CN1128019A - 芳基乙酰胺类化合物、其制备方法、含有这些化合物的组合物及其作为杀真菌剂的用途 - Google Patents
芳基乙酰胺类化合物、其制备方法、含有这些化合物的组合物及其作为杀真菌剂的用途 Download PDFInfo
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Abstract
本发明涉及具有杀真菌活性、特别是抗植物致病真菌的式(I)化合物,其中:A是任意取代或不取代的芳基;A′是任意取代或不取代的芳基;B是羰基或被任意取代的羟基和其它任选取代基取代的亚甲基,并且可以任意地被进一步取代;X是任意被取代或不取代的含2-4个碳原子的亚烷基,其中在任何一个碳原子上的两个任意的取代基可以形成氧代基或者任意取代的亚氨基;和R7是杂环基、芳基、甲硅烷基、烷基、链烯基、环烷基、链炔基、环烯基、氨基、羟基、巯基,它们可以任意地被取代,或者是氢、氰基或酰基,其中当B被任意取代的羟基取代时,羟基上的取代基可以与R7或者与B上的其它取代基形成环。
Description
含有这些化合物的组合物及其作为杀真菌剂的用途
本发明涉及芳基乙酰胺类化合物、其制备方法、含有这些化合物的组合物及其作为杀真菌剂的用途。
据记载,其中在α-位含有任意地取代的羟基的取代芳基乙酰胺用作除草剂(JP-5 8032-853)和治疗皮肤病的组合物(EP-A-98743)的活性成分。还有许多有关这类化合物作为中间体的文献,并记载于化学文献中。
出人意料的是发现了具有有利的抗真菌、特别是抗植物致病真菌活性的新的芳基乙酰胺类化合物。
因此,本发明涉及式I化合物、其立体异构体及其混合物用于抗真菌的用途:其中:A是任意取代或不取代的芳基;A′是任意取代或不取代的芳基;B是羰基或被任选取代的羟基和另一个任意取代基取代的亚甲
基;X是任意被取代或不取代的含2-4个碳原子的亚烷基,其中在任
何一个碳原子上的两个任意的取代基可以形成氧代基团或
者任意取代的亚氨基;和R7是杂环基、芳基、甲硅烷基、烷基、链烯基、环烷基、链炔
基、环烯基、氨基、羟基、巯基,它们可以任意地被取
代,或者是氢、氰基或酰基,并且其中当B被任意取代的
羟基取代时,羟基上的取代基可以与R7或者与B上的其它
任选取代基形成环。
许多式I化合物是新的,因此本发明包括所有这些新化合物,特别是下列式I化合物,其中:X和R7如上所定义;B是被任意取代的羟基取代的亚甲基;A′是二烷氧基苯基,其中苯基还可以任意地被进一步取代;和A是被一个或多个选自卤素、氰基、硝基、任意取代的氨基、
任意取代的烷基、卤代烷氧基、芳基、杂环基的基团取代
的苯基,其中苯基可以任意地被进一步取代。
在新化合物中,A优选为被一个或多个选自卤素、氰基、烷基、三氟甲基和卤代烷氧基的基团取代的苯基。特别优选的是在4-位上有取代基。
A′优选为3,4-二甲氧基苯基或4-乙氧基-3-甲氧基苯基。
本发明还包括表中的所有新化合物,在表中给出了这些新化合物的熔点或物理描述,例如油状、胶状、蜡状或泡沫状。
上述烷基和含烷基基团的烷基部分优选具有1-20个、例如1-6个碳原子。链烯基和链炔基一般有3-6个碳原子。环烷基或环烯基优选具有3-8个碳原子。
当在任何一个烷基、环烷基、环烯基、链烯基、链炔基、烷氧基或烷硫基上存在取代基时,这些取代基包括卤素、氰基、烷氧基(例如含有1-4个碳原子,并且它可以被例如卤素取代)、羟基、烷硫基、硝基、任意取代的氨基、羧基、烷氧羰基、酰基、酰氧基、杂环基和芳基。
环烷基或环烯基也可以被烷基取代。
芳基是苯基,并且当其任意被取代时,取代基是例如卤素、任意取代的烷基或烷氧基、芳基、杂环基、芳氧基、氰基、硝基、任意取代的氨基或酰基,或者两个相邻基团可以形成以及稠合成苯并环,该苯并环可以任意地象芳基那样被取代或不取代。在任一芳基上的优选的取代基是卤素、烷基、三氟甲基、烷氧基、卤代烷氧基、硝基、二烷基氨基、氨基或氰基。
羟基和巯基可以被一些基团取代,这些基团包括例如任意取代的烷基、任意取代的环烷基、芳基、酰基、氰基和杂环基。
当B是羟基取代的亚甲基时,在B上的可有可无的其它取代基包括那些羟基上的任选取代基。
术语杂环基包括芳族和非芳族杂环基。杂环基一般是含有最多3个杂原子的5-或6-元环,所述杂原子是氮、氧和硫。杂环基可以与苯环稠合,形成稠合杂环基。杂环基的实例是噻吩基、呋喃基、吡啶基、嘧啶基、吡唑基、噻唑基、噻唑啉基、噁唑基、苯并咪唑基、四唑基、苯并噁唑基、噻二唑基、二氧戊环基、咪唑并吡啶基、1,3-苯并噁嗪基、1,3-苯并噻嗪基、噁唑并吡啶基、三唑基、三嗪基、咪唑基、吗啉代、苯并呋喃基、吡唑啉基、喹啉基、喹唑啉基、环丁砜基、二氢喹唑啉基、苯并噻唑基、哌啶基、苯二酰亚氨基、2-氧代吡咯烷基、2-氧代苯并噁唑啉-3-基和苯并呋喃基。杂环基本身可以例如象苯基一样被取代。
氨基可以例如被一个或两个任意取代的烷基或酰基取代,或者两个取代基可以形成环,优选5-7元环,该环可以被取代,并且可以含有其它杂原子,例如吗啉、硫代吗啉或哌啶。
术语酰基包括含硫和含磷的酸以及羧酸的残基。因此,酰基的实例是 -CORa,-COORa,-CO-Am,-CS-Am,-COSRa,-CSSRa,-S(O)qRa,-S(O)2ORa,-S(O)qAm,-P(=O)(ORa)(ORb),-P(=S)(ORa)(ORb)和-CO-COORa,其中Ra和Rb可以相同或不同,它们是氢、任意取代的烷基、任意取代的环烷基、任意取代的环烯基、任意取代的链烯基、任意取代的链炔基、芳基或杂环基,Am是任意取代或不取代的氨基,q是1或2。
m、n、m′和n′是整数;
m=1-5;
n=1-7;
m′=0-5;
n′=0-7;R1和R2相同或不同,并且它们彼此独立地为(C1-C18)-烷基,
(C3-C12)-环烷基,(C3-C12)-环烷基-(C1-C6)-烷基,(C6-
C18)-芳基,(C6-C18)-芳基-(C1-C6)-烷基,(C1-C8)-杂芳
基,(C1-C8)-非芳族杂环基,(C1-C8)-杂芳基-(C1-C6)-烷
基,(C1-C8)-非芳族杂环基-(C1-C6)-烷基,氰基,硝基,
卤素,
-COR3,-COOR3,-CONR3R4,-OR3,-OCOR3,-OCOOR3,
-OCO-NR3R4,-SR3,-SOR3,-SO2R3,-SO2-OR3,-SO2NR3R4,
-NR3R4,-NR3-SO2R4,-NR3-COR4,-P(O)(OR3)(OR4),
-O-P(O)(OR3)(OR4)或-SiR3 3,和其中,在前十个基团中,任选地满足至少一个下列条件:a)如果含有1、2或3个不在环上的CH-CH-单元,则其各自被
1、2或3个CH=CH-单元置换,b)如果含有不在环上的CH2-CH2-单元,则其被C≡C-单元置换,c)如果含有在环上的CH-CH-单元,则其被C=C-单元置换,d)在非环部分的碳原子上存在的氢原子被最多三个相同或不
同的取代基置换,这些取代基是氰基,硝基,卤素,
-COR3,-COOR3,-CONR3R4,-OR3,-OCOR3,
-OCOOR3,-O-CO-NR3R4,-SR3,-SOR3,-SO2R3,-SO2-OR3,
-SO2-NR3R4,-NR3R4,-NR3-COR4,-P(O)(OR3)(OR4),
-O-P(O)(OR3)(OR4)和-SiR3 3,e)按照d)所述进行取代后,在非环部分的碳原子上剩余的氢
原子被相同或不同的卤原子部分或全部置换,f)在环碳原子上存在的氢原子被最多3个相同或不同的取代基
R3(R3不是氢)和在d)中给出的取代基置换,g)按照f)所述进行取代后,在环碳原子上剩余的氢原子被相
同或不同的卤原子部分或全部置换,h)在非偶合位置存在的一个或两个CH2-单元可以被选自O、S、
CO和NR3的相同或不同的基团置换;R3和R4相同或不同,并且它们彼此独立地为氢,(C1-C18)-烷
基,(C3-C12)-环烷基,(C3-C12)-环烷基-(C1-C6)-烷基,
(C6-C18)-芳基,(C6-C18)-芳基-(C1-C6)-烷基,(C1-C8)-杂
芳基或(C1-C8)-杂芳基-(C1-C6)-烷基,其中,在前七个基
团中,任选地满足至少一个下列条件:a)如果含有1、2或3个不在环上的CH-CH-单元,则其各自被
1、2或3个CH=CH-单元置换,b)如果含有不在环上的CH2-CH2-单元,则其被C≡C-单元置换,c)如果含有在环上的CH-CH-单元,则其被C=C-单元置换,d)在非环部分的碳原子上存在的氢原子被最多三个相同或不
同的取代基置换,这些取代基是氰基,硝基,卤素,
-COR3’,-COOR3’,-CONR3’ 2,-OR3’,
-OCOR3’,-OCOOR3’,-O-CO-NR3’,-SR3’,-SOR3’,-SO2R3’,
-SO2-OR3’,-SO2-NR3’ 2,-NR3’ 2,-NR3’-COR3’,
-P(O)(OR3)(OR4),-O-P(O)(OR3)(OR4)和-SiR3’ 3,e)按照d)所述进行取代后,在非环部分的碳原子上剩余的氢
原子被相同或不同的卤原子部分或全部置换,f)在环碳原子上存在的氢原子被最多3个相同或不同的取代基
R3′(R3′不是氢)和在d)中给出的取代基置换,g)按照f)所述进行取代后,在环碳原子上剩余的氢原子被相
同或不同的卤原子部分或全部置换,h)在非偶合位置存在的一个或两个CH2-单元可以被选自O、S、
CO和NR3的相同或不同的基团置换;或R3和R4一起形成(C3-C6)-亚烷基,其中CH2基团任意地被CO、O、S或NR3置换;R3′是相同或不同的取代基,为氢,(C1-C6)-烷基,(C2-C6)-链
烯基,(C2-C6)-链炔基,(C1-C6)-卤代烷基,(C2-C6)-卤代
烯基,(C2-C6)-卤代炔基,(C3-C6)-环烷基,(C3-C6)-环烷
基-(C1-C4)-烷基,(C6-C10)-芳基,(C7-C11)-芳烷基和
(C1-C5)-杂芳基,其中后3个所述的基团可以在环上带有1
或2个相同或不同的取代基,这些取代基是氰基、硝基、
卤素、(C1-C4)-烷基、(C1-C4)-卤代烷基、(C1-C4)-烷氧
基、(C1-C4)-卤代烷氧基、苯基、苯氧基、苄基和苄氧
(C1-C6)-烷基,(C6-C18)-芳基,(C6-C18)-芳基-(C1-C6)-烷
基,(C1-C8)-杂芳基,(C1-C8)-杂芳基-(C1-C6)-烷基,氰
基,-COR3,-COOR3,-CONR3R4或-SiR3 3,并且R3和R4如上
所定义,其中第2-8个所述基团中任意地满足至少一个对
基团R1和R2所述的条件a)-h);R6是氢或者如对R1所定义,因此当R5=氢时,R6不通过O-、S-
或N-原子连接,或者R5和R6一起形成(C3-C6)-亚烷基,其中CH2-基团任意地被CO、
O、S或NR3′置换和/或一个CH-CH-单元任意地被C=C-单元
置换;R7是氢或者除硝基和卤素之外的如对R1的定义,或者R5和R7一起形成(C2-C5)-亚烷基,其中CH2-基团任意地被CO、
O、S或NR3′置换和/或一个CH-CH-单元任意地被C=C-单元
置换,并且R6如上所定义,R6和R7一起形成(C3-C6)-亚烷基,其中CH2-基团任意地被CO、
O、S或NR3′置换和/或一个CH-CH-单元任意地被C=C-单元
置换,并且R5如上所定义;X是式VIII基团,
-CR8R9-(CR10R11)p- (VIII)R8、R9、R10和R11相同或不同,并且彼此独立地如对R7所定
义,或者是卤素或硝基,而且其中R8和R9、或者R10和R11
通过形成氧代基可以一起为O,或者R10和R11可以一起形成=N-OR3基团,或者R7和R8一起形成(C2-C5)-亚烷基,R7和R10一起形成(C1-C4)-
亚烷基或者R8和R10一起形成(C3-C6)-亚烷基,其中在每
种情况下,CH2-基团任意地被CO、O、S或NR3′置换和/或
一个CH-CH-单元任意地被C=C-单元置换,并且这些不涉及
与此环连接的基团如上所定义;和p是1、2或3。
优选的式I化合物及其盐、特别是酸加成盐是如下的化合物,其中R1和R2相同或不同,并且它们彼此独立地为(C1-C12)-烷基,
(C3-C12)-环烷基,(C3-C12)-环烷基-(C1-C4)-烷基,(C6-
C12)-芳基,(C6-C12)-芳基-(C1-C4)-烷基,(C1-C8)-杂芳
基,(C1-C8)-杂芳基-(C1-C4)-烷基,氰基,硝基,卤素,
-COR3,-COOR3,-CONR3R4,
-OR3,-OCOR3,-OCOOR3,-OCO-NR3R4,-SR3,-SOR3,-SO2R3,
-SO2-OR3,-SO2NR3R4,-NR3R4,-NR3-SO2R4,-NR3-COR4或
-SiR3 3,其中,在前七个基团中,任选地满足对这些基团所定义的b)、c)、e)、g)和h)以及下列条件中的至少一个条件:a)如果含有1个不在环上的CH-CH-单元,则其被CH=CH-单元置
换,d)在非环部分的碳原子上存在的氢原子被最多三个相同或不
同的取代基置换,这些取代基是氰基,硝基,卤素,
-COR3,-COOR3,-CONR3R4,-OR3,-OCOR3,
-OCOOR3,-O-CO-NR3R4,-SR3,-SOR3,-SO2R3,-SO2-OR3,
-SO2-NR3R4,-NR3R4,-NR3-COR4,和-SiR3 3f)在环碳原子上存在的氢原子被最多3个相同或不同的取代基
R3(R3不是氢)和在d)中给出的取代基置换,R3和R4相同或不同,并且它们彼此独立地为(C1-C12)-烷基,
(C3-C8)-环烷基,(C3-C8)-环烷基-(C1-C4)-烷基,(C6-
C12)-芳基,(C6-C12)-芳基-(C1-C4)-烷基,(C1-C8)-杂芳
基或(C1-C8)-杂芳基-(C1-C4)-烷基,其中,在后七个基团
中,任选地满足对这些基团所定义的b)、c)、e)、g)和h)
以及下列条件中的至少一个条件:a)如果含有1个不在环上的CH-CH-单元,则其被CH=CH-单元置
换,d)在非环部分的碳原子上存在的氢原子被最多三个相同或不
同的取代基置换,这些取代基是氰基,硝基,卤素,
-COR3’,-COOR3’,-CONR3 2,-OR3’,
-OCOR3,-OCOOR3’,-O-CO-NR3’,-SR3’,-SOR3’,-SO2R3’,
-SO2-OR3,-SO2-NR3’ 2,-NR3’ 2,-NR3’-COR3’和-Si(R3)3,f)在环碳原子上存在的氢原子被最多3个相同或不同的取代基
R3′(R3′不是氢)和在d)中给出的取代基置换,R3′和B如上所定义;R5是氢,(C1-C12)-烷基,(C3-C12)-环烷基,(C3-C12)-环烷基-
(C1-C4)-烷基,(C6-C12)-芳基,(C6-C12)-芳基-(C1-C4)-烷
基,(C1-C8)-杂芳基,(C1-C8)-杂芳基-(C1-C4)-烷基,氰
基,-COR3,-COOR3,-CONR3R4或-SiR3 3,并且R3和R4如上
所定义,其中第2-8个所述基团中任意地满足至少一个对
基团R1和R2所述的条件a)-h);R6是氢或者如对R1所定义,因此当R5=氢时,R6不通过O-、S-
或N-原子连接,或者R5和R6一起形成上述定义的环;R7是氢或者除硝基和卤素之外的如对R1的定义,或者R5和R7一起形成上述定义的环;R6和R7一起形成上述定义的环;X如上所定义;R8、R9、R10和R11相同或不同,并且彼此独立地如对R7所定
义,或者是卤素,而且其中R8和R9、或者R10和R11通过形
成氧代基可以一起为O,或者R10和R11可以一起形成=N-OR3基团,或者R7+R8、R7+R10或者R8+R10一起形成上述定义的环,并且不
涉及与此环连接的基团如上所定义;和p如上所定义。
特别优选的化合物及其盐是如下的化合物,其中R1和R2相同或不同,并且它们彼此独立地为(C1-C12)-烷基,
(C2-C12)-链烯基,(C2-C12)-链炔基,(C6-C12)-芳基,(C7-
C13)-芳烷基,(C1-C12)-烷氧基,(C2-C12)-链烯氧基,
(C2-C12)-链炔氧基,(C1-C12)-烷硫基,(C6-C12)-芳氧
基,(C7-C13)-芳烷氧基,(C7-C13)-芳烷硫基,(C6-C12)-
芳硫基,杂芳基,杂芳基-(C1-C4)-烷基,杂芳氧基,杂芳
基-(C1-C4)-烷氧基,杂芳基-(C1-C4)-烷硫基,杂芳氧基-
(C1-C4)-烷基,其中杂环芳基各自具有最多8个碳原子和最
多4个选自N、S和O的相同或不同的杂原子,(C3-C12)-环烷
基,(C3-C12)-环烷氧基,(C3-C12)-环烯基,(C3-C12)-环
烯氧基, -CN,
OH,NO2,F,Cl,Br,I,-COOR3,-COR3,-OCOR3,
-CONR3R4,-R3COR4,-NR3R4,-SO2NR3R4,-NR3SO2R4,
-NR3COR4,-SiR3 3,-SO2R3或-SO3R3,
其中,前23个基团任意地如上所述被取代,和R3和R4的含义同上;R5和R6彼此独立地为氢,(C1-C12)-烷基,(C2-C12)-链烯基,
(C2-C12)-链炔基,(C6-C12)-芳基,(C7-C12)-芳烷基,(C7-
C12)-芳氧烷基,杂芳基,杂芳基-(C1-C4)-烷基,杂芳氧
基-(C1-C4)-烷基,其中杂环芳基各自具有最多8个碳原子
和最多4个选自N、S和O的相同或不同的杂原子,(C3-C12)-
环烷基,(C3-C12)-环烯基,-COOR3,-COR3,-CONR3R4或-
SiR3 3,其中,第2-12个所述基团任意地如上所述被取代,
或者R5与R6可以一起形成饱和或不饱和的5-、6-、7-或8-
元环,R3和R4的含义同上,并且当R5不是氢时,R6也可以
是(C1-C6)-烷氧基、(C1-C6)-卤代烷氧基、苯氧基、CN、
-NR3R4、-NR3SO2R4或-NR3COR4;R7为氢,(C1-C6)-烷基,(C2-C6)-链烯基,(C2-C6)-链炔基,
(C6-C12)-芳基,(C7-C12)-烷芳基,(C1-C6)-烷氧基,(C2-
C6)-链烯氧基,(C3-C6)-链炔氧基,(C6-C12)-芳氧基,
(C7-C13)-烷芳氧基,杂芳基,杂芳基-(C1-C4)-烷基,杂
芳氧基,杂芳基-(C1-C4)-烷氧基,其中杂环芳基各自具有
最多8个碳原子和最多4个选自N、S和O的相同或不同的杂
