
2-萘基 |
CH3 |
CH3 |
26.204 |
H |
H |
2-萘基 |
CH3 |
COCH3 |
26.205 |
H |
H |
2-萘基 |
CH3 |
COPh |
26.206 |
CH3 |
H |
2-萘基 |
CH3 |
H |
26.207 |
CH3 |
H |
2-萘基 |
CH3 |
CH3 |
26.208 |
CH3 |
H |
2-萘基 |
CH3 |
COCH3 |
26.209 |
CH3 |
H |
2-萘基 |
CH3 |
COPh |
26.210 |
CH3 |
H |
2-萘基 |
CH3 |
COCH2Ph |
26.211 |
H |
H |
2-萘基 |
CH3 |
CO2CH3 |
26.212 |
CH3 |
H |
2-萘基 |
CH3 |
CO2CH3 |
26.213 |
H |
CH3 |
Ph |
CH3 |
H |
26.214 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
H |
26.215 |
H |
CH3 |
4-Br(Ph) |
CH3 |
H |
26.216 |
H |
CH3 |
4-F(Ph) |
CH3 |
H |
26.217 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
H |
26.218 |
H |
CH3 |
4-CF3(Ph) |
CH3 |
H |
26.219 |
H |
CH3 |
Ph |
CH3 |
CH3 |
26.220 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
CH3 |
26.221 |
H |
CH3 |
4-Br(Ph) |
CH3 |
CH3 |
26.222 |
H |
CH3 |
4-F(Ph) |
CH3 |
CH3 |
26.223 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
CH3 |
26.224 |
H |
CH3 |
4-CF3(Ph) |
CH3 |
CH3 |
26.225 |
H |
CH3 |
Ph |
CH3 |
C2H5 |
26.226 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
正-C3H7 |
26.227 |
H |
CH3 |
4-Br(Ph) |
CH3 |
异-C3H7 |
26.228 |
H |
CH3 |
4-F(Ph) |
CH3 |
正-C4H9 |
26.229 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
异-C4H9 |
26.230 |
H |
CH3 |
4-CH3(Ph) |
CH3 |
C(CH3)3 |
26.231 |
H |
CH3 |
4-NO2(Ph) |
CH3 |
CH3 |
26.232 |
H |
CH3 |
2,4-Cl(Ph) |
CH3 |
CH3 |
26.233 |
H |
CH3 |
Ph |
CH3 |
COCH3 |
26.234 |
H |
CH3 |
4-(Cl(Ph) |
CH3 |
COCH3 |
26.235 |
H |
CH3 |
4-Br(Ph) |
CH3 |
COCH3 |
26.236 |
H |
CH3 |
4-F(Ph) |
CH3 |
COCH3 |
26.237 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
COCH3 |
26.238 |
H |
CH3 |
4-CH3(Ph) |
CH3 |
COCH3 |
26.239 |
H |
CH3 |
4-NO2(Ph) |
CH3 |
COCH3 |
26.240 |
H |
CH3 |
2,4-Cl(Ph) |
CH3 |
COCH3 |
26.241 |
H |
CH3 |
Ph |
CH3 |
COPh |
26.242 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
COPh |
26.243 |
H |
CH3 |
4-Br(Ph) |
CH3 |
COPh |
26.244 |
H |
CH3 |
4-F(Ph) |
CH3 |
COPh |
26.245 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
COPh |
26.246 |
H |
CH3 |
4-CH3(Ph) |
CH3 |
COPh |
26.247 |
H |
CH3 |
4-NO2(Ph) |
CH3 |
COPh |
26.248 |
H |
CH3 |
2,4-Cl(Ph) |
CH3 |
COPh |
26.249 |
CH3 |
CH3 |
Ph |
CH3 |
H |
26.250 |
CH3 |
CH3 |
4-Cl(Ph) |
CH3 |
H |
26.251 |
CH3 |
CH3 |
4-Br(Ph) |
CH3 |
H |
26.252 |
CH3 |
CH3 |
4-F(Ph) |
CH3 |
H |
26.253 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH3 |
H |
26.254 |
CH3 |
CH3 |
4-CH3(Ph) |
CH3 |
H |
26.255 |
CH3 |
CH3 |
4-NO2(Ph) |
CH3 |
H |
26.256 |
CH3 |
CH3 |
2,4-Cl(Ph) |
CH3 |
H |
26.257 |
CH3 |
CH3 |
Ph |
CH3 |
COCH3 |
26.258 |
CH3 |
CH3 |
4-Cl(Ph) |
CH3 |
COCH3 |
26.259 |
CH3 |
CH3 |
4-Br(Ph) |
CH3 |
COCH3 |
26.260 |
CH3 |
CH3 |
4-F(Ph) |
CH3 |
COCH3 |
26.261 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH3 |
COCH3 |
26.262 |
CH3 |
CH3 |
4-CH3(Ph) |
CH3 |
COCH3 |
26.263 |
CH3 |
CH3 |
4-NO2(Ph) |
CH3 |
COCH3 |
26.264 |
CH3 |
CH3 |
2.4-Cl(Ph) |
CH3 |
COCH3 |
26.265 |
CN |
CH3 |
Ph |
CH3 |
H |
26.266 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
H |
26.267 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
H |
26.268 |
CN |
CH3 |
4-F(Ph) |
CH3 |
H |
26.269 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
H |
26.270 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
H |
26.271 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
H |
26.272 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
H |
26.273 |
CN |
CH3 |
Ph |
CH3 |
CH3 |
26.274 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
CH3 |
26.275 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
CH3 |
26.276 |
CN |
CH3 |
4-F(Ph) |
CH3 |
CH3 |
26.277 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
CH3 |
26.278 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
CH3 |
26.279 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
CH3 |
26.280 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
CH3 |
26.281 |
CN |
CH3 |
Ph |
CH3 |
COCH3 |
26.282 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
COCH3 |
26.283 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
COCH3 |
26.284 |
CN |
CH3 |
4-F(Ph) |
CH3 |
COCH3 |
26.285 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
COCH3 |
26.286 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
COCH3 |
26.287 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
COCH3 |
26.288 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
COCH3 |
26.289 |
CN |
CH3 |
Ph |
CH3 |
COPh |
26.290 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
COPh |
26.291 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
COPh |
26.292 |
CN |
CH3 |
4-F(Ph) |
CH3 |
COPh |
26.293 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
COPh |
26.294 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
COPh |
26.295 |
CN |
CH3 |
2,4-F(Ph) |
CH3 |
COPh |
26.296 |
CN |
H |
Ph |
C2H5 |
H |
26.297 |
CN |
H |
2-Cl(Ph) |
正-C3H7 |
H |
26.298 |
CN |
H |
3-Cl(Ph) |
异-C3H7 |
H |
26.299 |
CN |
H |
4-Cl(Ph) |
正-C4H9 |
H |
26.300 |
CN |
H |
4-Br(Ph) |
异-C4H9 |
H |
26.301 |
CN |
H |
4-F(Ph) |
C(CH3)3 |
H |
26.302 |
CN |
H |
4-OCH3(Ph) |
C2H5 |
COCH3 |
26.303 |
CN |
H |
4-CH3(Ph) |
正-C3H7 |
COCH3 |
26.304 |
CN |
H |
4-NO2(Ph) |
异-C3H7 |
COCH3 |
26.305 |
CN |
H |
2.4-Cl(Ph) |
正-C4H9 |
COCH3 |
26.306 |
CN |
H |
2,4-F(Ph) |
异-C4H9 |
COCH3 |
26.307 |
CN |
H |
Ph |
C(CH3)3 |
COCH3 |
26.308 |
CN |
H |
2-Cl(Ph) |
C2H5 |
COPh |
26.309 |
CN |
H |
3-Cl(Ph) |
正-C3H7 |
COPh |
26.310 |
CN |
H |
4-Cl(Ph) |
异-C3H7 |
COPh |
26.311 |
CH3 |
H |
4-Br(Ph) |
正-C4H9 |
COPh |
26.312 |
CH3 |
H |
4-F(Ph) |
异-C4H9 |
COPh |
26.313 |
CH3 |
H |
4-OCH3(Ph) |
C(CH3)3 |
COPh |
本发明式Ⅰ所涵盖的典型化合物包括式Ⅻ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH,Z=NR10且其中R10为NR8R9的式Ⅰ化合物,其中的R2、R3、R7、R8和R9如表27所定义。
表27
化合物 |
R2 |
R3 |
R7 |
R8 |
R9 |
27.1 |
H |
H |
Ph |
CH3 |
H |
27.2 |
H |
H |
4-Cl(Ph) |
CH3 |
H |
27.3 |
H |
H |
4-Br(Ph) |
CH3 |
H |
27.4 |
H |
H |
4-F(Ph) |
CH3 |
H |
27.5 |
H |
H |
4-OCH3(Ph) |
CH3 |
H |
27.6 |
H |
H |
4-CF3(Ph) |
CH3 |
H |
27.7 |
H |
H |
Ph |
CH3 |
CH3 |
27.8 |
H |
H |
4-Cl(Ph) |
CH3 |
CH3 |
27.9 |
H |
H |
4-Br(Ph) |
CH3 |
CH3 |
27.10 |
H |
H |
4-F(Ph) |
CH3 |
CH3 |
27.11 |
CH3 |
H |
Ph |
CH3 |
H |
27.12 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
H |
27.13 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
H |
27.14 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
H |
27.15 |
CH3 |
H |
2-Br(Ph) |
CH3 |
H |
27.16 |
CH3 |
H |
3-Br(Ph) |
CH3 |
H |
27.17 |
CH3 |
H |
4-Br(Ph) |
CH3 |
H |
27.18 |
CH3 |
H |
Ph |
CH3 |
CH3 |
27.19 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
CHx |
27.20 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
CH3 |
27.21 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
CH3 |
27.22 |
CH3 |
H |
2-Br(Ph) |
CH3 |
CH3 |
27.23 |
CH3 |
H |
3-Br(Ph) |
CH3 |
CH3 |
27.24 |
CH3 |
H |
4-Br(Ph) |
CH3 |
CH3 |
27.25 |
CH3 |
H |
2-CH3(Ph) |
CH3 |
CH3 |
27.26 |
CH3 |
H |
3-CH3(Ph) |
CH3 |
CH3 |
27.27 |
CH3 |
H |
2-CF3(Ph) |
CH3 |
CH3 |
27.28 |
CH3 |
H |
3-CF3(Ph) |
CH3 |
CH3 |
27.29 |
CH3 |
H |
4-CF3(PH) |
CH3 |
CH3 |
27.30 |
CH3 |
H |
2-NO2(Ph) |
CH3 |
CH3 |
27.31 |
CH3 |
H |
3-NO2(Ph) |
CH3 |
CH3 |
27.32 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
CH3 |
27.33 |
CH3 |
H |
2,3-Cl(Ph) |
CH3 |
CH3 |
27.34 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
CH3 |
27.35 |
CH3 |
H |
2,5-Cl(Ph) |
CH3 |
CH3 |
27.36 |
CH3 |
H |
2,6-Cl(Ph) |
CH3 |
CH3 |
27.37 |
CH3 |
H |
3,4-Cl(Ph) |
CH3 |
CH3 |
27.38 |
CH3 |
H |
3,5-Cl(Ph) |
CH3 |
CH3 |
27.39 |
CH3 |
H |
Ph |
C2H5 |
CH3 |
27.40 |
CH3 |
H |
Ph |
正-C3H7 |
CH3 |
27.41 |
CH3 |
H |
Ph |
异-C3H7 |
CH3 |
27.42 |
CH3 |
H |
Ph |
正-C4H9 |
CH3 |
27.43 |
CH3 |
H |
Ph |
异-C4H9 |
CH3 |
27.44 |
CH3 |
H |
Ph |
C(CH3)3 |
CH3 |
27.45 |
CH3 |
H |
Ph |
H |
COCH3 |
27.46 |
CH3 |
H |
2-Cl(Ph) |
H |
COCH3 |
27.47 |
CH3 |
H |
3-Cl(Ph) |
H |
COCH3 |
27.48 |
CH3 |
H |
4-Cl(Ph) |
H |
COCH3 |
27.49 |
CH3 |
H |
4-Br(Ph) |
H |
COCH3 |
27.50 |
CH3 |
H |
4-F(Ph) |
H |
COCH3 |
27.51 |
CH3 |
H |
4-OCH3(Ph) |
H |
COCH3 |
27.52 |
CH3 |
H |
4-CH3(Ph) |
H |
COCH3 |
27.53 |
CH3 |
H |
4-NO2(Ph) |
H |
COCH3 |
27.54 |
CH3 |
H |
2,4-Cl(Ph) |
H |
COCH3 |
27.55 |
CH3 |
H |
2,4-F(Ph) |
H |
COCH3 |
27.56 |
CH3 |
H |
Ph |
CH3 |
COCH3 |
27.57 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
COCH3 |
27.58 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
COCH3 |
27.59 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
COCH3 |
27.60 |
CH3 |
H |
4-F(Ph) |
CH3 |
COCH3 |
27.61 |
CH3 |
H |
3-OCH3(Ph) |
CH3 |
COCH3 |
27.62 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
COCH3 |
27.63 |
CH3 |
H |
4-CH3(Ph) |
CH3 |
COCH3 |
27.64 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
COCH3 |
27.65 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
COCH3 |
27.66 |
CH3 |
H |
2.4-F(Ph) |
CH3 |
COCH3 |
27.67 |
CH3 |
H |
Ph |
H |
COPh |
27.68 |
CH3 |
H |
2-Cl(Ph) |
H |
COPh |
27.69 |
CH3 |
H |
3-Cl(Ph) |
H |
COPh |
27.70 |
CH3 |
H |
4-Cl(Ph) |
H |
COPh |
27.71 |
CH3 |
H |
4-Br(Ph) |
H |
COPh |
27.72 |
CH3 |
H |
4-F(Ph) |
H |
COPh |
27.73 |
CH3 |
H |
4-OCH3(Ph) |
H |
COPh |
27.74 |
CH3 |
H |
4-CH3(Ph) |
H |
COPh |
27.75 |
CH3 |
H |
4-NO2(Ph) |
H |
COPh |
27.76 |
CH3 |
H |
2,4-Cl(Ph) |
H |
COPh |
27.77 |
CH3 |
H |
2,4-F(Ph) |
H |
COPh |
27.78 |
CH3 |
H |
Ph |
CH3 |
COPh |
27.79 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
COPh |
27.80 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
COPh |
27.81 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
COPh |
27.82 |
CH3 |
H |
4-Br(Ph) |
CH3 |
COPh |
27.83 |
CH3 |
H |
4-F(Ph) |
CH3 |
COPh |
27.84 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
COPh |
27.85 |
CH3 |
H |
4-CH3(Ph) |
CH3 |
COPh |
27.86 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
COPh |
27.87 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
COPh |
27.88 |
CH3 |
H |
2.4-F(Ph) |
CH3 |
COPh |
27.89 |
C2H5 |
H |
Ph |
H |
COCH3 |
27.90 |
C2H5 |
H |
2-Cl(Ph) |
H |
COCH3 |
27.91 |
C2H5 |
H |
3-Cl(Ph) |
H |
COCH3 |
27.92 |
C2H5 |
H |
4-Cl(Ph) |
H |
COCH3 |
27.93 |
C2H5 |
H |
4-F(Ph) |
H |
COCH3 |
27.94 |
C2H5 |
H |
3-OCH3(Ph) |
H |
COCH3 |
27.95 |
C2H5 |
H |
4-OCH3(Ph) |
H |
COCH3 |
27.96 |
C2H5 |
H |
4-CH3(Ph) |
H |
COCH3 |
27.97 |
C2H5 |
H |
4-NO2(Ph) |
H |
COCH3 |
27.98 |
C2H5 |
H |
2,4-Cl(Ph) |
H |
COCH3 |
27.99 |
C2H5 |
H |
2,4-F(Ph) |
H |
COCH3 |
27.100 |
C2H5 |
H |
Ph |
CH3 |
COCH3 |
27.101 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
COCH3 |
27.102 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
COCH3 |
27.103 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
COCH3 |
27.104 |
C2H5 |
H |
4-F(Ph) |
CH3 |
COCH3 |
27.105 |
C2H5 |
H |
3-OCH3(Ph) |
CH3 |
COCH3 |
27.106 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
COCH3 |
27.107 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
COCH3 |
27.108 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
COCH3 |
27.109 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
COCH3 |
27.110 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
COCH3 |
27.111 |
C2H5 |
H |
Ph |
H |
COPh |
27.112 |
C2H5 |
H |
2-Cl(Ph) |
H |
COPh |
27.113 |
C2H5 |
H |
3-Cl(Ph) |
H |
COPh |
27.114 |
C2H5 |
H |
4-Cl(Ph) |
H |
COPh |
27.115 |
C2H5 |
H |
4-Br(Ph) |
H |
COPh |
27.116 |
C2H5 |
H |
3-OCH3(Ph) |
H |
COPh |
27.117 |
C2H5 |
H |
4-OCH3(Ph) |
H |
COPh |
27.118 |
C2H5 |
H |
4-CH3(Ph) |
H |
COPh |
27.119 |
C2H5 |
H |
4-NO2(Ph) |
H |
COPh |
27.120 |
C2H5 |
H |
2,4-Cl(Ph) |
H |
COPh |
27.121 |
C2H5 |
H |
2,4-F(Ph) |
H |
COPh |
27.122 |
C2H5 |
H |
Ph |
CH3 |
COPh |
27.123 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
COPh |
27.124 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
COPh |
27.125 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
COPh |
27.126 |
C2H5 |
H |
4-Br(Ph) |
CH3 |
COPh |
27.127 |
C2H5 |
H |
4-F(Ph) |
CH3 |
COPh |
27.128 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
COPh |
27.129 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
COPh |
27.130 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
COPh |
27.131 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
COPh |
27.132 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
COPh |
27.133 |
CH3 |
H |
Ph |
C2H5 |
COCH3 |
27.134 |
CH3 |
H |
Ph |
正-C3H7 |
COCH3 |
27.135 |
CH3 |
H |
Ph |
异-C3H7 |
COCH3 |
27.136 |
CH3 |
H |
Ph |
正-C4H9 |
COCH3 |
27.137 |
CH3 |
H |
Ph |
异-C4H9 |
COCH3 |
27.138 |
CH3 |
H |
Ph |
C(CH3)3 |
COCH3 |
27.139 |
CH3 |
H |
4-Cl(Ph) |
C2H5 |
COCH3 |
27.140 |
CH3 |
H |
4-Cl(Ph) |
正-C3H7 |
COCH3 |
27.141 |
CH3 |
H |
4-Cl(Ph) |
异-C3H7 |
COCH3 |
27.142 |
CH3 |
H |
4-Cl(Ph) |
正-C4H9 |
COCH3 |
27.143 |
CH3 |
H |
4-Cl(Ph) |
异-C4H9 |
COCH3 |
27.144 |
CH3 |
H |
4-Cl(Ph) |
C(CH3)3 |
COCH3 |
27.145 |
CH3 |
H |
Ph |
C2H5 |
COPh |
27.146 |
CH3 |
H |
Ph |
正-C3H7 |
COPh |
27.147 |
CH3 |
H |
Ph |
异-C3H7 |
COPh |
27.148 |
CH3 |
H |
Ph |
正-C4H9 |
COPh |
27.149 |
CH3 |
H |
Ph |
C(CH3)3 |
COPh |
27.150 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
COCH2Ph |
27.151 |
CH3 |
H |
4-Br(Ph) |
CH3 |
COCH2Ph |
27.152 |
CH3 |
H |
4-F(Ph) |
CH3 |
COCH2Ph |
27.153 |
CH3 |
H |
4-OCH3(Ph) |
CH3 |
COCH2Ph |
27.154 |
CH3 |
H |
4-CH3(Ph) |
CH3 |
COCH2Ph |
27.155 |
CH3 |
H |
4-NO2(Ph) |
CH3 |
COCH2Ph |
27.156 |
CH3 |
H |
2,4-Cl(Ph) |
CH3 |
COCH2Ph |
27.157 |
CH3 |
H |
2,4-F(Ph) |
CH3 |
COCH2Ph |
27.158 |
CH3 |
H |
4-Cl(Ph) |
C2H5 |
COCH2Ph |
27.159 |
CH3 |
H |
4-Br(Ph) |
正-C3H7 |
COCH2Ph |
27.160 |
CH3 |
H |
4-F(Ph) |
异-C3H7 |
COCH2Ph |
27.161 |
CH3 |
H |
4-OCH3(Ph) |
正-C4H9 |
COCH2Ph |
27.162 |
CH3 |
H |
4-CH3(Ph) |
异-C4H9 |
COCH2Ph |
27.163 |
CH3 |
H |
4-NO2(Ph) |
C(CH3)3 |
COCH2Ph |
27.164 |
Ph |
H |
Ph |
CH3 |
H |
27.165 |
Ph |
H |
2-Cl(Ph) |
CH3 |
H |
27.166 |
Ph |
H |
3-Cl(Ph) |
CH3 |
H |
27.167 |
Ph |
H |
4-Cl(Ph) |
CH3 |
H |
27.168 |
Ph |
H |
4-Br(Ph) |
CH3 |
H |
27.169 |
Ph |
H |
4-F(Ph) |
CH3 |
H |
27.170 |
Ph |
H |
4-OCH3(Ph) |
CH3 |
H |
27.171 |
Ph |
H |
4-CH3(Ph) |
CH3 |
H |
27.172 |
Ph |
H |
4-NO2(Ph) |
CH3 |
H |
27.173 |
Ph |
H |
2,4-Cl(Ph) |
CH3 |
H |
27.174 |
Ph |
H |
Ph |
CH3 |
CH3 |
27.175 |
Ph |
H |
2-Cl(Ph) |
CH3 |
CH3 |
27.176 |
Ph |
H |
3-Cl(Ph) |
CH3 |
CH3 |
27.177 |
Ph |
H |
4-Cl(Ph) |
CH3 |
CH3 |
27.178 |
Ph |
H |
4-Br(Ph) |
CH3 |
CH3 |
27.179 |
Ph |
H |
4-F(Ph) |
CH3 |
CH3 |
27.180 |
CN |
H |
4-Cl(Ph) |
CH3 |
H |
27.181 |
CN |
H |
4-Br(Ph) |
CH3 |
H |
27.182 |
CN |
H |
4-F(Ph) |
CH3 |
H |
27.183 |
CN |
H |
4-OCH3(Ph) |
CH3 |
H |
27.184 |
CN |
H |
4-CH3(Ph) |
CH3 |
H |
27.185 |
CN |
H |
4-NO2(Ph) |
CH3 |
H |
27.186 |
CN |
H |
2,4-Cl(Ph) |
CH3 |
H |
27.187 |
CN |
H |
2,4-F(Ph) |
CH3 |
H |
27.188 |
CN |
H |
4-CF3(Ph) |
CH3 |
H |
27.189 |
CN |
H |
Ph |
CH3 |
CH3 |
27.190 |
CN |
H |
Ph |
CH3 |
COCH3 |
27.191 |
H |
H |
1-萘基 |
CH3 |
H |
27.192 |
H |
H |
1-萘基 |
CH3 |
CH3 |
27.193 |
H |
H |
1-萘基 |
CH3 |
COCH3 |
27.194 |
H |
H |
1-萘基 |
CH3 |
COPh |
27.195 |
CH3 |
H |
1-萘基 |
CH3 |
H |
27.196 |
CH3 |
H |
1-萘基 |
CH3 |
CH3 |
27.197 |
CH3 |
H |
1-萘基 |
CH3 |
COCH3 |
27.198 |
CH3 |
H |
1-萘基 |
CH3 |
COPh |
27.199 |
CH3 |
H |
1-萘基 |
CH3 |
COCH2Ph |
27.200 |
H |
H |
1-萘基 |
CH3 |
CO2CH3 |
27.201 |
CH3 |
H |
1-萘基 |
CH3 |
CO2CH3 |
27.202 |
H |
H |
2-萘基 |
CH3 |
H |
27.203 |
H |
H |
2-萘基 |
CH3 |
CH3 |
27.204 |
H |
H |
2-萘基 |
CH3 |
COCH3 |
27.205 |
H |
H |
2-萘基 |
CH3 |
COPh |
27.206 |
CH3 |
H |
2-萘基 |
CH3 |
H |
27.207 |
CH3 |
H |
2-萘基 |
CH3 |
CH3 |
27.208 |
CH3 |
H |
2-萘基 |
CH3 |
COCH3 |
27.209 |
CH3 |
H |
2-萘基 |
CH3 |
COPh |
27.210 |
CH3 |
H |
2-萘基 |
CH3 |
COCH2Ph |
27.211 |
H |
H |
2-萘基 |
CH3 |
CO2CH3 |
27.212 |
CH3 |
H |
2-萘基 |
CH3 |
CO2CH3 |
27.213 |
H |
CH3 |
Ph |
CH3 |
H |
27.214 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
H |
27.215 |
H |
CH3 |
4-Br(Ph) |
CH3 |
H |
27.216 |
H |
CH3 |
4-F(Ph) |
CH3 |
H |
27.217 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
H |
27.218 |
H |
CH3 |
4-CF3(Ph) |
CH3 |
H |
27.219 |
H |
CH3 |
Ph |
CH3 |
CH3 |
27.220 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
CH3 |
27.221 |
H |
CH3 |
4-Br(Ph) |
CH3 |
CH3 |
27.222 |
H |
CH3 |
4-F(Ph) |
CH3 |
CH3 |
27.223 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
CH3 |
27.224 |
H |
CH3 |
4-CF3(Ph) |
CH3 |
CH3 |
27.225 |
H |
CH3 |
Ph |
CH3 |
C2H5 |
27.226 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
正-C3H7 |
27.227 |
H |
CH3 |
4-Br(Ph) |
CH3 |
异-C3H7 |
27.228 |
H |
CH3 |
4-F(Ph) |
CH3 |
正-C4H9 |
27.229 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
异-C4H9 |
27.230 |
H |
CH3 |
4-CH3(Ph) |
CH3 |
C(CH3)3 |
27.231 |
H |
CH3 |
4-NO2(Ph) |
CH3 |
CH3 |
27.232 |
H |
CH3 |
2,4-Cl(Ph) |
CH3 |
CH3 |
27.233 |
H |
CH3 |
Ph |
CH3 |
COCH3 |
27.234 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
COCH3 |
27.235 |
H |
CH3 |
4-Br(Ph) |
CH3 |
COCH3 |
27.236 |
H |
CH3 |
4-F(Ph) |
CH3 |
COCH3 |
27.237 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
COCH3 |
27.238 |
H |
CH3 |
4-CH3(Ph) |
CH3 |
COCH3 |
27.239 |
H |
CH3 |
4-NO2(Ph) |
CH3 |
COCH3 |
27.240 |
H |
CH3 |
2,4-Cl(Ph) |
CH3 |
COCH3 |
27.241 |
H |
CH3 |
Ph |
CH3 |
COPh |
27.242 |
H |
CH3 |
4-Cl(Ph) |
CH3 |
COPh |
27.243 |
H |
CH3 |
4-Br(Ph) |
CH3 |
COPh |
27.244 |
H |
CH3 |
4-F(Ph) |
CH3 |
COPh |
27.245 |
H |
CH3 |
4-OCH3(Ph) |
CH3 |
COPh |
27.246 |
H |
CH3 |
4-CH3(Ph) |
CH3 |
COPh |
27.247 |
H |
CH3 |
4-NO2(Ph) |
CH3 |
COPh |
27.248 |
H |
CH3 |
2,4-Cl(Ph) |
CH3 |
COPh |
27.249 |
CH3 |
CH3 |
Ph |
CH3 |
H |
27.250 |