原子,(C3-C8)-环烷基,(C3-C8)-环烷氧基,(C3-C8)-环烯
基,(C3-C8)-环烯氧基,-OH,-COOR3,-COR3,-OCOR3,
-CONR3R4,-NR3COR4,-SiR3 3或NR3R4,其中,第2-19个所述
基团任意地如上所述被取代,R3和R4的含义同上,或者R7
与R5或R6形成饱和或不饱和的5-或6-元环部分;R8、R9、R10和R11相同或不同,并且彼此独立地为F、Cl、
Br、I、CN或具有与R7相同的定义,或者R7+R8、R7+R10
或者R8+R10一起形成饱和或不饱和的5-、6-、7-或8-元
环部分,并且剩余的基团和可变基团如上所定义。
特别优选的是如下的式I化合物及其盐、特别是酸加成盐,其中,R1和R2相同或不同,并且它们彼此独立地为(C1-C6)-烷基,(C2-
C6)-链烯基,(C3-C6)-链炔基,(C3-C7)-环烷基,(C3-C7)-
环烯基,(C3-C6)-烷氧基,苄氧基,(C1-C6)-烷硫基,苯
基,苯氧基,苯硫基,(C2-C6)-链烯氧基,(C3-C6)-链炔
氧基,(C7-C13)-苯基烷氧基,(C7-C13)-苯基烷硫基,(C1-
C6)-卤代烷基,(C1-C6)-卤代烷氧基,(C2-C6)-卤代烯氧
基,(C3-C6)-卤代炔氧基,特别是氟代烷基和氟代烷氧
基,(C3-C7)-环烷氧基,(C3-C7)-环烯氧基,(C1-C6)-卤代
烷硫基,(C2-C6)-卤代链烯硫基,(C3-C7)-卤代环烷基,
(C3-C7)-卤代环烯基,(C3-C7)-卤代环烷氧基,(C3-C7)-卤
代环烯氧基,(C3-C7)-卤代环烷硫基,特别是氟代烷硫
基,CN,OH,NO2,F,Cl,Br,I,CO2R3,OCOR3,COR3,
NR3COR4,NR3R4,SO3R3,SO2NR3R4,杂芳基,杂芳氧基,
其中杂环芳基各自具有最多5个碳原子和最多3个选自N、S
和O的相同或不同的杂原子,并且R3和R4具有上述含义;m=1-5;n=1-4;m′=2-5,和n′=2-4;R5和R6相同或不同,并且彼此独立地为氢,(C1-C6)-烷基,(C2-
C6)-链烯基,(C2-C6)-链炔基,(C3-C7)-环烷基,(C3-C7)-
环烯基,苯基,杂芳基,其中杂环芳基各自具有最多5个
碳原子和最多3个选自N、S和O的相同或不同的杂原子,
(C1-C6)-羟烷基,(C1-C6)-卤代烷基,(C2-C6)-卤代烯基,
COOR3,COR3,CONR3R4或-SiR3 3,并且当R5不是氢时,R6还
可以是(C1-C6)-烷氧基,苯氧基,(C1-C6)-卤代烷氧基,
CN、NR3R4或NR3COR4,或者R5与R6可以一起形成饱和或不饱
和的5-或6-元环,并且R3和R4的含义同上;R7为氢,(C1-C6)-烷基,(C2-C6)-链烯基,(C2-C6)-链炔基,苯
基,(C1-C6)-烷氧基,苯氧基,(C2-C6)-链烯氧基,(C3-
C6)-链炔氧基,(C3-C7)-环烯氧基,(C1-C6)-卤代烷基,
(C1-C6)-卤代烷氧基,OH,COOR3,COR3,OCOR3,
CONR3R4,NR3COR4,NR3R4或SiR3 3,或者R7与R5或R6形成饱
和或不饱和的5-或6-元环,并且R3和R4具有上述含义;R8、R9、R10和R11相同或不同,并且彼此独立地为F、Cl、
Br、I或CN或具有与R7相同的定义,或者R7+R8或R7+R10
或者R8+R10一起可为饱和或不饱和的5-或6-元环的组成
部分,并且剩余的基团和可变基团如上所定义。
特别优选的还有下列式I化合物及其盐、特别是酸加成盐,其中R1是(C1-C6)-烷基,(C2-C6)-链烯基,(C3-C6)-链炔基,(C3-
C7)-环烷基,(C3-C7)-环烯基,苯基,(C1-C6)-卤代烷
基,(C2-C6)-卤代烯基,(C2-C6)-卤代炔基,(C1-C6)-卤代
烷氧基,(C2-C6)-卤代烯氧基,(C3-C6)-卤代炔氧基,
(C3-C7)-环烷氧基,(C1-C6)-卤代烷硫基,(C2-C6)-卤代链
烯硫基,(C3-C7)-卤代环烷基,(C3-C7)-卤代环烯基,
(C3-C7)-卤代环烷氧基,(C3-C7)-卤代环烯氧基,(C3-C7)-
卤代环烷硫基,CN,OH,NO2,F,Cl,Br,I,CO2R3,
OCOR3,COR3,NR3COR4,NR3R4,SO3R3,SO2NR3R4,杂芳
基,其中杂环芳基各自具有最多5个碳原子和最多3个选自
N、S和O的相同或不同的杂原子,并且R3和R4具有上述含
义,和下列式I化合物及其盐、特别是酸加成盐,其中R2是(C1-C6)-烷基,(C2-C6)-链烯基,(C3-C6)-链炔基,(C3-
C7)-环烷基,(C3-C7)-环烯基,(C1-C6)-烷氧基,苄氧
基,(C1-C6)-烷硫基,苯氧基,苯硫基,(C2-C6)-链烯氧
基,(C3-C6)-链炔氧基,(C7-C13)-苯基烷氧基,(C7-C13)-
苯基烷硫基,(C1-C6)-卤代烷基,(C1-C6)-卤代烷氧基,
(C2-C6)-卤代烯氧基,(C3-C6)-卤代炔氧基,(C3-C7)-环烷
氧基,(C3-C7)-环烯氧基,(C1-C6)-卤代烷硫基,(C2-C6)-
卤代链烯硫基,(C3-C7)-卤代环烷基,(C3-C7)-卤代环烯
基,(C3-C7)-卤代环烷氧基,(C3-C7)-卤代环烯氧基,
(C3-C7)-卤代环烷硫基,CO2R3,OCOR3,COR3,NR3COR4,
NR3R4,杂芳氧基,其中杂环芳基各自具有最多5个碳原子
和最多3个选自N、S和O的相同或不同的杂原子,并且R3和
R4具有上述含义,
特别优选的化合物是下列化合物,其中A是式II,其中m是1或2,R1是卤素、C1-C4-烷基(特别是甲
基)、卤代-C1-C4-烷基(特别是三氟甲基),并且优选R1
在3和/或4位;B是-CH(OH)-、-CH(O-酰基)-或-CH(O-烷基);R7是氢;X是任意取代或不取代的亚乙基;和A′是式IV,其中m′是2,R2是C1-C4-烷氧基(特别是甲氧基或乙
氧基),并且优选R2在3和4位。
特别优选的是B是-CH(OH)-且X是亚乙基。
在前面和下面的描述中,术语“卤素”是指氟、氯、溴或碘原子;
术语“烷基”是指直链或支链烃基,例如甲基、乙基、丙基、1-甲基乙基、2-甲基丙基、1,1-二甲基乙基、戊基、2-甲基丁基、1,1-二甲基丙基、己基、庚基、辛基、1,1,3,3-四甲基丁基、壬基、异壬基、癸基、十一烷基或十二烷基;
术语“环烷基”是单-、二-或三环,优选单环,它们是指例如环丙基、环丁基、环戊基、环己基、环庚基或环辛基;
术语“环烷基烷基”是指具有上述术语“烷基”的含义、并且被术语“环烷基”下给出的烃基取代的烃基,例如环己基甲基、2-环己基乙基或2-环己基-2-丙基;
术语“烷氧基”是指具有上述术语“烷基”下给出的含义的烃基;
术语“烷氧基烷基”是指例如1-甲氧基乙基、2-甲氧基乙基、2-乙氧基乙基、甲氧基甲基、乙氧基甲基、3-甲氧基丙基或4-丁氧基丁基;
术语“卤代烷基”是指术语“烷基”下所定义的烷基,其中-个或多个氢原子被上述卤原子(优选氯或氟)置换,例如CF3,CF2CHF2,CCl3,CCl2F,CF2CF2CF3,CF2CHFCF3,CH2CF3,(CF2)3CF3,CF2H,CHF2,CH2Cl,CHCl2或CC13CH2和相应的卤代烯基和卤代炔基等;
术语“卤代烷氧基”是指卤代烷氧基,其卤-烃残基具有术语“卤代烷基”下给出的含义,例如OCH2F,OCHF2,OCF3,OCH2CF3,OCH2CCl3,OCH(CF3)2或OCF2CHFCF3,和相应的卤代烯氧基和卤代炔氧基等;
术语“芳基”是指例如苯基、萘基或联苯基,特别是苯基;
术语“芳基-烷基”是指上述一种烷基,该烷基被芳基取代,例如苄基、2-苯基乙基、1-苯基乙基、1-甲基-1-苯基乙基、3-苯基丙基或4-苯基丁基;
术语“杂芳基”是指上述芳基,其中至少一个CH-基团被N置换和/或至少两个相邻的CH-基团被S、NH或O置换。这些基团的实例是噻吩基、呋喃基、苯并呋喃基、吡咯基、咪唑基、吡唑基、吡啶基、吡嗪基、嘧啶基、哒嗪基、噁唑基、异噁唑基、噻唑基、异噻唑基和四唑基;
术语“环烷氧基”是指其中烃基具有术语“烷基”下给出的含义的环烷氧基;
术语“烷硫基-烷基”是指例如甲硫基甲基、乙硫基甲基、丙硫基甲基、2-甲硫基乙基、2-乙硫基乙基或3-甲硫基丙基;
术语“链烯基”是指例如烯丙基、1-甲基烯丙基、2-丁烯基或3-甲基-2-丁烯基;
术语“链炔基”是指例如乙炔基、炔丙基、2-丁炔基或2-戊炔基。
未具体提及的所有其它基团可以从上述基团中衍生,例如通过引入双键或三键,通过用一个或多个相同或不同的取代基取代,或者通过用例如NR3、S、O或CO等替换一个或多个CH2。
通常被取代的、在烃上含有羟基-、巯基-或任意地单取代氨基的基团,其本身再与氧、硫或氮原子连接(例如以半缩醛和半缩酮形式),由于它们不能通过特殊的基团稳定,因此其通常是不稳定的;这类基团不是优选的。
本发明包括未出现在本发明式I化合物中的所有的立体异构体,特别是单个的对映体及其任何比例的混合物及其盐、特别是酸加成盐。
为了制备优选的式I化合物的酸加成盐,可以使用下列酸:氢卤酸例如盐酸或氢溴酸,以及磷酸,硝酸,硫酸,单-或双-官能羧酸和羟基羧酸例如乙酸、琥珀酸、富马酸、酒石酸、柠檬酸、水杨酸或乳酸,以及磺酸如对甲苯磺酸或1,5-萘二磺酸。式I化合物的酸加成盐可以采用常规成盐的相似的方法获得,例如通过溶解在有机溶剂中并加入酸,按已知方法纯化,例如过滤、分离和任意地用惰性溶剂洗涤。
碱加成盐可以通过用碱金属或碱土金属氢氧化物或碳酸盐处理或者用有机胺处理获得。
新的式I的芳基乙酰胺可以按照已知方法获得,例如a)例如按照Synthesis(1985,)12,1153中所述相似的方法,通过用式X的胺(其中各取代基如式I所定义)处理式IX的二氧戊环酮(其中R12、R13彼此独立地为H、(C1-C8)-烷基、(C1-C8)-卤代烷基或者R11和R12可以是5-、6-或7-元饱和或单不饱和的碳环的组成部分,剩余的取代基如式I中所定义),得到式I的芳基乙酰胺(其中B是式VII基团,R5=H,剩余的取代基如式I中所定义)。
采用例如下列文献中所述的已知方法可以得到胺:
Bull.Chem.Soc.Jap.1990,63,1252;Angew.Chem.1989,101,202 and 1992,104,914;Heterocycles,1987,26,1595 and J.Med.Chem.1988,31,1282,1981,24,1063 and 1980,23,990.
该反应在0℃至混合物的沸点之间的温度下进行,优选回流0.5-120小时。按照每1当量式IX的二氧戊环处理1-10、优选1-2摩尔当量比例的式X的胺。该反应任选地在惰性溶剂中进行。优选的溶剂是醚类、芳族或脂族烃、卤代烃、酮、醇或其混合物,特别是乙醚、二噁烷、四氢呋喃、甲基叔丁基醚、二甲氧基乙烷、甲苯、二甲苯、氯苯、己烷、环己烷、庚烷、石油醚、丙酮、甲乙酮、二氯甲烷、1,2-二氯乙烷、甲醇或乙醇。
式IX的二氧戊环酮可以采用与下列文献所述类似的方法获得:
Organic Synthesis,
Coll Vol3,536和J.Org.Chem.Vol.51(19),3747,
(1986).b)还可以通过用式X的胺(其中各取代基如式I中所定义)处理式XI的羧酸(其中各取代基如式I中所定义)或者处理式XI的活性衍生物(任选地就地获得,其中各取代基如式I中所定义),制备式I化合物
该反应代表了用式X化合物与式XI的羧酸的酰化作用,因此,优选在酸XI活化化合物或脱氢剂存在下,或者用羧酸XI或离析物X的活性衍生物进行该反应。
任选地在反应混合物中制备的式XI衍生物的实例是例如其烷基酯、芳基酯或芳烷基酯,例如甲酯、乙酯、苯基酯或苄基酯,其咪唑烷化物(imidazolides),其酰卤例如酰基氯或酰基溴,其酸酐,与脂族或芳族羧酸、磺酸或碳酸酯例如乙酸、丙酸、对甲苯磺酸或O-乙基或O-异丁基碳酸或其N-羟基酰亚胺酯的混合酸酐。
酸活化剂和/或脱水剂的实例是氯化碳酸酯例如氯甲酸乙酯、氯甲酸异丁酯、五氧化二磷、N,N′-二环己基碳二亚胺、N,N′-羰基二亚胺、N,N′-羰基二咪唑或N,N′-亚硫酰二亚胺。
为了活化所任选制备的羧酸酯,其实例是钛的四醇盐,例如四异丙醇钛、四乙醇钛、四甲醇钛、四丙醇钛,或者采用加压法(Angew Chemie,(1986),6,569)。
该反应适合在-78℃至120℃、优选在-78℃至反应混合物的沸点之间的温度下,在无机碱例如碳酸钠或碳酸钾或有机碱如三乙胺、N-甲基吗啉或吡啶存在下(它们同时还可以作为溶剂),以及任意地在酸活化剂存在下,在溶剂或溶剂的混合物中进行,所述溶剂是例如二氯甲烷、氯仿、四氯化碳、乙醚、四氢呋喃、二噁烷、苯、甲苯、乙腈、N-甲基吡咯烷或二甲基甲酰胺。不需要分离通式X或XI化合物的反应混合物中任意产生的可反应衍生物,并且还可以在过量通式X化合物作为溶剂存在下进行反应。
在反应混合物中任意获得的式XI的羧酸及其衍生物的制备是已知的。例如按照与下列文献所述类似的方法进行:
J.Org.Chem.(1978),43,(13),2702;Org.Synth.(1945),25,33;Org.Synth.Col.Vol.IV,(1963),110;Org.Synth.Col.Vol.I,(1941),336-SE7604030-2,Synthesis(1975),163,Synth.Commun(1981),11,943;Org.Prep.Proced.(1970),2,249,EP 140454.c)其中B是式VII基团并且R4和R5各自为氢的式I化合物可以按照已知的氧化方法(例如J.Org.Chem.(1987),52,(22),4978;Heterocycles(1984)22,(4),773)转化成其中B如式VI的基团所定义的相应的式I的酮化合物。d)其中B是式C基团的式I化合物可以按照已知方法还原(例如J.Chem.Soc.Perkin.Trans.I(1989),1555),得到相应的式I的羟基化合物,其中B是式VII基团并且R4和R5各自为氢。e)采用与Tetrahedron letters(1988),44,(15),4805所述类似的方法,通过式XII的卤代化合物(其中R14=F、Cl、Br或I,剩余的取代基如式I中所定义)与式XIII的羟基化合物(其中各取代基如式I中所定义)反应,可以制备其中B是式VII基团并且剩余的取代基如式I所定义的式I化合物。结构XII化合物是已知的或者可以按照已知方法制备(例如J Org Chem(1955),20,237)。f)还可以通过用式Z-R5的烷基化试剂和/或酰基化试剂(其中Z是亲核离去基团,例如F、Cl、Br、I、烷氧基磺酰基、烷基磺酰氧基或卤代烷基磺酰氧基,并且R5具有上述含义)处理其中B是式VII基团且R5=H的式I化合物,制备其中B是式VII基团且R5不是氢的式I化合物。该反应可以按照与下列文献所述相似的方法进行:
J Org Chem(1978),43,1893;Org SynthCol Vol I,(1941),12;Tetrahedron Letters(1980),21,(52),4997.g)式I化合物还可以通过下列方法获得:按照已知方法(例如Chemical Abstracts 35 3634)将式XIV化合物闭环A-CH(OH)-CONH2 (XIV)得到式XV化合物然后将其与下式化合物反应A′-X-Q其中Q是离去基团例如卤素。
本发明的式I化合物具有极好的抗植物致病真菌的杀真菌活性。特别有价值的是这些化合物的治疗活性。这对于用常规杀真菌剂无法有效控制的真菌疾病是特别重要和有利的。所要求专利保护的化合物的活性谱包括各种经济上重要的植物致病真菌,例如蔓延疫霉(Phytophthora infestans)和葡萄生单轴霉(Plasmopara viticola)。
可以用该化合物处理作物种子以防止种子带有的疾病。
本发明化合物还适用于技术领域,例如作为木材防腐剂,作为涂料、增稠剂、金属加工用的冷却润滑剂中的防腐剂,或者作为钻孔和切割用油的防腐剂。
本发明组合物一般含有1-95%(重量)的活性成分。
它们可以按照生物和/或化学物理参数以各种形式进行配制。可能的制剂包括例如,可湿性粉末(WP)、可乳化的浓缩液(EC)、油或水基的水分散液(SC)、悬乳液(SC)、粉末(DP)、消毒剂、水分散颗粒形式的颗粒剂(WG)、ULV-制剂、微囊、蜡或饵。
这些制剂类型是已知的,并且描述于例如下列文献中:Winnacker-Küchler,"Chemische Technologie",Band 7,C-Hauser Verlag München,4.Aufl.1986;van Falkenberg,"Pesticides Formulations",Marcel Dekker N.Y.,2nd Ed.1972-73;K.Martens,"Spray Drying Handbook",3rd Ed.1979,G. Goodwin Ltd.London.
所需的制剂添加剂也是已知的惰性物质、表面活性剂、溶剂和其它添加剂,其描述例如见于下列文献:Watkins,"Handbook of Insecticide Dust Diluents andCarrier"2nd Clay Colloid Chemistry 2nd Ed.J Wiley &Sons,N.Y.;Marschen,"Solvents Guide",2nd Ed.,Interscience,N.Y.1950;McCutcheon′s "Detergents andEmulsifiers Annual",MC Publ. Corp.,Ridgewood N. J.;Sisley and Wood,"Encyclopedia of Surface Active Agents",Chem.Publ.Co.Inc.,N.Y.1964;Sch_nfeldt,"Grenzfl_chenaktive _thylenoxidaddukte",Wiss.Verlagsgesell.,Stuttgart 1976;Winnacker-Küchler,"Chemische Technologie",Band 7,C.Hauser Verlag München,4. Aufl.1986.
基于这些制剂,可以制备与其它杀虫活性物质、肥料和/或生长调节剂的组合物,例如制备成即用制剂形式或罐装混合物形式。
可湿性粉末是可均匀分散于水中的制剂,它除了含有该活性物质之外,还含有稀释剂或惰性物质,包括表面活性剂例如聚氧乙烯烷基酚、聚氧乙烯脂肪醇、烷基磺酸酯或烷基酚磺酸酯和分散剂例如木素磺酸钠、2,2′-二萘基-甲-6,6′-二磺酸钠、二丁基萘磺酸钠或/和油基甲基牛磺酸钠。通过加入一种或多种乳化剂,将活性成分溶于有机溶剂例如丁醇、环己酮、二甲基甲酰胺、N-辛基吡咯烷酮、二甲苯或高沸点芳族或烃中,制备可乳化的浓缩液。可以使用的乳化剂的实例是烷基芳基磺酸的钙盐例如十二烷基苯磺酸钙,或非离子乳化剂如脂肪酸聚乙二醇酯、烷基芳基聚乙二醇醚、脂肪醇聚乙二醇醚、氧化丙烯、环氧乙烷、脱水山梨醇脂肪酸酯、聚氧乙烯脱水山梨醇脂肪酸酯或聚氧乙烯脱水山梨醇酯。
通过将活性成分与细分散的固体物质一起研磨可以制备粉剂,所述固体物质是例如滑石、天然粘土例如高岭土、膨润土、叶蜡土或硅藻土。通过将活性成分分散到吸附颗粒性惰性物质上或者借助粘着剂(例如聚乙烯醇、聚丙烯酸钠或矿物油)将活性成分的浓缩物吸附到载体(例如砂子、高岭土或颗粒状惰性物质)的表面上,可以制备颗粒剂。还可以按照常规方法将合适的活性成分制粒,以制备肥料颗粒,它可以任意与肥料混合。
在可湿性粉末中,活性成分的浓度是大约10-9%,剩余的至100%的成分含有常规制剂部分。在可乳化浓缩液中,活性成分的浓度是大约5-80%。粉末制剂含有最多5-20%活性成分。在颗粒制剂中,活性成分的含量部分取决于活性化合物是液体的还是固体的以及哪个化合物是液体的或固体的和使用哪种颗粒物质和填料等。
除了上述活性成分配制试剂之外,还可以任选地使用常规的粘结剂、表面活性剂、分散剂、乳化剂、渗透剂、溶剂、填充剂或载体物质。
应用时,通常按照常规方法将市售形式的浓缩物稀释,例如用水将可湿性粉末、可乳化浓缩液、分散剂和微粒稀释。
粉末和颗粒制剂以及可喷雾溶液在使用前一般不用其它惰性物质稀释。
除了温度、湿度等条件外,可以改变所需的使用比例。该比例可以限制在例如0.005-10.0kg/公顷或更多的活性物质,例如0.01-5kg/公顷。
本发明的活性成分可以以其市售形式使用,它们可以单独使用或者与文献中已知的杀真菌剂联合使用。
本发明化合物可以与最公知的杀真菌剂联合使用,这些杀真菌剂包括例如:(i)conazole甾族脱甲基作用抑制剂,(ii)以1-[3-(4-叔丁基苯基)-2-甲基丙基]为基础,通过N-原子与哌啶或2,6-二甲基吗啉连接的甾族还原抑制剂,(iii)二硫代氨基甲酸酯类杀真菌剂,(iV)邻苯二甲酰亚胺杀真菌剂,其中氯代烷硫基通过N-原子与任意氢化的邻苯二甲酰亚胺基团连接,(v)N-酰苯胺类杀真菌剂,(vi)mbc杀真菌剂,(vii)氨基甲酸酯类杀真菌剂,(viii)铜化合物杀真菌剂,(ix)锡化合物杀真菌剂,(x)strobilurine类杀真菌剂,和(xi)苯胺基嘧啶(xii)含磷化合物(xiii)选自下列一组的杀真菌剂:四氯二氰苯、烯酰吗啉、拌种咯、氟啶胺、土菌消、氟苯嘧啶醇、戊菌隆、啶斑肟、噻菌腈、烯丙异噻唑、咯喹酮、三环唑、季铵化合物、fludioxonil、5-氯-2-甲基-4-异噻唑啉-3-酮、2-甲基-4-异噻唑啉-3-酮(以及二者的混合物)、furmecyclox、丁基氨基甲酸3-碘代-2-丙炔酯和硫。
在ISO标准257中定义了conazoles,这是咪唑或1,2,4-三唑基的化合物,其含有卤代苯基。其实例包括丙氯灵(及其金属配合物-特别是锰和铜配合物)、丙环唑、氟喹唑、己唑醇、戊唑醇、噁醚唑、糠菌唑、环唑醇、烯唑醇、fenbuconazole、酰胺唑、呋菌唑、氟醚唑、腈菌唑、戊菌唑、fluquinconazole、戊环唑、烯菌灵、氟菌唑、epoxiconazole、triticonazole、metconazole和编号为SSF109的杀真菌剂。
第(ii)类杀真菌剂的实例包括fenpropimorph和fenpropidin。
第(iii)类杀真菌剂的实例包括mancozeb和塞仑。
第(iv)类杀真菌剂的实例包括folpet、captafol和captan。
第(v)类杀真菌剂的实例包括a)3′,5′-二氯-N-酰苯胺杀真菌剂,其中苯胺基的氮在与氮毗邻的位置上包括一个带有两个氧代取代基的环,例如异丙定、烯菌酮或rocymidone,或者b)乙酰苯胺杀真菌剂,例如氨丙灵或ofurace,c)磺酰苯胺杀真菌剂,例如dichlofluanid,d)N-苯甲酰苯胺,例如flutolanil,和e)杂芳基-N-酰苯胺杀真菌剂,例如thifluzamide。
第(vi)类杀真菌剂的实例包括carbendazim、benomyl和甲基托布津。
第(vii)类杀真菌剂的实例包括diethofencarb和propamocarb。
第(viii)类杀真菌剂的实例包括波尔多液混合物、喔星-铜、氯氧化铜和环烷酸铜。
第(ix)类杀真菌剂的实例包括三丁基氧化锡和环烷酸三丁基锡。
strobilurine类杀真菌剂(第(x)类杀真菌剂)是芳基乙酸甲酯类化合物,其中乙酸还带有甲氧基亚甲基或甲氧基亚氨基取代基。芳基通常为2-取代苯基。该化合物的实例是许多申请中公开的那些,这些专利申请包括欧洲专利申请
178826,203606,203608,206523,229974,226917,242070,242081,243012,243014,251082,256667,260794,260832,267734,270252,273572,274825,278595,291196,299694,307101,307103,310954,312221,312243,329011和336211.具体的化合物编号是BAS490F和ICIA5504。
第(xi)类杀真菌剂的实例yrimethanil、cyprodinil和mepanipyrim。
第(xii)类杀真菌剂的实例包括pyrazophos、fosetylaluminium和tolclofos-methyl。
这些化合物的引用名称并非是专有的通用名称,其化学结构可参见例如"Pesticide Manual",第9版,1991,由BritishCrop Protection Council出版,或者参见近期的其它出版物。
除此之外,可以将市售制剂的本发明化合物及由市售制剂得到的即用形式与其它活性成分例如杀虫剂、干燥剂、杀毒剂、杀螨剂、杀线虫剂或除草剂混合。杀虫剂的实例包括磷酸酯类、氨基甲酸酯类、羧酸酯类、甲脒、锡化合物、由微生物制备的化合物等。
优选的混合配合成分是:1.磷化合物高灭磷、甲基吡噁磷、azinphos-ethyl、azinphos-methyl、tebupirimifos、溴硫磷、bromophos-ethyl、硫线磷、氯芬磷、氯甲磷、毒死蜱、chlorpyrifos-methyl、内吸磷、demeton-s-methyl、demeton-S-methyl sulfone、dialifos、敌匹硫磷、敌敌畏、百治磷、chlorethoxyfos、乐果、乙拌磷、EPN、乙硫磷、灭克磷、etrimfos、氨磺磷、fenamiphos、杀螟松、丰索磷、倍硫磷、地虫磷、安果、heptenophos、isazophos、isothioate、isoxathion、马拉硫磷、methacrifos、methamidophos、杀扑磷、mevinphos、久效磷、naled、omethoate、oxydemeton-methyl、parathion、parathion-methyl、phenthioate、phorate、phosalone、phosfolan、phosmet、phosphamidon、肟硫磷、pirimiphos-ethyl、pirimiphos-methyl、profenofos、丙虫磷、propetamphos、prothiofos、吡唑硫磷、pyridapenthion、喹噁磷、sulprofos、替美福司、terbufos、司替罗磷、甲基乙拌磷、triazophos、敌百虫、蚜灭多。2.氨基甲酸酯类aldicarb、甲基氨基甲酸2-仲丁基苯基酯(BPMC)、卡巴立、虫螨威、丁硫克百威、cloethocarb、丙硫克百威、ethiofencarb、呋线威、isoprocarb、methomyl、5-甲基间枯烯基丁酰基(甲基)氨基甲酸酯、草氨酰(oxamyl)、pirimicarb、残杀威、硫双灭多威、thiofanox和棉铃威。3.合成除虫菊酯类acrinathrin、allethrin、α-氯氰菊酯、5-苄基-3-呋喃基甲基-(E)-(1R)-顺-2,2-二二甲基-3-(2-oxothiolan-3-ylidene甲基)环丙烷-甲酸酯、bioallethrin、bioallethrin((S)-环戊基异构体)、除虫菊酯、biphenate、乙氰菊酯、cyhalothrin、氯氰菊酯、苯醚氰菊酯、deltamethrin、烯炔菊酯、高氰戊菊酯、芬氟司林、甲氰菊酯、高氰戊菊酯、氟氰戊菊酯、flumethrin、氟胺氰菊酯(D-异构体)、氟氯菊酯、扑灭司林、苯氧司林((R)-异构体)、炔酮菊酯、除虫菊酯(天然产物)、苄呋菊酯、七氟菊酯、四甲司林、四溴菊酯。4.其它阿米曲士、fenbutatin oxide、阿巴美丁、苏云金牙孢杆菌、bensultap、乐杀螨、bromopropylate、噻嗪酮、巴丹、乙酯杀螨醇、定虫隆、四螨嗪、灭蝇胺、dicofol、氟铃脲、diflubenzuron、N-(2,3-二氢-3-甲基-1,3-噻唑-2-亚基)-2,4-二甲代苯胺、dinobuton、dinocap、硫丹、醚菊酯、(4-乙氧基苯基)(二甲基)(3-(3-苯氧基苯基)丙基)硅烷、silafluofen、唑螨酯、喹螨醚、双氧威、fipronil、fluazuron、氟虫脲、flubenzimine、氟螨脲、γ-HCH、hexathiazox、氟铃脲、伏蚁腙、咪蚜胺、伊维菌素、lufenuron、acetamiprid、nithiazine、propargite、pymetrozin、梅笠草烯、哒螨酮、triazamate、tebufenozid、tebufenpyrod、仪虫隆、四氯二苯砜、tetrasul、thiocyclam、triflumuron。
在由市售制剂制备的即用剂型中的活性成分的含量可以在很宽的范围内变化,活性成分的浓度范围是0.0001-95%(重量),优选0.001-1%(重量)。按照适用于具体施用形式的常规方法进行使用。
下列实施例用于说明本发明、而非限制其范围。A.制剂实施例a)通过将10份(重量)的活性成分与作为惰性成分的90份(重量)的滑石混合,并在锤磨机上粉碎,制备尘剂组合物。b)通过将25份(重量)活性成分、作为惰性成分的65份(重量)含石英高岭土、10份(重量)木素磺酸钾和作为润湿剂和分散剂的1份(重量)油基甲基牛磺酸钠盐混合,并在pinneddisk磨机上研磨,制备可湿性粉末。c)通过将40份(重量)活性成分与7份(重量)磺酰琥珀酸半酯、2份(重量)木素磺酸钠和51份(重量)水混合,并在球磨机上研磨成小于5微米,制备易分散于水中的可分散浓缩液。d)由15份(重量)活性成分、作为溶剂的75份(重量)环己酮和作为乳化剂的10份(重量)壬酚乙氧基化物(10 AeO)制备可乳化的浓缩物。e)由2-15份(重量)活性成分和惰性颗粒载体物质如美国活性白土、浮石颗粒和/或石英砂制备颗粒剂。将含有30%固体物质成分的实施例b)的合适的可湿性粉末悬浮液喷雾在美国活性白土颗粒的表面,干燥并紧密混合。由此,该即用颗粒含有约5%(重量)可湿性粉末和约95%(重量)载体物质。B.化学实施例
所得化合物的结构由nmr和/或其它合适的分析方法证实。实施例1N-[2-(3,4-二甲氧基苯基)乙基]-4-氯扁桃酰胺
向在250ml丙酮中的269.5g(1.19mol)2,2-二甲基-4-(4-二氯苯基)-1,3-二氧戊环酮溶液中加入323.3g(1.78mol)2-(3,4-二甲氧基苯基)乙胺。在50℃搅拌反应混合物24小时。真空蒸馏掉低沸点物质,将残余物溶于1500ml乙酸乙酯中,用各1000ml的1N的盐酸、饱和碳酸氢钠水溶液和饱和氯化钠水溶液洗涤该溶液。用硫酸钠干燥有机相后,将有机相浓缩,吸滤残余物,并洗涤4次,每次用500ml正丙烷洗涤。真空干燥后,得到377.8g(理论值的90.5%)淡米色固体物质,熔点为100-101℃。实施例2N-(3-苯基丙基)-4-三氟甲基扁桃酰胺
向在25ml乙醚中的3g(0.0115mol)2,2-二甲基-4-(4-三氟甲基苯基)-1,3-二氧戊环酮溶液中加入1.55g(0.012mol)3-苯基丙胺。在室温搅拌该混合物16小时。吸滤出沉淀,用少量乙醚和正戊烷洗涤,并真空干燥。由此得到30g(理论值的77%)白色固体物质,熔点为107℃。实施例3N-(1-苯基环戊基)-甲基-4-氯扁桃酰胺
向在25ml乙醚中的2.2g(0.0097mol)2,2-二甲基-4-(4-氯苯基)-1,3-二氧戊环酮溶液中加入3.06g(0.0175mol)(1-苯基环戊基)甲胺。在室温搅拌该混合物16小时。然后将其溶于100ml乙酸乙酯中,有机溶液用各100ml的1N盐酸、饱和碳酸氢钠水溶液和饱和氯化钠水溶液洗涤,用硫酸钠干燥有机相。真空除去溶剂后,得到2.9g(理论值的87%)白色固体物质,熔点为84℃。实施例4N-[2-(3,4-二甲氧基苯基)乙基]-α-炔丙基-4-氯扁桃酰胺
向在5ml四氢呋喃中的3.97g(0.015mol)2,2-二甲基-4-(4-氯苯基)-4-炔丙基-1,3-二氧戊环酮溶液中加入4.08g(0.0225mol)2-(3,4-二甲氧基苯基)-乙胺。在60℃搅拌该混合物16小时,真空蒸馏除去低沸点物质。将残余物溶于100ml乙酸乙酯中,用各100ml的1N的盐酸、饱和碳酸氢钠水溶液和饱和氯化钠水溶液洗涤。用硫酸钠干燥有机相后,真空除去溶剂,由此得到5.0g(理论值的86%)无色油状物。实施例5N-甲基-N-[2-(3,4-二甲氧基苯基)-乙基]-4-氯扁桃酰胺
在搅拌下,向3.0g(0.013mol)2,2-二甲基-4-(4-氯苯基)-1,3-二氧戊环酮中加入5.08g(0.026mol)N-[2-(3,4-二甲氧基苯基)乙基]甲胺。在室温搅拌16小时后,将反应混合物溶于100ml乙酸乙酯中,用各100ml的1N的盐酸、饱和碳酸氢钠水溶液和饱和氯化钠水溶液洗涤。用硫酸钠干燥有机相后,真空分离低沸点物质,由此得到2.2g(理论值的46%)淡黄色油状物。实施例6N-[2-(3,4-二甲氧基苯基)乙基]-N,O-二甲基-4-氯扁桃酰胺
在0-10℃和搅拌下,向在100ml二甲基甲酰胺中的5.0g(0.0143mol)N-[2-(3,4-二甲氧基苯基)乙基]-4-氯扁桃酰胺溶液中分批加入1.25g(0.0313mol)60%氢化钠。在10℃搅拌30分钟后,滴加5.82g(0.0313mol)碘甲烷,并在此温度下搅拌该混合物1小时,然后在室温搅拌2小时。将反应混合物倒入冰水中,各用200ml乙酸乙酯萃取2次,合并的有机相用硫酸钠干燥并真空浓缩。残余物在硅胶上过滤(乙酸乙酯/石油醚1∶1)。由此得到4.5g(理论值的83%)淡黄色油状物。实施例75-(4-氯苯基)-3-[2-(3,4-二甲氧基苯基)乙基-1,3-噁唑烷-4-酮
在0-10℃和搅拌下,向在100ml二甲基甲酰胺中的5g(0.0143mol)N-[2-(3,4-二甲氧基苯基)乙基]-4-氯扁桃酰胺溶液中分批加入1.25g(0.313mol)60%氢化钠。在0-5℃保持30分钟后,滴加5.832g(0.313mol)二溴甲烷,并在0-5℃搅拌该混合物1小时,然后在室温搅拌2小时。将反应混合物倒入800ml冰水中,用乙酸乙酯萃取2次,合并的有机相用硫酸钠干燥并真空浓缩。残余物在硅胶上过滤(乙酸乙酯/石油醚1∶1)后。得到3.0g(理论值的58%)淡黄色油状物。实施例8O-乙酰基-N-[2-(3,4-二甲氧基苯基)乙基]-4-溴扁桃酰胺
向在50ml二氯甲烷中的1.0g(0.0025mol)N-[2-(3,4-二甲氧基苯基)乙基]-4-溴扁桃酰胺溶液中滴加在10ml二氯甲烷中的1.75g(0.02mol)乙酰氯,在0-10℃保持10分钟后,滴加2.02g(0.02mol)三乙胺,并在此温度搅拌该混合物1.5小时。加入5ml甲醇后,将反应混合物加入150ml饱和碳酸氢钠水溶液中,用二氯甲烷萃取2次,合并的有机相用硫酸钠干燥。残余物在硅胶上过滤(乙酸乙酯/石油醚1∶1)后,得到3.7g(理论值的94%)米色固体,熔点91℃。实施例9N-[2-(3,4-二甲氧基苯基)乙基]苯基乙醛酰胺
在搅拌和回流下,向在100ml氯仿中的3.15g(0.01mol)N-[2-(3,4-二甲氧基苯基)乙基]扁桃酰胺溶液中分批加入5.22g(0.06mol)活性二氧化锰。回流2小时后,将该混合物过滤,将滤饼煮沸3次,每次用150ml氯仿,并用热的氯仿洗涤3次。真空分离溶剂,得到3.0g(理论值的96%)无色固体,熔点80℃。实施例10N-[2-(3,4-二甲氧基苯基)乙基]苯基乙醛酰胺
在室温和搅拌下,向在40ml无水二氯甲烷中的3.37g(0.02mol)苯基乙醛酰氯溶液中滴加4.35g(0.022mol)2-(3,4-二甲氧基苯基)乙胺和2.42g(0.022mol)三乙胺的混合物。在42℃温热反应混合物。30分钟后,将反应混合物倒入40ml 2N盐酸中,有机相用各50ml的饱和碳酸氢钠水溶液和饱和氯化钠水溶液洗涤,用硫酸钠干燥,并真空蒸馏除去低沸点物质。由此得到5.7g(理论值的91%)无色固体,熔点80℃。实施例11N-[2-(3,4-二甲氧基苯基)乙基]-2-氟-4-三氟甲基扁桃酰胺
在室温和氮气氛下,将2-氟-4-三氟甲基扁桃酸(1.00g)和N-羟基琥珀酰亚胺(0.48g)溶于无水二甲氧基乙烷(50ml)中。一次加入二环己基碳二亚胺(0.87g),10分钟后形成白色沉淀(二环己基脲)。在室温再搅拌15分钟后,加入2-(3,4-二甲氧基苯基)乙胺(0.86g)。将悬浮液搅拌2小时,滤出二环己基脲,并蒸发残余物。得到3.0g粗品物质,将其经硅胶色谱纯化(乙酸乙酯),然后用二异丙醚中重结晶。产量:1.52g=理论值的90.5%。熔点108-9℃。实施例12N-[2-(3,4-二甲氧基苯基)乙基]-4-氰基扁桃酰胺
在搅拌下,向在无水二氯甲烷(8ml)和吡啶(0.67ml)中的4-氰基扁桃酸(0.7g,4.0mmol)与催化量的二甲基氨基吡啶的混合物中滴加三甲基甲硅烷基氯(1.1ml)。将该混合物在室温搅拌4小时,冷却至0℃,加入3滴二甲基甲酰胺,然后加入草酰氯(0.36ml)。在0℃再搅拌该混合物1小时,并在室温搅拌30分钟。将其冷却至0℃,加入在无水吡啶(1ml)中的2-(3,4-二甲氧基苯基)乙胺(0.8g)。在室温搅拌该混合物2小时。加入在甲醇(8ml)中的柠檬酸(0.92g),在室温搅拌该混合物0.5小时。将其放置过夜。加入乙酸乙酯(50ml),用1N盐酸(40ml)洗涤该溶液,并用乙酸乙酯萃取含水萃取液。萃取液用饱和碳酸氢钠水溶液(15ml)、盐水(15ml)洗涤,干燥并蒸发。残余物经硅胶色谱纯化,得到0.9g棕色胶状产物。实施例13N-[2-(3,4-二甲氧基苯基)-2-羟基-1,1-二甲基乙基]-4-氯扁桃酰胺
将4-氯扁桃酸甲酯(0.44g)和2-氨基-2-(3,4-二甲氧基苯基)-2-甲基丙醇(0.86g)的混合物在120-130℃一起加热4小时。将所得胶状物溶于乙醚中,并蒸发该溶液。残余物经硅胶色谱纯化(乙酸乙酯/石油醚(沸点60-80℃);4∶1),得到0.35g玻璃状产物(Rf=0.5)。实施例14N-苯基乙基扁桃酰胺
制备在甲醇(25ml)中的钠(1.27g)溶液并冷却。加入扁桃酰胺(7.6g)和碳酸二乙酯(6.5g)在甲醇(20ml)中的溶液。加热至70℃使所形成的白色固体沉淀溶解。该混合物在此温度下保持1小时。蒸发甲醇并将冷却的液体溶于水(75ml)中,用浓盐酸酸化至pH1。该混合物用乙酸乙酯萃取,将萃取物干燥并蒸发,得到5-苯基噁唑烷-2,4-二酮,熔点95-8℃。
将该产物(4.4g)、无水碳酸钾(3.75g)和丙酮(75ml)的混合物在室温搅拌1小时。加入在丙酮(25ml)中的2-溴乙基苯(3.5ml),并将该混合物加热回流过夜。将该混合物过滤并蒸发滤液,用二异丙醚萃取。蒸发萃取液,将残余物冷却,得到3-(2-苯基乙基)-5-苯基噁唑烷-2,4-二酮,熔点82-3℃。
将该产物加至用氮气吹扫的无水甲醇(50ml)中,然后加入固体甲醇钠(0.29g)。将该混合物搅拌5小时,倒入稀盐酸中,蒸发有机层,用乙酸乙酯/水萃取,有机层用水洗涤,干燥并蒸发,得到0.48g油状标题化合物。实施例15N-[2-(3,4-二甲氧基苯基)乙基]-O-甲基-3,4-二氯扁桃酰胺
将2-(3,4-二甲氧基苯基)乙胺(0.37g)加入O-甲基-3,4-二氯扁桃酸甲酯(0.37g)中,将该混合物加热至103℃,保持3小时。该混合物用乙酸乙酯萃取,用2M盐酸洗涤萃取液。有机部分用硫酸镁干燥、过滤并蒸发溶剂。残余物经硅胶色谱纯化,得到黄色油状标题产物,产率55%。实施例16N-[2-(3,4-二甲氧基苯基)-1,1-二甲基乙基]-4-氯扁桃酰胺
在-60℃和氮气氛下,用注射器向在无水四氢呋喃(150ml)中的二异丙胺(8.08g)中滴加丁基锂(32ml)。将该混合物温热至-5℃,然后再冷却至-60℃,并用在四氢呋喃(20ml)中的异丁酸(3.52g)溶液处理。将混合物温热至室温,加入在四氢呋喃(15ml)中的1,3-二甲基-3,4,5,6-四氢-2(1H)-嘧啶酮(5.12g)。在室温搅拌该混合物5小时。在-5℃用注射器向该混合物中加入在四氢呋喃(15ml)中的3,4-二甲氧基苄基氯(7.44g)。在室温搅拌该混合物16小时。加入饱和氯化铵(10ml)。用氢氧化钠水溶液(7%)萃取该混合物。萃取液用乙醚萃取。水层用盐酸酸化。固体用二氯甲烷萃取,将萃取液干燥、蒸发。残余物用冷水研制并过滤。白色固体用二氯甲烷萃取,干燥并蒸发,得到3-(3,4-二甲氧基苯基)-2,2-二甲基丙酸,熔点102-8℃。
用亚硫酰氯(2.46g)处理在甲苯(10ml)中的该产物(4.9g)的悬浮液,并将该混合物在80℃搅拌2小时。将该混合物减压蒸发,将残余的液体加入无水丙酮(10ml)中,并在0℃将该溶液加入搅拌着的叠氮化钠(2.68h)的丙酮(28ml)和水(22ml)溶液中。向该溶液中加入水(30ml),用甲苯萃取该混合物。萃取液用无水硫酸镁干燥,并且在氮气氛和搅拌下,于80-90℃加热2小时。将该混合物冷却至室温,用浓盐酸(3.8ml)处理,在80-90℃搅拌5分钟。将其冷却至室温并过滤,用乙醚洗涤后收集片状固体。滤液用水洗涤,干燥并蒸发。残余物溶于四氢呋喃中,加入浓盐酸(2ml)。将其搅拌20分钟并蒸发。将固体残余物溶于水中,用碳酸钠水溶液使其碱化并用二氯甲烷萃取。将其与溶于水中的片状固体合并,碱化,并用二氯甲烷反萃取,将这两种萃取物干燥并蒸发,得到2-(3,4-二甲氧基苯基)-1-甲基丙胺,熔点116-8℃。
然后按照与实施例12相似的方法,将其与三甲基甲硅烷基氯和4-氯扁桃酸反应,经硅胶色谱纯化(乙酸乙酯/石油醚(沸点60-80℃,4∶1)),得到玻璃状的标题化合物(Rf=0.5)。
可以如上所述进行制备的本发明典型的实施例化合物描述于下表1-7中。
表1:
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1 | H | 3,4-(OMe)2 | H | H | H | CH2CH2 | 103 |
2 | 2-F | 3,4-(OMe)2 | H | H | H | CH2CH2 | 108 |
3 | 3-F | 3,4-(OMe)2 | H | H | H | CH2CH2 | 69 |
4 | 4-F | 3,4-(OMe)2 | H | H | H | CH2CH2 | 95 |
5 | 2,3-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 93 |
6 | 2,4-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 92-94 |
7 | 2,5-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 71 |
8 | 2,6-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 133 |
9 | 3,4-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 79-80 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
10 | 3,5-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 80 |
11 | 2,3,4-F3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
12 | -F5 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
13 | 2-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | 84 |
14 | 3-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
15 | 4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | 102 |
16 | 2,3-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 103 |
17 | 2,4-Cl2 | 3,4-(OMó)2 | H | H | H | CH2CH2 | 83 |
18 | 2,5-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
19 | 2,6-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
20 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 71 |
21 | 3,5-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 胶状 |
22 | 2,3,4-Cl3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
23 | 2,3,5-Cl3 | 3,4-(OMe)2 | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.P.[℃] |
24 | 3,4,5-Cl3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
25 | 4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2 | 96 |
26 | 3,4-Br2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
27 | 3,4,5-Br3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
28 | 4-I | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
29 | 3,4-I2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
30 | 3,4,5-I3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
31 | 3-Br,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
32 | 3-Cl,4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
33 | 3-I.4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
34 | 3-Cl,4-I | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
35 | 3-F,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
36 | 3-F,4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
37 | 2,3,5,6-F4,4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
38 | 2,3,5,6-F4,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
39 | 4-CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 105 |
40 | 3,4-(CF3)2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
41 | 3-OH4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
42 | 3-Cl.4-OH | 3,4-(OMe)2 | H | H | H | CH2CH2 | 144 |
43 | 3-CF3,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
44 | 3-CF3,4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
45 | 4-NO2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
46 | 4-CN | 3,4-(OMe)2 | H | H | H | CH2CH2 | 胶状 |
47 | 4-SO2CH3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
48 | 4-SO2CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
49 | 4-SO2 NH2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
50 | 4-SO2NHMe | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
51 | 4-SO2NMe2 | 3,4-(OMe)2 | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
52 | 4-SO3Me | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
53 | 4-SO3CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
54 | 4-SO3H | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
55 | 4-CO2H | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
56 | 4-CO2Me | 34-(OMe)2 | H | H | H | CH2CH2 | 117 |
57 | 4-OCOMe | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
58 | 4-NHCOMe | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
59 | 4-COMe | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
60 | 4-CONMe2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
61 | 4-Me | 3,4-(OMe)2 | H | H | H | CH2CH2 | 129 |
62 | 3,4-Me2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 104 |
63 | 2,4,6-Me3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 127 |
64 | 3,4,5-Me3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
65 | 3-Cl,4-Me | 3,4-(OMe)2 | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
66 | 3-Br,4-Me | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
67 | 3-Me,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
68 | 3-Me,4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
69 | 4-tBu | 3,4-(OMe)2 | H | H | H | CH2CH2 | 97 |
70 | 4-SiMe3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
71 | 4-Ph | 3,4-(OMe)2 | H | H | H | CH2CH2 | 149 |
72 | 2-Ph | 3,4-(OMe)2 | H | H | H | CH2CH2 | 122-3 |
73 | 4-Et | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
74 | 4-Pr | 3,4-(OMe) | H | H | H | CH2CH2 | |
75 | 4-iPr | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
76 | 4-Bu | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
77 | 4-C12H25 | 3,4-(OMe)2 | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
116 | 4-OP(O)(OMe)2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
117 | 4-P(O)(OMe)2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
118 | 3-Br | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
119 | 2,4-(OMe)2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 122 |
120 | 2-Br | 3,4-(OMe)2 | H | H | H | CH2CH2 | 85 |
121 | H | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
122 | 2-F | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
123 | 3-F | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
124 | 4-F | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
125 | 2,3-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
126 | 2,4-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
127 | 2,5-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
128 | 2,6-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
129 | 3,4-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
130 | 3,5-F2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
132 | 2,3,4-F3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
133 | -F5 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
134 | 2-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
135 | 3-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
136 | 4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | 105 |
137 | 2,3-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
138 | 2,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
139 | 2,5-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
140 | 2,6-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
141 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | 107 |
142 | 3,5-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
143 | 2,3,4-Cl3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
144 | 2,3,5-Cl3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
145 | 3,4,5-Cl3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
146 | 4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | 120 |
147 | 3,4-Br2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
148 | 3,4,5-Br3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
149 | 4-I | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
150 | 3,4-I2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
151 | 3,4,5-I3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
152 | 3-Br,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
153 | 3-Cl,4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2C-H2 | |
154 | 3-I,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
155 | 3-Cl.4-I | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
156 | 3-F,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
157 | 3-F,4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
158 | 2,3,5,6-F4,4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
159 | 2,3,5,6-F4 4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
160 | 4-CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
161 | 3,4-(CF3)2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
162 | 3-OH,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
163 | 3-Cl,4-OH | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
164 | 3-CF3,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
165 | 3-CF3,4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
166 | 4-NO2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
167 | 4-CN | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
168 | 4-SO2CH3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