CH3 |
CH3 |
4-Cl(Ph) |
CH3 |
H |
27.251 |
CH3 |
CH3 |
4-Br(Ph) |
CH3 |
H |
27.252 |
CH3 |
CH3 |
4-F(Ph) |
CH3 |
H |
27.253 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH3 |
H |
27.254 |
CH3 |
CH3 |
4-CH3(Ph) |
CH3 |
H |
27.255 |
CH3 |
CH3 |
4-NO2(Ph) |
CH3 |
H |
27.256 |
CH3 |
CH3 |
2,4-Cl(Ph) |
CH3 |
H |
27.257 |
CH3 |
CH3 |
Ph |
CH3 |
COCH3 |
27.258 |
CH3 |
CH3 |
4-Cl(Ph) |
CH3 |
COCH3 |
27.259 |
CH3 |
CH3 |
4-Br(Ph) |
CH3 |
COCH3 |
27.260 |
CH3 |
CH3 |
4-F(Ph) |
CH3 |
COCH3 |
27.261 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH3 |
COCH3 |
27.262 |
CH3 |
CH3 |
4-CH3(Ph) |
CH3 |
COCH3 |
27.263 |
CH3 |
CH3 |
4-NO2(Ph) |
CH3 |
COCH3 |
27.264 |
CH3 |
CH3 |
2,4-Cl(Ph) |
CH3 |
COCH3 |
27.265 |
CN |
CH3 |
Ph |
CH3 |
H |
27.266 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
H |
27.267 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
H |
27.268 |
CN |
CH3 |
4-F(Ph) |
CH3 |
H |
27.269 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
H |
27.270 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
H |
27.271 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
H |
27.272 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
H |
27.273 |
CN |
CH3 |
Ph |
CH3 |
CH3 |
27.274 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
CH3 |
27.275 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
CH3 |
27.276 |
CN |
CH3 |
4-F(Ph) |
CH3 |
CH3 |
27.277 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
CH3 |
27.278 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
CH3 |
27.279 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
CH3 |
27.280 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
CH3 |
27.281 |
CN |
CH3 |
Ph |
CH3 |
COCH3 |
27.282 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
COCH3 |
27.283 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
COCH3 |
27.284 |
CN |
CH3 |
4-F(Ph) |
CH3 |
COCH3 |
27.285 |
CN |
CH3 |
4-OCH3(Ph) |
CH3 |
COCH3 |
27.286 |
CN |
CH3 |
4-CH3(Ph) |
CH3 |
COCH3 |
27.287 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
COCH3 |
27.288 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
COCH3 |
27.289 |
CN |
CH3 |
Ph |
CH3 |
COPh |
27.290 |
CN |
CH3 |
4-Cl(Ph) |
CH3 |
COPh |
27.291 |
CN |
CH3 |
4-Br(Ph) |
CH3 |
COPh |
27.292 |
CN |
CH3 |
4-F(Ph) |
CH3 |
COPh |
27.293 |
CN |
CH3 |
4-NO2(Ph) |
CH3 |
COPh |
27.294 |
CN |
CH3 |
2,4-Cl(Ph) |
CH3 |
COPh |
27.295 |
CN |
CH3 |
2,4-F(Ph) |
CH3 |
COPh |
27.296 |
CN |
H |
Ph |
C2H5 |
H |
27.297 |
CN |
H |
2-Cl(Ph) |
正-C3H7 |
H |
27.298 |
CN |
H |
3-Cl(Ph) |
异-C3H7 |
H |
27.299 |
CN |
H |
4-Cl(Ph) |
正-C4H9 |
H |
27.300 |
CN |
H |
4-Br(Ph) |
异-C4H9 |
H |
27.301 |
CN |
H |
4-F(Ph) |
C(CH3)3 |
H |
27.302 |
CN |
H |
4-OCH3(Ph) |
C2H5 |
COCH3 |
27.303 |
CN |
H |
4-CH3(Ph) |
正-C3H7 |
COCH3 |
27.304 |
CN |
H |
4-NO2(Ph) |
异-C3H7 |
COCH3 |
27.305 |
CN |
H |
2,4-Cl(Ph) |
正-C4H9 |
COCH3 |
27.306 |
CN |
H |
2,4-F(Ph) |
异-C4H9 |
COCH3 |
27.307 |
CN |
H |
Ph |
C(CH3)3 |
COCH3 |
27.308 |
CN |
H |
2-Cl(Ph) |
C2H5 |
COPh |
27.309 |
CN |
H |
3-Cl(Ph) |
正-C3H7 |
COPh |
27.310 |
CN |
H |
4-Cl(Ph) |
异-C3H7 |
COPh |
27.311 |
CH3 |
H |
4-Br(Ph) |
正-C4H9 |
COPh |
27.312 |
CH3 |
H |
4-F(Ph) |
异-C4H9 |
COPh |
27.313 |
CH3 |
H |
4-OCH3(Ph) |
C(CH3)3 |
COPh |
表28:化合物28.1-28.226为式Ⅹ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NR10,R10为NHCOCH3的式Ⅰ化合物,且其中的R2、R3和R7如表4所定义。
表29:化合物29.1-29.226为式Ⅺ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NR10,R10为NHCOCH3的式Ⅰ化合物,且其中的R2、R3和R7如表4所定义。
表30:化合物30.1-30.226为式Ⅻ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NR10,R10为NHCOCH3的式Ⅰ化合物,且其中的R2、R3和R7如表4所定义。
表31:化合物31.1-31.221为式Ⅹ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NR10,R10为NHCOC2H5的式Ⅰ化合物,且其中的R2、R3和R7如表7所定义。
表32:化合物32.1-32.221为式Ⅺ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NR10,R10为NHCOC2H5的式Ⅰ化合物,且其中的R2、R3和R7如表7所定义。
表33:化合物33.1-33.221为式Ⅻ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NR10,R10为NHCOC2H5的式Ⅰ化合物,且其中的R2、R3和R7如表7所定义。
表34:化合物34.1-34.139为式Ⅹ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NR10,R10为NHCOPh的式Ⅰ化合物,且其中的R2、R3和R7如表10所定义。
表35:化合物35.1-35.139为式Ⅺ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NR10,R10为NHCOPh的式Ⅰ化合物,且其中的R2、R3和R7如表10所定义。
表36:化合物36.1-36.139为式Ⅻ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NR10,R10为NHCOPh的式Ⅰ化合物,且其中的R2、R3和R7如表10所定义。
本发明式Ⅰ所涵盖的典型化合物包括式Ⅹ化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=CH,Y=O,Z=NR
10的式Ⅰ化合物,且其中的R
2、R
3、R
7和R
10如表37所定义。
表37
化合物 |
R2 |
R3 |
R7 |
R10 |
37.1 |
H |
H |
Ph |
CH3 |
37.2 |
H |
H |
4-Cl(Ph) |
CH3 |
37.3 |
H |
H |
4-Br(Ph) |
CH3 |
37.4 |
H |
H |
4-F(Ph) |
CH3 |
37.5 |
H |
H |
4-OCH3(Ph) |
CH3 |
37.6 |
H |
H |
4-CF3(Ph) |
CH3 |
37.7 |
H |
H |
Ph |
CH3 |
37.8 |
H |
H |
4-Cl(Ph) |
CH3 |
37.9 |
H |
H |
4-Br(Ph) |
CH3 |
37.10 |
H |
H |
4-F(Ph) |
CH3 |
37.1l |
CH3 |
H |
Ph |
CH3 |
37.12 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
37.13 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
37.14 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
37.15 |
CH3 |
H |
2-Br(Ph) |
CH3 |
37.16 |
CH3 |
H |
3-Br(Ph) |
CH3 |
37.17 |
CH3 |
H |
4-Br(Ph) |
CH3 |
37.18 |
CH3 |
H |
Ph |
C2H5 |
37.19 |
CH3 |
H |
2-Cl(Ph) |
C2H5 |
37.20 |
CH3 |
H |
3-Cl(Ph) |
C2H5 |
37.21 |
CH3 |
H |
4-Cl(Ph) |
C2H5 |
37.22 |
CH3 |
H |
2-Br(Ph) |
C2H5 |
37.23 |
CH3 |
H |
3-Br(Ph) |
C2H5 |
37.24 |
CH3 |
H |
4-Br(Ph) |
C2H5 |
37.25 |
CH3 |
H |
2-CH3(Ph) |
C2H5 |
37.26 |
CH3 |
H |
3-CH3(Ph) |
C2H5 |
37.27 |
CH3 |
H |
2-CF3(Ph) |
C2H5 |
37.28 |
CH3 |
H |
3-CF3(Ph) |
C2H5 |
37.29 |
CH3 |
H |
4-CF3(Ph) |
C2H5 |
37.30 |
CH3 |
H |
2-NO2(Ph) |
C2H5 |
37.31 |
CH3 |
H |
3-NO2(Ph) |
C2H5 |
37.32 |
CH3 |
H |
4-NO2(Ph) |
C2H5 |
37.33 |
CH3 |
H |
2,3-Cl(Ph) |
C2H5 |
37.34 |
CH3 |
H |
2,4-Cl(Ph) |
C2H5 |
37.35 |
CH3 |
H |
2,5-Cl(Ph) |
C2H5 |
37.36 |
CH3 |
H |
2,6-Cl(Ph) |
C2H5 |
37.37 |
CH3 |
H |
3,4-Cl(Ph) |
C2H5 |
37.38 |
CH3 |
H |
3,5-Cl(Ph) |
C2H5 |
37.39 |
CH3 |
H |
Ph |
正-C3H7 |
37.40 |
CH3 |
H |
Ph |
异-C3H7 |
37.41 |
CH3 |
H |
Ph |
正-C4H9 |
37.42 |
CH3 |
H |
Ph |
异-C4H9 |
37.43 |
CH3 |
H |
Ph |
C(CH3)3 |
37.44 |
CH3 |
H |
Ph |
CH2CH=CH2 |
37.45 |
CH3 |
H |
Ph |
CH2C-CH |
37.46 |
CH3 |
H |
Ph |
PhCH2 |
37.47 |
CH3 |
CH3 |
Ph |
CH3 |
37.48 |
CH3 |
CH3 |
4-Cl(Ph) |
CH3 |
37.49 |
CH3 |
CH3 |
4-Br(Ph) |
CH3 |
37.50 |
CH3 |
CH3 |
4-F(Ph) |
CH3 |
37.51 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH3 |
37.52 |
CH3 |
CH3 |
4-CH3(Ph) |
CH3 |
37.53 |
CH3 |
CH3 |
4-NO2(Ph) |
CH3 |
37.54 |
CH3 |
CH3 |
2,4-Cl(Ph) |
CH3 |
37.55 |
CH3 |
CH3 |
2,4-F(Ph) |
CH3 |
37.56 |
CH3 |
CH3 |
Ph |
C2H5 |
37.57 |
CH3 |
CH3 |
2-Cl(Ph) |
C2H5 |
37.58 |
CH3 |
CH3 |
3-Cl(Ph) |
C2H5 |
37.59 |
CH3 |
CH3 |
4-Cl(Ph) |
C2H5 |
37.60 |
CH3 |
CH3 |
4-F(Ph) |
C2H5 |
37.61 |
CH3 |
CH3 |
3-OCH3(Ph) |
C2H5 |
37.62 |
CH3 |
CH3 |
4-OCH3(Ph) |
C2H5 |
37.63 |
CH3 |
CH3 |
4-CH3(Ph) |
C2H5 |
37.64 |
CH3 |
CH3 |
4-NO2(Ph) |
C2H5 |
37.65 |
CH3 |
CH3 |
2,4-Cl(Ph) |
C2H5 |
37.66 |
CH3 |
CH3 |
2,4-F(Ph) |
C2H5 |
37.67 |
CH3 |
CH3 |
Ph |
正-C3H7 |
37.68 |
CH3 |
CH3 |
2-Cl(Ph) |
异-C3H7 |
37.69 |
CH3 |
CH3 |
3-Cl(Ph) |
正-C4H9 |
37.70 |
CH3 |
CH3 |
4-Cl(Ph) |
异-C4H9 |
37.71 |
CH3 |
CH3 |
4-Br(Ph) |
仲-C4H9 |
37.72 |
CH3 |
CH3 |
4-F(Ph) |
C(CH3)3 |
37.73 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH2CH=CH2 |
37.74 |
CH3 |
CH3 |
4-CH3(Ph) |
CH2C≡CH |
37.75 |
CH3 |
CH3 |
4-NO2(Ph) |
PhCH2 |
37.76 |
CH3 |
CH3 |
2,4-Cl(Ph) |
PhCH2CH2 |
37.77 |
CH3 |
CH3 |
2,4-F(Ph) |
PhCH2CH2 |
37.78 |
C2H5 |
H |
Ph |
CH3 |
37.79 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
37.80 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
37.81 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
37.82 |
C2H5 |
H |
4-Br(Ph) |
CH3 |
37.83 |
C2H5 |
H |
4-F(Ph) |
CH3 |
37.84 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
37.85 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
37.86 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
37.87 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
37.88 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
37.89 |
C2H5 |
H |
Ph |
C2H5 |
37.90 |
C2H5 |
H |
2-Cl(Ph) |
C2H5 |
37.91 |
C2H5 |
H |
3-Cl(Ph) |
C2H5 |
37.92 |
C2H5 |
H |
4-Cl(Ph) |
C2H5 |
37.93 |
C2H5 |
H |
4-F(Ph) |
C2H5 |
37.94 |
C2H5 |
H |
3-OCH3(Ph) |
C2H5 |
37.95 |
C2H5 |
H |
4-OCH3(Ph) |
C2H5 |
37.96 |
C2H5 |
H |
4-CH3(Ph) |
C2H5 |
37.97 |
C2H5 |
H |
4-NO2(Ph) |
C2H5 |
37.98 |
C2H5 |
H |
2,4-Cl(Ph) |
C2H5 |
37.99 |
C2H5 |
H |
2,4-F(Ph) |
C2H5 |
37.100 |
C2H5 |
H |
Ph |
正-C3H7 |
37.101 |
C2H5 |
H |
2-Cl(Ph) |
异-C3H7 |
37.102 |
C2H5 |
H |
3-Cl(Ph) |
正-C4H9 |
37.103 |
C2H5 |
H |
4-Cl(Ph) |
异-C4H9 |
37.104 |
C2H5 |
H |
4-F(Ph) |
仲-C4H9 |
37.105 |
C2H5 |
H |
3-OCH3(Ph) |
C(CH3)3 |
37.106 |
C2H5 |
H |
4-OCH3(Ph) |
CH2CH=CH2 |
37.107 |
C2H5 |
H |
4-CH3(Ph) |
CH2C≡CH |
37.108 |
C2H5 |
H |
4-NO2(Ph) |
PhCH2 |
37.109 |
C2H5 |
H |
2,4-Cl(Ph) |
PhCH2CH2 |
37.110 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
37.111 |
正-C3H7 |
H |
Ph |
CH3 |
37.112 |
正-C3H7 |
H |
2-Cl(Ph) |
CH3 |
37.113 |
正-C3H7 |
H |
3-Cl(Ph) |
CH3 |
37.114 |
正-C3H7 |
H |
4-Cl(Ph) |
CH3 |
37.115 |
正-C3H7 |
H |
4-Br(Ph) |
CH3 |
37.116 |
正-C3H7 |
H |
3-OCH3(Ph) |
CH3 |
37.117 |
正-C3H7 |
H |
4-OCH3(Ph) |
CH3 |
37.118 |
正-C3H7 |
H |
4-CH3(Ph) |
CH3 |
37.119 |
正-C3H7 |
H |
4-NO2(Ph) |
CH3 |
37.120 |
正-C3H7 |
H |
2,4-Cl(Ph) |
CH3 |
37.121 |
正-C3H7 |
H |
2,4-F(Ph) |
CH3 |
37.122 |
正-C3H7 |
H |
Ph |
C2H5 |
37.123 |
正-C3H7 |
H |
2-Cl(Ph) |
C2H5 |
37.124 |
正-C3H7 |
H |
3-Cl(Ph) |
C2H5 |
37.125 |
正-C3H7 |
H |
4-Cl(Ph) |
C2H5 |
37.126 |
正-C3H7 |
H |
4-Br(Ph) |
C2H5 |
37.127 |
正-C3H7 |
H |
4-F(Ph) |
C2H5 |
37.128 |
正-C3H7 |
H |
4-OCH3(Ph) |
C2H5 |
37.129 |
正-C3H7 |
H |
4-CH3(Ph) |
C2H5 |
37.130 |
正-C3H7 |
H |
4-NO2(Ph) |
C2H5 |
37.131 |
正-C3H7 |
H |
2,4-Cl(Ph) |
C2H5 |
37.132 |
正-C3H7 |
H |
2,4-F(Ph) |
C2H5 |
37.133 |
正-C3H7 |
H |
Ph |
正-C3H7 |
37.134 |
正-C3H7 |
H |
Ph |
异-C3H7 |
37.135 |
正-C3H7 |
H |
Ph |
正-C4H9 |
37.136 |
正-C3H7 |
H |
Ph |
异-C4H9 |
37.137 |
正-C3H7 |
H |
Ph |
C(CH3)3 |
37.138 |
正-C3H7 |
H |
Ph |
CH2CH=CH2 |
37.139 |
正-C3H7 |
H |
Ph |
CH2C≡CH |
37.140 |
正-C3H7 |
H |
Ph |
PhCH2 |
37.141 |
正-C3H7 |
H |
Ph |
PhCH2CH2 |
37.142 |
异-C3H7 |
H |
Ph |
C2H5 |
37.143 |
异-C3H7 |
H |
Ph |
正-C3H7 |
37.144 |
异-C3H7 |
H |
Ph |
异-C3H7 |
37.145 |
异-C3H7 |
H |
Ph |
正-C4H9 |
37.146 |
异-C3H7 |
H |
Ph |
异-C4H9 |
37.147 |
异-C3H7 |
H |
Ph |
C(CH3)3 |
37.148 |
异-C3H7 |
H |
Ph |
CH2CH=CH2 |
37.149 |
异-C3H7 |
H |
Ph |
CH2C≡CH |
37.150 |
异-C3H7 |
H |
Ph |
PhCH2 |
37.151 |
异-C3H7 |
H |
Ph |
PhCH2CH2 |
37.152 |
环丙基 |
H |
Ph |
CH3 |
37.153 |
环丙基 |
H |
2-Cl(Ph) |
CH3 |
37.154 |
环丙基 |
H |
3-Cl(Ph) |
CH3 |
37.155 |
环丙基 |
H |
4-Cl(Ph) |
CH3 |
37.156 |
环丙基 |
H |
4-Br(Ph) |
CH3 |
37.157 |
环丙基 |
H |
4-F(Ph) |
CH3 |
37.158 |
环丙基 |
H |
4-OCH3(Ph) |
CH3 |
37.159 |
环丙基 |
H |
4-CH3(Ph) |
CH3 |
37.160 |
环丙基 |
H |
4-NO2(Ph) |
CH3 |
37.161 |
环丙基 |
H |
2,4-Cl(Ph) |
CH3 |
37.162 |
环丙基 |
H |
2,4-F(Ph) |
CH3 |
37.163 |
环丙基 |
H |
3,4-F(Ph) |
CH3 |
37.164 |
Ph |
H |
Ph |
CH3 |
37.165 |
Ph |
H |
2-Cl(Ph) |
C2H5 |
37.166 |
Ph |
H |
3-Cl(Ph) |
正-C3H7 |
37.167 |
Ph |
H |
4-C(Ph) |
异-C3H7 |
37.168 |
Ph |
H |
4-Br(Ph) |
正-C4H9 |
37.169 |
Ph |
H |
4-F(Ph) |
异-C4H9 |
37.170 |
Ph |
H |
4-OCH3(Ph) |
C(CH3)3 |
37.171 |
Ph |
H |
4-CH3(Ph) |
CH2CH=CH2 |
37.172 |
Ph |
H |
4-NO2(Ph) |
CH2C≡CH |
37.173 |
PH |
H |
2,4-Cl(Ph) |
PhCH2 |
37.174 |
CN |
H |
Ph |
CH3 |
37.175 |
CN |
H |
2-Cl(Ph) |
CH3 |
37.176 |
CN |
H |
3-Cl(Ph) |
CH3 |
37.177 |
CN |
H |
4-Cl(Ph) |
CH3 |
37.178 |
CN |
H |
4-Br(Ph) |
CH3 |
37.179 |
CN |
H |
4-F(Ph) |
CH3 |
37.180 |
CN |
H |
4-Cl(Ph) |
CH3 |
37.181 |
CN |
H |
4-Br(Ph) |
CH3 |
37.182 |
CN |
H |
4-F(Ph) |
CH3 |
37.183 |
CN |
H |
4-OCH3(Ph) |
CH3 |
37.184 |
CN |
H |
4-CH3(Ph) |
CH3 |
37.185 |
CN |
H |
4-NO2(Ph) |
CH3 |
37.186 |
CN |
H |
2,4-Cl(Ph) |
CH3 |
37.187 |
CN |
H |
2,4-F(Ph) |
CH3 |
37.188 |
CN |
H |
4-CF3(Ph) |
CH3 |
37.189 |
CN |
H |
Ph |
C2H5 |
37.190 |
CN |
H |
Ph |
正-C3H7 |
37.191 |
CN |
H |
Ph |
异-C3H7 |
37.192 |
CN |
H |
Ph |
正-C4H9 |
37.193 |
CN |
H |
Ph |
异-C4H9 |
37.194 |
CN |
H |
Ph |
C(CH3)3 |
37.195 |
CN |
H |
Ph |
CH2CH=CH2 |
37.196 |
CN |
H |
Ph |
CH2C≡CH |
37.197 |
CN |
H |
Ph |
PhCH2 |
37.198 |
CH3 |
H |
1-萘基 |
CH3 |
37.199 |
CH3 |
H |
1-萘基 |
C2H5 |
37.200 |
CH3 |
H |
1-萘基 |
正-C3H7 |
37.201 |
CH3 |
H |
1-萘基 |
异-C3H7 |
37.202 |
CH3 |
H |
1-萘基 |
正-C4H9 |
37.203 |
CH3 |
H |
1-萘基 |
异-C4H9 |
37.204 |
CH3 |
H |
1-萘基 |
C(CH3)3 |
37.205 |
CH3 |
H |
1-萘基 |
CH2CH=CH2 |
37.206 |
CH3 |
H |
1-萘基 |
CH2C≡CH |
37.207 |
CH3 |
H |
1-萘基 |
PhCH2 |
37.208 |
CH3 |
H |
2-萘基 |
CH3 |
37.209 |
CH3 |
H |
2-萘基 |
C2H5 |
37.210 |
CH3 |
H |
2-萘基 |
正-C3H7 |
37.211 |
CH3 |
H |
2-萘基 |
异-C3H7 |
37.212 |
CH3 |
H |
2-萘基 |
正-C4H9 |
37.213 |
CH3 |
H |
2-萘基 |
异-C4H9 |
37.214 |
CH3 |
H |
2-萘基 |
C(CH3)3 |
37.215 |
CH3 |
H |
2-萘基 |
CH2CH=CH2 |
37.216 |
CH3 |
H |
2-萘基 |
CH2C≡CH |
37.217 |
CH3 |
H |
2-萘基 |
PhCH2 |
37.218 |
CN |
H |
1-萘基 |
CH3 |
37.219 |
CN |
H |
1-萘基 |
C2H5 |
37.220 |
CN |
H |
1-萘基 |
正-C3H7 |
37.221 |
CN |
H |
1-萘基 |
异-C3H7 |
37.222 |
CN |
H |
1-萘基 |
正-C4H9 |
37.223 |
CN |
H |
1-萘基 |
异-C4H9 |
37.224 |
CN |
H |
1-萘基 |
C(CH3)3 |
37.225 |
CN |
H |
1-萘基 |
CH2CH=CH2 |
37.226 |
CN |
H |
1-萘基 |
CH2C≡CH |
37.227 |
CN |
H |
1-萘基 |
PhCH2 |
37.228 |
CN |
H |
2-萘基 |
CH3 |
37.229 |
CN |
H |
2-萘基 |
C2H5 |
37.230 |
CN |
H |
2-萘基 |
正-C3H7 |
37.231 |
CN |
H |
2-萘基 |
异-C3H7 |
37.232 |
CN |
H |
2-萘基 |
正-C4H9 |
37.233 |
CN |
H |
2-萘基 |
异-C4H9 |
37.234 |
CN |
H |
2-萘基 |
C(CH3)3 |
37.235 |
CN |
H |
2-萘基 |
CH2CH=CH2 |
37.236 |
CN |
H |
2-萘基 |
CH2C≡CH |
37.237 |
CN |
H |
2-萘基 |
PhCH2 |
37.238 |
CH3 |
CH3 |
1-萘基 |
CH3 |
37.239 |
CH3 |
CH3 |
1-萘基 |
C2H5 |
37.240 |
CH3 |
CH3 |
1-萘基 |
正-C3H7 |
37.24l |
CH3 |
CH3 |
1-萘基 |
异-C3H7 |
37.242 |
CH3 |
CH3 |
1-萘基 |
正-C4H9 |
37.243 |
CH3 |
CH3 |
1-萘基 |
异-C4H9 |
37.244 |
CH3 |
CH3 |
1-萘基 |
C(CH3)3 |
37.245 |
CH3 |
CH3 |
1-萘基 |
CH2CH=CH2 |
37.246 |
CH3 |
CH3 |
1-萘基 |
CH2C≡CH |
37.247 |
CH3 |
CH3 |
1-萘基 |
PhCH2 |
37.248 |
CH3 |
CH3 |
2-萘基 |
CH3 |
37.249 |
CH3 |
CH3 |
2-萘基 |
C2H5 |
37.250 |
CH3 |
CH3 |
2-萘基 |
正-C3H7 |
37.251 |
CH3 |
CH3 |
2-萘基 |
异-C3H7 |
37.252 |
CH3 |
CH3 |
2-萘基 |
正-C4H9 |
37.253 |
CH3 |
CH3 |
2-萘基 |
异-C4H9 |
37.254 |
CH3 |
CH3 |
2-萘基 |
C(CH3)3 |
37.255 |
CH3 |
CH3 |
2-萘基 |
CH2CH=CH2 |
37.256 |
CH3 |
CH3 |
2-萘基 |
CH2C≡CH |
37.257 |
CH3 |
CH3 |
2-萘基 |
PhCH2 |
37.258 |
CN |
CH3 |
1-萘基 |
CH3 |
37.259 |
CN |
CH3 |
1-萘基 |
C2H5 |
37.260 |
CN |
CH3 |
1-萘基 |
正-C3H7 |
37.261 |
CN |
CH3 |
1-萘基 |
异-C3H7 |
37.262 |
CN |
CH3 |
1-萘基 |
正-C4H9 |
37.263 |
CN |
CH3 |
1-萘基 |
异-C4H9 |
37.264 |
CN |
CH3 |
1-萘基 |
C(CH3)3 |
37.265 |
CN |
CH3 |
1-萘基 |
CH2CH=CH2 |
37.266 |
CN |
CH3 |
1-萘基 |
CH2C≡CH |
37.267 |
CN |
CH3 |
1-萘基 |
PhCH2 |
37.268 |
CN |
CH3 |
2-萘基 |
CH3 |
37.269 |
CN |
CH3 |
2-萘基 |
C2H5 |
37.270 |
CN |
CH3 |
2-萘基 |
正-C3H7 |
37.271 |
CN |
CH3 |
2-萘基 |
异-C3H7 |
37.272 |
CN |
CH3 |
2-萘基 |
正-C4H9 |
本发明式Ⅰ所涵盖的典型化合物包括式Ⅺ化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=N,Y=O,Z=NR
10的式Ⅰ化合物,且其中的R
2、R
3、R
7和R
10如表38所定义。
表38
化合物 |
R2 |
R3 |
R7 |
R10 |
38.1 |
H |
H |
Ph |
CH3 |
38.2 |
H |
H |
4-Cl(Ph) |
CH3 |
38.3 |
H |
H |
4-Br(Ph) |
CH3 |
38.4 |
H |
H |
4-F(Ph) |
CH3 |
38.5 |
H |
H |
4-OCH3(Ph) |
CH3 |
38.6 |
H |
H |
4-CF3(Ph) |
CH3 |
38.7 |
H |
H |
Ph |
CH3 |
38.8 |
H |
H |
4-Cl(Ph) |
CH3 |
38.9 |
H |
H |
4-Br(Ph) |
CH3 |
38.10 |
H |
H |
4-F(Ph) |
CH3 |
38.11 |
CH3 |
H |
Ph |
CH3 |
38.12 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
38.13 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
38.14 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
38.15 |
CH3 |
H |
2-Br(Ph) |
CH3 |
38.16 |
CH3 |
H |
3-Br(Ph) |
CH3 |
38.17 |
CH3 |
H |
4-Br(Ph) |
CH3 |
38.18 |
CH3 |
H |
Ph |
C2H5 |
38.19 |
CH3 |
H |
2-Cl(Ph) |
C2H5 |
38.20 |
CH3 |
H |
3-Cl(Ph) |
C2H5 |
38.21 |
CH3 |
H |
4-Cl(Ph) |
C2H5 |
38.22 |
CH3 |
H |
2-Br(Ph) |
C2H5 |
38.23 |
CH3 |
H |
3-Br(Ph) |
C2H5 |
38.24 |
CH3 |
H |
4-Br(Ph) |
C2H5 |
38.25 |
CH3 |
H |
2-CH3(Ph) |
C2H5 |
38.26 |
CH3 |
H |
3-CH3(Ph) |
C2H5 |
38.27 |
CH3 |
H |
2-CF3(Ph) |
C2H5 |
38.28 |
CH3 |
H |
3-CF3(Ph) |
C2H5 |
38.29 |
CH3 |
H |
4-CF3(Ph) |
C2H5 |
38.30 |
CH3 |
H |
2-NO2(Ph) |
C2H5 |
38.31 |
CH3 |
H |
3-NO2(Ph) |
C2H5 |
38.32 |
CH3 |
H |
4-NO2(Ph) |
C2H5 |
38.33 |
CH3 |
H |
2,3-Cl(Ph) |
C2H5 |
38.34 |
CH3 |
H |
2,4-Cl(Ph) |
C2H5 |
38.35 |
CH3 |
H |
2,5-Cl(Ph) |
C2H5 |
38.36 |
CH3 |
H |
2,6-Cl(Ph) |
C2H5 |
38.37 |
CH3 |
H |
3,4-Cl(Ph) |
C2H5 |
38.38 |
CH3 |
H |
3,5-Cl(Ph) |
C2H5 |
38.39 |
CH3 |
H |
Ph |
正-C3H7 |
38.40 |
CH3 |
H |
Ph |
异-C3H7 |
38.41 |
CH3 |
H |
Ph |
正-C4H9 |
38.42 |
CH3 |
H |
Ph |
异-C4H9 |
38.43 |
CH3 |
H |
Ph |
C(CH3)3 |
33.44 |
CH3 |
H |
Ph |
CH2CH=CH2 |
38.45 |
CH3 |
H |
Ph |
CH2C≡CH |
38.46 |
CH3 |
H |
Ph |
PhCH2 |
38.47 |
CH3 |
CH3 |
Ph |
CH3 |
38.48 |
CH3 |
CH3 |
4-Cl(Ph) |
CH3 |
38.49 |
CH3 |
CH3 |
4-Br(Ph) |
CH3 |
38.50 |
CH3 |
CH3 |
4-F(Ph) |
CH3 |
38.51 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH3 |
38.52 |
CH3 |
CH3 |
4-CH3(Ph) |
CH3 |
38.53 |
CH3 |
CH3 |
4-NO2(Ph) |
CH3 |
38.54 |
CH3 |
CH3 |
2,4-Cl(Ph) |
CH3 |
38.55 |
CH3 |
CH3 |
2,4-F(Ph) |
CH3 |
38.56 |
CH3 |
CH3 |
Ph |
C2H5 |
38.57 |
CH3 |
CH3 |
2-Cl(Ph) |
C2H5 |
38.58 |
CH3 |
CH3 |
3-Cl(Ph) |
C2H5 |
38.59 |
CH3 |
CH3 |
4-Cl(Ph) |
C2H5 |
38.60 |
CH3 |
CH3 |
4-F(Ph) |
C2H5 |
38.61 |
CH3 |
CH3 |
3-OCH3(Ph) |
C2H5 |
38.62 |
CH3 |
CH3 |
4-OCH3(Ph) |
C2H5 |
38.63 |
CH3 |
CH3 |