169 | 4-SO2CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
170 | 4-SO2NH2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
171 | 4-SO2NMe | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
172 | 4-SO2NMe2 | 3-4-(OMe)2 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
173 | 4-SO3Me | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
174 | 4-SO3CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
175 | 4-SO3H | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
176 | 4-CO2H | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
177 | 4-CO2Me | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
178 | 4-OCOMe | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
179 | 4-NHCOMe | 3.4-(OMe)2 | H | H | H | CH2CH2CH2 | |
180 | 4-COMe | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
181 | 4-CONMe2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
182 | 4-COMe | 3,4-(OMo)2 | H | H | H | CH2CH2CH2 | |
183 | 3,4-Me2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
184 | 2,4,6-Me3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
185 | 3,4,5-Me3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
186 | 3-Cl,4-Me | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.(℃] |
187 | 3-Br,4-Me | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
188 | 3-Me,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
189 | 3-Me,4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
190 | 4-tBu | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
191 | 4-SiMe3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
192 | 4-Ph | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
193 | 2-Ph | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
194 | 4-Et | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
195 | 4-Pr | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
196 | 4-iPr | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
197 | 4-Bu | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 | |
198 | 4-C12H25 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
245 | 2,5-F2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
246 | 2,6-F2 | B-OMe,4-OEt | H | H | H | CH2CH2 | |
247 | 3,4-F2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
248 | 3,5-F2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
249 | 2,3,4-F3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
250 | -F5 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
251 | 2-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
252 | 3-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
253 | 4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2 | 96 |
254 | 2,3-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
255 | 2,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
256 | 2,5-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
257 | 2,6-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
258 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | 95 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
259 | 3,5-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
260 | 2,3,4-Cl3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
261 | 2,3,5-Cl3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
261 | 3,4,5-Cl3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
262 | 4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2 | 96-7 |
263 | 3,4-Br2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
264 | 3,4,5-Br3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
265 | 4-I | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
266 | 3,4-I2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
267 | 3,4,5-I3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
268 | 3-Br,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
269 | 3-Cl,4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
270 | 3-I,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
271 | 3-Cl,4-I | 3-OMe,4-OEt | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
271 | 3-F,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
272 | 3-F,4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
273 | 2,3,5,6-F4,4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
274 | 2,3,5,G-F4,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
275 | 4-CF3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | 87 |
276 | 3,4-(CF3)2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
277 | 3-OH,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
278 | 3-Cl,4-OH | 3-OMe, 4-OEt | H | H | H | CH2CH2 | |
279 | 3-CF3,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
280 | 3-CF3,4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
281 | 4-NO2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
282 | 4-CN | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
283 | 4-SO2CH3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
284 | 4-SO2CF3 | 3,OMe,4-OEt | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
285 | 4-SO2NH2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
286 | 4-SO2NHMe | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
287 | 4-SO2NMe2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
288 | 4-SO3Me | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
289 | 4-SO3CF3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
290 | 4-SO3H | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
291 | 4-CO2H | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
292 | 4-CO2Me | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
293 | 4-OCOMe | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
294 | 4-NHCOMe | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
295 | 4-COMe | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
296 | 4-CONMe2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
297 | 4-Me | 3-OMe,4-OEt | H | H | H | CH2CH2 | 81 |
298 | 3,4-Me2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | 113 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
299 | 2,4,6-Me3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
300 | 3,4,5-Me3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
301 | 3-Cl,4-Me | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
302 | 3-Br,4-Me | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
302 | 3-Me,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
303 | 3-Me,4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
304 | 4-tBu | 3-OMe,4-OEt | H | H | H | CH2CH2 | 油状 |
305 | 4-SiMe3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
306 | 4-Ph | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
307 | 2-Ph | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
308 | 4-Et | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
309 | 4-Pr | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
310 | 4-iPr | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
311 | 4-Bu | 3-OMe,4-OEt | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[C] |
357 | 4-F | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
358 | 2,3-F2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
359 | 2,4-F2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
360 | 2,5-F2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
361 | 2,6-F2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
362 | 3,4-F2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
363 | 3,5-F2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
364 | 2,3,4-F3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
365 | -F5 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
366 | 2-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
367 | 3-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
368 | 4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
369 | 2,3-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
370 | 2,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
371 | 2,5-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
372 | 2,6-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
373 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
374 | 3,5-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
375 | 2,3,4-Cl3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
376 | 2,3,5-Cl3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
377 | 3,4,5-Cl3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
378 | 4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
379 | 3,4-Br2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
380 | 3,4,5-Br3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
381 | 4-I | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
382 | 3,4-I2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
383 | 3,4,5-I3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
384 | 3-Br,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
385 | 3-Cl-4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
386 | 3-I,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
387 | 3-Cl,4-I | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
388 | 3-F,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
389 | 3-F,4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
390 | 2,3,5,6-F4,4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
400 | 2,3,5,6-F4,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
401 | 4-CF3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
402 | 3,4-(CF3)2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
403 | 3-OH,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
404 | 3-Cl,4-OH | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
405 | 3-CF3,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
405 | 3-CF3,4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
406 | 4-NO2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
407 | 4-CN | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
408 | 4-SO2CH3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
409 | 4-SO2CF3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
410 | 4-SO2NH2 | B-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
411 | 4-SO2NHMe | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
412 | 4-SO2NMe2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
413 | 4-SO3Me | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
414 | 4-SO3CF3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
415 | 4-SO3H | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
416 | 4-CO2H | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
417 | 4-CO2Me | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
418 | 4-OCOMe | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
419 | 4-NHCOMe | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
420 | 4-COMe | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
421 | 4-CONMe2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
422 | 4-Me | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
423 | 3,4-Me2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
424 | 2,4,6-Me3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
425 | 3,4,5-Me3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
426 | 3-Cl,4-Me | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
427 | 3-Br,4-Me | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
428 | 3-Me,4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
429 | 3-Me,4-Br | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
430 | 4-lBu | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
431 | 4-SiMe3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
432 | 4-Ph | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
433 | 2-Ph | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
434 | 4-Et | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p-[℃] |
462 | 4-OCF3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
463 | 3,4-(OCF3)2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
464 | 3,4-(OCF2O) | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
465 | 4-OCH(CF3)CF2H | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
466 | 4-SMe | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
467 | 4-SCF3 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
468 | 4-SPh | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
469 | 4-SBu | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
470 | 4-CHO | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
471 | 4-NH2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 | |
472 | 4-NMe2 | 3-OMe,4-OEt | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.(℃] |
480 | 2-F | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
481 | 3-F | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
482 | 4-F | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
483 | 2,3-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
484 | 2,4-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
485 | 2,5-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
486 | 2,6-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
487 | 3,4-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
488 | 3,5-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
489 | 2,3,4-F3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
490 | -F5 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
491 | 2-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
492 | 3-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
493 | 4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | 122 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
494 | 2,3-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
495 | 2,4-Cl2 | 3,,5-(OMe)3 | H | H | H | CH2CH2 | |
496 | 2,5-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
497 | 2,6-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
498 | 3,4-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
499 | 3,5-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
500 | 2,3,4-Cl3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
501 | 2,3,5-Cl3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
501 | 3,4,5-Cl3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
502 | 4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | 120 |
503 | 3,4-Br2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
504 | 3,4,5-Br3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
505 | 4-I | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
506 | 3,4-I2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
507 | 3,4,5-I3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
508 | 3-Br,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
509 | 3-Cl,4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
510 | 3-I,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
511 | 3-Cl,4-I | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
512 | 3-F,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
513 | 3-F,4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
514 | 2,3,5,6-F4,4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
515 | 2,3,5,6-F4,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
516 | 4-CF3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
517 | 3,4-(CF3)2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
518 | 3-OH,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
519 | 3-Cl,4-OH | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
520 | 3-CF3,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
521 | 3-CF3,4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
522 | 4-NO2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
523 | 4-CN | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
524 | 4-SO2CH3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
525 | 4-SO2CF3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
526 | 4-SO2NH2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
527 | 4-SO2NHMe | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
528 | 4-SO2NHMe2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
529 | 4-SO3Me | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
530 | 4-SO3CF3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
531 | 4-SO3H | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
532 | 4-CO2H | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
533 | 4-CO2Me | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
534 | 4-OCOMe | 3,4,5-(OMe)3 | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
535 | 4-NHCOMe | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
536 | 4-COMe | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
537 | 4-CONMe2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
538 | 4-Me | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
539 | 3,4-Me2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
540 | 2,4,6-Me3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
541 | 3,4,5-Me3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
542 | 3-Cl,4-Me | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
543 | 3-Br,4-Me | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
544 | 3-Me,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
545 | 3-Me,4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
546 | 4-tBu | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
547 | 4-SiMe3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
548 | 4-Ph | 3,4,5-(OMe)3 | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
577 | 4-OCFH2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
578 | 4-OCF3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
579 | 3,4-(OCF3)2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
580 | 3,4-(OCF2O) | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
581 | 4-OCH(CF3)CF2H | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
582 | 4-SMe | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
583 | 4-SCF3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
584 | 4-SPh | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
585 | 4-SBu | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
586 | 4-CHO | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
587 | 4-NH2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 | |
588 | 4-NMe2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
598 | 4-F | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
599 | 2,3-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
600 | 2,4-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
601 | 2,5-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
602 | 2,6-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
603 | 3,4-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
604 | 3,5-F2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
605 | 2,3,4-F3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
606 | -F5 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
607 | 2-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
608 | 3-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
609 | 4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
610 | 2,3-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
611 | 2,4-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
612 | 2,5-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
613 | 2,6-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
614 | 3,4-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
615 | 3,5-Cl2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
616 | 2,3,4-Cl3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
617 | 2,3,5-Cl3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
618 | 3,4,5-Cl3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
619 | 4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
620 | 3,4-Br2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
621 | 3,4,5-Br3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
622 | 4-I | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
623 | 3,4-I2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
624 | 3,4,5-I3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
625 | 3-Br,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.P[℃] |
626 | 3-Cl,4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
627 | 3-I,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
628 | 3-Cl,4-I | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
629 | 3-F,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
630 | 3-F,4-B | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
631 | 2,3,5,6-F4,4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
632 | 2,3,5,6-F4,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
633 | 4-CF3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
634 | 3,4-(CF3)2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
635 | 3-OH,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
636 | 3-Cl,4-OH | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
637 | 3-CF3,4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
638 | 3-CF3,4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
639 | 4-NO2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
640 | 4-CN | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
641 | 4-SO2CH3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
642 | 4-SO2CF3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
643 | 4-SO2NH2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
644 | 4-SO2NHMe | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
645 | 4-SO2NMe2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
646 | 4-SO3Me | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
647 | 4-CO3CF3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
648 | 4-SO3H | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
649 | 4-CO2H | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
650 | 4-CO2Me | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
651 | 4-OCOMe | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
652 | 4-NHCOMe | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
653 | 4-COMe | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p [℃] |
654 | 4-CONMe2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
655 | 4-Me | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
656 | 3,4-Me2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
658 | 2,4,6-Me3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
659 | 3,4,5-Me3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
660 | 3-Cl,4-Me | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
661 | 3-Br,4-Me | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
662 | 3-Me,4-Cl | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
663 | 3-Me,4-Br | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
664 | 4-tBu | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
665 | 4-SiMe3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
666 | 4-Ph | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
667 | 2-Ph | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
668 | 4-Et | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | n1.p.[℃] |
695 | 4-OCFH2 | 3,4,5(OMe)3 | H | H | H | CH2CH2CH2 | |
696 | 4-OCF3 | 3,4,5[OMe]3 | H | H | H | CH2CH2CH2 | |
697 | 3,4-[OCF3]2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
698 | 3,1(OCF2O) | 3,4,5(OMe)3 | H | H | H | CH2CH2CH2 | |
699 | 4-OCH(CF3)CF2H | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
700 | 4-SMe | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
701 | 4-SCF3 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
702 | 4-SPh | 3,4,5(OMe)3 | H | H | H | CH2CH2CH2 | |
703 | 4-SPh | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
704 | 4-SBn | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 | |
705 | 4-CHO | 3,4,5(OMe)3 | H | H | H | CH2CH2CH2 | |
706 | 4-NH2 | 3,4,5(OMe)3 | H | H | H | CH2CH2CH2 | |
707 | 4-NMo2 | 3,4,5-(OMe)3 | H | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
717 | 3,4-Br2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
718 | 4-I | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
719 | 4-Me | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
720 | 3,4-Me2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
721 | 3-Cl,4-Me | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
722 | 3-Me,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
723 | 4-CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
724 | 3,4-(CF3)2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
725 | 4-Cl,3-CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
726 | 4-NO2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
727 | 4-CN | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
728 | 4-CHO | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
729 | 4-NHCOCH3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
730 | 4-SO2CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
731 | 4-OCF3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
732 | 4-SCF3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
733 | 3,4,5-Cl3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
734 | 4-OCOCH3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
735 | 4-OH | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
736 | 4-Cl,3-F | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
737 | 4-Br,3-F | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
738 | 4-CO2Me | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
739 | 4-Et | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
740 | 4-Cl | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | 93 |
741 | 4-Br | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | 91 |
742 | 3,4-Cl2 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | 胶状 |
743 | 4-CF3 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | 108 |
744 | 4-Me | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p [℃] |
745 | 4-NO2 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | |
746 | 4-CN | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | |
747 | 4-OCOCH3 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | |
748 | 4-SO2CF3 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | |
749 | 3-F,4-Cl | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | |
750 | 4-NHCOCH3 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | |
751 | 4-Cl | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2CH2 | |
752 | 4-Br | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2CH2 | |
753 | 3,4-Cl2 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2CH2 | 油状 |
754 | 4-CF3 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2CH2 | |
755 | 4-Me | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2CH2 | |
756 | 4-NO2 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2CH2 | |
757 | 4-CN | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2CH2 | |
758 | 4-OCOCH3 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
834 | 4-Br | 3,4-(OMe)2 | CO2Me | H | H | CH2CH2 | |
835 | 3,4-Cl2 | 3,4-(OMe)2 | CO2Me | H | H | CH2CH2 | |
836 | 4-CF3 | 3,4-(OMe)2 | CO2Me | H | H | CH2CH2 | |
837 | 4-Me | 3,4-(OMe)2 | CO2Me | H | H | CH2CH2 | |
838 | 4-NO2 | 3,4-(OMe)2 | CO2Me | H | H | CH2CH2 | |
839 | 4-CN | 3,4-(OMe)2 | CO2Me | H | H | CH2CH2 | |
840 | 4-OCOCH3 | 3,4-(OMe)2 | CO2Me | H | H | CH2CH2 | |
841 | 4-SO2CF3 | 3,4-(OMe)2 | CO2Me | H | H | CH2CH2 | |
842 | 3-F,4Cl | 3,4-(OMe)2 | CO2Me | H | H | CH2CH2 | |
843 | 4-NCOCH3 | 3,4-(OMe)2 | CO2Me | H | H | CH2CH2 | |
844 | 4-Cl | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 | |
845 | 4-Br | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 | |
846 | 3,4-Cl2 | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 | |
847 | 4-CF3 | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
848 | 4-Me | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 | |
849 | 4-NO2 | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 | |
850 | 4-CN | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 | |
851 | 4-OCOCH2 | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 | |
852 | 4-SO2CF3 | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 | |
853 | 3-F,4-Cl | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 | |
854 | 4-NHCOCH3 | 3,4-(OMe)2 | CO2Ph | H | H | CH2CH2 | |
855 | 4-Cl | 3,4-(OMe)2 | Ph | H | H | CH2CH2 | |
856 | 4-Br | 3,4-(OMe)2 | Ph | H | H | CH2CH2 | |
857 | 3,4-Cl2 | 3,4-(OMe)2 | Ph | H | H | CH2CH2 | |
858 | 4-CF3 | 3,4-(OMe)2 | Ph | H | H | CH2CH2 | |
859 | 4-Me | 3,4-(OMe)2 | Ph | H | H | CH2CH2 | |
860 | 4-NO2 | 3,4-(OMe)2 | Ph | H | H | CH2CH2 | |
861 | 4-CN | 3,4-(OMe)2 | Ph | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
907 | 4-SO2CF3 | 3,4-(OMe)2 | H | CO2Me | H | CH2CH2 | |
908 | 3-F.4-Cl | 3,4-(OMe)2 | H | CO2Me | H | CH2CH2 | |
909 | 4-NHCOCH3 | 3,4-(OMe)2 | H | CO2Me | H | CH2CH2 | |
910 | 4-Cl | 3,4-(OMe)2 | H | CON2 | H | CH2CH2 | |
911 | 4-Br | 3,4-(OMe)2 | H | CONH2 | H | CH2CH2 | |
912 | 3,4-Cl2 | 3,4-(OMe)2 | H | CONH2 | H | CH2CH2 | |
913 | 4-CF3 | 3,4-(OMe)2 | H | CON2 | H | CH2CH2 | |
914 | 4-Me | 3,4-(OMe)2 | H | CONH2 | H | CH2CH2 | |
915 | 4-NO2 | 3,4-(OMe)2 | H | CONH2 | H | CH2CH2 | |
916 | 4-CN | 3,4-(OMe)2 | H | CONH2 | H | CH2CH2 | |
917 | 4-OCOCH3 | 3,4-(OMe)2 | H | CON-H2 | H | CH2CH2 | |
918 | 4-SO2CF3 | 3,4-(OMe)2 | H | CONH2 | H | CH2CH2 | |
919 | 3-F,4-Cl | 3,4-(OMe)2 | H | CONH2 | H | CH2CH2 | |
920 | 4-NHCOCH3 | 3,4-(OMe)2 | H | CONH2 | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
921 | 4-Cl | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | 120 |
922 | 4-Br | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | |
923 | 3,4-Cl2 | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | |
924 | 4-CF3 | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | |
925 | 4-Me | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | |
926 | 4-NO2 | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | |
927 | 4-CN | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | |
928 | 4-OCOCH3 | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | |
929 | 4-SO2CF3 | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | |
930 | 3-F,4-Cl | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | |
931 | 4-NHCOCH3 | 3,4-(OMe)2 | H | CH2Ph | H | CH2CH2 | |
932 | 4-Cl | 3,4-(OMe)2 | H | Me | H | CH2CH2 | 蜡状 |
933 | 4-Br | 3,4-(OMe)2 | H | Me | H | CH2CH2 | |
934 | 3,4-Cl2 | 3,4-(OMe)2 | H | Me | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
935 | 4-CF3 | 3,4-(OMe)2 | H | Me | H | CH2CH2 | |
936 | 4-Me | 3,4-(OMe)2 | H | Me | H | CH2CH2 | |
937 | 4-NO2 | 3,4-(OMe)2 | H | Me | H | CH2CH2 | |
938 | 4-CN | 3,4-(OMe)2 | H | Me | H | CH2CH2 | |
939 | 4-OCOCH3 | 3,4-(OMe)2 | H | Me | H | CH2CH2 | |
940 | 4-SO3CF3 | 3,4-(OMe)2 | H | Me | H | CH2CH2 | |
941 | 3-F,4-Cl | 3,4-(OMe)2 | H | Me | H | CH2CH2 | |
942 | 4-NHCOCH3 | 3,4-(OMe)2 | H | Me | H | CH2CH2 | |
943 | 4-Cl | 3,4-(OMe)2 | H | Bu | H | CH2CH2 | 油状 |
944 | 4-Br | 3,4-(OMe)2 | H | Bu | H | CH2CH2 | |
945 | 3,4-Cl2 | 3,4-(OMe)2 | H | Bu | H | CH2CH2 | |
946 | 4-CF3 | 3,4-(OMe)2 | H | Bu | H | CH2CH2 | |
947 | 4-Me | 3,4-(OMe)2 | H | Bu | H | CH2CH2 | |
948 | 4-NO2 | 3,4-(OMe)2 | H | Bu | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
949 | 4-CN | 3,4-(OMe)2 | H | Bu | H | CH2CH2 | |
950 | 4-OCOCH3 | 3,4-(OMe)2 | H | Bu | H | CH2CH2 | |
951 | 4-SO2CF3 | 3,4-(OMe)2 | H | Bu | H | CH2CH2 | |
952 | 3-F,4-Cl | 3,4-(OMe)2 | H | Bu | H | CH2CH2 | |
953 | 4-NHCOCH3 | 3,4-(OMe)2 | H | Bu | H | CH2CH2 | |
954 | 4-Cl | 3,4-(OMe)2 | Me | OMe | H | CH2CH2 | |
955 | 4-Br | 3,4-(OMe)2 | Me | OMe | H | CH2CH2 | |
956 | 3,4-Cl2 | 3,4-(OMe)2 | Me | OMe | H | CH2CH2 | |
957 | 4-CF3 | 3,4-(OMe)2 | Me | OMe | H | CH2CH2 | |
958 | 4-Me | 3,4-(OMe)2 | Me | OMe | H | CH2CH2 | |
959 | 4-NOx | 3,4-(OMe)2 | Me | OMe | H | CH2CH2 | |
960 | 4-CN | 3,4-(OMe)2 | Me | OMe | H | CH2CH2 | |
961 | 4-OCOCH3 | 3,4-(OMe)2 | Me | OMe | H | CH2CH2 | |
962 | 4-SO2CF3 | 3,4-(OMe)2 | Me | OMe | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
980 | 4-NO2 | 3,4-(OMe)2 | Me | CONH2 | H | CH2CH2 | |
981 | 4-CN | 3,4-(OMe)2 | Me | CONH2 | H | CH2CH2 | |
982 | 4-OCOCH3 | 3,4-(OMe)2 | Me | CONH2 | H | CH2CH2 | |
983 | 4-SO2CF3 | 3,4-(OMe)2 | Me | CONH2 | H | CH2CH2 | |
984 | 3-F,4-Cl | 3,4-(OMe)2 | Me | CONH2 | H | CH2CH2 | |
985 | 4-NHCOCH3 | 3,4-(OMe)2 | Me | CONH2 | H | CH2CH2 | |
986 | 4-Cl | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 | |
987 | 4-Br | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 | |
988 | 3,4-Cl2 | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 | |
989 | 4-CF3 | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 | |
99O | 4-Me | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 | |
991 | 4-NO2 | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 | |
992 | 4-CN | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 | |
993 | 4-OCOCH3 | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
994 | 4-SO2CF3 | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 | |
995 | 3-F,4-Cl | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 | |
996 | 4-NHCOCH3 | 3,4-(OMe)2 | COCH3 | CN | H | CH2CH2 | |
997 | 4-Cl | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 | |
998 | 4-Br | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 | |
999 | 3,4-Cl2 | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 | |
1.000 | 4-CF3 | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 | |
1.001 | 4-Me | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 | |
1.002 | 4-NO2 | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 | |
1.003 | 4-CN | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 | |
1 004 | 4-OCOCH3 | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 | |
1.005 | 4-SO2CF3 | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 | |
1.006 | 3-F,4-Cl | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 | |
1.007 | 4-NHCOCH3 | 3,4-(OMe)2 | -SiMe3 | CN | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.008 | 4-Cl | 3,4-(OMe)2 | COPh | H | H | CH2CH2 | 106 |
1.009 | 3,4-Cl2 | 3,4-(OMe)2 | COPh | H | H | CH2CH2 | |
1.010 | 4-Br | 3,4-(OMe)2 | COPh | H | H | CH2CH2 | |
1.011 | 4-l | 3,4-(OMe)2 | COPh | H | H | CH2CH2 | |
1.012 | 4-Me | 3,4-(OMe)2 | COPh | H | H | CH2CH2 | |
1.013 | 3,4-Me2 | 3,4-(OMe)2 | COPh | H | H | CH2CH2 | |
1.014 | 3,4-Br2 | 3,4-(OMe)2 | COPh | H | H | CH2CH2 | |
1.015 | 4-CF3 | 3,4-(OMe)2 | COPh | H | H | CH2CH2 | |
1.016 | 4-Cl | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 | |
1.017 | 4-Br | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 | |
1.018 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 | |
1.019 | 4-CF3 | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 | |
1.020 | 4-Me | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 | |
1.021 | 4-NO2 | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.022 | 4-CN | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 | |
1.023 | 4-OCOCH3 | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 | |
1.024 | 4-SO2CF3 | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 | |
1.025 | 3-F,4-Cl | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 | |
1.026 | 4-NCOCH3 | 3,4-(OMe)2 | H | H | COCH3 | CH2CH2 | |
1.027 | 4-Cl | 3,4-(OMe)2 | H | H | CO2Me | CH2CH2 | |
1.028 | 4-Br | 3,4-(OMe)2 | H | H | CO2Me | CH2CH2 | |
1.029 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | CO2Me | CH2CH2 | |
1.030 | 4-CF3 | 3,4-(OMe)2 | H | H | CO2Me | CH2CH2 | |
1.031 | 4-Me | 3,4-(OMe)2 | H | H | CO2Me | CH2CH2 | |
1.032 | 4-NO2 | 3,4-(OMe)2 | H | H | CO2Me | CH2CH2 | |
1.033 | 4-CN | 3,4-(OMe)2 | H | H | CO2Me | CH2CH2 | |
1.034 | 4-OCOCH3 | 3,4-(OMe)2 | H | H | CO2Me | CH2CH2 | |
1.035 | 4-SO2CF3 | 3,4-(OMe)2 | H | H | CO2Me | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.036 | 3-F,4-Cl | 3,4-(OMe)2 | H | H | CO2Me | CH2CH2 | |
1.037 | 4-NHCOCH3 | 3,4-(OMe)2 | H | H | COx2Me | CH2CH2 | |
1.038 | 4-Cl | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.039 | 4-Br | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.040 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.041 | 4-CF3 | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.042 | 4-Me | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.043 | 4-NO2 | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.044 | 4-CN | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.045 | 4-OCOCH3 | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.046 | 4-SO2CF3 | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.047 | 3-F,4-Cl | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.048 | 4-NHCOCH3 | 3,4-(OMe)2 | H | H | CONMe2 | CH2CH2 | |
1.049 | 4-Cl | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.050 | 4-Br | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 | |
1.051 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 | |
1.052 | 4-CF3 | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 | |
1.053 | 4-Me | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 | |
1.054 | 4-NO2 | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 | |
1.055 | 4-CN | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 | |
1.056 | 4-OCOCH3 | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 | |
1.057 | 4-SO2CF3 | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 | |
1.058 | 3-F,4-Cl | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 | |
1.059 | 4-NHCOCH3 | 3,4-(OMe)2 | H | H | NOMe | CH2CH2 | |
1.060 | 4-Cl | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 | |
1.061 | 4-Br | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 | |
1.062 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 | |
1.063 | 4-CF3 | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.064 | 4-Me | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 | |
1.065 | 4-NO2 | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 | |