4-CH3(Ph) |
C2H5 |
38.64 |
CH3 |
CH3 |
4-NO2(Ph) |
C2H5 |
38.65 |
CH3 |
CH3 |
2,4-Cl(Ph) |
C2H5 |
38.66 |
CH3 |
CH3 |
2,4-F(Ph) |
C2H5 |
38.67 |
CH3 |
CH3 |
Ph |
正-C3H7 |
38.68 |
CH3 |
CH3 |
2-Cl(Ph) |
异-C3H7 |
38.69 |
CH3 |
CH3 |
3-Cl(Ph) |
正-C4H9 |
38.70 |
CH3 |
CH3 |
4-Cl(Ph) |
异-C4H9 |
38.71 |
CH3 |
CH3 |
4-Br(Ph) |
仲-C4H9 |
38.72 |
CH3 |
CH3 |
4-F(Ph) |
C(CH3)3 |
38.73 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH2CH=CH2 |
38.74 |
CH3 |
CH3 |
4-CH3(Ph) |
CH2C≡CH |
38.75 |
CH3 |
CH3 |
4-NO2(Ph) |
PhCH2 |
38.76 |
CH3 |
CH3 |
2,4-Cl(Ph) |
PhCH2CH2 |
38.77 |
CH3 |
CH3 |
2,4-F(Ph) |
PhCH2CH2 |
38.78 |
C2H5 |
H |
Ph |
CH3 |
38.79 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
38.80 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
38.81 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
38.82 |
C2H5 |
H |
4-Br(Ph) |
CH3 |
38.83 |
C2H5 |
H |
4-F(Ph) |
CH3 |
38.84 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
38.85 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
38.86 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
38.87 |
C2H5 |
H |
2,7-Cl(Ph) |
CH3 |
38.88 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
38.89 |
C2H5 |
H |
Ph |
C2H5 |
38.90 |
C2H5 |
H |
2-C(Ph) |
C2H5 |
38.91 |
C2H5 |
H |
3-Cl(Ph) |
C2H5 |
38.92 |
C2H5 |
H |
4-Cl(Ph) |
C2H5 |
38.93 |
C2H5 |
H |
4-F(Ph) |
C2H5 |
38.94 |
C2H5 |
H |
3-OCH3(Ph) |
C2H5 |
38.95 |
C2H5 |
H |
4-OCH3(Ph) |
C2H5 |
38.96 |
C2H5 |
H |
4-CH3(Ph) |
C2H5 |
38.97 |
C2H5 |
H |
4-NO2(Ph) |
C2H5 |
38.98 |
C2H5 |
H |
2,4-Cl(Ph) |
C2H5 |
38.99 |
C2H5 |
H |
2,4-F(Ph) |
C2H5 |
38.100 |
C2H5 |
H |
Ph |
正-C3H7 |
38.101 |
C2H5 |
H |
2-Cl(Ph) |
异-C3H7 |
38.102 |
C2H5 |
H |
3-Cl(Ph) |
正-C4H9 |
38.103 |
C2H5 |
H |
4-Cl(Ph) |
异-C4H9 |
38.104 |
C2H5 |
H |
4-F(Ph) |
仲-C4H9 |
38.105 |
C2H5 |
H |
3-OCH3(Ph) |
C(CH3)3 |
38.106 |
C2H5 |
H |
4-OCH3(Ph) |
CH2CH=CH2 |
38.107 |
C2H5 |
H |
4-CH3(Ph) |
CH2C≡CH |
38.108 |
C2H5 |
H |
4-NO2(Ph) |
PhCH2 |
38.109 |
C2H5 |
H |
2,4-Cl(Ph) |
PhCH2CH2 |
38.110 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
38.111 |
正-C3H7 |
H |
Ph |
CH3 |
38.112 |
正-C3H7 |
H |
2-Cl(Ph) |
CH3 |
38.113 |
正-C3H7 |
H |
3-Cl(Ph) |
CH3 |
38.114 |
正-C3H7 |
H |
4-Cl(Ph) |
CH3 |
38.115 |
正-C3H7 |
H |
4-Br(Ph) |
CH3 |
38.116 |
正-C3H7 |
H |
3-OCH3(Ph) |
CH3 |
38117 |
正-C3H7 |
H |
4-OCH3(Ph) |
CH3 |
38.118 |
正-C3H7 |
H |
4-CH3(Ph) |
CH3 |
38.119 |
正-C3H7 |
H |
4-NO2(Ph) |
CH3 |
38.120 |
正-C3H7 |
H |
2,4-Cl(Ph) |
CH3 |
38.12l |
正-C3H7 |
H |
2,4-F(Ph) |
CH3 |
38.122 |
正-C3H7 |
H |
Ph |
C2H5 |
38.123 |
正-C3H7 |
H |
2-Cl(Ph) |
C2H5 |
38.124 |
正-C3H7 |
H |
3-Cl(Ph) |
C2H5 |
38.125 |
正-C3H7 |
H |
4-Cl(Ph) |
C2H5 |
38.126 |
正-C3H7 |
H |
4-Br(Ph) |
C2H5 |
38.127 |
正-C3H7 |
H |
4-F(Ph) |
C2H5 |
38.128 |
正-C3H7 |
H |
4-OCH3(Ph) |
C2H5 |
38.129 |
正-C3H7 |
H |
4-CH3(Ph) |
C2H5 |
38.130 |
正-C3H7 |
H |
4-NO2(Ph) |
C2H5 |
38.131 |
正-C3H7 |
H |
2,4-Cl(Ph) |
C2H5 |
38.132 |
正-C3H7 |
H |
2,4-F(Ph) |
C2H5 |
38.133 |
正-C3H7 |
H |
Ph |
正-C3H7 |
38.134 |
正-C3H7 |
H |
Ph |
异-C3H7 |
38.135 |
正-C3H7 |
H |
Ph |
正-C4H9 |
38.136 |
正-C3H7 |
H |
Ph |
异-C4H9 |
38.137 |
正-C3H7 |
H |
Ph |
C(CH3)3 |
38.138 |
正-C3H7 |
H |
Ph |
CH2CH=CH2 |
38.139 |
正-C3H7 |
H |
Ph |
CH2C≡CH |
38.140 |
正-C3H7 |
H |
Ph |
PhCH2 |
38.141 |
正-C3H7 |
H |
Ph |
PhCH2CH2 |
38.142 |
异-C3H7 |
H |
Ph |
C2H5 |
38.143 |
异-C3H7 |
H |
Ph |
正-C3H7 |
38.144 |
异-C3H7 |
H |
Ph |
异-C3H7 |
38.145 |
异-C3H7 |
H |
Ph |
正-C4H9 |
38.146 |
异-C3H7 |
H |
Ph |
异-C4H9 |
38.147 |
异-C3H7 |
H |
Ph |
C(CH3)3 |
38.148 |
异-C3H7 |
H |
Ph |
CH2CH=CH2 |
38.149 |
异-C3H7 |
H |
Ph |
CH2C≡CH |
38.150 |
异-C3H7 |
H |
Ph |
PhCH2 |
38.151 |
异-C3H7 |
H |
Ph |
PhCH2CH2 |
38.152 |
环丙基 |
H |
4-F(Ph) |
CH3 |
38.153 |
环丙基 |
H |
4-OCH3(Ph) |
CH3 |
38.154 |
环丙基 |
H |
4-CH3(Ph) |
CH3 |
38.155 |
环丙基 |
H |
4-NO2(Ph) |
CH3 |
38.156 |
环丙基 |
H |
2,4-Cl(Ph) |
CH3 |
38.157 |
环丙基 |
H |
2,4-F(Ph) |
CH3 |
38.158 |
环丙基 |
H |
4-Cl(Ph) |
CH3 |
38.159 |
环丙基 |
H |
4-Br(Ph) |
CH3 |
38.160 |
环丙基 |
H |
4-F(Ph) |
CH3 |
38.161 |
环丙基 |
H |
4-OCH3(Ph) |
CH3 |
38.162 |
环丙基 |
H |
4-CH3(Ph) |
CH3 |
38.163 |
环丙基 |
H |
4-NO2(Ph) |
CH3 |
38.164 |
Ph |
H |
Ph |
CH3 |
38.165 |
Ph |
H |
2-Cl(Ph) |
C2H5 |
38.166 |
Ph |
H |
3-Cl(Ph) |
正-C3H7 |
38.167 |
Ph |
H |
4-Cl(Ph) |
异-C3H7 |
38.168 |
Ph |
H |
4-Br(Ph) |
正-C4H9 |
38.169 |
Ph |
H |
4-F(Ph) |
异-C4H9 |
38.170 |
Ph |
H |
4-OCH3(Ph) |
C(CH3)3 |
38.171 |
Ph |
H |
4-CH3(Ph) |
CH2CH=CH2 |
38.172 |
Ph |
H |
4-NO2(Ph) |
CH2C≡CH |
38.173 |
Ph |
H |
2,4-Cl(Ph) |
PhCH2 |
38.174 |
CN |
H |
Ph |
CH3 |
38.175 |
CN |
H |
2-Cl(Ph) |
CH3 |
38.176 |
CN |
H |
3-Cl(Ph) |
CH3 |
38.177 |
CN |
H |
4-Cl(Ph) |
CH3 |
38.178 |
CN |
H |
4-Br(Ph) |
CH3 |
38.179 |
CN |
H |
4-F(Ph) |
CH3 |
38.180 |
CN |
H |
4-Cl(Ph) |
CH3 |
38.181 |
CN |
H |
4-Br(Ph) |
CH3 |
38.182 |
CN |
H |
4-F(Ph) |
CH3 |
38.183 |
CN |
H |
4-OCH3(Ph) |
CH3 |
38.184 |
CN |
H |
4-CH3(Ph) |
CH3 |
38.185 |
CN |
H |
4-NO2(Ph) |
CH3 |
38.186 |
CN |
H |
2,4-Cl(Ph) |
CH3 |
38.187 |
CN |
H |
2,4-F(Ph) |
CH3 |
38.188 |
CN |
H |
4-CF3(Ph) |
CH3 |
38.189 |
CN |
H |
Ph |
C2H5 |
38.190 |
CN |
H |
Ph |
正-C3H7 |
38.191 |
CN |
H |
Ph |
异-C3H7 |
38.192 |
CN |
H |
Ph |
正-C4H9 |
38.193 |
CN |
H |
Ph |
异-C4H9 |
38.194 |
CN |
H |
Ph |
C(CH3)3 |
38.195 |
CN |
H |
Ph |
CH2CH=CH2 |
38.196 |
CN |
H |
Ph |
CH2C≡CH |
38.197 |
CN |
H |
Ph |
PhCH2 |
38.198 |
CH3 |
H |
1-萘基 |
CH3 |
38.199 |
CH3 |
H |
1-萘基 |
C2H5 |
38.200 |
CH3 |
H |
1-萘基 |
正-C3H7 |
38.201 |
CH3 |
H |
1-萘基 |
异-C3H7 |
38.202 |
CH3 |
H |
1-萘基 |
正-C4H9 |
38.203 |
CH3 |
H |
1-萘基 |
异-C4H9 |
38.204 |
CH3 |
H |
1-萘基 |
C(CH3)3 |
38.205 |
CH3 |
H |
1-萘基 |
CH2CH=CH2 |
38.206 |
CH3 |
H |
1-萘基 |
CH2C≡CH |
38.207 |
CH3 |
H |
1-萘基 |
PhCH2 |
38.208 |
CH3 |
H |
2-萘基 |
CH3 |
38.209 |
CH3 |
H |
2-萘基 |
C2H5 |
38.210 |
CH3 |
H |
2-萘基 |
正-C3H7 |
38.211 |
CH3 |
H |
2-萘基 |
异-C3H7 |
38.212 |
CH3 |
H |
2-萘基 |
正-C4H9 |
38.213 |
CH3 |
H |
2-萘基 |
异-C4H9 |
38.214 |
CH3 |
H |
2-萘基 |
C(CH3)3 |
38.215 |
CH3 |
H |
2-萘基 |
CH2CH=CH2 |
38.216 |
CH3 |
H |
2-萘基 |
CH2C≡CH |
38.217 |
CH3 |
H |
2-萘基 |
PhCH2 |
38.218 |
CN |
H |
1-萘基 |
CH3 |
38.219 |
CN |
H |
1-萘基 |
C2H5 |
38.220 |
CN |
H |
1-萘基 |
正-C3H7 |
38.221 |
CN |
H |
1-萘基 |
异-C3H7 |
38.222 |
CN |
H |
1-萘基 |
正-C4H9 |
38.223 |
CN |
H |
1-萘基 |
异-C4H9 |
38.224 |
CN |
H |
1-萘基 |
C(CH3)3 |
38.225 |
CN |
H |
1-萘基 |
CH2CH=CH2 |
38.226 |
CN |
H |
1-萘基 |
CH2C≡CH |
38.227 |
CN |
H |
1-萘基 |
PhCH2 |
38.228 |
CN |
H |
2-萘基 |
CH3 |
38.229 |
CN |
H |
2-萘基 |
C2H5 |
38.230 |
CN |
H |
2-萘基 |
正-C3H7 |
38.231 |
CN |
H |
2-萘基 |
异-C3H7 |
38.232 |
CN |
H |
2-萘基 |
正-C4H9 |
38.233 |
CN |
H |
2-萘基 |
异-C4H9 |
38.234 |
CN |
H |
2-萘基 |
C(CH3)3 |
38.235 |
CN |
H |
2-萘基 |
CH2CH=CH2 |
38.236 |
CN |
H |
2-萘基 |
CH2C≡CH |
38.237 |
CN |
H |
2-萘基 |
PhCH2 |
38.238 |
CH3 |
CH3 |
1-萘基 |
CH3 |
38.239 |
CH3 |
CH3 |
1-萘基 |
C2H5 |
38.240 |
CH3 |
CH3 |
1-萘基 |
正-C3H7 |
38.241 |
CH3 |
CH3 |
1-萘基 |
异-C3H7 |
38.242 |
CH3 |
CH3 |
1-萘基 |
正-C4H9 |
38.243 |
CH3 |
CH3 |
1-萘基 |
异-C4H9 |
38.244 |
CH3 |
CH3 |
1-萘基 |
C(CH3)3 |
38.245 |
CH3 |
CH3 |
1-萘基 |
CH2CH=CH2 |
38.246 |
CH3 |
CH3 |
1-萘基 |
CH2C≡CH |
38.247 |
CH3 |
CH3 |
1-萘基 |
PhCH2 |
38.248 |
CH3 |
CH3 |
2-萘基 |
CH3 |
38.249 |
CH3 |
CH3 |
2-萘基 |
C2H5 |
38.250 |
CH3 |
CH3 |
2-萘基 |
正-C3H7 |
38.251 |
CH3 |
CH3 |
2-萘基 |
异-C3H7 |
38.252 |
CH3 |
CH3 |
2-萘基 |
正-C4H9 |
38.253 |
CH3 |
CH3 |
2-萘基 |
异-C4H9 |
38.254 |
CH3 |
CH3 |
2-萘基 |
C(CH3)3 |
38.255 |
CH3 |
CH3 |
2-萘基 |
CH2CH=CH2 |
38.256 |
CH3 |
CH3 |
2-萘基 |
CH2C≡CH |
38.257 |
CH3 |
CH3 |
2-萘基 |
PhCH2 |
38.258 |
CN |
CH3 |
1-萘基 |
CH3 |
38.259 |
CN |
CH3 |
1-萘基 |
C2H5 |
38.260 |
CN |
CH3 |
1-萘基 |
正-C3H7 |
38.261 |
CN |
CH3 |
1-萘基 |
异-C3H7 |
38.262 |
CN |
CH3 |
1-萘基 |
正-C4H9 |
38.263 |
CN |
CH3 |
1-萘基 |
异-C4H9 |
38.264 |
CN |
CH3 |
1-萘基 |
C(CH3)3 |
38.265 |
CN |
CH3 |
1-萘基 |
CH2CH=CH2 |
38.266 |
CN |
CH3 |
1-萘基 |
CH2C≡CH |
38.267 |
CN |
CH3 |
1-萘基 |
PhCH2 |
38.268 |
CN |
CH3 |
2-萘基 |
CH3 |
38.269 |
CN |
CH3 |
2-萘基 |
C2H5 |
38.270 |
CN |
CH3 |
2-萘基 |
正-C3H7 |
38.271 |
CN |
CH3 |
2-萘基 |
异-C3H7 |
38.272 |
CN |
CH3 |
2-萘基 |
正-C4H9 |
本发明式Ⅰ所涵盖的典型化合物包括式Ⅻ化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=N,Y=NH,Z=NR
10的式Ⅰ化合物,且其中的R
2、R
3、R
7和R
10如表39所定义。
表39
化合物 |
R2 |
R3 |
R7 |
R10 |
39.1 |
H |
H |
Ph |
CH3 |
39.2 |
H |
H |
4-Cl(Ph) |
CH3 |
39.3 |
H |
H |
4-Br(Ph) |
CH3 |
39.4 |
H |
H |
4-F(Ph) |
CH3 |
39.5 |
H |
H |
4-OCH3(Ph) |
CH3 |
39.6 |
H |
H |
4-CF3(Ph) |
CH3 |
39.7 |
H |
H |
Ph |
CH3 |
39.8 |
H |
H |
4-Cl(Ph) |
CH3 |
39.9 |
H |
H |
4-Br(Ph) |
CH3 |
39.10 |
H |
H |
4-F(Ph) |
CH3 |
39.11 |
CH3 |
H |
Ph |
CH3 |
39.12 |
CH3 |
H |
2-Cl(Ph) |
CH3 |
39.13 |
CH3 |
H |
3-Cl(Ph) |
CH3 |
39.14 |
CH3 |
H |
4-Cl(Ph) |
CH3 |
39.15 |
CH3 |
H |
2-Br(Ph) |
CH3 |
39.16 |
CH3 |
H |
3-Br(Ph) |
CH3 |
39.17 |
CH3 |
H |
4-Br(Ph) |
CH3 |
39.18 |
CH3 |
H |
Ph |
C2H5 |
39.19 |
CH3 |
H |
2-Cl(Ph) |
C2H5 |
39.20 |
CH3 |
H |
3-Cl(Ph) |
C2H5 |
39.21 |
CH3 |
H |
4-Cl(Ph) |
C2H5 |
39.22 |
CH3 |
H |
2-Br(Ph) |
C2H5 |
39.23 |
CH3 |
H |
3-Br(Ph) |
C2H5 |
39.24 |
CH3 |
H |
4-Br(Ph) |
C2H5 |
39.25 |
CH3 |
H |
2-CH3(Ph) |
C2H5 |
39.26 |
CH3 |
H |
3-CH3(Ph) |
C2H5 |
39.27 |
CH3 |
H |
2-CF3(Ph) |
C2H5 |
39.28 |
CH3 |
H |
3-CF3(Ph) |
C2H5 |
39.29 |
CH3 |
H |
4-CF3(Ph) |
C2H5 |
39.30 |
CH3 |
H |
2-NO2(Ph) |
C2H5 |
39.31 |
CH3 |
H |
3-NO2(Ph) |
C2H5 |
39.32 |
CH3 |
H |
4-NO2(Ph) |
C2H5 |
39.33 |
CH3 |
H |
2,3-Cl(Ph) |
C2H5 |
39.34 |
CH3 |
H |
2,4-Cl(Ph) |
C2H5 |
39.35 |
CH3 |
H |
2,5-Cl(Ph) |
C2H5 |
39.36 |
CH3 |
H |
2,6-Cl(Ph) |
C2H5 |
39.37 |
CH3 |
H |
3,4-Cl(Ph) |
C2H5 |
39.38 |
CH3 |
H |
3,5-Cl(Ph) |
C2H5 |
39.39 |
CH3 |
H |
Ph |
正-C3H7 |
39.40 |
CH3 |
H |
Ph |
异-C3H7 |
39.41 |
CH3 |
H |
Ph |
正-C4H9 |
39.42 |
CH3 |
H |
Ph |
异-C4H9 |
39.43 |
CH3 |
H |
Ph |
C(CH3)3 |
39.44 |
CH3 |
H |
Ph |
CH2CH=CH2 |
39.45 |
CH3 |
H |
Ph |
CH2C≡CH |
39.46 |
CH3 |
H |
Ph |
PhCH2 |
39.47 |
CH3 |
CH3 |
Ph |
CH3 |
39.48 |
CH3 |
CH3 |
4-Cl(Ph) |
CH3 |
39.49 |
CH3 |
CH3 |
4-Br(Ph) |
CH3 |
39.50 |
CH3 |
CH3 |
4-F(Ph) |
CH3 |
39.51 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH3 |
39.52 |
CH3 |
CH3 |
4-CH3(Ph) |
CH3 |
39.53 |
CH3 |
CH3 |
4-NO2(Ph) |
CH3 |
39.54 |
CH3 |
CH3 |
2,4-Cl(Ph) |
CH3 |
39.55 |
CH3 |
CH3 |
2,4-F(Ph) |
CH3 |
39.56 |
CH3 |
CH3 |
Ph |
C2H5 |
39.57 |
CH3 |
CH3 |
2-Cl(Ph) |
C2H5 |
39.58 |
CH3 |
CH3 |
3-Cl(Ph) |
C2H5 |
39.59 |
CH3 |
CH3 |
4-Cl(Ph) |
C2H5 |
39.60 |
CH3 |
CH3 |
4-F(Ph) |
C2H5 |
39.61 |
CH3 |
CH3 |
3-OCH3(Ph) |
C2H5 |
39.62 |
CH3 |
CH3 |
4-OCH3(Ph) |
C2H5 |
39.63 |
CH3 |
CH3 |
4-CH3(Ph) |
C2H5 |
39.64 |
CH3 |
CH3 |
4-NO2(Ph) |
C2H5 |
39.65 |
CH3 |
CH3 |
2,4-Cl(Ph) |
C2H5 |
39.66 |
CH3 |
CH3 |
2,4-F(Ph) |
C2H5 |
39.67 |
CH3 |
CH3 |
Ph |
正-C3H7 |
39.68 |
CH3 |
CH3 |
2-Cl(Ph) |
异-C3H7 |
39.69 |
CH3 |
CH3 |
3-Cl(Ph) |
正-C4H9 |
39.70 |
CH3 |
CH3 |
4-Cl(Ph) |
异-C4H9 |
39.71 |
CH3 |
CH3 |
4-Br(Ph) |
仲-C4H9 |
39.72 |
CH3 |
CH3 |
4-F(Ph) |
C(CH3)3 |
39.73 |
CH3 |
CH3 |
4-OCH3(Ph) |
CH2CH=CH2 |
39.74 |
CH3 |
CH3 |
4-CH3(Ph) |
CH2C≡CH |
39.75 |
CH3 |
CH3 |
4-NO2(Ph) |
PhCH2 |
39.76 |
CH3 |
CH3 |
2,4-Cl(Ph) |
PhCH2CH2 |
39.77 |
CH3 |
CH3 |
2,4-F(Ph) |
PhCH2CH2 |
39.78 |
C2H5 |
H |
Ph |
CH3 |
39.79 |
C2H5 |
H |
2-Cl(Ph) |
CH3 |
39.80 |
C2H5 |
H |
3-Cl(Ph) |
CH3 |
39.81 |
C2H5 |
H |
4-Cl(Ph) |
CH3 |
39.82 |
C2H5 |
H |
4-Br(Ph) |
CH3 |
39.83 |
C2H5 |
H |
4-F(Ph) |
CH3 |
39.84 |
C2H5 |
H |
4-OCH3(Ph) |
CH3 |
39.85 |
C2H5 |
H |
4-CH3(Ph) |
CH3 |
39.86 |
C2H5 |
H |
4-NO2(Ph) |
CH3 |
39.87 |
C2H5 |
H |
2,4-Cl(Ph) |
CH3 |
39.88 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
39.89 |
C2H5 |
H |
Ph |
C2H5 |
39.90 |
C2H5 |
H |
2-Cl(Ph) |
C2H5 |
39.91 |
C2H5 |
H |
3-Cl(Ph) |
C2H5 |
39.92 |
C2H5 |
H |
4-Cl(Ph) |
C2H5 |
39.93 |
C2H5 |
H |
4-F(Ph) |
C2H5 |
39.94 |
C2H5 |
H |
3-OCH3(Ph) |
C2H5 |
39.95 |
C2H5 |
H |
4-OCH3(Ph) |
C2H5 |
39.96 |
C2H5 |
H |
4-CH3(Ph) |
C2H5 |
39.97 |
C2H5 |
H |
4-NO2(Ph) |
C2H6 |
39.98 |
C2H5 |
H |
2,4-Cl(Ph) |
C2H5 |
39.99 |
C2H5 |
H |
2.4-F(Ph) |
C2H5 |
39.100 |
C2H5 |
H |
Ph |
正-C3H7 |
39.101 |
C2H5 |
H |
2-Cl(Ph) |
异-C3H7 |
39.102 |
C2H5 |
H |
3-Cl(Ph) |
正-C4H9 |
39.103 |
C2H5 |
H |
4-Cl(Ph) |
异-C4H9 |
39.104 |
C2H5 |
H |
4-F(Ph) |
仲-C4H9 |
39.105 |
C2H5 |
H |
3-OCH3(Ph) |
C(CH3)3 |
39.106 |
C2H5 |
H |
4-OCH3(Ph) |
CH2CH=CH2 |
39.107 |
C2H5 |
H |
4-CH3(Ph) |
CH2C≡CH |
39.108 |
C2H5 |
H |
4-NO2(Ph) |
PhCH2 |
39.109 |
C2H5 |
H |
2,4-Cl(Ph) |
PhCH2CH2 |
39.110 |
C2H5 |
H |
2,4-F(Ph) |
CH3 |
39.111 |
正-C3H7 |
H |
Ph |
CH3 |
39.112 |
正-C3H7 |
H |
2-Cl(Ph) |
CH3 |
39.113 |
正-C3H7 |
H |
3-Cl(Ph) |
CH3 |
39.114 |
正-C3H7 |
H |
4-Cl(Ph) |
CH3 |
39.115 |
正-C3H7 |
H |
4-Br(Ph) |
CH3 |
39.116 |
正-C3H7 |
H |
3-OCH3(Ph) |
CH3 |
39.117 |
正-C3H7 |
H |
4-OCH3(Ph) |
CH3 |
39.118 |
正-C3H7 |
H |
4-CH3(Ph) |
CH3 |
39.119 |
正-C3H7 |
H |
4-NO2(Ph) |
CH3 |
39.120 |
正-C3H7 |
H |
2,4-Cl(Ph) |
CH3 |
39.121 |
正-C3H7 |
H |
2,4-F(Ph) |
CH3 |
39.122 |
正-C3H7 |
H |
Ph |
C2H5 |
39.123 |
正-C3H7 |
H |
2-Cl(Ph) |
C2H5 |
39.124 |
正-C3H7 |
H |
3-Cl(Ph) |
C2H5 |
39.125 |
正-C3H7 |
H |
4-Cl(Ph) |
C2H5 |
39.126 |
正-C3H7 |
H |
4-Br(Ph) |
C2H5 |
39.127 |
正-C3H7 |
H |
4-F(Ph) |
C2H5 |
39.128 |
正-C3H7 |
H |
4-OCH3(Ph) |
C2H5 |
39.129 |
正-C3H7 |
H |
4-CH3(Ph) |
C2H5 |
39.130 |
正-C3H7 |
H |
4-NO2(Ph) |
C2H5 |
39.131 |
正-C3H7 |
H |
2,4-Cl(Ph) |
C2H5 |
39.132 |
正-C3H7 |
H |
2,4-F(Ph) |
C2H5 |
39.133 |
正-C3H7 |
H |
Ph |
正-C3H7 |
39.134 |
正-C3H7 |
H |
Ph |
异-C3H7 |
39.135 |
正-C3H7 |
H |
Ph |
正-C4H9 |
39.136 |
正-C3H7 |
H |
Ph |
异-C4H9 |
39.137 |
正-C3H7 |
H |
Ph |
C(CH3)3 |
39.138 |
正-C3H7 |
H |
Ph |
CH2CH=CH2 |
39.139 |
正-C3H7 |
H |
Ph |
CH2C≡CH |
39.140 |
正-C3H7 |
H |
Ph |
PhCH2 |
39.141 |
正-C3H7 |
H |
Ph |
PhCH2CH2 |
39.142 |
异-C3H7 |
H |
Ph |
C2H5 |
39.143 |
异-C3H7 |
H |
Ph |
正-C3H7 |
39.144 |
异-C3H7 |
H |
Ph |
异-C3H7 |
39.145 |
异-C3H7 |
H |
Ph |
正-C4H9 |
39.146 |
异-C3H7 |
H |
Ph |
异-C4H9 |
39.147 |
异-C3H7 |
H |
Ph |
C(CH3)3 |
39.148 |
异-C3H7 |
H |
Ph |
CH2CH=CH2 |
39.149 |
异-C3H7 |
H |
Ph |
CH2C≡CH |
39.150 |
异-C3H7 |
H |
Ph |
PhCH2 |
39.151 |
异-C3H7 |
H |
Ph |
PhCH2CH2 |
39.152 |
环丙基 |
H |
4-F(Ph) |
CH3 |
39.153 |
环丙基 |
H |
4-OCH3(Ph) |
CH3 |
39.154 |
环丙基 |
H |
4-CH3(Ph) |
CH3 |
39.155 |
环丙基 |
H |
4-NO2(Ph) |
CH3 |
39.156 |
环丙基 |
H |
2,4-Cl(Ph) |
CH3 |
39.157 |
环丙基 |
H |
2,4-F(Ph) |
CH3 |
39.158 |
环丙基 |
H |
4-Cl(Ph) |
CH3 |
39.159 |
环丙基 |
H |
4-Br(Ph) |
CH3 |
39.160 |
环丙基 |
H |
4-F(Ph) |
CH3 |
39.161 |
环丙基 |
H |
4-OCH3(Ph) |
CH3 |
39.162 |
环丙基 |
H |
4-CH3(Ph) |
CH3 |
39.163 |
环丙基 |
H |
4-NO2(Ph) |
CH3 |
39.164 |
Ph |
H |
Ph |
CH3 |
39.165 |
Ph |
H |
2-Cl(Ph) |
C2H5 |
39.166 |
Ph |
H |
3-Cl(Ph) |
正-C3H7 |
39.167 |
Ph |
H |
4-Cl(Ph) |
异-C3H7 |
39.168 |
Ph |
H |
4-Br(Ph) |
正-C4H9 |
39.169 |
Ph |
H |
4-F(Ph) |
异-C4H9 |
39.170 |
Ph |
H |
4-OCH3(Ph) |
C(CH3)3 |
39.171 |
Ph |
H |
4-CH3(Ph) |
CH2CH=CH2 |
39.172 |
Ph |
H |
4-NO2(Ph) |
CH2C≡CH |
39.173 |
Ph |
H |
2,4-Cl(Ph) |
PhCH2 |
39.174 |
CN |
H |
Ph |
CH3 |
39.175 |
CN |
H |
2-Cl(Ph) |
CH3 |
39.176 |
CN |
H |
3-Cl(Ph) |
CH3 |
39.177 |
CN |
H |
4-Cl(Ph) |
CH3 |
39.178 |
CN |
H |
4-Br(Ph) |
CH3 |
39.179 |
CN |
H |
4-F(Ph) |
CH3 |
39.180 |
CN |
H |
4-Cl(Ph) |
CH3 |
39.181 |
CN |
H |
4-Br(Ph) |
CH3 |
39.182 |
CN |
H |
4-F(Ph) |
CH3 |
39.183 |
CN |
H |
4-OCH3(Ph) |
CH3 |
39.184 |
CN |
H |
4-CH3(Ph) |
CH3 |
39.185 |
CN |
H |
4-NO2(Ph) |
CH3 |
39.186 |
CN |
H |
2,4-Cl(Ph) |
CH3 |
39.187 |
CN |
H |
2,4-F(Ph) |
CH3 |
39.188 |
CN |
H |
4-CF3(Ph) |
CH3 |
39.189 |
CN |
H |
Ph |
C2H5 |
39.190 |
CN |
H |
Ph |
正-C3H7 |
39.191 |
CN |
H |
Ph |
异-C3H7 |
39.192 |
CN |
H |
Ph |
正-C4H9 |
39.193 |
CN |
H |
Ph |
异-C4H9 |
39.194 |
CN |
H |
Ph |
C(CH3)3 |
39.195 |
CN |
H |
Ph |
CH2CH=CH2 |
39.196 |
CN |
H |
Ph |
CH2C≡CH |
39.197 |
CN |
H |
Ph |
PhCH2 |
39.198 |
CH3 |
H |
1-萘基 |
CH3 |
39.199 |
CH3 |
H |
1-萘基 |
C2H5 |
39.200 |
CH3 |
H |
1-萘基 |
正-C3H7 |
39.201 |
CH3 |
H |
1-萘基 |
异-C3H7 |
39.202 |
CH3 |
H |
1-萘基 |
正-C4H9 |
39.203 |
CH3 |
H |
1-萘基 |
异-C4H9 |
39.204 |
CH3 |
H |
1-萘基 |
C(CH3)3 |
39.205 |
CH3 |
H |
1-萘基 |
CH2CH=CH2 |
39.206 |
CH3 |
H |
1-萘基 |
CH2C≡CH |
39.207 |
CH3 |
H |
1-萘基 |
PhCH2 |
39.208 |
CH3 |
H |
2-萘基 |
CH3 |
39.209 |
CH3 |
H |
2-萘基 |
C2H5 |
39.210 |
CH3 |
H |
2-萘基 |
正-C3H7 |
39.211 |
CH3 |
H |
2-萘基 |
异-C3H7 |
39.212 |
CH3 |
H |
2-萘基 |
正-C4H9 |
39.213 |
CH3 |
H |
2-萘基 |
异-C4H9 |
39.214 |
CH3 |
H |
2-萘基 |
C(CH3)3 |
39.215 |
CH3 |
H |
2-萘基 |
CH2CH=CH2 |
39.216 |
CH3 |
H |
2-萘基 |
CH2C≡CH |
39.217 |
CH3 |
H |
2-萘基 |
PhCH2 |
39.218 |
CN |
H |
1-萘基 |
CH3 |
39.219 |
CN |
H |
1-萘基 |
C2H5 |
39.220 |
CN |
H |
1-萘基 |
正-C3H7 |
39.221 |
CN |
H |
1-萘基 |
异-C3H7 |
39.222 |
CN |
H |
1-萘基 |
正-C4H9 |
39.223 |
CN |
H |
1-萘基 |
异-C4H9 |
39.224 |
CN |
H |
1-萘基 |
C(CH3)3 |
39.225 |
CN |
H |
1-萘基 |
CH2CH=CH2 |
39.226 |
CN |
H |
1-萘基 |
CH2C≡CH |
39.227 |
CN |
H |
1-萘基 |
PhCH2 |
39.228 |
CN |
H |
2-萘基 |
CH3 |
39.229 |
CN |
H |
2-萘基 |
C2H5 |
39.230 |
CN |
H |
2-萘基 |
正-C3H7 |
39.231 |
CN |
H |
2-萘基 |
异-C3H7 |
39.232 |
CN |
H |
2-萘基 |
正-C4H9 |
39.233 |
CN |
H |
2-萘基 |
异-C4H9 |
39.234 |
CN |
H |
2-萘基 |
C(CH3)3 |
39.235 |
CN |
H |
2-萘基 |
CH2CH=CH2 |
39.236 |
CN |
H |
2-萘基 |
CH2C≡CH |
39.237 |
CN |
H |
2-萘基 |
PhCH2 |
39.238 |
CH3 |
CH3 |
1-萘基 |
CH3 |
39.239 |
CH3 |
CH3 |
1-萘基 |
C2H5 |
39.240 |
CH3 |
CH3 |
1-萘基 |
正-C3H7 |
39.241 |
CH3 |
CH3 |
1-萘基 |
异-C3H7 |
39.242 |
CH3 |
CH3 |
1-萘基 |
正-C4H9 |
39.243 |
CH3 |
CH3 |
1-萘基 |
异-C4H9 |
39.244 |
CH3 |
CH3 |
1-萘基 |
C(CH3)3 |
39.245 |
CH3 |
CH3 |
1-萘基 |
CH2CH=CH2 |
39.246 |
CH3 |
CH3 |
1-萘基 |
CH2C≡CH |
39.247 |
CH3 |
CH3 |
1-萘基 |
PhCH2 |