1.066 | 4-CN | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 | |
1.067 | 4-OCOCH3 | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 | |
1.068 | 4-SO2CF3 | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 | |
1.069 | 3-F,4-Cl | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 | |
1.070 | 4-NHCOCH3 | 3,4-(OMe)2 | H | H | NMe2 | CH2CH2 | |
1.071 | 4-Cl | 3,4-(OMe)2 | H | H | Me | CH2CH2 | 油状 |
1.072 | 4-Br | 3,4-(OMe)2 | H | H | Me | CH2CH2 | |
1.073 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | Me | CH2CH2 | |
1.074 | 4-CF3 | 3,4-(OMe)2 | H | H | Me | CH2CH2 | |
1.075 | 4-Me | 3,4-(OMe)2 | H | H | Me | CH2CH2 | |
1.076 | 4-NO2 | 3,4-(OMe)2 | H | H | Me | CH2CH2 | |
1.077 | 4-CN | 3,4-(OMe)2 | H | H | Me | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.078 | 4-OCOCH3 | 3,4-(OMe)2 | H | H | Me | CH2CH2 | |
1.079 | 4-SO2CF3 | 3,4-(OMe)2 | H | H | Me | CH2CH2 | |
1 080 | 3-F,4-Cl | 3,4-(OMe)2 | H | H | Me | CH2CH2 | |
1.081 | 4-NHCOCH3 | 3,4-(OMe)2 | H | H | Me | CH2CH2 | |
1.082 | 4-Cl | 3,4-(OMe)2 | Me | H | Me | CH2CH2 | 油状 |
1.083 | 4-Br | 3,4-(OMe)2 | Me | H | Me | CH2CH2 | |
1.084 | 3,4-Cl2 | 3,4-(OMe)2 | Me | H | Me | CH2CH2 | |
1.085 | 4-CF3 | 3,4-(OMe)2 | Me | H | Me | CH2CH2 | |
1.086 | 4-Me | 3,4-(OMe)2 | Me | H | Me | CH2CH2 | |
1.087 | 4-NO2 | 3,4-(OMe)2 | Me | H | Me | CH2CH2 | |
1.088 | 4-CN | 3,4-(OMe)2 | Me | H | Me | CH2CH2 | |
1.089 | 4-OCOCH3 | 3,4-(OMe)2 | Me | H | Me | CH2CH2 | |
1.090 | 4-SO2CF3 | 3,4-(OMe)2 | Me | H | Me | CH2CH2 | |
1.091 | 3-F,4-Cl | 3,4-(OMe)2 | Me | H | Me | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.092 | 4-NHCOCH3 | 3,4-(OMe)2 | Me | H | Me | CH2CH2 | |
1.093 | 4-Cl | 3,4-(OMe)2 | COCH3 | H | COCH3 | CH2CH2 | 油状 |
1.094 | 4-Br | 3,4-(OMe)2 | COCH3 | H | COCH3 | CH2CH2 | |
1.095 | 3,4-Cl2 | 3,4-(OMe)2 | COCH3 | H | COCH3 | CH2CH2 | |
1.096 | 4-CF3 | 3,4-(OMe)2 | COCH3 | H | COCH3 | CH2CH2 | |
1.097 | 4-Me | 3,4-(OMe)2 | COCH3 | H | COCH3 | CH2CH2 | |
1.098 | 4-NO2 | 3,4-(OMe)2 | COCH3 | H | COCH3 | CH2CH2 | |
1.099 | 4-CN | 3,4-(OMe)2 | COCH3 | H | COCH3 | CH2CH2 | |
1.100 | 4-OCOCH3 | 3,4-(OMe)2 | COCH3 | H | COCHH3 | CH2CH2 | |
1.101 | 4-SO2CF3 | 3,4-(OMe)2 | COCH3 | H | COCH3 | CH2CH2 | |
1.102 | 3-F,4-Cl | 3,4-(OMe)2 | COCH3 | H | COCH3 | CH2CH2 | |
1.103 | 4-NHCOCH3 | 3,4-(OMe)2 | COCH3 | H | COCH3 | CH2CH2 | |
1.104 | 4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
1.105 | 4-Br | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.106 | 4-CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
1.107 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
1.108 | 3,4-Br2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
1.109 | 4-Me | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
1.110 | 2,4-Me2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
1.111 | 4-NO2 | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | |
1.112 | 4-Cl | H | H | H | H | CH2CH2CH2 | 89 |
1.113 | 4-Cl | H | H | H | H | CH2CH2 | 99 |
1.114 | 4-Cl | 4-OEt,3-NHMe | H | H | H | CH2CH2 | |
1.115 | 4-Cl | 3,4-Me2 | H | H | H | CH2CH2 | 87 |
1.116 | 4-Cl | 2-OMe | H | H | H | CH2CH2 | 油状 |
1.117 | 4-Cl | 4-Ph | H | H | H | CH2CH2 | |
1.118 | 4-Cl | 3-OMe | H | H | H | CH2CH2 | 93 |
1.119 | 4-Cl | 4-Et,3-Me | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.130 | 4-Cl | 2,4-Cl2 | H | H | H | CH2CH2 | 83 |
1.131 | 4-Cl | 3-OMe,4-OBu | H | H | H | CH2CH2 | 81 |
1.132 | 4-Cl | 4-Me | H | H | H | CH2CH2 | 114 |
1.133 | 4-Cl | 3-OMe,4-OBu | H | H | H | CH2CH2CH2 | |
1.134 | 4-Cl | 4-tBu | H | H | H | CH2CH2 | 86 |
1.135 | 4-Cl | 3-OMe,4-OBu | COCH3 | H | H | CH2CH2 | |
1.136 | 4-Cl | 4-tBu | H | H | H | CH2CH2 | 86 |
1.137 | 4-Cl | 3-OMe,4-OC-H2Ph | H | H | H | CH2CH2 | 99 |
1.138 | 4-Cl | 4-tBu | H | H | H | -CH2CH(CH3)CH2- | 油状 |
1.139 | 3,4-Cl2 | 3,4-(OMe)2 | COCH=CH2 | H | H | CH2Cl2 | 油状 |
1.140 | 4-Cl | 3-OMe | H | H | H | -CH2C(Et)2- | 油状 |
1.141 | 4-Cl | 2-OEt | H | H | H | CH2CH2 | 油状 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.151 | 4-Br | 4-OMe,3-OEt | H | H | H | CH2CH2 | |
1.152 | 3,4-Br2 | 4-OMe,3-OEt | H | H | H | CH2CH2 | |
1.153 | 4-Me | 4-OMe,3-OEt | H | H | H | CH2CH2 | |
1.154 | 3,4-Me2 | 4-OMe,3-OEt | H | H | H | CH2CH2 | |
1.155 | 4-CF3 | 4-OMe,3-OEt | H | H | H | CH2CH2 | |
1.156 | 4-NO2 | 4-OMe,3-OEt | H | H | H | CH2CH2 | |
1.157 | 4-I | 4-OMe,3-OEt | H | H | H | CH2CH2 | |
1.158 | 4-Cl | 4-OEt | H | H | H | CH2CH2 | 110 |
1.159 | 4-Cl | 4-Et | H | H | H | CH2CH2 | 104 |
1.160 | 4-Cl | 3,5-(OMe)2 | H | H | H | CH2CH2 | 油状 |
1.161 | 4-Cl | 2,3-(OMe)2 | H | H | H | CH2CH2 | 122 |
1.162 | 4-Br | H | H | H | H | CH2CH2CH2 | 103 |
1.163 | 4-Cl | H | H | Bu | H | CH2CH2CH2 | 油状 |
1.164 | 4-Cl | H | H | Me | H | CH2CH2CH2 | 76 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.250 | 3,4-Me2 | 3,4-(OMe)2 | H | H | H | CH2CH(O) | |
1.251 | 3,4-Me2 | 3,4-(OMe)2 | H | H | H | CH2CHCN) | |
1.252 | 3,4-Me2 | 3,4-(OMe)2 | H | H | H | CH(CH3)CH(CH3) | |
1.253 | 4-Cl | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.254 | 4-Br | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.255 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.256 | 4-CF3 | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.257 | 4-Me | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.258 | 4-NO2 | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.259 | 4-CN | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.260 | 4-OCOCH3 | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.261 | 4-SO2CF3 | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.262 | 3-F,4-Cl | 3,4-(OMe)2 | H | H | H | COCH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.263 | 4-NHCOCH3 | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.264 | 4-Cl | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1.265 | 4-Br | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1.266 | 3,4-Cl2 | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1.267 | 4-CF3 | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1.268 | 4-Me | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1.269 | 4-NO2 | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1.270 | 4-CN | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1.271 | 4-OCOCH3 | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1.272 | 4-SO2CF3 | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1.273 | 3-F,4-Cl | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1.274 | 4-NCOCH3 | 3,4-(OMe)2 | COCH3 | H | H | COCH2 | |
1 275 | 3,4-Me2 | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.276 | 4-Cl,3-Me | 3,4-(OMe)2 | H | H | H | COCH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.277 | 3,4-Br2 | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.278 | 3,4,5-Cl3 | 3,4-(OMe)2 | H | H | H | COCH2 | |
1.279 | 4-Cl | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.280 | 4-Br | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.281 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.282 | 4-CF3 | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.283 | 4-Me | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.284 | 4-NO2 | 3-OMe, 4-OEt | H | H | H | COCH2 | |
1.285 | 4-CN | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.286 | 4-OCOCH3 | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.287 | 4-SO2CF3 | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.288 | 3-F,4-Cl | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.289 | 4-NHCOCH3 | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.290 | 4-Cl | 3-OMe,4-OEt | COCH3 | H | H | COCH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.P.[℃] |
1.291 | 4-Br | 3-OMe,4-OEt | COCH3 | H | H | COCH2 | |
1.292 | 3,4-Cl2 | 3-OMe,4-OEt | COCH3 | H | H | COCH2 | |
1.293 | 4-CF3 | 3-OMe,4-OEt | COCH3 | H | H | COCH2 | |
1.294 | 4-Me | 3-OMe,4-OEt | COCH3 | H | H | COCH2 | |
1.295 | 4-NO2 | 3-OMo,4-OEt | COCH3 | H | H | COCH2 | |
1.296 | 4-CN | 3-OMe,4-OEt | COCH3 | H | H | COCH2 | |
1.297 | 4-OCOCH3 | 3-OMe,4-OEt | COCH3 | H | H | COCH2 | |
1.298 | 4-SO2CF3 | 3-OMe,4-OEt | COCH3 | H | H | COCH2 | |
1.299 | 3-F,4-Cl | 3-OMe,4-OEt | COCH3 | H | H | COCH2 | |
1.300 | 4-NHCOCH3 | 3-OMe,4-OEt | COCH3 | H | H | COCH2 | |
1.301 | 3,4-Me2 | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.302 | 3-Me,4-Cl | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.303 | 3,4-Br2 | 3-OMe,4-OEt | H | H | H | COCH2 | |
1.304 | 3,4,5-Cl3 | 3-OMe,4-OEt | H | H | H | COCH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.305 | 4-Cl | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.306 | 4-Br | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.307 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.308 | 4-CF3 | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.309 | 4-Me | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.310 | 4-NO2 | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.311 | 4-CN | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.312 | 4-OCOCH3 | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.313 | 4-CO2CF3 | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.314 | 3-F,4-Cl | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.315 | 4-NHCOCH3 | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.316 | 4-Cl | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 | |
1.317 | 4-Br | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 | |
1.318 | 3,4-Cl2 | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.319 | 4-CF3 | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 | |
1.320 | 4-Me | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 | |
1.321 | 4-NO2 | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 | |
1.322 | 4-CN | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 | |
1.323 | 4-OCOCH3 | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 | |
1.324 | 4-SO2CF3 | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 | |
1.325 | 3-F.4-Cl | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 | |
1.326 | 4-NHCOCH3 | 3,4-(OMe)2 | COCH3 | H | H | COCH2CH2 | |
1.327 | 3,4-Me2 | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.328 | 3-Me,4-Cl | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.329 | 3,4-Br2 | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.330 | 3,4,5-Cl3 | 3,4-(OMe)2 | H | H | H | COCH2CH2 | |
1.331 | 4-Cl | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.332 | 4-Br | 3-OMe,4-OEt | H | H | H | COCH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.333 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.334 | 4-CF3 | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.335 | 4-Me | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.336 | 4-NO2 | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.337 | 4-CN | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.338 | 4-OCOCH3 | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.339 | 4-SO2CF3 | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.340 | 3-F,4-Cl | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.341 | 4-NHCOCH3 | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.342 | 4-Cl | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 | |
1.343 | 4-Br | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 | |
1.344 | 3,4-Cl2 | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 | |
1.345 | 4-CF3 | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 | |
1.346 | 4-Me | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.P.[℃] |
1.347 | 4-NO2 | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 | |
1.348 | 4-CN | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 | |
1.349 | 4-OCOCH3 | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 | |
1.350 | 4-SO2CF3 | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 | |
1.351 | 3-F,4-Cl | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 | |
1.352 | 4-NHCOCH3 | 3-OMe,4-OEt | COCH3 | H | H | COCH2CH2 | |
1.353 | 3,4-Me2 | 3-OMe,4-OEt | H | H | F | COCH2CH2 | |
1.354 | 3-Me,4-Cl | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.355 | 3,4-Br2 | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.356 | 3,4,5-Cl3 | 3-OMe,4-OEt | H | H | H | COCH2CH2 | |
1.357 | 4-Cl | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1-358 | 4-Br | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.359 | 3,4-Cl2 | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.360 | 4-CF3 | 3,4,5-(OMe)3 | H | H | H | COCH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.P.[℃] |
1.361 | 4-Me | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.362 | 4-NO2 | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.363 | 4-CN | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.364 | 4-OCOCH3 | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.365 | 4-CO2CF3 | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.366 | 3-F,4-Cl | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.367 | 4-NHCOCH3 | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.376 | 4-Cl | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 | |
1.377 | 4-Br | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 | |
1.378 | 3,4-Cl2 | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 | |
1.379 | 4-CF3 | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 | |
1.380 | 4-Me | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 | |
1.381 | 4-NO2 | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 | |
1.382 | 4-CN | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
1.383 | 4-OCOCH3 | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 | |
1.384 | 4-SO2CF3 | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 | |
1.385 | 3-F,4-Cl | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 | |
1.386 | 4-NH-COCH3 | 3,4,5-(OMe)3 | COCH3 | H | H | COCH2 | |
1.387 | 3,4-Me2 | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.388 | 3-Me,4-Cl | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.389 | 3,4-Br2 | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
1.390 | 3,4,5-Cl3 | 3,4,5-(OMe)3 | H | H | H | COCH2 | |
2.091 | 4-Br | 3,4-Me2 | H | H | H | CH2CH2 | 84 |
2.092 | 3,4-Cl2 | 3,4-Me2 | H | H | H | CH2CH2 | 76 |
2.093 | 4-Me | H | H | H | H | CH2CH2 | |
2.094 | 4-Ph | H | H | H | H | CH2CH2CH2 | 140 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.095 | 3,4-Cl2 | 3,4-Me2 | COCH3 | H | H | CH2CH2 | |
2.096 | 4-Br | 3-OMe,4-OBu | H | H | H | CH2CH2 | 84 |
2.097 | 3,4-Cl2 | 3-OMe,4-OBu | H | H | H | CH2CH2 | 102 |
2.098 | 3,4-Cl2 | 3-OMe,4-OBu | COCH3 | H | H | CH2CH2 | |
2.099 | 4-Br | 3-OMe,4-OCH2Ph | H | H | H | CH2CH2 | 100 |
2.100 | 3,4-Cl2 | 3-OMe,4-OCH2Ph | H | H | H | CH2CH2 | 110 |
2.101 | 3,4-Cl2 | 3-OMe,4-OCH2Ph | COCH3 | H | H | CH2CH2 | |
2.102 | 4-Cl | 3-CF3 | H | H | H | CH2CH2 | 85 |
2.103 | 3,4-Me2 | 3-OMe,4-OEt | H | H | H | CH2CH2 | 113 |
2.104 | 3,4-Me2 | 3-OMe,4-OEt | COCH3 | H | H | CH2CH2 | |
2.105 | 3,4-Me2 | 3-OMe,4-OEt | H | H | H | CH(CH3)CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.106 | 3,4-Me2 | 3-OMe,4-OEt | COCH3 | H | H | CH(CH3)CH2 | |
2.107 | 2,4-Cl2 | H | H | H | H | CH2CH2CH2 | 125 |
2.108 | H | 3,4-(OMe)2 | H | H | H | CH2CH2 | 97(S) |
2.109 | H | 3,4-(OMe)2 | H | H | H | CH2CH2 | 97(R) |
2.110 | H | H | H | H | H | CH2CH2CH2 | 蜡状(S) |
2.111 | H | H | H | H | H | CH2CH2CH2 | 蜡状(R) |
2.112 | 4-F | H | H | H | H | CH2CH2CH2 | 87 |
2.113 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH(SO2CH3) | 玻璃状 |
2.114 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH(SOCH3) | 玻璃状 |
2.115 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2C(SMe2)2 | 油状 |
2.116 | 3,4-Br2 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | |
2.117 | 3-CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 蜡状 |
2.118 | 3-CH3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
2.119 | 3-NO2,4-CH3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 蜡状 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.120 | 3-NO2,4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
2.121 | 3-CH3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | 116 |
2.122 | 3-Br | 3-OMe,4-OEt | H | H | H | CH2CH2 | 98 |
2.123 | 3,4-Cl2 | 3,4-(OCF3)2 | H | H | H | CH2CH2 | |
2.124 | 3,4-Cl2 | 3,4-(NHCH3)2 | H | H | H | CH2CH2 | |
2.125 | 4-Cl | 3-OMe,4-OCF3 | H | H | H | CH2CH2 | |
2.126 | 4-Br | 3-OMe,4-OCF3 | H | H | H | CH2CH2 | |
2.127 | 4-CH3 | 3-OMe,4-OCF3 | H | H | H | CH2CH2 | |
2.128 | 4-CF3 | 3-OMe,4-OCF3 | H | H | H | CH2CH2 | |
2.129 | 3,4-Cl2 | 3-OMe,4-OCF3 | H | H | H | CH2CH2 | |
2.130 | 4,Cl | 3-OMe,4-OPr | H | H | H | CH2CH2 | 油状 |
2.131 | 4-Br | 3-OMe,4-OPr | H | H | H | CH2CH2 | 油状 |
2.132 | 4-CH3 | 3-(OMe),4-OPr | H | H | H | CH2CH2 | |
2.133 | 4-CF3 | 3-(OMe),4-OPr | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.P.[℃] |
2.134 | 3,4-Cl2 | 3-(OMe),4-OPr | H | H | H | CH2CH2 | 80 |
2.135 | 4-Br | 3,4-CH3)2 | H | H | H | CH2CH2 | 84 |
2.136 | 3,4-Cl2 | 3,4-(CH3)2 | H | H | H | CH2CH2 | 76 |
2.137 | 4-CH3 | 3,4-(CH3)2 | H | H | H | CH2CH2 | |
2.138 | 4-CF3 | 3,4-(CH2)2 | H | H | H | CH2CH2 | |
2.139 | 3,4-Cl2 | 3,OMe,4-OBu | H | H | H | CH2CH2 | 102 |
2.140 | 4-Br | 3,OMe,4-OBu | H | H | H | CH2CH2 | 84 |
2.141 | 4-CH3 | 3,OMe,4-OBu | H | H | H | CH2CH2 | |
2.142 | 4-Br | 3-OMe,4-OCH2Ph | H | H | H | CH2CH2 | 100 |
2.143 | 4-CH3 | 3-OMe,4-OCH2PH | H | H | H | CH2CH2 | |
2.144 | 4-OCF3 | 3-OMe,4-OCH2Ph | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.145 | 3,4-Cl2 | 3-OMe,4-OCH2Ph | H | H | H | CH2CH2 | 油状 |
2.146 | 4-Cl | 3-OMe,4-CH3 | H | H | H | CH2CH2 | 84 |
2.147 | 4-Br | 3-OMe,4-CH3 | H | H | H | CH2CH2 | 85 |
2.148 | 4-CF3 | 3-OMe,4-CH3 | H | H | H | CH2CH2 | |
2.149 | 4-CH3 | 3-OMe,4-CH3 | H | H | H | CH2CH2 | |
2.150 | 3,4-Cl2 | 3-OMe,4-CH3 | H | H | H | CH2CH2 | 油状 |
2.151 | 3-CF3 | 3-OMe,4-OEt | H | H | H | CH2CH2 | 88 |
2.152 | 4-Cl | 2-Cl,3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.153 | 4-Br | 2-Cl,3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.154 | 4-CF3 | 2-Cl,3-OMe,4-OEt | H | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.155 | 4-CH3 | 2-Cl,3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.156 | 3,4-Cl2 | 2-Cl,3-OMe,4-OEt | H | H | H | CH2CH2 | 蜡状 |
2.157 | 3,4,5-Cl3 | 2-Cl,3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.158 | 3,4-Br2 | 2-Cl,3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.159 | 3,4-(CH3)2 | 2-Cl,3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.160 | 3-Cl,4-CH3 | 2-Cl,3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.161 | 3,4-Cl2 | 2-Cl,3-OMe,4-OEt | COCH3 | H | H | CH2CH2 | |
2.162 | 3,4-Cl2 | 2-Cl,3-OMe,4-OEt | COCH2CH3 | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.163 | 3,4-Cl2 | 2-Cl,3-OMe,4-OEt | COCH2Cl | H | H | CH2CH2 | |
2.164 | 3,4-Cl2 | 2-Cl,3-OMe,4-OEt | H | H | H | CH(CH2)CH2 | |
2.165 | 3,4-Cl2 | 2-Cl,3-OMe,4-OEt | H | H | H | CH2CCH(CH2) | |
2.166 | 3,4-Cl2 | 2-Cl,3-OMe,4-OEt | H | H | H | CH(CH2)CH(CH3) | |
2.167 | 3,4-Cl2 | 2-Cl,3-OMe,4-OEt | COCH3 | H | H | CH(CH3)CH2 | |
2.168 | 4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH(OCH3) | |
2.169 | 4-Br | 3,4-(OMe)2 | H | H | H | CH2CH(OClH3) | |
2.170 | 4-CF3 | 3,4-(OMe)2 | H | H | H | CH2CH(OCH3) | |
2.171 | 4-CH3 | 3,4-(OMe)2 | H | H | H | CH2CH(OCH3) | |
2.172 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH(OCH3) |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.173 | 4-Cl | 3-OMe,4-OEt | H | H | H | CH2CH(OCH3) | 油状 |
2.174 | 4-Br | 3-OMe,4-OEt | H | H | H | CH2CH(OCH3) | 油状 |
2.175 | 4-CF3 | 3-OMe,4-OEt | H | H | H | CH2CH(OCH3) | |
2.176 | 4-CH3 | 3-OMe,4-OEt | H | H | H | CH2CH(OCH3) | |
2.177 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH(OCH3) | 油状 |
2.178 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH(CH3)CH2 | |
2.179 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | C(CH3)2CH2 | |
2.180 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH(CH3)CH(CH3) | 44-8 |
2.181 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH(CH3) | |
2.182 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH(CH3)CH2 | 油状 |
2.183 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH(CH3) | 油状 |
2.184 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH(CH3)CH(CH3) | |
2.185 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | C(CH3)2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.186 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH(CH2-cyclohexyl) | 玻璃状 |
2.187 | 4-Cl | 3,4-(OMe)2 | H | H | H | CH(CH2CH3)CH2 | 116-8 |
2.188 | 4-Br | 3,4-(OMe)2 | H | H | H | CH(CH2CH3)CH2 | |
2.189 | 4-CH3 | 3,4-(OMe)2 | H | H | H | CH(CH2CH3)CH2 | |
2.190 | 4-CF3 | 3,4-(OMe)2 | H | H | H | CH(CH2CH3)CH2 | |
2.191 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH(CH2CH3)CH2 | |
2.192 | 4-Cl | 3-OMe,4-OEt | H | H | H | CH(CH2CH3)CH2 | |
2.193 | 4-Br | 3-OMe,4-OEt | H | H | H | CH(CH2CH3)CH2 | |
2.194 | 4-CH3 | 3-OMe,4-OEt | H | H | H | CH(CH2CH3)CH2 | |
2.195 | 4-CF3 | 3-OMe,4-OEt | H | H | H | CH(CH2CH3)CH2 | |
2.196 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH(CH2CH3)CH2 | |
2.197 | 4-Cl | 3,4-(OMe)2 | H | H | H | C(CH3)2CH(OH) | 玻璃状 |
2.198 | 4-Br | 3,4-(OMe)2 | H | H | H | C(CH3)2CH(OH) |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.199 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | C(CH3)2CH(OH) | |
2.200 | 3,4-Cl2 | 3-OMe,4-OEt | COCH3 | H | H | C(CH3)2CH(OH) | |
2.201 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | C(CH3)2CH(OH) | |
2.202 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH(SCH3) | |
2.203 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH(SCH3) | 138 |
2.204 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CO | 玻璃状 |
2.205 | 3,4-Cl2 | 3-OMe,4-OEt | H | H | H | CH2CH(OH) | 149-52 |
2.206 | 4-Cl | 3-OMe,4-OEt | H | H | H | CH(CH3)CH2 | 129-31 |
2.207 | 4-Cl | H | H | H | H | CH2CH2CH2CH2 | 78-9 |
2.208 | 2,4-Cl2 | H | H | H | H | CH2CH2CH2 | |
2.209 | 3,4-Cl2 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | |
2.210 | 3,4-Cl2 | 3,4-(OMe)2 | COCH2CH3 | H | H | CH2CH2 | |
2.211 | 3,4-Cl2 | 3,4-(OMe)2 | COCH2Cl | H | H | CH2CH2 | |
2.212 | 3,4-Cl2 | 3,4-(OMe)2 | COCF3 | H | H | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.213 | 3,4-Cl2 | 3,4-(OMe)2 | COCH2CH2CF3 | H | H | CH2CH2 | |
2.214 | 3,4-Cl2 | 3-OMe,4-OEt | COCH3 | H | H | CH2CH2 | 油状 |
2.215 | 3,4-Cl2 | 3-OMe,4-OEt | COCH2CH3 | H | H | CH2CH2 | 油状 |
2.216 | 3,4-Cl2 | 3-OMe,4-OEt | COCH2Cl | H | H | CH2CH2 | 油状 |
2.217 | 3,4-Cl2 | 3-OMe,4-OEt | COCF3 | H | H | CH2CH2 | |
2.218 | 3,4-Cl2 | 3-OMe,4-OEt | COCH2CH2CH3 | H | H | CH2CH2 | |
2.219 | 3,4-Cl2 | 3-OMe,4-OEt | COCH(CH3)2 | H | H | CH2CH2 | |
2.220 | 3,4-Cl2 | 3-OMe,4-OEt | COBu1 | H | H | CH2CH2 | |
2.221 | 4-Cl | 3,4-(OMe)2 | COOEt | H | H | CH2CH2 | 油状 |
2.222 | 4-Cl | 3-OMe,4-OEt | CO(4-NO2-Ph) | H | H | CH2CH2 | 133-5 |
2.223 | 3,4-Cl2 | 3,4-(OMe)2 | CO(4-NO2-Ph) | H | H | CH2CH2 | 151-3 |
2.224 | 4-Cl | 3-OMe,4-OEt | CONHPh | H | H | CH2CH2 | 54-8 |
2.225 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2C(NOH) | 184-5 |
2.226 | 3,4-Cl2 | 3-OMe,4OEt | COCH3 | H | COCH3 | CH2CH2 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.239 | 3-O-(3-CF3-Ph) | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
2.240 | 3-OCH2Ph | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
2.241 | 3-OCH2Ph | 3-OMe,4-OEt | H | H | H | CH2CH2 | 油状 |
2.242 | 3-OCH2-(4-CH3-Ph) | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.243 | 3-O-(3,5-Cl2-Ph) | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
2.244 | 3-O-(3,5-Cl2-Ph) | 3-OMe,4-OEt | H | H | H | CH2CH2 | 油状 |
2.245 | 3-O-(3,4-Cl2-Ph) | 3-OMe,4-OEt | H | H | H | CH2CH2 | 99 |
2.246 | 2-OCH2Ph | 3,4-(OMe)2 | H | H | H | CH2CH2 | 85 |
2.247 | 2-OCH2Ph | 3-OMe,4-OEt | H | H | H | CH2CH2 | 111 |
2.248 | 2-OCH2Ph,3-OMe | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
2.249 | 2-OCH2Ph,3-OMe | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.25O | 3-OMe,4-OCH2Ph | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
2.251 | 3-OMe,4-OCH2Ph | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.252 | 4-O-(4-Cl-Ph) | 3-OMe,4-OEt | H | H | H | CH2CH2 | 46-8 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.253 | 4-O-(4-F-Ph) | 3-OMe,4-OEt | H | H | H | CH2CH2 | 油状 |
2.254 | 4-O-(4-F-Ph) | 3,4-(OMe)2 | H | H | H | CH2CH2 | 蜡状 |
2.255 | 4-O-(4-Cl-Ph) | 3,4-(OMe)2 | H | H | H | CH2CH2 | 121 |
2.256 | 4-O-(4-CH3-Ph) | 3,4-(OMe)2 | H | H | H | CH2CH2 | |
2.257 | 4-O-(4-CH3-Ph) | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.258 | 4-OCH2-(4-CH3-Ph) | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.259 | 4-OCH2-(4-Cl-Ph) | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.260 | 4-OCH2-(3,4-Cl2-Ph) | 3-OMe,4-OEt | H | H | H | CH2CH2 | |
2.261 | 4-Cl | 2-Br,4-OEt,5-OMe | COCH3 | H | H | CH2CH2 | 140-2 |
2.262 | 4-Cl | 2-Br,4-OEt,5-OMe | H | H | H | CH2CH2 | 96-8 |
2.263 | 4-Cl | 3,4-(OMe)2 | H | H | H | CH2CH2CH2CH2 | 101-5 |
2.264 | 4-Cl | 4-NO2 | H | H | H | CH2CH2 | 102-5 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.265 | 4-Cl | 3-OMe,4-OEt | CONHCH3 | H | H | CH2CH2 | 76-8 |
2.266 | 3,4-Cl2 | 3,4-(OMe)2 | COSEt | H | H | CH2CH2 | 油状 |
2.267 | 3,4-Cl2 | 3,4-(OMe)2 | SO2CH3 | H | H | CH2CH2 | 107-9 |
2.268 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 110-11 |
2.269 | 3,4-Cl2 | 3,4-(OMe)2 | CO-cyclopropyl | H | H | CH2CH2 | 胶状 |
2.270 | 3,4-Cl2 | 3,4-(OMe)2 | CO-CO-COOEt | H | H | CH2CH2 | 95-7 |
2.271 | 3,4-Cl2 | 3-OMe,4-OEt | CO(3,4-Cl2-Ph) | H | H | CH2CH2 | 151-2 |
2.272 | 4-Cl | 3-OMe,4-OEt | COCH2OMe | H | H | CH2CH2 | 胶状 |
2.273 | 4-Cl | 3-OMe,4-OEt | COCH2OCOMe | H | H | CH2CH2 | 80-2 |
2.274 | 3,4-Cl2 | 3,4-(OMe)2 | CONHCH3 | H | H | CH2CH2 | 油状 |
2.275 | 3,4-Cl2 | 3,4-(OMe)2 | CO-(2-thieny) | H | H | CH2CH2 | 119-21 |
2.276 | 3,4-Cl23,4-(OMe)2 | 3,4-Cl2 | CO-(2-furyl) | H | H | CH2CH2 | 127-9 |
2.277 | 3,4-Cl2 | 3,4-(OMe)2 | COMe | H | H | CH2C(=NCOMe) | 玻璃状 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.278 | 3,4-Cl2 | 3-OMe,4-OEt | CONH-环己基 | H | H | CH2CH2 | 127-9 |
2.279 | 2-F,4-CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 108-9 |
2.280 | 4-Br,3-NO2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 玻璃状 |
2.281 | 2-F,4-CF3 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | 85-7 |
2.282 | 4-CN | 3,4-(OMe)2 | H | H | H | CH2CH2 | 胶状 |
2.283 | 4 Br,3-NO2 | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | 玻璃状 |
2.284 | 3,4-(OCHF2)2 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
2.285 | 4-[4-tBu-噻唑-2-基] | 3,4-(OMe)2 | H | H | H | CH2CH2 | 胶状 |
2.286 | 4-[4-tBu-噻唑-2-基] | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | 胶状 |
2.287 | 4-SOMe | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
2.288 | 4-Cl | 2-Br,4,5-(OMe)2 | H | H | H | CH2CH2 | 94-5 |
2.289 | 4-Cl | 2-Br,4,5-(OMe)2 | COCH3 | H | H | CH2CH2 | 132-3 |
2.290 | 4-Br | 2-Br,4,5-(OMe)2 | H | H | H | CH2CH2 | 106-7 |
编号 | R1 | R2 | R5 | R6 | R7 | X | m.p.[℃] |
2.291 | 4-Br | 2-Br,4,5-(OMe)2 | COCH3 | H | H | CH2CH2 | 123-4 |
2.292 | 3,4-Cl2 | 2-Br,4,5-(OMe)2 | H | H | H | CH2CH2 | 102-4 |
2.293 | 3,4-Cl2 | 2-Br,4,5-(OMe)2 | COCH3 | H | H | CH2CH2 | 127-8 |
2.294 | H | 2-Br,4,5-(OMe)2 | H | H | H | CH2CH2 | 104-10 |
2.295 | H | 2-Br,4,5-(OMe)2 | COCH3 | H | H | CH2CH2 | 116-7 |
2.296 | 4-Cl,3-Me | 3,4-(OMe)2 | H | H | H | CH2CH2 | 98-9 |
2.297 | 3,4-Cl2 | 3,4-(OMe)2 | H | H | H | CH2CH(CN) | 玻璃状 |
2.298 | 4-环己基-甲基 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 胶状 |
2.299 | 4-F,3-CF3 | 3,4-(OMe)2 | H | H | H | CH2CH2 | 油状 |
2.300 | 4-CN | 3,4-(OMe)2 | COCH3 | H | H | CH2CH2 | 泡沫 |
2.301 | 4-[4-tBu-5-Cl-噻唑-2-基] | 3,4-(OMe)2 | H | H | H | CH2CH2 | 泡沫 |
2.302 | 3-Cl,4-NHCOMe | 3,4-(OMe)2 | H | H | H | CH2CH2 | 泡沫 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.391 | H | 3,4-(OMe)2 | H | CH2CH2 | 80 |
1.392 | 2-F | 3,4-(OMe)2 | H | CH2CH2 | |
1.393 | 3-F | 3,4-(OMe)2 | H | CH2CH2 | |
1.394 | 4-F | 3,4-(OMe)2 | H | CH2CH2 | |
1.395 | 2,3-F2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.396 | 2,4-F2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.397 | 2,5-F2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.398 | 2,6-F2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.399 | 3,4-F2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.400 | 3,5-F2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.401 | 2,3,4-F3 | 3,4-(OMe)2 | H | CH2CH2 | |
1.402 | -F5 | 3,4-(OMe)2 | H | CH2CH2 | |
1.403 | 2-Cl | 3,4-(OMe)2 | H | CH2CH2 | |
1.404 | 3-Cl | 3,4-(OMe)2 | H | CH2CH2 | |
1.405 | 4-Cl | 3,4-(OMe)2 | H | CH2CH2 | 80 |
1.406 | 2,3-Cl2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.407 | 2,4-Cl2 | 3,4-(OMe)2 | H | CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.408 | 2,5-Cl2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.409 | 2,6-Cl2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.410 | 3,4-Cl2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.411 | 3,5-Cl2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.412 | 2,3,4-Cl5 | 3,4-(OMe)2 | H | CH2CH2 | |
1.413 | 2,3,5-Cl3 | 3,4-(OMe)2 | H | CH2CH2 | |
1.414 | 3,4,5-Cl3 | 3,4-(OMe)2 | H | CH2CH2 | |
1.415 | 4-Br | 3,4-(OMe)2 | H | CH2CH2 | |
1.416 | 3,4-Br2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.417 | 3,4,5-Br3 | 3,4-(OMe)2 | H | CH2CH2 | |
1.418 | 4-l | 3,4-(OMe)2 | H | CH2CH2 | |
1.419 | 3,4-l2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.420 | 3,4,5-l3 | 3,4-(OMe)2 | H | CH2CH2 | |
1.421 | 3-Br,4-Cl | 3,4-(OMe)2 | H | CH2CH2 | |
1.422 | 3-Cl,4-Br | 3,4-(OMe)2 | H | CH2CH2 | |
1.423 | 3-l,4-Cl | 3,4-(OMe)2 | H | CH2CH2 | |
1.424 | 3-Cl,4-l | 3,4-(OMe)2 | H | CH2CH2 | |
1.425 | 3-F,4-Cl | 3,4-(OMe)2 | H | CH2CH2 | |
1.426 | 3-F,4-Br | 3,4-(OMe)2 | H | CH2CH2 | |
1.427 | 2,3,5,6-F4,4-Br | 3,4-(OMe)2 | H | CH2CH2 | |
1.428 | 2,3,5,6-F4,4-Cl | 3,4-(OMe)2 | H | CH2CH2 | |
1.429 | 4-CF3 | 3,4-(OMe)2 | H | CH2CH2 | 72 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.430 | 3,4-(CF3)2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.431 | 3-OH,4-Cl | 3,4-(OMe)2 | H | CH2CH2 | |
1.432 | 3-Cl,4-OH | 3,4-(OMe)2 | H | CH2CH2 | |
1.433 | 3-CF3,4-Cl | 3,4-(OMe)2 | H | CH2CH2 | |
1.434 | 3-CF3,4-Br | 3,4-(OMe)2 | H | CH2CH2 | |
1.435 | 4-NO2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.436 | 4-CN | 3,4-(OMe)2 | H | CH2CH2 | |
1.437 | 4-SO2CH3 | 3,4-(OMe)2 | H | CH2CH2 | |
1.438 | 4-SO2CF3 | 3,4-(OMe)2 | H | CH2CH2 | |
1.439 | 4-SO2NH2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.440 | 4-SO2NHMe | 3,4-(OMe)2 | H | CH2CH2 | |
1.441 | 4-SO2NMe2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.442 | 4-SO3Me | 3,4-(OMe)2 | H | CH2CH2 | |
1.443 | 4-SO3CF3 | 3,4-(OMe)2 | H | CH2CH2 | |
1.444 | 4-SO3H | 3,4-(OMe)2 | H | CH2CH2 | |
1.445 | 4-CO2H | 3,4-(OMe)2 | H | CH2CH2 | |
1.446 | 4-CO2Me | 3,4-(OMe)2 | H | CH2CH2 | |
1.447 | 4-OCOMe | 3,4-(OMe)2 | H | CH2CH2 | |
1.448 | 4-NHCOMe | 3,4-(OMe)2 | H | CH2CH2 | |
1.449 | 4-COMe | 3,4-(OMe)2 | H | CH2CH2 | |
1.450 | 4-CONMe2 | 3,4-(OMe)2 | H | CH2CH2 | |
1.451 | 4-Me | 3,4-(OMe)2 | H | CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.511 | 4-F | 3-OMe,4-OEt | H | CH2CH2 | |
1.512 | 2,3-F2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.513 | 2,4-F2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.514 | 2,5-F2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.515 | 2,6-F2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.516 | 3,4-F2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.517 | 3,5-F2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.518 | 2,3,4-F3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.519 | -F5 | 3-OMe,4-OEt | H | CH2CH2 | |
1.520 | 2-Cl | 3-OMe,4-OEt | H | CH2CH2 | |
1.521 | 3-Cl | 3-OMe,4-OEt | H | CH2CH2 | |
1.522 | 4-Cl | 3-OMe,4-OEt | H | CH2CH2 | |
1.523 | 3,4-Cl2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.524 | 2,4-Cl2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.525 | 2,5-Cl2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.526 | 2,6-Cl2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.527 | 3,4-Cl2 | 3-OMe,4-OEt | H | CH2CH2 | 92-4 |
1.528 | 3,5-Cl2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.529 | 2,3,4-Cl3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.530 | 2,3,5-Cl3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.531 | 3,4,5-Cl3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.532 | 4-Br | 3-OMe,4-OEt | H | CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.533 | 3,4-Br | 3-OMe,4-OEt | H | CH2CH2 | |
1.534 | 3,4,5-Br3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.535 | 4-1 | 3-OMe,4-OEt | H | CH2CH2 | |
1.536 | 3,4-l2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.537 | 3,4,5-l3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.538 | 3-Br,4-Cl | 3-OMe,4-OEt | H | CH2CH2 | |
1.539 | 3-Cl,4-Br | 3-OMe,4-OEt | H | CH2CH2 | |
1.540 | 3-l,4-Cl | 3-OMe,4-OEt | H | CH2CH2 | |
1.541 | 3-Cl,4-l | 3-OMe,4-OEt | H | CH2CH2 | |
1.542 | 3-F,4-Cl | 3-OMe,4-OEt | H | CH2CH2 | |
1.543 | 3-F,4-Br | 3-OMe,4-OEt | H | CH2CH2 | |
1.544 | 2,3,5,6-F4,4-Br | 3-OMe,4-OEt | H | CH2CH2 | |
1.545 | 2,3,5,6-F4,4-Cl | 3-OMe,4-OEt | H | CH2CH2 | |
1.546 | 4-CF3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.547 | 3,4-(CF3)2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.548 | 3-OH,4-Cl | 3-OMe,4-OEt | H | CH2CH2 | |
1.549 | 3-Cl,4-OH | 3-OMe,4-OEt | H | CH2CH2 | |
1.550 | 3-CF3,4-Cl | 3-OMe,4-OEt | H | CH2CH2 | |
1.551 | 3-CF,4-Br | 3-OMe,4-OEt | H | CH2CH2 | |
1.552 | 4-NO2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.553 | 4-CN | 3-OMe,4-OEt | H | CH2CH2 | |
1.554 | 4-SO2CH3 | 3-OMe,4-OEt | H | CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.555 | 4-SO2CF3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.556 | 4-SO2NH2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.557 | 4-SO2NHMe | 3-OMe,4-OEt | H | CH2CH2 | |
1.558 | 4-SO2NMe2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.559 | 4-SO3Me | 3-OMe,4-OEt | H | CH2CH2 | |
1.560 | 4-SO3CF3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.561 | 4-SO3H | 3-OMe,4-OEt | H | CH2CH2 | |
1.562 | 4-CO2H | 3-OMe,4-OEt | H | CH2CH2 | |
1.563 | 4-CO2Me | 3-OMe,4-OEt | H | CH2CH2 | |
1.564 | 4-OCOMe | 3-OMe,4-OEt | H | CH2CH2 | |
1.565 | 4-NHCOMe | 3-OMe,4-OEt | H | CH2CH2 | |
1.566 | 4-COMe | 3-OMe,4-OEt | H | CH2CH2 | |
1.567 | 4-CONMe2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.568 | 4-Me | 3-OMe,4-OEt | H | CH2CH2 | |
1.569 | 3,4-Me2 | 3-OMe,4-OEt | H | CH2CH2 | |
1.570 | 2,4,6-Me3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.571 | 3,4,5-Me3 | 3-OMe,4-OEt | H | CH2CH2 | |
1.572 | 3-Cl,4-Me | 3-OMe,4-OEt | H | CH2CH2 | |
1.573 | 3-Br,4-Me | 3-OMe,4-OEt | H | CH2CH2 | |
1.574 | 3-Me,4-Cl | 3-OMe,4-OEt | H | CH2CH2 | |
1.575 | 3-Me,4-Br | 3-OMe,4-OEt | H | CH2CH2 | |
1.576 | 4-tBu | 3-OMe,4-OEt | H | CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.636 | -F5 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.637 | 2-Cl | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.638 | 3-Cl | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.639 | 4-Cl | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.640 | 2,3-Cl2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.641 | 2.4-Cl2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.642 | 2,5-Cl2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.643 | 2,6-Cl2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.644 | 3,4-Cl2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.645 | 3,5-Cl2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.646 | 2,3,4-Cl3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.647 | 2,3,5-Cl3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.648 | 3,4,5-Cl3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.649 | 4-Br | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.650 | 3,4-Br2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.651 | 3,4,5-Br3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.652 | 4-1 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.653 | 3,4-l2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.654 | 3,4,5-l3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.655 | 3-Br,4-Cl | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.656 | 3-Cl,4-Br | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.657 | 3-l,4-Cl | 3,4,5-(OMe)3 | H | CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.658 | 3-Cl,4-l | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.659 | 3-F,4-Cl | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.660 | 3-F,4-Br | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.661 | 2,3,5,6-F4,4-Br | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.662 | 2,3,5,6-F4,4-Cl | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.663 | 4-CF3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.664 | 3,4-(CF3)2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.665 | 3-OH,4-Cl | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.666 | 3-Cl,4-OH | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.667 | 3-CF3,4-Cl | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.668 | 3-CF3,4-Br | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.669 | 4-NO2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.670 | 4-CN | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.671 | 4-SO2CH3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.672 | 4-SO2CF3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.673 | 4-SO2NH2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.674 | 4-SO2NHMe | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.675 | 4-SO2NMe2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.676 | 4-SO3Me | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.677 | 4-SO3CF3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.678 | 4-SO2H | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.679 | 4-CO2H | 3,4,5-(OMe)3 | H | CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.680 | 4-CO2Me | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.681 | 4-OCOMe | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.682 | 4-NHCOMe | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.683 | 4-COMe | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.684 | 4-CONMe2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.685 | 4-Me | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.686 | 3,4-Me2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.687 | 2,4,6-Me3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.688 | 3,4,5-Me3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.689 | 3-Cl,4-Me | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.690 | 3-Br,4-Me | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.691 | 3-Me,4-Cl | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.692 | 3-Me,4-Br | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.693 | 4-tBu | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.694 | 4-SiMe3 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.695 | 4-Ph | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.696 | 2-Ph | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.697 | 4-Et | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.698 | 4-Pr | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.699 | 4-iPr | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.700 | 4-Bu | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.701 | 4-C12H25 | 3,4,5-(OMe)3 | H | CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.738 | 4-OCH2Ph | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.739 | 4-OCONMe2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.740 | 4-OP(O)(OMe)2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.741 | 4-P(O)(OMe)2 | 3,4,5-(OMe)3 | H | CH2CH2 | |