39.248 |
CH3 |
CH3 |
2-萘基 |
CH3 |
39.249 |
CH3 |
CH3 |
2-萘基 |
C2H5 |
39.250 |
CH3 |
CH3 |
2-萘基 |
正-C3H7 |
39.251 |
CH3 |
CH3 |
2-萘基 |
异-C3H7 |
39.252 |
CH3 |
CH3 |
2-萘基 |
正-C4H9 |
39.253 |
CH3 |
CH3 |
2-萘基 |
异-C4H9 |
39.254 |
CH3 |
CH3 |
2-萘基 |
C(CH3)3 |
39.255 |
CH3 |
CH3 |
2-萘基 |
CH2CH=CH2 |
39.256 |
CH3 |
CH3 |
2-萘基 |
CH2C≡CH |
39.257 |
CH3 |
CH3 |
2-萘基 |
PhCH2 |
39.258 |
CN |
CH3 |
1-萘基 |
CH3 |
39.259 |
CN |
CH3 |
1-萘基 |
C2H5 |
39.260 |
CN |
CH3 |
1-萘基 |
正-C3H7 |
39.261 |
CN |
CH3 |
1-萘基 |
异-C3H7 |
39.262 |
CN |
CH3 |
1-萘萘 |
正-C4H9 |
39.263 |
CN |
CH3 |
1-萘基 |
异-C4H9 |
39.264 |
CN |
CH3 |
1-萘基 |
C(CH3)3 |
39.265 |
CN |
CH3 |
1-萘基 |
CH2CH=CH2 |
39.266 |
CN |
CH3 |
1-萘基 |
CH2C≡CH |
39.267 |
CN |
CH3 |
1-萘基 |
PhCH2 |
39.268 |
CN |
CH3 |
2-萘基 |
CH3 |
39.269 |
CN |
CH3 |
2-萘基 |
C2H5 |
39.270 |
CN |
CH3 |
2-萘基 |
正-C3H7 |
39.271 |
CN |
CH3 |
2-萘基 |
异-C3H7 |
39.272 |
CN |
CH3 |
2-萘基 |
正-C4H9 |
表40:化合物40.1-40.226为式Ⅹ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NR10的式Ⅰ化合物,其中R10为CH3,且取代基R2、R3和R7如表4所定义。
表41:化合物41.1-41.226为式Ⅺ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NR10的式Ⅰ化合物,其中R10为CH3,且取代基R2、R3和R7如表4所定义。
表42:化合物42.1-42.226为式Ⅻ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NR10的式Ⅰ化合物,其中R10为CH3,且取代基R2、R3和R7如表4所定义。
表43:化合物43.1-43.221为式Ⅹ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NR10的式Ⅰ化合物,其中R10为C2H5,且取代基R2、R3和R7如表7所定义。
表44:化合物44.1-44.221为式Ⅺ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NR10的式Ⅰ化合物,其中R10为C2H5,且取代基R2、R3和R7如表7所定义。
表45:化合物45.1-45.221为式Ⅻ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NR10的式Ⅰ化合物,其中R10为C2H5,且取代基R2、R3和R7如表7所定义。
表46:化合物46.1-46.139为式Ⅹ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NR10的式Ⅰ化合物,其中R10为Ph,且取代基R2、R3和R7如表10所定义。
表47:化合物47.1-47.139为式Ⅺ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NR10的式Ⅰ化合物,其中R10为Ph,且取代基R2、R3和R7如表10所定义。
表48:化合物48.1-48.139为式Ⅻ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NR10的式Ⅰ化合物,其中R10为Ph,且取代基R2、R3和R7如表10所定义。
本发明式Ⅰ所涵盖的典型化合物包括式Ⅹ化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=CH,Y=O,Z=NR
10的式Ⅰ化合物,且其中的R
2、R
3、R
7、R
10、R
11和R
12如表49所定义。
表49
化合物 |
R2 |
R3 |
R7 |
R10 |
R11 |
R12 |
49.1 |
H |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
49.2 |
H |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.3 |
H |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.4 |
H |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.5 |
H |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.6 |
H |
H |
4-CF3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.7 |
H |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
49.8 |
H |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.9 |
H |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.10 |
H |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.11 |
CH3 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
49.12 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.13 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.14 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.15 |
CH3 |
H |
2-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.16 |
CH3 |
H |
3-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.17 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.18 |
CH3 |
H |
Ph |
N=CR11R12 |
H |
Ph |
49.19 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.20 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.21 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.22 |
CH3 |
H |
2-Br(Ph) |
N=CR11R12 |
H |
Ph |
49.23 |
CH3 |
H |
3-Br(Ph) |
N=CR11R12 |
H |
Ph |
49.24 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
49.25 |
CH3 |
H |
2-CH3(Ph) |
N=CR11R12 |
H |
Ph |
49.26 |
CH3 |
H |
3-CH3(Ph) |
N=CR11R12 |
H |
Ph |
49.27 |
CH3 |
H |
2-CF3(Ph) |
N=CR11R12 |
H |
Ph |
49.28 |
CH3 |
H |
3-CF3(Ph) |
N=CR11R12 |
H |
Ph |
49.29 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
H |
Ph |
49.30 |
CH3 |
H |
2-NO2(Ph) |
N=CR11R12 |
H |
Ph |
49.31 |
CH3 |
H |
3-NO2(Ph) |
N=CR11R12 |
H |
Ph |
49.32 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
H |
Ph |
49.33 |
CH3 |
H |
2,3-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.34 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.35 |
CH3 |
H |
2,5-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.36 |
CH3 |
H |
2,6-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.37 |
CH3 |
H |
3,4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.38 |
CH3 |
H |
3,5-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.39 |
CH3 |
H |
Ph |
N=CR11R12 |
CH3 |
Ph |
49.40 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.41 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.42 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.43 |
CH3 |
H |
2-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.44 |
CH3 |
H |
3-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.45 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.46 |
CH3 |
H |
2-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.47 |
CH3 |
H |
3-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.48 |
CH3 |
H |
2-CF3(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.49 |
CH3 |
H |
3-CF3(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.50 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.5l |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.52 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.53 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.54 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.55 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.56 |
CH3 |
H |
Ph |
N=CR11R12 |
Ph |
Ph |
49.57 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
49.58 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
49.59 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
49.60 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
49.61 |
CH3 |
H |
3-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
49.62 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
49.63 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
Ph |
49.64 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
Ph |
49.65 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
49.66 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
49.67 |
C2H5 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
49.68 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.69 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.70 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.7l |
C2H5 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.72 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.73 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.74 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.75 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.76 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.77 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.78 |
C2H5 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
49.79 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.80 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.81 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.82 |
C2H5 |
H |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
49.83 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
H |
Ph |
49.84 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
H |
Ph |
49.85 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
H |
Ph |
49.86 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
H |
Ph |
49.87 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.88 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
H |
Ph |
49.89 |
C2H5 |
H |
Ph |
N=CR11R12 |
CH3 |
Ph |
49.90 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.91 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.92 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.93 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.94 |
C2H5 |
H |
3-OCH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.95 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.96 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.97 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.98 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.99 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.100 |
C2H5 |
H |
Ph |
N=CR11R12 |
Ph |
Ph |
49.10l |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
49.102 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
49.103 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
49.104 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
49.105 |
C2H5 |
H |
3-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
49.106 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
49.107 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
Ph |
49.108 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
Ph |
49.109 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
49.110 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
49.111 |
异-C3H7 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
49.112 |
异-C3H7 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.113 |
异-C3H7 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.114 |
异-C3H7 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
49.115 |
异-C3H7 |
H |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
49.116 |
异-C3 H7 |
H |
3-OCH3(Ph) |
N=CR11R12 |
H |
Ph |
49.117 |
异-C3H7 |
H |
4-OCH3(Ph) |
N=CR11R12 |
H |
Ph |
49.118 |
异-C3H7 |
H |
4-CH3(Ph) |
N=CR11R12 |
H |
Ph |
49.119 |
异-C3H7 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.120 |
异-C3H7 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.121 |
异-C3H7 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.122 |
环丙基 |
H |
Ph |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.123 |
环丙基 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.124 |
环丙基 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.125 |
环丙基 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.126 |
环丙基 |
H |
4-Br(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.127 |
环丙基 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.128 |
环丙基 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.129 |
环丙基 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.130 |
环丙基 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.131 |
环丙基 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.132 |
环丙基 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.133 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
49.134 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
49.135 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
49.136 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
49.137 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
49.138 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
49.139 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
49.140 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
49.141 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
49.142 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
49.143 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
49.144 |
C2H5 |
H |
l-萘基 |
N=CR11R12 |
CH3 |
Ph |
49.145 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
49.146 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
49.147 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
49.148 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
49.149 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
49.150 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
49.151 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
49.152 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
49.153 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
49.154 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
49.155 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
49.156 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
49.157 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
49.158 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
49.159 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
49.160 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
49.16l |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
49.162 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
49.163 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
49.164 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
49.165 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
49.166 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
49.167 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
49.168 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
49.169 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
49.170 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
49.171 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
49.172 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
49.173 |
CH3 |
H |
Ph |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.174 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.175 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.176 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.177 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.178 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.179 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.180 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.181 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.182 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.183 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.184 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.185 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.186 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.187 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.188 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.189 |
CH3 |
H |
Ph |
N=CR11R12 |
Ph |
4-吡啶基 |
49.190 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.191 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.192 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.193 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.194 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.195 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.196 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.197 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.198 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
49.199 |
CH3 |
H |
Ph |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.200 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.201 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.202 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.203 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.204 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.205 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.206 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.207 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.208 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.209 |
CH3 |
H |
Ph |
N=环戊基 | | |
49.210 |
CH3 |
H |
4-Cl(Ph) |
N=环戊基 | | |
49.211 |
CH3 |
H |
4-Br(Ph) |
N=环戊基 | | |
49.212 |
CH3 |
H |
4-F(Ph) |
N=环戊基 | | |
49.213 |
CH3 |
H |
4-OCH3(Ph) |
N=环戊基 | | |
49.214 |
CH3 |
H |
4-CH3(Ph) |
N=环戊基 | | |
49.215 |
CH3 |
H |
4-NO2(Ph) |
N=环戊基 | | |
49.216 |
CH3 |
H |
2,4-Cl(Ph) |
N=环戊基 | | |
49.217 |
CH3 |
H |
2,4-F(Ph) |
N=环戊基 | | |
49.218 |
CH3 |
H |
4-CF3(Ph) |
N=环戊基 | | |
49.219 |
CH3 |
H |
Ph |
N=环己基 | | |
49.220 |
CH3 |
H |
4-Cl(Ph) |
N=环己基 | | |
49.221 |
CH3 |
H |
4-Br(Ph) |
N=环己基 | | |
49.222 |
CH3 |
H |
4-F(Ph) |
N=环己基 | | |
49.223 |
CH3 |
H |
4-OCH3(Ph) |
N=环己基 | | |
49.224 |
CH3 |
H |
4-CH3(Ph) |
N=环己基 | | |
49.225 |
CH3 |
H |
4-NO2(Ph) |
N=环己基 | | |
49.226 |
CH3 |
H |
2,4-Cl(Ph) |
N=环己基 | | |
49.227 |
CH3 |
H |
2,4-F(Ph) |
N=环己基 | | |
49.228 |
CH3 |
H |
4-CF3(Ph) |
N=环己基 | | |
49.229 |
CH3 |
H |
1-萘基 |
N=环戊基 | | |
49.230 |
C2H5 |
H |
1-萘基 |
N=环戊基 | | |
49.231 |
正-C3H7 |
H |
1-萘基 |
N=环戊基 | | |
49.232 |
异-C3H7 |
H |
1-萘基 |
N=环戊基 | | |
49.233 |
环丙基 |
H |
1-萘基 |
N=环戊基 | | |
49.234 |
CH3 |
H |
1-萘基 |
N=环己基 | | |
49.235 |
C2H5 |
H |
1-萘基 |
N=环己基 | | |
49.236 |
正-C3H7 |
H |
1-萘基 |
N=环己基 | | |
49.237 |
异-C3H7 |
H |
1-萘基 |
N=环己基 | | |
49.238 |
环丙基 |
H |
1-萘基 |
N=环己基 | | |
49.239 |
CH3 |
H |
2-萘基 |
N=环戊基 | | |
49.240 |
C2H5 |
H |
2-萘基 |
N=环戊基 | | |
49.241 |
正-C3H7 |
H |
2-萘基 |
N=环戊基 | | |
49.242 |
异-C3H7 |
H |
2-萘基 |
N=环戊基 | | |
49.243 |
环丙基 |
H |
2-萘基 |
N=环戊基 | | |
49.244 |
CH3 |
H |
2-萘基 |
N=环己基 | | |
49.245 |
C2H5 |
H |
2-萘基 |
N=环己基 | | |
49.246 |
正-C3H7 |
H |
2-萘基 |
N=环己基 | | |
49.247 |
异-C3H7 |
H |
2-萘基 |
N=环己基 | | |
49.248 |
环丙基 |
H |
2-萘基 |
N=环己基 | | |
49.249 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.250 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.251 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.252 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.253 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.254 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.255 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.256 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.257 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.258 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
49.259 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
H |
Ph |
49.260 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
49.261 |
正-C3H7 |
CH3 |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
49.262 |
异-C3H7 |
CH3 |
4-F(Ph) |
N=CR11R12 |
H |
Ph |
49.263 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
CH3 |
Ph |
49.264 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.265 |
正-C3H7 |
CH3 |
4-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.266 |
异-C3H7 |
CH3 |
4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
49.267 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
Ph |
Ph |
49.268 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
49.269 |
正-C3H7 |
CH3 |
4-Br(Ph) |
N=CR11R12 |
Ph |
Ph |
49.270 |
异-C3H7 |
CH3 |
4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
49.27l |
CH3 |
CH3 |
Ph |
N=CR11R12 |
Ph |
4-Cl(Ph) |
49.272 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
本发明式Ⅰ所涵盖的典型化合物包括式Ⅺ化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=N,Y=O,Z=NR
10的式Ⅰ化合物,且其中的R
2、R
3、R
7、R
10、R
11和R
12如表50所定义。
表50
化合物 |
R2 |
R3 |
R7 |
R10 |
R11 |
R12 |
50.1 |
H |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
50.2 |
H |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.3 |
H |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.4 |
H |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.5 |
H |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.6 |
H |
H |
4-CF3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.7 |
H |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
50.8 |
H |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.9 |
H |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.10 |
H |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.11 |
CH3 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
50.12 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.13 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.14 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.15 |
CH3 |
H |
2-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.16 |
CH3 |
H |
3-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.17 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.18 |
CH3 |
H |
Ph |
N=CR11R12 |
H |
Ph |
50.19 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.20 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.21 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.22 |
CH3 |
H |
2-Br(Ph) |
N=CR11R12 |
H |
Ph |
50.23 |
CH3 |
H |
3-Br(Ph) |
N=CR11R12 |
H |
Ph |
50.24 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
50.25 |
CH3 |
H |
2-CH3(Ph) |
N=CR11R12 |
H |
Ph |
50.26 |
CH3 |
H |
3-CH3(Ph) |
N=CR11R12 |
H |
Ph |
50.27 |
CH3 |
H |
2-CF3(Ph) |
N=CR11R12 |
H |
Ph |
50.28 |
CH3 |
H |
3-CF3(Ph) |
N=CR11R12 |
H |
Ph |
50.29 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
H |
Ph |
50.30 |
CH3 |
H |
2-NO2(Ph) |
N=CR11R12 |
H |
Ph |
50.3l |
CH3 |
H |
3-NO2(Ph) |
N=CR11R12 |
H |
Ph |
50.32 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
H |
Ph |
50.33 |
CH3 |
H |
2,3-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.34 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.35 |
CH3 |
H |
2,5-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.36 |
CH3 |
H |
2,6-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.37 |
CH3 |
H |
3,4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.38 |
CH3 |
H |
3,5-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.39 |
CH3 |
H |
Ph |
N=CR11R12 |
CH3 |
Ph |
50.40 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.4l |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.42 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.43 |
CH3 |
H |
2-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.44 |
CH3 |
H |
3-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.45 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.46 |
CH3 |
H |
2-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.47 |
CH3 |
H |
3-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.48 |
CH3 |
H |
2-CF3(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.49 |
CH3 |
H |
3-CF3(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.50 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.51 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.52 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.53 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.54 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.55 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.56 |
CH3 |
H |
Ph |
N=CR11R12 |
Ph |
Ph |
50.57 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
50.58 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
50.59 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
50.60 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
50.61 |
CH3 |
H |
3-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
50.62 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
50.63 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
Ph |
50.64 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
Ph |
50.65 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
50.66 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
50.67 |
C2H5 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
50.68 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.69 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.70 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.71 |
C2H5 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.72 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.73 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.74 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.75 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.76 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.77 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.78 |
C2H5 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
50.79 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.80 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.81 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.82 |
C2H5 |
H |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
50.83 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
H |
Ph |
50.84 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
H |
Ph |
50.85 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
H |
Ph |
50.86 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
H |
Ph |
50.87 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.88 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
H |
Ph |
50.89 |
C2H5 |
H |
Ph |
N=CR11R12 |
CH3 |
Ph |
50.90 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.91 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.92 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.93 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.94 |
C2H5 |
H |
3-OCH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.95 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.96 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.97 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.98 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.99 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.100 |
C2H5 |
H |
Ph |
N=CR11R12 |
Ph |
Ph |
50.101 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
50.102 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
50.103 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
50.104 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
50.105 |
C2H5 |
H |
3-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
50.106 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
50.107 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
Ph |
50.108 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
Ph |
50.109 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
50.110 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
50.111 |
异-C3H7 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
50.112 |
异-C3H7 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.113 |
异-C3H7 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.114 |
异-C3H7 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
50.115 |
异-C3H7 |
H |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
50.116 |
异-C3H7 |
H |
3-OCH3(Ph) |
N=CR11R12 |
H |
Ph |
50.117 |
异-C3H7 |
H |
4-OCH3(Ph) |
N=CR11R12 |
H |
Ph |
50.118 |
异-C3H7 |
H |
4-CH3(Ph) |
N=CR11R12 |
H |
Ph |
50.119 |
异-C3H7 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.120 |
异-C3H7 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.121 |
异-C3H7 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.122 |
环丙基 |
H |
Ph |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.123 |
环丙基 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.124 |
环丙基 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.125 |
环丙基 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.126 |
环丙基 |
H |
4-Br(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.127 |
环丙基 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.128 |
环丙基 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.129 |
环丙基 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.130 |
环丙基 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.131 |
环丙基 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.132 |
环丙基 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.133 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
50.134 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
50.135 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
50.136 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
50.137 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
50.138 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
50.139 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
50.140 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
50.141 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
50.142 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
50.143 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
50.144 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
50.145 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
50.146 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
50.147 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
50.148 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
50.149 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
50.150 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
50.151 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
50.152 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
50.153 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
50.154 |
C2H5 |
H |
3-萘基 |
N=CR11R12 |
CH3 |
CH3 |
50.155 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
50.156 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
50.157 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
50.158 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
50.159 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
50.160 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
50.161 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
50.162 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
50.163 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
50.164 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
50.165 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
50.166 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
50.167 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
50.168 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
50.169 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
50.170 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
50.171 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
50.172 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
50.173 |
CH3 |
H |
Ph |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.174 |
CH3 |
H |
2-C1(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.175 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.176 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.177 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.178 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.179 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.180 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.181 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.182 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.183 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.184 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.185 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.186 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.187 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.188 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.189 |
CH3 |
H |
Ph |
N=CR11R12 |
Ph |
4-吡啶基 |
50.190 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.191 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.192 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.193 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.194 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.195 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.196 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.197 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.198 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
50.199 |
CH3 |
H |
Ph |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.200 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.201 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.202 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.203 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.204 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.205 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.206 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.207 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.208 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.209 |
CH3 |
H |
Ph |
N=环戊基 | | |
50.210 |
CH3 |
H |
4-Cl(Ph) |
N=环戊基 | | |
50.211 |
CH3 |
H |
4-Br(Ph) |
N=环戊基 | | |
50.212 |
CH3 |
H |
4-F(Ph) |
N=环戊基 | | |
50.213 |
CH3 |
H |
4-OCH3(Ph) |
N=环戊基 | | |
50.214 |
CH3 |
H |
4-CH3(Ph) |
N=环戊基 | | |
50.215 |
CH3 |
H |
4-NO2(Ph) |
N=环戊基 | | |
50.216 |
CH3 |
H |
2,4-Cl(Ph) |
N=环戊基 | | |
50.217 |
CH3 |
H |
2,4-F(Ph) |
N=环戊基 | | |
50.218 |
CH3 |
H |
4-CF3(Ph) |
N=环戊基 | | |
50.219 |
CH3 |
H |
Ph |
N=环己基 | | |
50.220 |
CH3 |
H |
4-Cl(Ph) |
N=环己基 | | |
50.221 |
CH3 |
H |
4-Br(Ph) |
N=环己基 | | |
50.222 |
CH3 |
H |
4-F(Ph) |
N=环己基 | | |
50.223 |
CH3 |
H |
4-OCH3(Ph) |
N=环己基 | | |
50.224 |
CH3 |
H |
4-CH3(Ph) |
N=环己基 | | |
50.225 |
CH3 |
H |
4-NO2(Ph) |
N=环己基 | | |
50.226 |
CH3 |
H |
2,4-Cl(Ph) |
N=环己基 | | |
50.227 |
CH3 |
H |
2,4-F(Ph) |
N=环己基 | | |
50.228 |
CH3 |
H |
4-CF3(Ph) |
N=环己基 | | |
50.229 |
CH3 |
H |
1-萘基 |
N=环戊基 | | |
50.230 |
C2H5 |
H |
1-萘基 |
N=环戊基 | | |
50.231 |
正-C3H7 |
H |
1-萘基 |
N=环戊基 | | |
50.232 |
异-C3H7 |
H |
1-萘基 |
N=环戊基 | | |
50.233 |
环丙基 |
H |
1-萘基 |
N=环戊基 | | |
50.234 |
CH3 |
H |
1-萘基 |
N=环己基 | | |
50.235 |
C2H5 |
H |
1-萘基 |
N=环己基 | | |
50.236 |
正-C3H7 |
H |
1-萘基 |
N=环己基 | | |
50.237 |
异-C3H7 |
H |
1-萘基 |
N=环己基 | | |
50.238 |
环丙基 |
H |
1-萘基 |
N=环己基 | | |
50.239 |
CH3 |
H |
2-萘基 |
N=环戊基 | | |
50.240 |
C2H5 |
H |
2-萘基 |
N=环戊基 | | |
50.241 |
正-C3H7 |
H |
2-萘基 |
N=环戊基 | | |
50.242 |
异-C3H7 |
H |
2-萘基 |
N=环戊基 | | |
50.243 |
环丙基 |
H |
2-萘基 |
N=环戊基 | | |
50.244 |
CH3 |
H |
2-萘基 |
N=环己基 | | |
50.245 |
C2H5 |
H |
2-萘基 |
N=环己基 | | |
50.246 |
正-C3H7 |
H |
2-萘基 |
N=环己基 | | |
50.247 |
异-C3H7 |
H |
2-萘基 |
N=环己基 | | |
50.248 |
环丙基 |
H |
2-萘基 |
N=环己基 | | |
50.249 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.250 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.251 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.252 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.253 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.254 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.255 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.256 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.257 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.258 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
50.259 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
H |
Ph |
50.260 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
50.261 |
正-C3H7 |
CH3 |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
50.262 |
异-C3H7 |
CH3 |
4-F(Ph) |
N=CR11R12 |
H |
Ph |
50.263 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
CH3 |
Ph |
50.264 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.265 |
正-C3H7 |
CH3 |
4-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.266 |
异-C3H7 |
CH3 |
4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
50.267 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
Ph |
Ph |
50.268 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
50.269 |
正-C3H7 |
CH3 |
4-Br(Ph) |
N=CR11R12 |
Ph |
Ph |
50.270 |
异-C3H7 |
CH3 |
4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
50.271 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
Ph |
4-Cl(Ph) |
50.272 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
本发明式Ⅰ所涵盖的典型化合物包括式Ⅻ化合物,它们是A=R
4=R
5=R
6=H,R
1=CH
3,X=N,Y=NH,Z=NR
10的式Ⅰ化合物,且其中的R
2、R
3、R
7、R
10、R
11和R
12如表51所定义。
表51
化合物 |
R2 |
R3 |
R7 |
R10 |
R11 |
R12 |
51.1 |
H |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
51.2 |
H |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.3 |
H |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.4 |
H |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.5 |
H |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.6 |
H |
H |
4-CF3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.7 |
H |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
51.8 |
H |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.9 |
H |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.10 |
H |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.11 |
CH3 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
51.12 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.13 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.14 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.15 |
CH3 |
H |
2-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.16 |
CH3 |
H |
3-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.17 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.18 |
CH3 |
H |
Ph |
N=CR11R12 |
H |
Ph |
51.19 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.20 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.21 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.22 |
CH3 |
H |
2-Br(Ph) |
N=CR11R12 |
H |
Ph |
51.23 |
CH3 |
H |
3-Br(Ph) |
N=CR11R12 |
H |
Ph |
51.24 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
51.25 |
CH3 |
H |
2-CH3(Ph) |
N=CR11R12 |
H |
Ph |
51.26 |
CH3 |
H |
3-CH3(Ph) |
N=CR11R12 |
H |
Ph |
51.27 |
CH3 |
H |
2-CF3(Ph) |
N=CR11R12 |
H |
Ph |
51.28 |
CH3 |
H |
3-CF3(Ph) |
N=CR11R12 |
H |
Ph |
51.29 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
H |
Ph |
51.30 |
CH3 |
H |
2-NO2(Ph) |
N=CR11R12 |
H |
Ph |
51.31 |
CH3 |
H |
3-NO2(Ph) |
N=CR11R12 |
H |
Ph |
51.32 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
H |
Ph |
51.33 |
CH3 |
H |
2,3-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.34 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.35 |
CH3 |
H |
2,5-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.36 |
CH3 |
H |
2,6-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.37 |
CH3 |
H |
3,4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.38 |
CH3 |
H |
3,5-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.39 |
CH3 |
H |
Ph |
N=CR11R12 |
CH3 |
Ph |
51.40 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.41 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.42 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.43 |
CH3 |
H |
2-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.44 |
CH3 |
H |
3-Br(Ph) |
N=CR11Rx |
CH3 |
Ph |
51.45 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.46 |
CH3 |
H |
2-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.47 |
CH3 |
H |
3-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.48 |
CH3 |
H |
2-CF3(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.49 |
CH3 |
H |
3-CF3(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.50 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.51 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.52 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.53 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.54 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.55 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.56 |
CH3 |
H |
Ph |
N=CR11R12 |
Ph |
Ph |
51.57 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
51.58 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
51.59 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
51.60 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
51.61 |
CH3 |
H |
3-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
51.62 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
51.63 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
Ph |
51.64 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
Ph |
51.65 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
51.66 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
51.67 |
C2H5 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
51.68 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.69 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.70 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.71 |
C2H5 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.72 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.73 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.74 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.75 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.76 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.77 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.78 |
C2H5 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
51.79 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.80 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.81 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.82 |
C2H5 |
H |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
51.83 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
H |
Ph |
51.84 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
H |
Ph |
51.85 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
H |
Ph |
51.86 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
H |
Ph |
51.87 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.88 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
H |
Ph |
51.89 |
C2H5 |
H |
Ph |
N=CR11R12 |
CH3 |
Ph |
51.90 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.91 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.92 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.93 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.94 |
C2H5 |
H |
3-OCH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.95 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.96 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.97 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.98 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.99 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.100 |
C2H5 |
H |
Ph |
N=CR11R12 |
Ph |
Ph |
51.101 |
C2H5 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
51.102 |
C2H5 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
51.103 |
C2H5 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
51.104 |
C2H5 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
51.105 |
C2H5 |
H |
3-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
51.106 |
C2H5 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
Ph |
51.107 |
C2H5 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
Ph |
51.108 |
C2H5 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
Ph |
51.109 |
C2H5 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
51.110 |
C2H5 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
51.111 |
异-C3H7 |
H |
Ph |
N=CR11R12 |
CH3 |
CH3 |
51.112 |
异-C3H7 |
H |
2-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.113 |
异-C3H7 |
H |
3-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.114 |
异-C3H7 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
CH3 |
51.115 |
异-C3H7 |
H |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
51.116 |
异-C3H7 |
H |
3-OCH3(Ph) |
N=CR11R12 |
H |
Ph |
51.117 |
异-C3H7 |
H |
4-OCH3(Ph) |
N=CR11R12 |
H |
Ph |
51.118 |
异-C3H7 |
H |
4-CH3(Ph) |
N=CR11R12 |
H |
Ph |
51.119 |
异-C3H7 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.120 |
异-C3H7 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.121 |
异-C3H7 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.122 |
环丙基 |
H |
Ph |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.123 |
环内基 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.124 |
环丙基 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.125 |
环丙基 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.126 |
环丙基 |
H |
4-Br(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.127 |
环丙基 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.128 |
环丙基 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.129 |
环丙基 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.130 |
环丙基 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.131 |
环丙基 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.132 |
环丙基 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.133 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
51.134 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
51.135 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
51.136 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
51.137 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
CH3 |
51.138 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
51.139 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
51.140 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
51.141 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
51.142 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
H |
Ph |
51.143 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
51.144 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
51.145 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
51.146 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
51.147 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
Ph |
51.148 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
51.149 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
51.150 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
51.151 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
51.152 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
Ph |
Ph |
51.153 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
51.154 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
51.155 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
51.156 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
51.157 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
CH3 |
51.158 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
51.159 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
51.160 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
51.161 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
51.162 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
H |
Ph |
51.163 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
51.164 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
51.165 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
51.166 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
51.167 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
Ph |
51.168 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
51.169 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
51.170 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
51.171 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
51.172 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
Ph |
Ph |
51.173 |
CH3 |
H |
Ph |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.174 |
CH3 |
H |
2-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.175 |
CH3 |
H |
3-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.176 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.177 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.178 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.179 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.180 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.181 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.182 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.183 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.184 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.185 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.186 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.187 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.188 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.189 |
CH3 |
H |
Ph |
N=CR11R12 |
Ph |
4-吡啶基 |
51.190 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.191 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.192 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.193 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.194 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.195 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.196 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.197 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.198 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
Ph |
4-吡啶基 |
51.199 |
CH3 |
H |
Ph |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.200 |
CH3 |
H |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.201 |
CH3 |
H |
4-Br(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.202 |
CH3 |
H |
4-F(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.203 |
CH3 |
H |
4-OCH3(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.204 |
CH3 |
H |
4-CH3(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.205 |
CH3 |
H |
4-NO2(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.206 |
CH3 |
H |
2,4-Cl(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.207 |
CH3 |
H |
2,4-F(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.208 |
CH3 |
H |
4-CF3(Ph) |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.209 |
CH3 |
H |
Ph |
N=环戊基 | | |
51.210 |
CH3 |
H |
4-Cl(Ph) |
N=环戊基 | | |
51.211 |
CH3 |
H |
4-Br(Ph) |
N=环戊基 | | |
51.212 |
CH3 |
H |
4-F(Ph) |
N=环戊基 | | |
51.213 |
CH3 |
H |
4-OCH3(Ph) |
N=环戊基 | | |
51.214 |
CH3 |
H |
4-CH3(Ph) |
N=环戊基 | | |
51.215 |
CH3 |
H |
4-NO2(Ph) |
N=环戊基 | | |
51.216 |
CH3 |
H |
2,4-Cl(Ph) |
N=环戊基 | | |
51.217 |
CH3 |
H |
2,4-F(Ph) |
N=环戊基 | | |
51.218 |
CH3 |
H |
4-CF3(Ph) |
N=环戊基 | | |
51.219 |
CH3 |
H |
Ph |
N=环己基 | | |
51.220 |
CH3 |
H |
4-Cl(Ph) |
N=环己基 | | |
51.221 |
CH3 |
H |
4-Br(Ph) |
N=环己基 | | |
51.222 |
CH3 |
H |
4-F(Ph) |
N=环己基 | | |
51.223 |
CH3 |
H |
4-OCH3(Ph) |
N=环己基 | | |
51.224 |
CH3 |
H |
4-CH3(Ph) |
N=环己基 | | |
51.225 |
CH3 |
H |
4-NO2(Ph) |
N=环己基 | | |
51.226 |
CH3 |
H |
2,4-Cl(Ph) |
N=环己基 | | |
51.227 |
CH3 |
H |
2,4-F(Ph) |
N=环己基 | | |
51.228 |
CH3 |
H |
4-CF3(Ph) |
N=环己基 | | |
51.229 |
CH3 |
H |
1-萘基 |
N=环戊基 | | |
51.230 |
C2H5 |
H |
1-萘基 |
N=环戊基 | | |
51.231 |
正-C3H7 |
H |
1-萘基 |
N=环戊基 | | |
51.232 |
异-C3H7 |
H |
1-萘基 |
N=环戊基 | | |
51.233 |
环丙基 |
H |
1-萘基 |
N=环戊基 | | |
51.234 |
CH3 |
H |
1-萘基 |
N=环己基 | | |
51.235 |
C2H5 |
H |
1-萘基 |
N=环己基 | | |
51.236 |
正-C3H7 |
H |
1-萘基 |
N=环己基 | | |
51.237 |
异-C3H7 |
H |
1-萘基 |
N=环己基 | | |
51.238 |
环丙基 |
H |
1-萘基 |
N=环己基 | | |
51.239 |
CH3 |
H |
2-萘基 |
N=环戊基 | | |
51.240 |
C2H5 |
H |
2-萘基 |
N=环戊基 | | |
51.241 |
正-C3H7 |
H |
2-萘基 |
N=环戊基 | | |
51.242 |
异-C3H7 |
H |
2-萘基 |
N=环戊基 | | |
51.243 |
环丙基 |
H |
2-萘基 |
N=环戊基 | | |
51.244 |
CH3 |
H |
2-萘基 |
N=环己基 | | |
51.245 |
C2H5 |
H |
2-萘基 |
N=环己基 | | |
51.246 |
正-C3H7 |
H |
2-萘基 |
N=环己基 | | |
51.247 |
异-C3H7 |
H |
2-萘基 |
N=环己基 | | |
51.248 |
环丙基 |
H |
2-萘基 |
N=环己基 | | |
51.249 |
CH3 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.250 |
C2H5 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.251 |
正-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.252 |
异-C3H7 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.253 |
环丙基 |
H |
1-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.254 |
CH3 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.255 |
C2H5 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.256 |
正-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.257 |
异-C3H7 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.258 |
环丙基 |
H |
2-萘基 |
N=CR11R12 |
CH3 |
N(CH3)2 |
51.259 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
H |
Ph |
51.260 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
H |
Ph |
51.261 |
正-C3H7 |
CH3 |
4-Br(Ph) |
N=CR11R12 |
H |
Ph |
51.262 |
异-C3H7 |
CH3 |
4-F(Ph) |
N=CR11R12 |
H |
Ph |
51.263 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
CH3 |
Ph |
51.264 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.265 |
正-C3H7 |
CH3 |
4-Br(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.266 |
异-C3H7 |
CH3 |
4-F(Ph) |
N=CR11R12 |
CH3 |
Ph |
51.267 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
Ph |
Ph |
51.268 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
Ph |
Ph |
51.269 |
正-C3H7 |
CH3 |
4-Br(Ph) |
N=CR11R12 |
Ph |
Ph |
51.270 |
异-C3H7 |
CH3 |
4-F(Ph) |
N=CR11R12 |
Ph |
Ph |
51.271 |
CH3 |
CH3 |
Ph |
N=CR11R12 |
Ph |
4-Cl(Ph) |
51.272 |
C2H5 |
CH3 |
4-Cl(Ph) |
N=CR11R12 |
Ph |
4-Cl(Ph) |
表52:化合物52.1-52.226为式Ⅹ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NR10的式Ⅰ化合物,其中R10为N=C(H)Ph,且取代基R2、R3和R7如表4所定义。
表53:化合物53.1-53.226为式Ⅺ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NR10的式Ⅰ化合物,其中R10为N=C(H)Ph,且取代基R2、R3和R7如表4所定义。
表54:化合物54.1-54.226为式Ⅻ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NR10的式Ⅰ化合物,其中R10为N=C(H)Ph,且取代基R2、R3和R7如表4所定义。
表55:化合物55.1-55.221为式Ⅹ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NR10的式Ⅰ化合物,其中R10为N=C(CH3)Ph,且取代基R2、R3和R7如表7所定义。
表56:化合物56.1-56.221为式Ⅺ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NR10的式Ⅰ化合物,其中R10为N=C(CH3)Ph,且取代基R2、R3和R7如表7所定义。
表57:化合物57.1-57.221为式Ⅻ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NR10的式Ⅰ化合物,其中R10为N=C(CH3)Ph,且取代基R2、R3和R7如表7所定义。
表58:化合物58.1-58.139为式Ⅹ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=CH,Y=O及Z=NR10的式Ⅰ化合物,其中R10为N=CCPh2,且取代基R2、R3和R7如表7所定义。
表59:化合物59.1-59.139为式Ⅺ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=O及Z=NR10的式Ⅰ化合物,其中R10为N=CCPh2,且取代基R2、R3和R7如表7所定义。
表60:化合物60.1-60.139为式Ⅻ化合物,它们是A=R4=R5=R6=H,R1=CH3,X=N,Y=NH及Z=NR10的式Ⅰ化合物,其中R10为N=C=CPh2,且取代基R2、R3和R7如表7所定义。
在表1-60中所用的Ph应理解为苯基。
在US5,756,426和5,863,951以及本文引用的参考参考文献中,描述了某些双肟化合物的制备。用于制备本发明的式Ⅰ环丙基双肟化合物的具体方法描述在以下的流程中。流程A描述了其中X为CH或N,Y是O的式(Ⅰ)化合物(式ⅩⅤ和ⅩⅥ化合物)的制备。环丙基肟(ⅩⅢ)与适当取代的苄基衍生物(ⅩⅣ)反应,其中ⅩⅣ中L为卤素,如溴、氯或碘,优选苄基溴。通式(ⅩⅢ)表示的环丙基取代肟在室温下与适当的碱作用,形成阴离子,然后加入苄基溴(ⅩⅣ)。所用的碱一般是金属氢化物如氢化钠、烷醇如甲醇钠、氢氧化物碱如氢氧化钠或氢氧化钾,以及诸如碳酸钠或碳酸钾之类的碱性盐。使用氢化物作为碱时,常用溶剂为N,N-二甲基甲酰胺(DMF)和四氢呋喃(THF);使用氢氧化物作为碱时,常用溶剂为DMF、THF、甲乙酮(MEK)和丙酮;以及使用碱性盐作为碱时,溶剂如DMF、丙酮和MEK。如流程A所示,C(R2)=N-O-中的N-O键和
可以E和Z式异构体存在,应当认为E和Z异构体和混合物一样可以制备。当制得异构体时,将它们指定为异构体A(薄层色谱上的高Rf值)和异构体B(薄层色谱上的低Rf值),确定A或B哪个异构体具有E或Z几何构型,可以通过常规技术如晶体X射线或通过光谱学方法如核磁共振谱来实现。本发明的式Ⅰ化合物已经制备出C(R2)=N-O-中N-O键的单一立体异构体,并且已经通过核磁共振谱将其确定为E构型。此外,式Ⅰ化合物对于Z=C可以以异构体形式存在,应当认为区域异构体和混合物一样可以制备。当制得异构体时,将它们指定为异构体A(薄层色谱上的高Rf值)和异构体B(薄层色谱上的低Rf值),确定A或B哪个异构体具有E或Z几何构型,可以通过常规技术如晶体X射线或通过光谱学方法如核磁共振谱来实现。当Z为NOR9时,指定为异构体A的化合物对于R9ON=C具有E构型,指定为异构体B的化合物对于R9ON=C具有Z构型。在后面的表中,指定为异构体A或B的化合物,是指NOR9异构体。
流程A
式Ⅳ化合物(X为CH)的制备,是在碱(优选氢氧化钠或氢氧化钾)的存在下,于溶剂(优选丙酮或甲乙酮)中,用E-α-(2-溴甲基苯基)-β-甲氧基丙烯酸甲酯(ⅩⅣ,其中A=H,X=CH以及L是Br)进行烷基化作用。E-α-(2-溴甲基苯基)-β-甲氧基丙烯酸甲酯的单一E异构体,可以按照上述US专利号4914128,3-4栏所述,由2-甲基苯基乙酸酯经两个步骤制备。式Ⅳ化合物(X为N)的制备,是在碱(优选氢氧化钠或氢氧化钾)的存在下,于溶剂(优选丙酮或甲乙酮)中,与E-2-(溴甲基)苯基-乙醛酸甲酯的O-甲基肟(ⅩⅣ,其中A=H,X=N以及L是Br)进行反应。2-(溴甲基)苯基-乙醛酸甲酯的O-甲基肟可以按照US专利号4999042,第17-18栏和5157144第17-18栏所述进行制备。2-(溴甲基)苯基-乙醛酸甲酯的O-甲基肟的制备,是由2-甲基苯基乙酸酯出发,在碱性条件下和亚硝酸烷基酯作用,经甲基化作用后得到2-甲基苯基-乙醛酸甲酯的O-甲基肟,该化合物也可以从2-甲基苯基-乙醛酸甲酯出发,用羟胺盐酸盐处理并进行甲基化,或者用甲氧基胺盐酸盐处理。
如流程B所示,式ⅩⅧ化合物(X=N,Y=NH)可以通过肟基乙酸酯ⅩⅥ的氨解来制备。在US专利号5185342的第22、48和57栏,5221691的第26-27栏以及5407902的第8栏中,对肟基乙酸酯氨解为肟基乙酰胺已经有所描述,例如,X为N、Y为O的式Ⅷ的表14化合物,与40%含水甲胺的甲醇溶液作用,得到Y为NH的式Ⅸ的表15化合物。此外,如流程B所示,中间产物环丙烷肟ⅩⅢ与N-甲基(E)-2-甲氧基亚胺基-2-[2-(溴甲基)苯基]-乙酰胺(ⅩⅣ,其中A=H,L=Br),在诸如氢氧化物碱的存在下,优选在诸如丙酮或甲乙酮的溶剂中进行反应,得到式Ⅸ的表15化合物。N-甲基(E)-2-甲氧基亚胺基-2-[2-(溴甲基)苯基]-乙酰胺描述于US专利号5387714的第14栏。
Z为O的式Ⅰ化合物的合成如流程C所示,和遵循流程A和B进行。在流程C中,式Ⅳ和化合物(A=H)可以由肟ⅩⅨ,用ⅩⅣ进行烷基化来制备。式Ⅳ化合物(A=H)的制备,可以将ⅩⅨ用溴化物ⅩⅦ烷基化,或者如流程C所示将进行氨解。
按照流程D所示,制备Z为NOR
9的式Ⅰ化合物(式Ⅻ、Ⅷ、Ⅸ化合物),可以将化合物Ⅳ、Ⅴ和Ⅵ与如R
9ONH
2的羟胺进行缩合。该缩合反应可以适当的碱(如氢氧化钠、碳酸钾或吡啶)的存在下、适当的溶剂(如甲醇或乙醇)中,于室温至回流温度下(优选室温)进行。此外,也可以使用盐酸羟胺(R
9是H),得到化合物Ⅶ'、Ⅷ'和Ⅸ',用R
9-L(其中L是离去基团如Br或Cl)进行烷基化得到化合物Ⅶ、Ⅷ、Ⅸ。如流程D所示,Z为NR
10的式Ⅹ、Ⅺ和Ⅻ化合物如亚胺和腙化合物的制备是通过将酮化合物Ⅳ、Ⅴ和Ⅵ与胺或肼的衍生物进行缩合。March,Advanced Organic Chemistrv,第4版,第896-897,904-907页对肟和亚胺的合成进行了概括性的描述,在此引作参考。若所得到的是顺式和反式的混合物时,通式Ⅶ-Ⅻ的肟、亚胺和腙可以通过常规的色谱技术分离为单一异构体。在薄层色谱上具有高R
f值的异构体指定为异构体A,在薄层色谱上具有低R
f值的异构体指定为异构体B,异构体A和B的立体化学可以通过常规技术如核磁共振谱来确定。
如流程E所示,通过流程B所述的缩合方法,可以得到肟中间体ⅩⅨ,由此制备式Ⅶ-Ⅻ化合物,得到肟中间体ⅩⅩ和ⅩⅪ,这些肟中间体可以按照流程A、B和C所述进行烷基化,得到产物Ⅶ-Ⅻ。
通式ⅩⅨ表示的肟可以按照流程F所示得到,March,AdvancedOrganic Chemistrv,第4版,第592-593页对经过亚硝化合成α-肟酮进行了概括性的描述,在此引作参考。要得到本发明化合物,在碱性条件下将环丙基酮ⅩⅫ与亚硝酸烷基酯(如亚硝酸叔丁酯,或亚硝酸异戊酯)反应得到相应的α-肟基环丙基酮。如流程F所示,该肟基中间体ⅩⅨ一般得到的是一种立体异构体立体异构体主。将溶于溶剂如叔丁醇和亚硝酸酯,典型的是亚硝酸叔丁酯中的环丙基酮加入含有碱如叔丁醇钾的叔丁醇之中,并在试问下搅拌。按照流程C和E所述,将α-肟基环丙基酮ⅩⅨ进行烷基化,得到式Ⅳ、Ⅴ和Ⅵ化合物。
环丙基酮ⅩⅫ可以按照流程G所示的常规方法来制备。将不饱和中间体ⅩⅩⅢ(流程G)与硫叶立德(在碱的存在下,从二甲基氧化锍盐制备)反应,得到取代的酰基环丙烷ⅩⅫ。硫叶立德化学的描述参见Trost和Melvin,Sulfur Ylids,Academic Press,New York,NY,1975,以及Block,Reactions of Organosulfur Compounds,pp.91-123,Academic Press,New York,NY,1978。从二甲基氧化锍盐形成硫叶立德的一般反应条件是使用诸如氢氧化物、金属氢化物和烷氧化物的碱,在诸如二甲氧基乙烷、二甲亚砜和水的溶剂中进行,所用溶剂依赖于使用的碱。反应0-20℃,优选10-15℃下进行,并优选在二甲亚砜中使用碱金属氢氧化物。通常,二甲基甲基锍盐是在二甲亚砜中,在室温和氢氧化钠粉末存在下,由碘化三甲基氧化锍制得的。一般将不饱和酮ⅩⅩⅢ滴加到该叶立德中,并在室温下搅拌。
α,β-不饱和酮ⅩⅩⅢ可以按照常规的缩合方法制备,March,Advanced Organic Chemistry,第4版,第937-955页对α,β-不饱和酮(烯酮)的合成进行了广泛的描述,在此引作参考。例如,Organic Reactions,Volume 16描述了酮和醛的一般的羟醛缩合。要得到本发明的式ⅩⅩⅢ中间体,所用的酮通常可以是R7COR6,其R7和R6中如前面所定义。例如,当R6是氢时,醛是取代的苯甲醛或杂环基甲醛。酮可以是R2CH2COCH2R3,其中R2和R3如前面所定义。要通过缩合反应生成烯酮,优选R3是氢,即甲基酮。同样,R2可以是氢,由它得到的烯酮和环丙烷,可生成R2是氢的式Ⅰ化合物。一般将酮R2CH2COCH2R3溶于羟基溶剂如甲醇或乙醇,往其中滴加醛或酮R7COR6,然后加入碱,或者加入醛的碱性水溶液,常用的碱是碱金属氢氧化物,如钡、钾或钠的氢氧化物,滴加是在0℃-35℃,优选在室温下进行。由甲基酮(R3是氢)生成烯酮时,溶剂可以是甲基酮,往其中加入R7COR6,然后加入氢氧化物水溶液。
此外,α,β-不饱和酮ⅩⅩⅢ可以环丙基腈ⅩⅩⅤ制备,该环丙基腈可以通过丙烯腈ⅩⅩⅣ的环丙烷化制备,如流程H所示。制备流程H所示的起始物丙烯腈ⅩⅩⅣ可以按照March在Advanced OrganicChemistry,第4版,第937-955页所述的方法制备,在此引作参考。例如,腈衍生物R3CH2CN与酮或醛R7COR6,在碱的存在下进行缩合,得到丙烯腈ⅩⅩⅣ。优选R3CH2CN中的R3是前述R3所定义的芳基或杂芳基,一般将腈溶于诸如乙醇和水的溶剂中,往其中加入醛或酮,然后加入碱,常用的碱是碱金属氨氧化物,如钡、钾或钠的氢氧化物,混合物一般室温下进行搅拌。丙烯腈ⅩⅩⅣ按照流程H所述用硫叶立德处理,得到环丙基腈ⅩⅩⅤ,环丙基腈ⅩⅩⅤ通过有机金属对腈的加成反应,随后水解转化为环丙基酮。例如常规的Grignard试剂R2CH2MgX或有机锂试剂R2CH2Li加成到腈官能团上,得到酮ⅩⅫ。有关腈加成反应的描述参见March,Advanced Organic Chemistry,第4版,第935-936页和本文引用的文献。当R2MgX是甲基Grignard试剂如甲基溴化镁时,得到甲基酮。R2=H时所得到的本发明化合物,其中的R2=H。
本发明化合物可以按照下述方法来制备:实施例1
制备(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂戊-3-烯-1-基)苯基]丙烯酸甲酯,表1的1.11化合物反式-1-苯基-1-戊烯-3-酮的制备
往装备有磁搅拌器的250ml圆底烧瓶中装入36g(0.5mol)甲乙酮、100ml乙醇和10ml水,向该溶液中加入0.5g一水合氢氧化钡,然后加入10.6g(0.1mol)的苯甲醛,塞住烧瓶,于室温下搅拌过夜,将反应混合物中倒入200ml水中,并用3×100ml乙醚萃取,乙醚萃取液用100ml饱和的亚硫酸氢钠水溶液洗涤,然后用100ml水和100ml饱和的氯化钠水溶液洗涤,乙醚萃取液用无水硫酸镁干燥、过滤并在旋转蒸发器上浓缩,以94%的分离产率得到15.1g浅黄色液体,根据300MHz 1H NMR分析,该产物与所需的反式-1-苯基-1-戊烯-3-酮一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)1.17(t,3H),2.7(q,2H),6.7(d,1H),7.4(m,3H),7.6(m,3H)反式-2-苯基环丙基乙基酮的制备
往装备有磁搅拌器、氮气进口和等压加料漏斗的500ml圆底烧瓶中装入22g(0.1mol)碘化三甲基氧化锍、4.0g(0.1mol)氢氧化钠粉末和150ml二甲亚砜。该溶液于室温下搅拌30分钟,随后快速加入反式-1-苯基-1-戊烯-3-酮(15.1g,0.0945mol)的100ml二甲亚砜溶液,于室温下搅拌反应10分钟,然后倒入200ml水中,并用3×100ml乙醚萃取,乙醚萃取液用2×100ml水和100ml饱和的氯化钠水溶液洗涤,乙醚萃取液用无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到12.5g浓稠黄色液体,高真空蒸馏纯化(78-85℃ @ 0.1mm Hg),合并纯净馏分,以50%分离产率得到8.2g无色透明液体,根据300MHz1H NMR分析,该产物与所需的反式-2-苯基环丙基乙基酮一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)1.1(t,3H),1.3(m,1H),1.7(m,1H),2.2(m,1H),2.5(m,1H),2.6(q,2H),7.1(d,2H),7.2-7.4(m,3H)。2-肟基-1-(反式-2-苯基环丙基)-1-丙酮的制备
往装备有磁搅拌器、氮气进口、回流冷凝器和侧臂滴液漏斗的干燥500ml圆底烧瓶中装入5.7g(0.0505mol)叔丁醇钾和150ml叔丁醇。当固体全部溶解时,一次加入反式-2-苯基环丙基乙基酮(8.0g,0.0459mol),然后滴加5.7g(0.0505mol)90%亚硝酸叔丁酯,于室温下搅拌反应3小时,然后小心地用100ml的0.1N盐酸水溶液终止反应。混合物用3×100ml乙醚萃取,乙醚萃取液用2×100ml水和100ml饱和的氯化钠水溶液洗涤,然后萃取液用无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到8.2g浓稠棕色液体,用二氯甲烷和己烷结晶,真空过滤,收集得到的固体,以55%分离产率得到5.1g黄褐色固体,根据300MHz 1H NMR分析,该产物与所需的2-肟基-1-(反式-2-苯基环丙基)-1-丙酮一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)1.4(m,1H),1.7(m,1H),2.0(s,3H),2.6(m,1H),3.1(m,1H),7.1(d,2H),7.2-7.4(m,3H),8.1(bs,1H)。制备(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂戊-3-烯-1-基)苯基]丙烯酸甲酯
往装备有磁搅拌器的250ml圆底烧瓶中装入溶于100ml无水二甲亚砜的3.0g(0.0148mol)2-肟基-1-(反式-2-苯基环丙基)-1-丙酮和4.1g(0.0295mol)碳酸钾粉末。于室温下搅拌反应混合物共0.5小时,然后一次加入(E)-α-[2-(溴甲基)苯基]-β-甲氧基丙烯酸甲酯(4.2g,0.0148mol)。塞封反应器,于室温下搅拌过夜。将反应混合物中倒入100ml水中,并用3×100ml乙醚萃取,乙醚萃取液用2×100ml水和100ml饱和的氯化钠水溶液洗涤,无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到6.0g浓稠琥珀色液体,用20%乙酸乙酯和80%己烷进行硅胶色谱纯化,合并纯馏分,在旋转蒸发器上浓缩,以91.3%分离产率得到5.5g浓稠的浅黄色油,根据300MHz 1H NMR分析,该产物与所需(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂戊-3-烯-1-基)苯基]丙烯酸甲酯的单一肟异构体相一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)1.4(m,1H),1.7(m,1H),1.95(s,3H),2.55(m,1H),3.2(m,1H),3.65(s,3H),3.75(s,3H),5.2(s,2H),7.1-7.4(m,9H),7.5(s,1H)实施例2
制备(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂辛-3,5-二烯-1-基)苯基]丙烯酸甲酯的甲氧基亚胺异构体A-表13的13.18A化合物
往装备有磁搅拌器的1000ml圆底烧瓶中装入溶于600ml无水甲醇的56.4g(0.138mol)(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂戊-3-烯-1-基)苯基]丙烯酸甲酯、23.2g(0.277mol)甲氧基胺盐酸盐和22g(0.277mol)无水吡啶,反应混合物于室温下共搅拌24小时,然后回流约2小时,冷却反应混合物并倒入1000ml水中,以3×200ml乙醚萃取,乙醚萃取液用200ml的0.1N盐酸水溶液、2×100ml水和200ml饱和氯化钠洗涤,无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到62g浓稠琥珀色液体,用20%乙酸乙酯、80%己烷进行硅胶色谱纯化,合并纯馏分,在旋转蒸发器上浓缩,以79.8%分离产率得到48g浓稠浅黄色油,根据300MHz 1H NMR分析,该产物与所需(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂辛-3,5-二烯-1-基)苯基]丙烯酸甲酯的甲氧基亚胺异构体A相一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)1.2(m,1H),1.8(m,1H),2.0(s,3H),2.45(m,1H),2.7(m,1H),3.66(s,3H),3.75(s,3H),3.9(s,3H),5.1(s,2H),7.1-7.4(m,9H),7.56(s,lH)。实施例3
制备(E)-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂戊-3-烯-1-烯-1-基)苯基]-2-甲氧基亚胺基乙酸甲酯-表2的2.1lA化合物
往装备有磁搅拌器的250ml圆底烧瓶中装入溶于100ml无水二甲基甲酰胺的2.0g(0.00985mol)2-肟基-1-(反式-2-苯基环丙基)-l-丙酮和2.58g(0.0197mol)碳酸钾粉末。于室温下搅拌反应混合物共0.5小时,然后一次加入2-(溴甲基)苯基乙醛酸甲酯(2.8g,0.00985mol)。塞封反应器,于室温下搅拌过夜,将反应混合物中倒入100ml水中,并用3×100ml乙醚萃取,乙醚萃取液用2×100ml水和100ml饱和的氯化钠水溶液洗涤,无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,以100%分离产率得到4.1g浓稠琥珀色液体。根据300MHz 1HNMR分析,该产物与所需(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂戊-3-烯-1-基)苯基]-2-甲氧基亚胺基乙酸甲酯相一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)1.4(m,1H),1.7(m,1H),1.95(s,3H),2.55(m,1H),3.1(m,1H),3.8(s,3H),4.0(s,3H),5.15(s,2H),7.1-7.4(m,9H)实施例4
制备(E)-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂辛-3,5-二烯-1-基)苯基]-2-甲氧基亚胺基乙酸甲酯的甲氧基亚胺异构体A-表14的14.18A化合物
往装备有磁搅拌器的1000ml圆底烧瓶中装入溶于600ml无水甲醇的87g(0.213mol)(E)-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂戊-3-烯-1-基)苯基]-2-甲氧基亚胺基乙酸甲酯、35.6g(0.426mol)甲氧基胺盐酸盐和33.7g(0.426mol)无水吡啶,反应混合物于室温下共搅拌24小时,然后回流约2小时,冷却反应混合物并倒入1000ml水中,用3×200ml乙醚萃取,乙醚萃取液用200ml的0.1N盐酸水溶液、2×100ml水和200ml饱和氯化钠水溶液洗涤,无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到浓稠琥珀色液体,在己烷中形成浆液,放置结晶,真空过滤收集,以71%分离产率得到66.1g黄褐色固体,根据300MHz 1H NMR分析,该产物与所需(E)-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂辛-3,5-二烯-1-基)苯基]-2-甲氧基亚胺基乙酸甲酯的甲氧基亚胺异构体A相一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)1.1(m,1H),1.8(m,lH),2.0(s,3H),2.45(m,1H),2.7(m,1H),3.8(s,3H),3.9(s,3H),4.0(s,3H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H)实施例5
制备N-甲基(E)-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂辛-3,5-二烯-1-基)苯基]-2-甲氧基亚胺基乙酰胺的甲氧基亚胺异构体A-表15的15.18A化合物
往装备有磁搅拌器的1000ml圆底烧瓶中装入66.1g(0.151mol)(E)-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂辛-3,5-二烯-1-基)苯基]-2-甲氧基亚胺基乙酸甲酯的甲氧基亚胺异构体A、500ml无水甲醇和23.5g(0.3mol)40%甲胺水溶液,反应混合物于室温下共搅拌24小时,然后倒入1000ml水中,用3×200ml乙醚萃取,乙醚萃取液用200ml的0.1N盐酸水溶液、2×100ml水和200ml饱和氯化钠水溶液洗涤,无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到浓稠琥珀色液体,放置结晶,以94%分离产率得到62g黄褐色固体,根据300MHz 1H NMR分析,该产物与所需N-甲基(E)-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂辛-3,5-二烯-1-基)苯基]-2-甲氧基亚胺基乙酰胺的甲氧基亚胺异构体A相一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)1.2(m,1H),1.8(m,1H),2.0(s,3H),2.45(m,lH),2.8(m,1H),2.9(d,3H),3.9(s,3H),3.92(s,3H),5.0(s,2H),6.8(bs,1H),7.0(d,2H),7.1-7.4(m,7H)。实施例6
制备(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂庚-3-烯-1-基)苯基]丙烯酸甲酯,表1的1.67化合物反式5-甲基-1-苯基-1-己烯-3-酮的制备
往装备有磁搅拌器的250ml圆底烧瓶中装入11.6g(0.116mol)4-甲基-2-戊酮、100ml乙醇和10ml水,向该溶液中加入0.5g一水合氢氧化钡,然后加入12.3g(0.116mol)的苯甲醛,塞住烧瓶,于室温下搅拌过夜。将反应混合物中倒入200ml水中,并用3×100ml乙醚萃取,乙醚萃取液用100ml饱和的亚硫酸氢钠水溶液洗涤,然后用100ml水和100ml饱和的氯化钠水溶液洗涤。乙醚萃取液用无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,以91%的分离产率得到19.8g浅黄色液体,根据300MHz 1H NMR分析,该产物与所需的反式5-甲基-1-苯基-1-己烯-3-酮一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)0.99(d,6H),2.2(m,1H),2.5(d,2H),7.7(d,1H),7.4(m,3H),7.6(m,3H)反式-2-苯基环丙基异丁基酮的制备
往装备有磁搅拌器、氮气进口和等压加料漏斗的500ml圆底烧瓶中装入23g(0.104mol)碘化三甲基氧化锍、4.2g(0.104mol)氢氧化钠粉末和150ml二甲亚砜。该溶液于室温下搅拌30分钟,随后快速加入反式5-甲基-1-苯基-1-己烯-3-酮(19.6g,0.104mol)的100ml二甲亚砜溶液,于室温下搅拌反应60mol,然后倒入200ml水中,并用3×100ml乙醚萃取,乙醚萃取液用2×100ml水和100ml饱和的氯化钠水溶液洗涤,萃取液用无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,以87.6%分离产率得到18.4g浓稠黄色液体,根据300MHz 1H NMR分析,该产物与所需的反式-2-苯基环丙基异丁基酮一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)0.95(d,6H),1.4(m,1H),1.7(m,1H),2.2(m,2H),2.4(d,2H),2.45(m,1H),7.1(d,2H),7.2-7.4(m,3H)。2-肟基-3-甲基-1-(反式-2-苯基环丙基)-1-丁酮的制备
往装备有磁搅拌器、氮气进口、回流冷凝器和侧臂滴液漏斗的干燥500ml圆底烧瓶中装入11.2g(0.1mol)叔丁醇钾和150ml叔丁醇。当固体全部溶解时,一次加入反式-2-苯基环丙基异丁基酮(18.4g,0.0911mol),然后滴加32g(0.282mol)90%亚硝酸叔丁酯,于室温下搅拌反应3小时,然后小心地用100ml的0.1N盐酸水溶液终止反应。混合物用3×100ml乙醚萃取,乙醚萃取液用2×100ml水和100ml饱和的氯化钠水溶液洗涤,萃取液用无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到9.1g浓稠棕色液体,放置结晶,将所得固体在己烷中形成浆液,真空过滤收集,以40%分离产率得到8.4g黄褐色固体,根据300MHz 1H NMR分析,该产物与所需的2-肟基-3-甲基-1-(反式-2-苯基环丙基)-1-丁酮的单一肟基异构体一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)1.2(d,6H),1.3(m,1H),1.7(m,1H),2.5(m,1H),3.1(m,1H),3.4(q,1H),7.1(d,2H),7.2-7.4(m,3H),8.1(1)s,1H)。制备(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂庚-3-烯-1-基)苯基]丙烯酸甲酯
往装备有磁搅拌器的50ml圆底烧瓶中装入1.0g(0.00432mol)2-肟基-3-甲基-1-(反式-2-苯基环丙基)-1-丁酮、10ml无水二甲基甲酰胺和1.2g(0.00865mol)碳酸钾粉末。于室温下搅拌反应混合物共0.5小时,然后一次加入(E)-α-[2-溴甲基)苯基]-β-甲氧基丙烯酸甲酯(1.3g,0.00432mol)。塞闭反应器,于室温下搅拌过夜,将反应混合物中倒入100ml水中,并用3×100ml乙醚萃取,乙醚萃取液用2×100ml水和100ml饱和的氯化钠水溶液洗涤,无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到1.8g浓稠琥珀色液体,用20%乙酸乙酯和80%己烷进行硅胶色谱纯化,合并纯馏分,在旋转蒸发器上浓缩,以64%分离产率得到1.2g浓稠浅黄色油,根据300MHz 1H NMR分析,该产物与所需(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂庚-3-烯-1-基)苯基]丙烯酸甲酯的单一肟基异构体相一致。
NMR(300MHz,1H NMR,CDCl3,TMS=0ppm)1.2(d,6H),1.3(m,1H),1.6(m,1H),2.55(m,1H),3.1(m,1H),3.4(q,1H),3.7(s,3H),3.78(s,3H),5.15(s,2H),7.1-7.5(m,9H),7.6(s,1H)实施例7
制备(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-异丙基-2,7-二氧杂-3,6-二氮杂辛-3,5-二烯-1-基)苯基]丙烯酸甲酯的甲氧基亚胺异构体A和B-表13的13.67A和13.67B化合物
往装备有磁搅拌器的100ml圆底烧瓶中装入1.0g(0.00229mol)(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂庚-3-烯-1-基)苯基]丙烯酸甲酯、50ml无水甲醇、1.0g(0.0115mol)甲氧基胺盐酸盐和1.0g(0.0115mol)无水吡啶,反应混合物于室温下共搅拌24小时,然后回流约10mol,冷却反应混合物并倒入100ml水中,以3×100ml乙醚萃取,乙醚萃取液用100ml的0.1N盐酸水溶液、2×100ml水和100ml饱和氯化钠水溶液洗涤,无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到1.1g浓稠琥珀色液体,用20%乙酸乙酯、80%己烷进行硅胶色谱纯化,合并纯馏分,在旋转蒸发器上浓缩,得到350mg浓稠浅黄色油,根据300MHz 1H NMR分析,与所需(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-异丙基-2,7-二氧杂-3,6-二氮杂辛-3,5-二烯-1-基)苯基]丙烯酸甲酯的甲氧基亚胺异构体A相一致,还得到530mg浓稠浅黄色油,根据300MHz 1H NMR分析,与所需(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-异丙基-2,7-二氧杂-3,6-二氮杂辛-3,5-二烯-1-基)苯基]丙烯酸甲酯的甲氧基亚胺异构体B相一致。总的分离产率为85%。
甲氧基亚胺异构体A:NMR(300MHz,1H NMR,CDCl3,TMS=0ppm)1.2(m,7H),1.3(m,lH),2.2(m,1H),2.4(m,1H),3.4(q,1H),3.7(s,3H),3.78(s,3H),3.9(s,3H),5.05(s,2H),7.1-7.5(m,9H),7.6(s,1H)
甲氧基亚胺异构体B:NMR(300MHz,1H NMR,CDCl3,TMS=0ppm)1.2(m,7H),1.3(m,1H),1.8(m,1H),2.2(m,1H),3.1(q,1H),3.6(s,3H),3.70(s,3H),3.75(s,3H),5.0(s,2H),7.1-7.4(m,9H),7.5(s,1H)。实施例8
制备(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂庚-3,5-二烯-1-基)苯基]丙烯酸甲酯的羟基亚胺异构体A-表13的13.11A化合物
往装备有磁搅拌器的100ml圆底烧瓶中装入1.0g(0.00245mol)(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂戊-3-烯-1-基)苯基]丙烯酸甲酯单一肟基异构体、50ml无水甲醇、1.7g(0.0245mol)盐酸羟胺和1.9g(0.0245mol)无水吡啶,反应混合物于室温下共搅拌24小时,然后回流约2小时,冷却反应混合物并倒入100ml水中,以3×100ml乙醚萃取,乙醚萃取液用100ml的0.1N盐酸水溶液、2×100ml水和100ml饱和氯化钠水溶液洗涤,无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到1.1g浓稠琥珀色液体,用15%乙酸乙酯、85%己烷进行硅胶色谱纯化,合并纯馏分,在旋转蒸发器上浓缩,以63%分离产率得到650mg浓稠无色透明油,根据300MHz1H NMR分析,该产物与所需(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂庚-3,5-二烯-1-基)苯基]丙烯酸甲酯的羟基亚胺异构体A相一致。
NMR(300MHz,1H,CDCl3,TMS=0ppm)1.8(m,1H),2.0(s,3H),2.5(m,1H),2.7(m,1H),3.65(s,3H),3.75(s,3H),5.05(s,2H),7.1(d,2H),7.2-7.5(m,7H),7.56(s,1H),8.3(bs,1H)实施例9
制备(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂-3,5-二烯-1-基)苯基]丙烯酸甲酯的n-丙氧基亚胺异构体A-表13的13.40A化合物
往装备有磁搅拌器的50ml圆底烧瓶中装入0.2g(0.000474mol)(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂庚-3,5-二烯-1-基)苯基]丙烯酸甲酯的羟基亚胺异构体A、10ml无水二甲亚砜和0.13g(0.00095mol)碳酸钾粉末。于室温下搅拌反应混合物共0.5小时,然后一次加入1-溴丙烷(0.065g,0.0005mol)。塞封反应器,于室温下搅拌过夜,将反应混合物中倒入100ml水中,并用3×100ml乙醚萃取,乙醚萃取液用2×100ml水和100ml饱和的氯化钠水溶液洗涤,无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,得到0.2g浓稠琥珀色液体,用20%乙酸乙酯、80%己烷进行硅胶色谱纯化,合并纯馏分,在旋转蒸发器上浓缩,以55%分离产率得到120mg浓稠无色透明油。根据300MHz 1H NMR分析,该产物与所需((E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2,7-二氧杂-3,6-二氮杂癸-3,5-二烯-1-基)苯基]丙烯酸甲酯的n-丙氧基亚胺异构体A相一致。
NMR(300MHz,1H NMR,CDCl3,TMS=0ppm)0.85(t,3H),1.1(m,1H),1.6(q,2H),1.8(m,1H),2.0(s,3H),2.4(m,lH),2.6(m,1H),3.6(s,3H),3.7(s,3H),4.0(t,2H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H),7.6(s,1H)实施例10
制备(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-8,8-二甲基-2,7-二氧杂-3,6-二氮杂壬-3,5-二烯-1-基)苯基]丙烯酸甲酯-表13的13.43化合物
往装备有磁搅拌器的100ml圆底烧瓶中装入0.5g(0.00122mol)(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-2-氧杂-5-氧代-3-氮杂戊-3-烯-1-基)苯基]丙烯酸甲酯单一肟基异构体、50ml无水甲醇、1.5g(0.0122mol)O-叔丁基盐酸羟胺和0.98g(0.0122mol)无水吡啶。反应混合物于室温下共搅拌24小时,然后回流约2小时,冷却反应混合物并倒入100ml水中,以3×100ml乙醚萃取,乙醚萃取液用100ml的0.1N盐酸水溶液、2×100ml水和100ml饱和氯化钠水溶液洗涤,无水硫酸镁干燥,过滤并在旋转蒸发器上浓缩,以100%分离产率得到0.6g浓稠黄色液体,根据300MHz 1H NMR分析,该产物与所需(E)-3-甲氧基-2-[2-(5-反式-(2-苯基环丙基)-4-甲基-8,8-二甲基-2,7-二氧杂-3,6-二氮杂癸-3,5-二烯-1-基)苯基]丙烯酸甲酯的叔丁基亚胺异构体混合物相一致。
NMR(300MHz,1H NMR,TMS=0ppm)1.2(m,10H),1.8(m,1H),2.0(s,3H),2.4(m,lH),2.6(m,lH),3.6(s,3H),3.7(s,3H),4.0(t,2H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H),7.6(s,1H)。
表61给出了表1-60中有代表性的实施例的质子NMR数据(300MHz),是对本发明的例证*。
表61
化合物# |
NMR数据 |
1.11 |
1.4(m,1H),1.8(m,1H),1.95(s,3H),2.5(m,1H),3.15(m,1H),3.65(s,3H),3.75(s,3H),5.2(s,2H),7.1-7.4(m,9H),7.55(s,1H) |
1.22 |
1.5(m,1H),1.8(m,1H),1.95(s,3H),2.6(m,1H),3.1(m,1H),3.65(s,3H),3.75(s,3H),3.8(s,3H),5.2(s,2H),6.8(m,3H),7.1-7.4(m,5H),7.55(s,1H) |
1.24 |
1.4(m,1H),1.75(m,1H),2.0(s,3H),2.3(s,3H),2.5(m,1H),3.1(m,1H),3.65(s,3H),3.75(s,3H),5.2(s,2H),7.1-7.4(m,8H),7.55(s,1H) |
1.25 |
1.5(m,1H),1.8(m,1H),1.95(s,3H),2.35(s,3H),2.5(m,1H),3.1(m,1H),3.65(s,3H),3.75(s,3H),5.2(s,2H),7.0-7.5(m,8H),7.55(s,1H) |
1.56 |
0.85(t,3H),1.4(m,3H),1.7(m,1H),2.5(m,3H),3.1(m,1H),3.7(s,3H),3.75(s,3H),5.2(s,2H),7.1-7.4(m,9H),7.6(s,1H) |
1.67 |
1.2(d,6H),1.3(m,1H),1.7(m,1H),2.5(m,1H),3.1(m,1H),3.4(m,1H),3.7(s,3H),3.75(s,3H),5.15(s,2H),7.0-7.5(m,9H),7.6(s,1H) |
1.78 |
0.9(t,3H),1.4(m,5H),1.8(m,1H),2.5(m,3H),3.2(m,1H),3.65(s,3H),3.75(s,3H),5.2(s,2H),7.1-7.4(m,9H),7.55(s,1H) |
2.1 |
1.4(m,1H),1.8(m,1H),2.6(m,1H),3.05(m,1H),3.8(s,3H),4.0(s,3H),5.2(s, |
|
2H),7.1-7.45(m,9H),7.5(s,1H) |
2.11 |
1.4(m,1H),1.8(m,1H),1.95(s,3H),2.5(m,1H),3.1(m,1H),3.8(s,3H),3.95(s,3H),5.15(s,2H),7.1-7.5(m,9H) |
2.14 |
1.4(m,1H),1.8(m,1H),1.95(s,3H),2.5(m,1H),3.1(m,1H),3.9(s,3H),4.05(s,3H),5.15(s,2H),7.0(d,2H),7.1-7.5(m,6H) |
2.22 |
1.45(m,1H),1.7(m,1H),1.9(s,3H),2.6(m,1H),3.1(m,1H),3.79(s,3H),3.8(s,3H),4.0(s,3H),5.2(s,2H),6.8(m,3H),7.1-7.4(m,5H) |
2.24 |
1.4(m,1H),1.75(m,1H),2.0(s,3H),2.25(s,3H),2.5(m,1H),3.05(m,1H),3.8(s,3H),4.0(s,3H),5.2(s,2H),7.1-7.4(m,8H) |
2.25 |
1.5(m,1H),1.8(m,1H),1.95(s,3H),2.3(s,3H),2.6(m,1H),3.1(m,1H),3.8(s,3H),4.0(s,3H),5.2(s,2H),7.1-7.4(m,8H) |
2.45 |
0.95(t,3H),1.3(m,1H),1.8(m,1H),2.5(m,3H),3.2(m,1H),3.7(s,3H),3.75(s,3H),5.2(s,2H),7.0-7.5(m,9H),7.55(s,1H) |
2.45 |
1.0(t,3H),1.3(m,1H),1.8(m,1H),2.5(m,3H),3.1(m,1H),3.8(s,3H),4.0(s,3H),5.15(s,2H),7.0-7.5(m,9H) |
2.56 |
0.9(t,3H),1.4(m,3H),1.7(m,1H),2.5(m,3H),3.1(m,1H),3.8(s,3H),4.0(s,3H),5.1(s,2H),7.1-7.4(m,9H) |
2.67 |
1.15(d,6H),1.25(m,1H),1.7(m,1H),2.5(m,1H),3.1(m,1H),3.4(m,1H),3.8(s,3H),4.0(s,3H),5.1(s,2H),7.0-7.5(m,9H) |
2.78 |
0.85(t,3H),1.4(m,5H),1.75(m,1H),2.5(m,3H),3.2(m,1H),3.8(s,3H),4.0(s,3H),5.15(s,2H),7.1-7.5(m,9H) |
3.22 |
1.4(m,1H),1.7(m,1H),1.85(s,3H),2.5(m,1H),2.8(d,3H),3.1(m,1H),3.75(s,3H),3.85(s,3H),5.1(s,2H),6.8(m,3H),7.1-7.4(m,6H) |
10.5 |
1.0(d,6H),1.3(m,1H),1.6(m,2H),3.55(m,1H),3.65(s,3H),3.75(s,3H),5.0(s,2H),7.1-7.4(m,9H),7.55(s,1H) |
13.7 |
1.15-1.3(m,2H),2.15-2.25(m,1H),2.26-2.4(m,1H),3.65(s,3H),3.85(s,3H),5.07(s,2H),7.0-7.6(m,10H),7.56(s,1H),8.33(s,1H) |
13.11A |
1.8(m,1H),2.0(s,3H),2.5(m,1H),2.7(m,1H),3.65(s,3H),3.75(s,3H),5.05(s,2H),7.1(d,2H),7.2-7.5(m,7H),7.56(s,1H),8.3(bs,1H) |
13.18A |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.45(m,1H),2.7(m,1H),3.66(s,3H),3.75(s,3H),3.9(s,3H),5.1(s,2H),7.1-7.4(m,9H),7.56(s,1H) |
13.18B |
1.2(m,1H),1.4(m,1H),1.8(m,1H),1.95(s,3H),2.2(m,1H),3.6(s,3H),3.7(s,3H),3.85(s,3H),5.1(s,2H),6.9(d,2H),7.1-7.4(m,7H),7.56(s,1H) |
13.20A |
1.1(m,1H),1.8(m,1H),2.0(s,3H),2.4(m,1H),2.7(m,1H),3.6(s,3H),3.7(s,3H),3.85(s,3H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,6H),7.6(s,1H) |
13.22A |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.4(m,1H),2.9(m,1H),3.7(s,3H),3.8(s,3H),3.95(s,3H),5.0(s,2H),6.9-7.0(m,3H),7.1-7.4(m,5H),7.6(s,1H) |
13.23 |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.3(m,1H),2.5(m,1H),3.65(s,3H),3.8(s,3H),3.9(s,3H),5.0(s,2H),6.8.0-7.0(m,3H),7.1-7.4(m,5H),7.6(s,1H) |
13.25A |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.25(s,3H),2.45(m,1H),2.8(m,1H),3.6(s,3H),3.75(s,3H),3.9(s,3H),5.1(s,2H),7.1-7.4(m,8H),7.6(s,1H) |
13.26 |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.3(s,3H),2.5(m,1H),2.8(m,1H),3.65(s,3H),3.75(s,3H),3.9(s,3H),5.1(s,2H),6.9-7.0(m,3H),7.1-7.4(m,5H),7.6(s,1H) |
13.39 |
1.1(m,1H),1.3(t,3H),1.8(m,1H),2.0(s,3H),2.4(m,1H),2.7(m,1H),3.6(s,3H),3.7(s,3H),4.1(m,2H),5.1(s,2H),7.0(d,2H),7.1-7.4(m,7H),7.6(s,1H) |
13.40A |
0.85(t,3H),1.1(m,1H),1.6(q,2H),1.8(m,1H),2.0(s,3H),2.4(m,1H),2.6(m,1H),3.6(s,3H),3.7(s,3H),4.0(t,2H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H),7.6(s,1H) |
13.42A |
0.9(t,3H),1.1(m,1H),1.3(m,2H),1.6(m,2H),1.8(m,1H),2.0(s,3H),2.4(m,1H),2.7(m,1H),3.65(s,3H),3.75(s,3H),4.1(t,2H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H),7.6(s,1H) |
13.43 |
1.2(m,10H),1.8(m,1H),2.0(s,3H),2.4(m,1H),2.6(m,1H),3.6(s,3H),3.7(s,3H),4.0(t,2H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H),7.6(s,1H) |
13.44A |
1.1(m,1H),1.8(m,1H),1.95(s,3H),2.4(m,1H),2.5(s,1H),2.7(m,1H),3.6(s,3H),3.7(s,3H),4.6(d,2H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H),7.6(s,1H) |
13.45A |
1.0(t,3H),1.1(m,1H),1.3(m,1H),1.8(m,1H),2.2(m,1H),2.5(q,2H),3.6(s,3H),3.7(s,3H),3.75(s,3H),5.0(s,2H).7.0(d.2H),7.1-7.4(m,7H),7.6(s,1H) |
13.45B |
1.0(t,3H),1.1(m,1H),1.3(m,1H),1.7(m,1H),2.5(m,1H),2.6(q,2H),3.65(s,3H),3.75(s,3H),3.9(s,3H),5.0(s.2H),7.0(d,2H),7.1-7.4(m,7H),7.6(s,1H) |
13.56A |
0.95(t,3H),1.2(m,1H),1.5(m,2H),1.7(m,1H),2.45(m,1H),2.7(m,3H),3.65(s,3H),3.75(s,3H),3.9(s,3H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H),7.6(s,1H) |
13.67A |
1.2(m,7H),1.3(m,1H),2.2(m,1H),2.4(m,1H),3.4(q,1H),3.7(s,3H),3.78(s,3H),3.9(s,3H),5.05(s,2H),7.1-7.5(m,9H),7.6(s,1H) |
13.67B |
1.2(m,7H),1.3(m,1H),1.8(m,1H),2.2(m,1H),3.1(q,1H),3.6(s,3H),3.70(s,3H),3.75(s,3H),5.0(s,2H),7.1-7.4(m,9H),7.5(s,1H) |
13.78A |
0.9(t,3H),1.2(m,1H),1.4(m,2H),1.5(m,2H),1.8(m,1H),2.4(m,1H),2.6(m,3H),3.65(s,3H),3.75(s,3H),3.9(s,3H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H),7.6(s,1H) |
14.7 |
1.10-1.25(m,2H),2.10-2.20(m,1H),2.25-2.35(m,1H),2.87-2.88(d,3H),3.85(s,3H),3.92(s,3H),5.05(s,2H),6.6-6.8(brs,1H),7.0-7.5(m.9H,)8.29(s.1H). |
14.18A |
1.1(m,1H),1.8(m,1H),2.0(s,3H),2.45(m,1H),2.7(m,1H),3.8(s,3H),3.9(s,3H),4.0(s,3H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H) |
14.20 |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.4(m,1H),2.6(m,1H),3.8(s,3H),3.9(s,3H),4.0(s,3H),5.0(s,2H),6.9(d,2H),7.1-7.4(m,6H) |
14.21 |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.4(m,1H),2.7(m,1H),3.8(s,3H),3.9(s,3H),4.0(s,3H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,6H) |
14.22 |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.4(m,1H),2.7(m,1H),3.75(s,3H),3.85(s,3H),3.95(s,3H),5.0(s,2H),6.9-7.2(m,3H),7.3-7.5(m,5H) |
14.23 |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.3(m,1H),2.5(m,1H),3.7(s,3H),3.85(s,3H),3.95(s,3H),4.95(s,2H),6.8.0-7.0(m,3H),7.1-7.4(m,5H) |
14.25A |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.25(s,3H),2.5(m,1H),2.8(m,1H),3.8(s,3H),3.9(s,3H),4.0(s,3H),5.1(s,2H),7.1-7.2(m,5H),7.4(m,3H) |
14.26 |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.3(s,3H),2.4(m,1H),2.6(m,1H),3.8(s,3H),3.9(s,3H),4.0(s,3H),5.0(s,2H),7.0-7.2(m,3H),7.3-7.5(m,5H) |
14.31 |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.4(m,1H),2.55(m,1H),3.7(s,3H),3.75(s,3H),3.9(s,3H),3.95(s,3H),5.0(s,2H),6.7(d,2H),7.1-7.4(m,6H) |
14.45 |
1.1(t,3H),1.2(m,1H),1.8(m,1H),2.4(m,2H),2.5(q,2H),3.8(s,3H),3.9(s,3H),4.0(s,3H),5.0(s,2H),7.0(d,21H),7.1-7.4(m,7H) |
14.56A |
0.95(t,3H),1.2(m,1H),1.5(m,2H),1.7(m,1H),2.45(m,1H),2.7(m,3H),3.8(s,3H),3.9(s,3H),4.0(s,3H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H) |
14.67A |
1.2(m,7H),1.4(m,1H),2.2(m,1H),2.4(m,1H),3.2(q,1H),3.8(s,3H),3.9(s,3H),4.0(s,3H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H) |
14.67B |
1.2(m,7H),1.3(m,1H),1.8(m,1H),2.2(m,1H),3.1(q,1H),3.8(s,6H),3.95(s,3H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H) |
14.78A |
0.9(t,3H),1.2(m,1H),1.4(m,2H),1.5(m,2H),1.7(m,1H),2.4(m,1H),2.6(m,3H),3.8(s,3H),3.9(s,3H),4.0(s,3H),5.0(s,2H),7.0(d,2H),7.1-7.4(m,7H) |
15.7 |
1.10-1.25(m,2H),2.10-2.20(m,1H),2.25-2.25(m,1H),3.82(s,3H),3.85(s,3H),3.99(s,3H),5.04(s,2H),7.0-7.5(m,9H),7.56(s,1H),8.28(s,1H) |
15.21 |
1.2(m,1H),1.7(m,1H),1.9(s,3H),2.2(m,1H),2.6(m,1H),2.9(d,3H),3.8(s,3H),3.9(s,3H),5.0(s,2H),6.8(bs,1H),7.0(d,2H),7.1-7.4(m,6H) |
15.18A |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.45(m,1H),2.8(m,1H),2.9(d,3H),3.9(s,3H),3.92(s,3H),5.0(s,2H),6.8(bs,1H),7.0(d,2H),7.1-7.4(m,7H) |
15.18B |
1.2(m,1H),1.4(m,1H),1.8(m,1H),1.95(s,3H),2.2(m,1H),2.85(d,3H),3.9(s,3H),3.95(s,3H),5.0(s,2H),6.7(bs,1H),7.0(d,2H),7.1-7.4(m,7H) |
15.20 |
1.1(m,1H),1.8(m,1H),1.9(s,3H),2.3(m,1H),2.6(m,1H),2.8(d,3H),3.85(d,6H),5.0(s,2H),6.7(bs,1H),6.9-7.4(m,8H) |
15.22A |
1.1(m,1H),1.8(m,1H),1.9(s,3H),2.3(m,1H),2.8(d,3H),2.9(m,1H),3.85(d,6H),5.0(s,2H),6.7(bs,1H),6.9-7.4(m,8H) |
15.24 |
1.1(m,1H),1.7(m,1H),1.9(s,3H),2.2(m,1H),2.6(m,1H),2.8(d,3H),3.85(d.6H),4.98(s,2H),6.8(bs,1H),6.9-7.4(m,8H) |
15.25A |
1.2(m,1H),1.8(m,1H),2.0(s,3H),2.2(s,3H),2.6(m,1H),2.8(m,1H),2.85(d,3H),3.85(s,6H),4.95(s,2H),6.8(bs,1H),7.0-7.4(m,8H) |
15.26A |
1.2(m,1H),1.7(m,1H),1.9(s,3H),2.2(s,3H),2.4(m,1H),2.7(m,1H),2.8(d,3H),3.85(d,6H),4.98(s,2H),6.8(bs,1H),6.9-7.4(m,8H) |
15.26B |
1.1(m,1H),1.4(m,1H),1.8(m,1H),1.9(s,3H),2.1(m,1H),2.2(s,3H),2.8(d,3H),3.75(s,3H),3.85(s,3H),4.95(s,2H),6.7(bs,1H),6.8(d,2H),6.9-7.4(m,6H) |
15.31 |
1.2(m,1H),1.8(m,1H),1.95(s,3H),2.4(m,1H),2.55(m,1H),2.9(d,3H),3.75(s,3H),3.8(s,3H),3.83(s,3H),5.0(s,2H),6.6(d,2H),7.1-7.4(m,6H) |
15.45 |
1.0(t,3H),1.2(m,1H),1.7(m,1H),2.3(m,2H),2.4(m,1H),2.5(q,2H),2.8(d,2H),3.8(s,3H),3.85(s,3H),4.95(s,2H),6.7(bs,1H),6.9(d,2H),7.1-7.4(m,7H) |
15.56A |
0.9(t,3H),1.2(m,1H),1.5(m,2H),1.8(m,1H),2.4(m,1H),2.6(m,3H),2.9(d,3H),3.9(s,3H),4.0(s,3H),5.0(s,2H),6.8(bs,1H),7.0(d,2H),7.1-7.4(m,7H) |
15.67A |
1.1(m,7H),1.2(m,1H),2.2(m,1H),2.4(m,1H),2.9(d,3H),3.1(q,1H),3.8(s,3H),3.9(s,3H),4.95(s,2H),6.8(bs,1H),7.0(d,2H),7.1-7.4(m,7H) |
15.67B |
1.1(m,6H),1.2(m,1H),1.4(m,1H),1.8(m,1H),2.2(m,1H),2.8(d,3H),3.0(q,1H),3.75(s,3H),3.9(s,3H),4.95(s,2H),6.7(bs,1H),7.0(d,2H),7.1-7.4(m,7H) |
15.78A |
0.9(t,3H),1.2(m,1H),1.4(m,2H),1.5(m,2H),1.7(m,1H),2.4(m,1H),2.6(m,3H),2.9(d,3H),3.9(s,3H).4.0(s,3H),5.0(s.2H),6.8(bs,1H),7.0(d,2H),7.1-7.4(m,7H) |
*以A或B指定的化合物NMR数据是对R9ON=C单一立体异构体的数据,未指定的化合物是立体异构体的混合物,所给出的数据是对主要异构体的。实施例11
就下述疾病,对本发明的许多化合物进行了体内杀真菌活性试验。将化合物依次用1∶1的丙酮和甲醇或N,N-二甲基甲酰胺混合物溶解,再分别用2∶1∶1水、丙酮和甲醇(体积比)混合物或者水稀释到适当的浓度。将溶液喷洒到作物上,令干(两小时)。然后对植物接种真菌孢子,每次试验采用喷洒有适当溶剂混合物并接种的植物作对照。在这些保护作用试验中,植物用杀真菌化合物处理一天之后,才进行接种。下面给出各个试验的其它技术条件,以及以化合物编号表示的各化合物在每公顷150克的剂量下,对各种真菌的试验结果,这些结果为相对于未经处理的对照样的控制病害百分数,其中100表示完全控制病害,0表示没有控制病害的作用。小麦叶锈病(WLR)
在温室中,将隐匿柄锈菌(Puccinia recondita)(f.sp.tritici)在7-天生长期的小麦(cultivar Fielder)上培养12-天期,从叶子上采集孢子到铝箔上,将孢子用250微米孔开口筛过筛净化,干燥储存。干燥的孢子在一个月内使用。制备孢子悬浮液,每毫升Soltrol油加入干的夏孢子堆20mg(9.5百万孢子)。将悬浮液分装到油雾化器附有的明胶胶囊(0.7ml容量)中,每20个植有7天生长期小麦(cultivarFielde)的两平方英寸盆所组成的平面使用一个胶囊,至少等15分钟使油从麦叶上挥发,将植物在阴暗潮湿的雾室(18-20℃,相对湿度100%)中放置24小时。然后把植物放于温室中,并于12天后对病害作出评价。小麦颖枯病(SNW)
将颖枯病菌(Septoria nodorum)培养物置于Czapek-Dox V-8液体琼脂培养基上,于20℃恒温箱中孵化2周,照明12小时和黑暗12小时交替进行。将含有真菌物质的部分培养基在去离子水中震荡,并用干酪包布过滤,得到孢子的水悬浮液。将含有孢子的水悬浮液稀释至浓度为每毫升3.0×106孢子,将培养液用DeVilbiss喷雾器分散到事先已喷洒了杀真菌化合物的一周龄Fielder小麦植株上,把接种的植株在20℃的潮湿箱室中放置7天,照明12小时和黑暗12小时交替进行。然后将接种的秧苗移至一个温度20℃的控制间内孵化2天。按控制百分数记录病害的控制值。小麦白粉病(WPM)
在18℃的温控间中,将禾白粉菌(Erysiphegrammis)(f.sp.tritici)于小麦(cultivar Fielder)秧苗上进行培养,将霉菌孢子从培养植株抖落到事先已喷洒了杀真菌化合物的7天生长期小麦秧苗上,将接种的秧苗保持在18℃的温控间,并进行地下灌溉。接种7天后测定控制病害百分数。黄瓜白粉病(CPM)
在温室中,将苍耳单丝壳菌(Sphaerotheca fulginea)在黄瓜(cultivar.Bush Champion)植株上培养。在盛有500ml水(每100ml水中含有1滴吐温80)的玻璃杯中放入5-10片严重发霉的黄瓜叶子,制备培养液,振荡液体和叶子后,用两层干酪包布过滤孢子悬浮液,用喷射瓶式雾化器对植物喷雾。孢子的计数为100,000孢子/ml。然后把植物放在温室中进行感染和孵化,接种7天后对植株进行评价,按控制百分数记录病害的控制值。西红柿晚疫病(TLB)
将蔓延疫霉(Phytophthora infestans)培养物在青豌豆改性的琼脂上培养2-3周。用水从琼脂上洗下孢子,用DeVilbiss喷雾器将其分散于事先己用试验杀真菌剂处理过的、生长期为3周的Pixie西红柿植株的叶子上。把接种的植株在20℃的潮湿箱室中感染24小时。然后植株移至一个温度20℃和湿度90%的控制间内。5天后对植株的病害控制情况进行评价。葡萄霜霉病(GDM)
在20℃温控室内,将葡萄生单轴霉(Plasmopara viticola)在葡萄(cultivar.Delaware)植株叶子上于光强适中的潮湿空气中培养7至8天。从感染的叶子得到孢子的水悬浮液,并将孢子的浓度调节为每毫升水大约3×l05。用DeVilbiss喷雾器在Delaware葡萄叶子的下侧喷洒,直到叶子上可观察到有小液滴为止,以进行接种。接种的植株在雾室中于20℃孵化24小时。然后将植株移至温度20℃的控制间中,接种7天后,按控制百分数记录病害的控制值。稻瘟病(RB)
将Pyricularia oryzae培养物在马铃薯葡萄糖琼脂上保持2-3周,用每l00ml水中含有1滴吐温80的水从琼脂上洗下孢子,用两层干酪包布过滤孢子悬浮液后,将孢子的浓度调节为每毫升水大约5×105。用DeVilbiss喷雾器将孢子悬浮液喷洒到12天生长期的稻株(cultivar.M-1)上,将接种的植株置于潮湿箱中于20℃孵化36小时,使其感染。感染期后,将植物置于温室。6天后对植株的病害控制情况进行评估。黄瓜炭疽病(CA)
将真菌病原体Colletotrichum lagenarium在马铃薯葡萄糖琼脂(PDA)上,于22℃的暗室中培养8-14天期,用蒸馏水冲洗PDA培养基表面,移取C.lagenarium孢子,补以0.5%v/w的酵母提取液,用钝器将真菌菌落的外表面击碎,直到大部分孢子释放到水液介质中,用干酪包布过滤孢子悬浮液,加入含酵母提取液的水,调节孢子计数直至达到每毫升3.0×106个孢子。
经过化学处理的黄瓜植株为15天生长期的cultivar BushChampion,使用手握唧筒式喷洒瓶,以孢子悬浮液喷洒植株的上层叶子,直至产生径流。将植物在荧光灯雾室中(照明12小时,黑暗12小时)放置48小时。感染期后,将植物于25℃和90%湿度下,在生长室放置3天。然后对经过处理的植株病害控制情况进行评估。灰霉病(BOT)
将真菌病原体Botrytis cinerea在马铃薯葡萄糖琼脂(PDA)上,在荧光灯下(12小时打开,12小时关闭)培养2-3周。用蒸馏水冲洗PDA培养基表面,移取B.cinerea孢子,补以0.5%v/w的酵母提取液,用橡皮器具将真菌菌落的外表面击碎,直到大部分孢子释放到水液介质中,用干酪包布过滤孢子悬浮液,加入含酵母提取液的水,调节孢子计数直至达到每毫升3.0×106个孢子。
经过化学处理的甜椒(sweet bell pepper)植株为19-天生长期的cultivar California Wonder。使用DeVilbiss喷雾器,以孢子悬浮液喷洒所有叶面,直至产生径流。将植物在低亮度的雾室中(照明12小时,黑暗12小时),于22℃放置4或5天。然后对经过处理的植株病害控制情况进行评估。
当化合物1.11,1.24,1.25,2.24,2.25,3.22,13.7,13.1lA,13.18A,13.18B,13.20A,13.22A,13.39,13.40A,13.42A,13.44A,13.45A,13.45B,13.56A,13.67B,14.18A,14.20,15.7,15.2l,15.18A,15.18B,15.20,15.22A,15.24,15.3l,15.45,15.56A,15.67A和15.78以150克/公顷用于防治小麦叶锈病试验时,给出99%或更好的控制率。
当化合物1.11,2.14,13.18A,13.18B,14.21,14.18A,15.7,15.18A和15.18B以150克/公顷用于防治小麦颍枯病(septoria nodorum)试验时,给出90%或更好的控制率。
当化合物1.24,1.25,2.11,2.45,3.22,13.7,13.18A,13.22A,13.23,14.7,14.18A 14.21,14,22,14.23,14.45,14.67A,15.18B,15.24,15.26A和15.31以150克/公顷用于防治小麦白粉病(powderymildew)试验时,给出90%或更好的控制率。
当化合物13.18A,13.20A,13.22A,13.23,13.25A,13.26,13.39,13.40A,13.42A,13.43,13.44A,13.45A,13.56A,13.67A,14.20,14.22,14.25A,14.26,14.31,14.45,14.67A,15.18A,15,18B,15.20,15.22A,15.24,15.25A,15.26A,15.26B,15.31,15.45,15.56A和15.67A以150克/公顷用于防治黄瓜白粉病(powdery mildew)试验时,给出100%的控制率。
当化合物1.11,1.22,1.24,1.25,2.11,2.45,3.22,13.18A,13.23,13.45B,13.67A,15.21,15.18A 15.26A,15.45,15.67A和15.67B以150克/公顷用于防治西红柿晚疫病试验时,给出90%或更好的控制率。
当化合物2.1,2.11,2.14,13.7,13.18A,13.18B,14.7,14.18A,14.21,15.7,15.18A,15.18B,15.25A,和15.67A以150克/公顷用于试验防治葡萄霜霉病时,给出99%或更好的控制率。
当化合物1.11,1.22,1.24,1.25,2.24,13.18A,13.18B,13.23,13.25A,13.45A,14.21,14.18A 14.23,14.26,14.45,15.18A,15.18B,15.2l,15.25A,15.26A,15.26B,16.24,15.31和15.45以150克/公顷用于试验防治稻瘟病时,给出90%或更好的控制率。
当化合物1.24,13.18A,13.18B,13.23,13.25A,13.26,13.45A,13.67A,14.21,14.22,14.26,15,7,15.21,15.18A,15.18B,15.25A,15.26A,15.26B,15.45,15.56A和15.67A以150克/公顷用于试验防治黄瓜炭疽病时,给出90%或更好的控制率。
当化合物1.22,3.22,13.22A,13.26,14.67B,15.7和15.18A以150克/公顷用于试验防治灰霉病时,给出85%或更好的控制率。
本发明化合物可用作农业杀真菌剂等,并可以用于不同的部位,如种子、土壤或叶子。
本发明化合物可一按照常用的方法,用作杀真菌喷雾剂,例如大体积水压喷雾剂、小体积喷雾剂、气流喷雾剂、空气喷雾剂和粉剂。使用的稀释度和比例取决于所用的设备类型、施用的方法、所处理的植物和所控制的病害。一般的说,本发明化合物的施用量为每公顷约0.005kg-约50kg,优选每公顷约0.025kg-约25kg活性成分。
作为种子保护剂时,在种子上的毒药涂用量通常是每100kg种子的剂量为约0.05-约20,优选约0.05-约4,更优选约0.1-约1克。作为土壤杀真菌剂时,可将化学品掺合到土壤中使用,或者用于土壤表面,一般来说,施用比例为每公顷大0.02-约20,优选约0.05-约10,更优选大约0.1-约5公斤。作为叶面杀真菌剂时,通常将此毒物施用于生长的植物,施用比例为每公顷约0.01-10,优选约0.02-约5,更优选约0.25-1公斤。
由于本发明化合物表现出杀真菌活性,所以,这些化合物可与其它己知的杀真菌剂结合使用,以提供广谱的活性。适当的杀真菌剂包括,但不限于US专利号5,252,594中所列出那些化合物(特别是其中14和15栏)。其它可以和本发明化合物结合使用的已知杀真菌剂为烯酰吗啉(dimethomorph)、噁唑酮菌(famoxadone)、zoxamide、霜脲氰(cymoxanil)、噻呋酰胺(thifluzamide)、呋霜灵(furalaxyl)、呋酰胺(ofurace)、苯霜灵(benalaxyl)、噁霜灵(oxadixyl)、霜霉威(propamocarb)、酯菌胺(cyprofuram)、拌种咯(fenpiclonil)、咯菌腈(fludioxonil)、嘧霉胺(pyrimethanil)、嘧菌环胺(cyprodinil)、灭菌唑(triticonazole)、氟喹唑(fluquinconazole)、叶菌唑(metconazole)、螺噁茂胺(spiroxamine)、氯环丙酰胺(carpropamid)、腈嘧菌酯(azoxystrobin)、亚胺菌(kresoxim-methyl)、叉氨苯酰胺(metominostrobin)和trifloxystrobin。
本发明化合物的优点是可以多种方法使用。因为这些化合物具有广谱的杀真菌活性,所以,可用于谷物的储存。这些化合物和可用作谷类(包括小麦、大麦和黑麦)的杀真菌剂,可用作稻、花生、大豆和葡萄的杀真菌剂,可用于草地、水果、坚果和菜园,以及用于高尔夫球场。
本发明化合物可应用的病害实例包括玉米和大麦的轮斑病、小麦和大麦的白粉病、小麦的叶锈病和杆锈病、西红柿早疫病、西红柿晚疫病、花生的早期叶斑、葡萄的白粉病、葡萄黑腐病、苹果结痂病,苹果白粉病、黄瓜白粉病、水果的褐腐病、灰霉病、大豆白粉病、黄瓜黑腐病、小麦颖枯病、稻子叶鞘枯萎病和稻瘟病。实施例12
用本发明的许多化合物对防治下述昆虫进行了体内杀昆虫活性试验。用下述方法对本发明化合物的杀昆虫活性进行评价。将待测化合物溶解于适当的溶剂中,通常是丙酮、甲醇和水的混合物,用扇形雾锥喷嘴将其喷洒在三个切叶盘上,喷洒后,让叶盘晾干。一个盘用食叶昆虫(南方黏虫(southern armyworm))感染,第二个叶盘在喷洒前已经用双斑蜘蛛螨(two-spotted spider mite)感染。试验昆虫种类为:
AW 南方黏虫 Spodoptera eridamia
MTA 双斑蜘蛛螨 Teranychus uricate
喷洒后24-48小时,通过目测获得百分控制率的观察结果。
当化合物13.20A,13.26,13.39,13.40A,13.42A和13.45A以150克/公顷用于试验抑制南方黏虫时,获得100%控制率。
当化合物1.22,13.20A,13.22A,13.26,13.39,13.40A,13.42A,13.45A,13.56A和15.20以150克/公顷用于试验抑制双斑蜘蛛螨时,获得100%控制率。
本发明的组合物和化合物可以直接应用于被保护的场所,例如,感染昆虫的经济植物区或周围地区,或者用于要防治感染的植物上。有害的昆虫属于鳞翅目(Lepidoptera)、鞘翅目(Coleoptera)、双翅目(Diptera)、缨尾翅目(Thysanoptera)、膜翅目(Hymenoptera)、异翅亚目(Heteroptera)、同翅目(Homoptera)、直翅目(Orthoptera)和螨目(Acarina)。化合物和组合物可用作接触性杀虫剂或内吸性杀虫剂。本发明化合物以每公顷0.0005-10千克应用于昆虫的习生地,优选每公顷0.05-5且最优选0.1-1千克。
在实施本发明方法时,活性化合物可以施用于土壤或植物上,在那里被植株吸收、转移到植株的其它部分,最终被害虫或昆虫通过食入部分植株而摄取。这种施用方式称为内吸性应用。另外活性化合物也可以施用到土壤,在那里与所要控制的昆虫或其它害虫相接触,这种施用方式称为土壤应用。在另一个选择方式中,将活性化合物经叶面施用到没有遭受那些以植物为食的昆虫和其它害虫的植物叶面上。
本发明的组合物和制剂还可以包括已知的杀虫化合物,这扩大了制剂的活性谱系并可以产生协同作用。本领域适当的已知杀虫剂包括美国专利号5,075,471,特别是14和15栏所列的那些杀虫剂。
本发明化合物可以组合物或制剂的形式使用。组合物和制剂的制备实例可见于Wade Van Valkenburg撰写、美国化学学会出版的“Pesticidal Formulation Research,”(1969),近代化学丛书第86卷(Advances in Chemistry Series No.86);以及Wade Van Valkenburg编写、Marcel Dekker,Inc.publication出版的“Pesticide Formulations”(1973)。
在这些组合物和制剂中,将活性物质与常规的农学上可接受的(即植物相容性的和/或农药惰性的)惰性农药稀释剂或增量剂相混合,如常规农药组合物和制剂所用的固体载体物质或液体载体物质。“农学上可接受的载体”是指组合物中那些用来溶解、分散或扩散组合物活性成分,但又不会减低活性成分有效性的物质,而其本身对土壤、设备需保护的植物或农业环境均没有显著的不利影响。如果需要,还可以与辅剂如表面活性剂、稳定剂、消泡剂和抗漂剂(anti-drift agents)结合使用。
本发明的组合物和制剂例子是水溶液和水性分散液、油性溶液或油性分散液、糊剂、粉剂、可湿性粉剂、乳油,流动剂、颗粒剂、饵剂、反乳剂(invert emulsions),气溶胶组合物和熏蒸罐。可湿性粉剂、糊剂、流动剂和乳油是浓缩制剂,在使用前或使用中用水将其稀释。在这些制剂中,化合物用液体或固体载体增量,需要时,可加入适当的表面活性剂。饵剂为通常含有食物或其它能吸引昆虫的物质的制剂,其中至少包括一种本发明的化合物。
根据农业实践,通常情况下,特别是用于叶片喷洒的制剂,要求包括辅剂如湿润剂、展开剂、分散剂、固着剂、粘合剂等。这些本领域常用的辅剂,以及关于辅剂的论述在很多参考文献中都可以找到,例如在John W.McCutcheon,Inc.publication,“Detergents andEmulsifiers Annual.”。
本发明的活性化合物可以单独使用,或者以混合物的形式使用,彼此相互混合,和/或与固体和/或液体分散载体赋型剂混合,和/或与其它已知的相容性活性剂相混合,尤其是植物保护剂,如其它杀虫剂、节肢动物杀灭剂、杀线虫剂、杀真菌剂、杀菌剂、灭鼠剂、除草剂、肥料、生长调节剂、增效剂。
在本发明组合物中,活性化合物的量一般是约0.0001(1∶999,999)-99(99∶1)%重量。为了适于储存和运输,混合物中活性组分的量优选是约0.5(1∶199)-90(9∶1)%重量,更优选为约l(1∶99)-75(3∶1)%重量。适于直接使用或田间使用的组合物通常含有活性化合物的量一般为混合物的约0.0001(1∶999,999)-95(19∶1)%重量,优选约0.0005(1∶199,999)-90(9∶1)%重量,更优选约0.001(1∶99,999)-75(3∶1)%重量。组合物还可以表示为化合物对载体的比例,在本发明中,这些位物质(活性化合物/载体)的重量比可以在99∶1(99%)-1∶4(20%),优选在10∶1(91%)-l∶3(25%)之间变化。
一般情况下本发明化合物可溶解于一些溶剂,如丙酮、甲醇、乙醇、二甲基甲酰胺、吡啶或二甲亚砜,其溶液可以用水稀释。溶液的浓度可以在约l%-约90%之间变化,优选范围是约5%-约50%。
对于浓缩乳油制剂,化合物可以溶解于适当的有机溶剂或溶剂的混合物,并一起加入乳化剂,以提高化合物在水中的分散作用。活性组分在乳油中的浓度一般是约10%-约90%,在流动性浓缩乳油中,可以高达约75%。
制备适于喷洒的可湿性粉剂,可以将化合物与细散的固体如粘土、无机硅酸盐和碳酸盐、硅石相混合,并在该混合物中掺入润湿剂、黏着剂、和/或分散剂。活性化合物在该类制剂中的浓度一般是约20%-约99%,优选约40%-约75%。制备典型的可湿性粉剂,是将50份的式Ⅰ化合物、45份合成的沉淀水合二氧化硅(如商标名为Hi-Sil_的售出商品)和5份木素磺酸钠盐相混合。在另一个制剂中,用高岭土(Barden)代替上述可湿性粉剂的Hi-Sil。在另一个这样的制剂中,将25%的Hi-Sil用商标名为Zeolex_7的合成硅铝酸钠代替。
粉剂的制备是将式Ⅰ化合物,或其对映体、盐或配合物与细散的惰性固体相混合,该固体性质上可以是无机的或有机的。用于此目的的材料包括植物面粉、硅石、硅酸盐、碳酸盐和粘土。一种制备粉剂的简单方法是将可湿性粉剂用细散的载体稀释。一般制成含有约20%-约80%活性组分的浓缩粉剂,然后稀释至约1%-约10%的使用浓度。
活性化合物可以作为杀虫喷洒剂,按照常用方法使用,如常见的大加仑量水压喷雾(high-gallonage hydraulic sprays)、小加仑量喷雾(low gallonage sprays)、超小体积(ultra-low-volume sprays)喷雾、气流喷雾、空气喷雾和粉剂。
本发明还涉及杀死、抑制或控制害虫的方法,包括将抑制剂量或杀死剂量(即有效杀虫剂量)的至少一种本发明的活性化合物接触害虫,单独使用或者与上述载体(组合物或制剂)一起使用。说明书和权利要求所用的术语“接触”,其意义是将本发明的活性化合物,单独或者作为组合物或制剂一个组分,应用到(a)和(b)的至少一处:(a)这类害虫;(b)它们相应的习生地(即被保护的场所,例如生长的作物或作物的种植区域)。
除了上述组分之外,本发明的组合物还可以包含其它这类制剂常用的物质,例如,润滑剂(如硬脂酸钙和硬脂酸镁)可以加入到可湿性粉剂或加入到造粒混合物中。此外,还可以加入粘结剂,如聚乙烯醇-纤维素衍生物或其它胶体材料如酪蛋白,以改善杀虫剂在保护面上的附着性能。