1.741 | H | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.742 | 2-F | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.743 | 3-F | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.744 | 4-F | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.745 | 2,3-F2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.746 | 2,4-F2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.747 | 2,5-F2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.748 | 2,6-F2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.749 | 3,4-F2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.750 | 3,5-F2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.751 | 2,3,4-F3 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.752 | -F5 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.753 | 2-Cl | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.754 | 3-Cl | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.755 | 4-Cl | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.756 | 2,3-Cl2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.757 | 2,4-Cl2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.758 | 2,5-Cl2 | 3,4-(OMe)2 | H | CH2CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.759 | 2,6-Cl2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.760 | 3,4-Cl2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.761 | 3,5-Cl2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.762 | 2,3,4-Cl3 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.763 | 2,3,5-Cl3 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.764 | 3,4,5-Cl3 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.765 | 4-Br | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.766 | 3,4-Br2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.767 | 3,4,5-Br3 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.768 | 4-1 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.769 | 3,4-l2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.770 | 3,4,5-l3 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.771 | 3-Br,4-Cl | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.772 | 3-Cl,4-Br | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.773 | 3-l,4-Cl | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.774 | 3-Cl,4-l | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.775 | 3-F,4-Cl | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.776 | 3-F,4-Br | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.777 | 2,3,5,6-F4,4-Br | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.778 | 2,3,5,6-F4,4-Cl | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.779 | 4-CF3 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.780 | 3,4-(CF3)2 | 3,4-(OMe)2 | H | CH2CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.781 | 3-OH,4-Cl | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.782 | 3-Cl,4-OH | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.783 | 3-CF3,4-Cl | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.784 | 3-CF3,4-Br | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.785 | 4-NO2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.786 | 4-CN | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.787 | 4-SO2CH3 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.788 | 4-SO2CF3 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.789 | 4-SO2NH2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.790 | 4-SO2NHMe | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.791 | 4-SO2NMe2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.792 | 4-SO3Me | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.793 | 4-SO3CF3 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.794 | 4-SO2H | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.795 | 4-CO2H | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.796 | 4-CO2Me | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.797 | 4-OCOMe | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.798 | 4-NHCOMe | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.799 | 4-COMe | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.800 | 4-CONMe2 | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.801 | 4-Me | 3,4-(OMe)2 | H | CH2CH2CH2 | |
1.802 | 3,4-Me2 | 3,4-(OMe)2 | H | CH2CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.862 | 2,3-F2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.863 | 2,4-F2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.864 | 2,5-F2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.865 | 2,6-F2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.866 | 3,4-F2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.867 | 3,5-F2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.868 | 2,3,4-F3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.869 | -F5 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.870 | 2-Cl | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.871 | 3-Cl | 3-OMe,4-OEt | H | ||
1.872 | 4-Cl | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.873 | 2,3-Cl2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.874 | 2,4-Cl2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.875 | 2,5-Cl2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.876 | 2,6-Cl2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.877 | 3,4-Cl2 | 3-OMe,4-OEt | H | CH2CH2CH2- | |
1.878 | 3,5-Cl2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.879 | 2,3,4-Cl3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.880 | 2,3,5-Cl3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.881 | 3,4,5-Cl3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.882 | 4-Br | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.883 | 3,4-Br2 | 3-OMe,4-OEt | H | CH2CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.884 | 3,4,5-Br3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.885 | 4-l | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.886 | 3,4-l2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.887 | 3,4,5-l3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.888 | 3-Br,4-Cl | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.889 | 3-Cl,4-Br | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.890 | 3-l,4-Cl | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.891 | 3-Cl,4-l | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.892 | 3-F,4-Cl | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.893 | 3-F,4-Br | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.894 | 2,3,5,6-F4,4-Br | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.895 | 2,3,5,6-F4,4-Cl | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.896 | 4-CF3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.897 | 3,4-(CF3)2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.898 | 3-OH,4-Cl | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.899 | 3-Cl,4-OH | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.900 | 3-CF3,4-Cl | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.901 | 3-CF3,4-Br | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.902 | 4-NO2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.903 | 4-CN | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.904 | 4-SO2CH3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.905 | 4-SO2CF3 | 3-OMe,4-OEt | H | CH2CH2CH2 |
编号 | R1 | R2 | R7 | X | m.p.[℃] |
1.906 | 4-SO2NH2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.907 | 4-SO2NHMe | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.908 | 4-SO2NMe2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.909 | 4-SO3Me | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.910 | 4-SO3CF3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.911 | 4-SO2H | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.912 | 4-CO2H | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.913 | 4-CO2Me | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.914 | 4-OCOMe | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.915 | 4-NHCOMe | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.916 | 4-COMe | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.917 | 4-CONMe2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.918 | 4-Me | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.919 | 3,4-Me2 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.920 | 2,4,6-Me3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.921 | 3,4,5-Me3 | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.922 | 3-Cl,4-Me | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.923 | 3-Br,4-Me | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.924 | 3-Me,4-Cl | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.925 | 3-Me,4-Br | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.926 | 4-tBu | 3-OMe,4-OEt | H | CH2CH2CH2 | |
1.927 | 4-SiMe3 | 3-OMe,4-OEt | H | CH2CH2CH2 |
表3:
编号 | R1 | R2 | R6 | X | Y | m.p.[℃] |
1.975 | 4-Cl | 3,4-(OMe)2 | H | CH2CH2 | CH2 | 油状 |
1.976 | 4-Cl | 3,4-(OMe)2 | H | CH2CH2 | CF2 | |
1.977 | 4-Cl | 3,4-(OMe)2 | H | CH2CH2 | C(CH3)2 | |
1.978 | 4-Cl | 3,4-(OMe)2 | H | CH2CH2 | CO | 玻璃状 |
1.979 | 4-Cl | 3,4-(OMe)2 | H | CH2CH2 | C(OMe)CH3 | |
1.980 | 4-Cl | 3-OMe,4-OEt | H | CH2CH2 | CH2 | 油状 |
1.981 | 4-Cl | 3-OMe,4-OEt | H | CH2CH2 | CF2 | 油状 |
1.982 | 4-Br | 3,4-(OMe)2 | H | CH2CH2 | CO | |
1.983 | 4-Br | 3,4-(OMe)2 | H | CH2CH2 | CF2 | |
1.984 | 4-Br | 3,4-(OMe)2 | H | CH2CH2 | C(OMe)CH3 | |
1.985 | 4-Me | 3,4-(OMe)2 | H | CH2CH2 | CO | |
1.986 | 4-Me | 3,4-(OMe)2 | H | CH2CH2 | CF2 | |
1.987 | 4-Me | 3,4-(OMe)2 | H | CH2CH2 | C(OMe)CH3 | |
1.988 | 4-CF3 | 3,4-(OMe)2 | H | CH2CH2 | CO | |
1.989 | 4-CF3 | 3,4-(OMe)2 | H | CH2CH2 | CF2 | |
1.990 | 4-CF3 | 3,4-(OMe)2 | H | CH2CH2 | C(OMe)2CH3 | |
1.991 | 3,4-Me2 | 3,4-(OMe)2 | H | CH2CH2 | CO |
编号 | R1 | R2 | R6 | X | Y | m.p.[℃] |
1.992 | 3,4-Me2 | 3,4-(OMe)2 | H | CH2CH2 | CF2 | |
1.993 | 3,4-Me2 | 3,4-(OMe)2 | H | CH2CH2 | C(OMe)2CH3 | |
1.994 | 3,4-Cl2 | 3,4-(OMe)2 | H | CH2CH2 | CO | |
1.995 | 3,4-Cl2 | 3,4-(OMe)2 | H | CH2CH2 | CF2 | |
1.996 | 3,4-Cl2 | 3,4-(OMe)2 | H | CH2CH2 | C(OMe)CH3 | |
1.997 | 4-Cl | 3,4-(OMe)2 | H | CH2CH2 | CO | |
1997a | 4-Cl | H | H | CH2CH2 | CO | 92-3 |
1997b | H | H | H | CH2CH2 | CO | 82-3 |
1997c | H | H | H | CH2CH2 | CH2 | 96-8 |
表4:
表5:
编号 | R1 | B | R2 | m.p.[℃] |
2.019 | 4-Cl | CH(OH) | 6,7-(OMe)2 | |
2.020 | 4-Br | CH(OH) | 6,7-(OMe)2 | |
2.021 | 3,4-Cl2 | CH(OH) | 6,7-(OMe)2 | |
2.022 | 4-CF3 | CH(OH) | 6,7-(OMe)2 | |
2.023 | 4-Me | CH(OH) | 6,7-(OMe)2 | |
2.024 | 3,4-Me2 | CH(OH) | 6,7-(OMe)2 | |
2.025 | 4-l | CH(OH) | 6,7-(OMe)2 | |
2.026 | 4-NO2 | CH(OH) | 6,7-(OMe)2 | |
2.027 | 4-Cl | CH(OH) | 6-OEt,7-OMe | |
2.028 | 4-Br | CH(OH) | 6-OEt,7-OMe | |
2.029 | 3,4-Cl2 | CH(OH) | 6-OEt,7-OMe | |
2.030 | 4-Cl | CO | 6,7-(OMe)2 | |
2.031 | 4-Br | CO | 6,7-(OMe)2 | |
2.032 | 3,4-Cl2 | CO | 6,7-(OMe)2 | |
2.033 | 4-CF3 | CO | 6,7-(OMe)2 | |
2.034 | 4-Me | CO | 6,7-(OMe)2 |
编号 | R1 | B | R2 | m.p.[℃] |
2.035 | 3,4-Me2- | CO | 6,7-(OMe)2 | |
2.036 | 4-l | CO | 6,7-(OMe)2 | |
2.037 | 4-NO2 | CO | 6,7-(OMe)2 | |
2.038 | 4-Cl | CO | 6-OEt,7-OMe | |
2.039 | 4-Br | CO | 6-OEt,7-OMe | |
2.040 | 3,4-Cl2 | CO | 6-OEt,7-OMe |
表6:
编号 | R1 | B | R2 | X | m.p.[℃] |
2.041 | H | CH(OH) | 3,4-OMe2 | CH2CH2 | 90 |
2.042 | 6-Cl | CH(OH) | 3,4-OMe2 | CH2CH2 | |
2.043 | 6-Br | CH(OH) | 3,4-OMe2 | CH2CH2 | |
2.O44 | 6-Me | CH(OH) | 3,4-OMe2 | CH2CH2 | |
2.045 | 6-CF3 | CH(OH) | 3,4-OMe2 | CH2CH2 | |
2.046 | 6,7-Cl2 | CH(OH) | 3,4-OMe2 | CH2CH2 | |
2.047 | 6-l | CH(OH) | 3,4-OMe2 | CH2CH2 | |
2.048 | 6-NO2 | CH(OH) | 3,4-OMe2 | CH2CH2 | |
2.049 | 6-Cl | CH(OH) | 3-OMe,4-OEt | CH2CH2 | |
2.050 | 6-Me | CH(OH) | 3-OMe,4-OEt | CH2CH2 | |
2.051 | 6-Br | CH(OH) | 3-OMe,4-OEt | CH2CH2 | |
2.052 | 6-Cl | CO | 3,4-(OMe)2 | CH2CH2 | |
2.053 | 6-Br | CO | 3,4-(OMe)2 | CH2CH2 | |
2.054 | 6-Cl | CO | 3,4-(OMe)2 | CH2CH2 | |
2.055 | 6-CF3 | CO | 3,4-(OMe)2 | CH2CH2 | |
2.056 | 6,7-Cl2 | CO | 3,4-(OMe)2 | CH2CH2 |
编号 | R1 | B | R2 | X | m.p.[℃] |
2.057 | 6,7-Me2 | CO | 3,4-(OMe)2 | CH2CH2 | |
2.058 | 6-l | CO | 3,4-(OMe)2 | CH2CH2 | |
2.059 | 6-NO2 | CO | 3,4-(OMe)2 | CH2CH2 | |
2.060 | 6-Cl | CO | 3-OMe,4-OEt | CH2CH2 | |
2.061 | 6-Br | CO | 3-OMe,4-OEt | CH2CH2 | |
2.062 | 6-Me | CO | 3-OMe,4-OEt | CH2CH2 | |
2.063 | 6,7-Me2 | CO | 3-OMe,4-OEt | CH2CH2 | |
2.064 | H | CH(OH) | H | CH2CH2CH2 | 92 |
表7:
编号 | R1 | B | R2 | m.p.[℃] |
2.065 | 6-Cl | CH(OH) | 6,7-(OMe)2 | |
2.066 | 6-Br | CH(OH) | 6,7-(OMe)2 | |
2.067 | 6-Me | CH(OH) | 6,7-(OMe)2 | |
2.068 | 6-CF3 | CH(OH) | 6,7-(OMe)2 | |
2.069 | 6,7-Cl2 | CH(OH) | 6,7-(OMe)2 | |
2.070 | 6,7-Me | CH(OH) | 6,7-(OMe)2 | |
2.071 | 6-l | CH(OH) | 6,7-(OMe)2 | |
2.072 | 6-NO2 | CH(OH) | 6,7-(OMe)2 | |
2.073 | 6-Cl | CH(OH) | 6-OEt,7-OMe | |
2.074 | 6-Br | CH(OH) | 6-OEt,7-OMe | |
2.075 | 6-Me | CH(OH) | 6-OEt,7-OMe | |
2.076 | 6-CF3 | CH(OH) | 6-OEt,7-OMe | |
2.077 | 6-Cl | CO | 6,7-(OMe)2 | |
2.078 | 6-Br | CO | 6,7-(OMe)2 | |
2.079 | 6-Me | CO | 6,7-(OMe)2 | |
2.080 | 6-CF3 | CO | 6,7-(OMe)2 |
编号 | R1 | B | R2 | m.p.[℃] |
2.081 | 6,7-Cl2 | CO | 6,7-(OMe)2 | |
2.082 | 6,7-Me2 | CO | 6,7-(OMe)2 | |
2.083 | 6-l | CO | 6,7-(OMe)2 | |
2.084 | 6-NO2 | CO | 6,7-(OMe)2 | |
2.085 | 6-Cl | CO | 6-OEt,7-OMe | |
2.086 | 6-Br | CO | 6-OEt,7-OMe | |
2.087 | 6-Me | CO | 6-OEt,7-OMe | |
2.088 | 6-CF3 | CO | 6-OEt,7-OMe | |
2.089 | 6,7-Cl2 | CO | 6-OEt,7-OMe | |
2.090 | H | CH(OH) | H |
实验实施例
对本发明化合物进行各种实验。
评价化合物的抗蔓延疫霉(晚番茄枯萎病-PI)和葡萄生单轴霉(葡萄绒毛状霉病-PV)活性。
将所需浓度的化合物水溶液或分散液,包括润湿剂,喷雾到合适的植物上,然后通过喷雾真菌的孢子悬浮液进行接种。将植物保持在适于植物生长和疾病发展的环境条件下。经过适当的时间后,肉眼评估叶面的感染程度。当浓度为500ppm或更低时,本发明的下列化合物对一种或两种疾病的控制作用达100%。2,15,20,25,39,61,62,253,258,262,275,297,298,304,740,741,762,764,767,866,1008,1149,1189,1190,1199,1200,1405,2119,2120,2134,2151,2173,2174,2177,2182,2183,2214,2215,2216,2221,2228,2229,2233,2233,2237,2238,2239
Claims (18)
2.按照权利要求1的化合物及其盐、特别是酸加成盐的用途,其中A是式II或III基团;A′是式IV或V基团;
m、n、m′和n′是整数;
m=1-5;
n=1-7;
m′=0-5;
n′=0-7;R1和R2相同或不同,并且它们彼此独立地为(C1-C18)-烷基,
(C3-C12)-环烷基,(C3-C12)-环烷基-(C1-C6)-烷基,(C6-
C18)-芳基,(C6-C18)-芳基-(C1-C6)-烷基,(C1-C8)-杂芳
基,(C1-C8)-非芳族杂环基,(C1-C8)-杂芳基-(C1-C6)-烷
基,(C1-C8)-非芳族杂环基-(C1-C6)-烷基,氰基,硝基,
卤素,-COR3,-COOR3,-CONR3R4,-OR3,-OCOR3,-OCOOR3,-OCO-NR3R4,-SR3,-SOR3,-SO2R3,-SO2-OR3,-SO2NR3R4,-NR3R4,-NR3-SO2R4,-NR3-COR4,-P(O)(OR3)(OR4),
-O-P(O)(OR3)(OR4)或-SiR3 3,和其中,在前十个基团中,任选地满足至少一个下列条件:a)如果含有1、2或3个不在环上的CH-CH-单元,则其各自被
1、2或3个CH=CH-单元置换,b)如果含有不在环上的CH2-CH2-单元,则其被C≡C-单元置换,c)如果含有在环上的CH-CH-单元,则其被C=C-单元置换,d)在非环部分的碳原子上存在的氢原子被最多三个相同或不
同的取代基置换,这些取代基是氰基,硝基,卤素,
-COR3,-COOR3,-CONR3R4,-OR3,-OCOR3,
-OCOOR3,-O-CO-NR3R4,-SR3,-SOR3,-SO2R3,-SO2-OR3,
-SO2-NR3R4,-NR3R4,-NR3-COR4,-P(O)(OR3)(OR4),
-O-P(O)(OR3)(OR4)和-SiR3 3,e)按照d)所述进行取代后,在非环部分的碳原子上剩余的氢
原子被相同或不同的卤原子部分或全部置换,f)在环碳原子上存在的氢原子被最多3个相同或不同的取代基
R3(R3不是氢)和在d)中给出的取代基置换,g)按照f)所述进行取代后,在环碳原子上剩余的氢原子被相
同或不同的卤原子部分或全部置换,h)在非偶合位置存在的一个或两个CH2-单元可以被选自O、S、
CO和NR3的相同或不同的基团置换;R3和R4相同或不同,并且它们彼此独立地为氢,(C1-C18)-烷
基,(C3-C12)-环烷基,(C3-C12)-环烷基-(C1-C6)-烷基,
(C6-C18)-芳基,(C6-C18)-芳基-(C1-C6)-烷基,(C1-C8)-杂
芳基或(C1-C8)-杂芳基-(C1-C6)-烷基,其中,在前七个基
团中,任选地满足至少一个下列条件:a)如果含有1、2或3个不在环上的CH-CH-单元,则其各自被
1、2或3个CH=CH-单元置换,b)如果含有不在环上的CH2-CH2-单元,则其被C≡C-单元置换,c)如果含有在环上的CH-CH-单元,则其被C=C-单元置换,d)在非环部分的碳原子上存在的氢原子被最多三个相同或不
同的取代基置换,这些取代基是氰基,硝基,卤素,
-COR3,-COOR3’,-CONR3’ 2,-OR3’,
-OCOR3’,-OCOOR3’,-O-CO-NR3’,-SR3,-SOR3’,-SO2R3’,
-SO2-OR3’,-SO2-NR3’ 2,-NR3’ 2,-NR3’-COR3’,
-P(O)(OR3)(OR4),-O-P(O)(OR3)(OR4)和-SiR3’ 3,e)按照d)所述进行取代后,在非环部分的碳原子上剩余的氢
原子被相同或不同的卤原子部分或全部置换,f)在环碳原子上存在的氢原子被最多3个相同或不同的取代基
R3′(R3′不是氢)和在d)中给出的取代基置换,g)按照f)所述进行取代后,在环碳原子上剩余的氢原子被相
同或不同的卤原子部分或全部置换,h)在非偶合位置存在的一个或两个CH2-单元可以被选自O、S、
CO和NR3的相同或不同的基团置换;或R3和R4一起形成(C3-C6)-亚烷基,其中CH2基团任意地被CO、O、S或NR3置换;R3′是相同或不同的取代基,为氢,(C1-C6)-烷基,(C2-C6)-链
烯基,(C2-C6)-链炔基,(C1-C6)-卤代烷基,(C2-C6)-卤代
烯基,(C2-C6)-卤代炔基,(C3-C6)-环烷基,(C3-C6)-环烷
基-(C1-C4)-烷基,(C6-C10)-芳基,(C7-C11)-芳烷基和
(C1-C5)-杂芳基,其中后3个所述的基团可以在环上带有1
或2个相同或不同的取代基,这些取代基是氰基、硝基、
卤素、(C1-C4)-烷基、(C1-C4)-卤代烷基、(C1-C4)-烷氧
基、(C1-C4)-卤代烷氧基、苯基、苯氧基、苄基和苄氧
(C1-C6)-烷基,(C6-C18)-芳基,(C6-C18)-芳基-(C1-C6)-烷
基,(C1-C8)-杂芳基,(C1-C8)-杂芳基-(C1-C6)-烷基,氰
基,-COR3,-COOR3,-CONR3R4或-SiR3 3,并且R3和R4如上
所定义,其中第2-8个所述基团中任意地满足至少一个对
基团R1和R2所述的条件a)-h);R6是氢或者如对R1所定义,因此当R5=氢时,R6不通过O-、S-或N-原子连接,或者R5和R6一起形成(C3-C6)-亚烷基,其中CH2-基团任意地被CO、
O、S或NR3′置换和/或一个CH-CH-单元任意地被C=C-单元
置换;R7是氢或者除硝基和卤素之外的如对R1的定义,或者R5和R7一起形成(C2-C5)-亚烷基,其中CH2-基团任意地被CO、
O、S或NR3′置换和/或一个CH-CH-单元任意地被C=C-单元
置换,并且R6如上所定义,R6和R7一起形成(C3-C6)-亚烷基,其中CH2-基团任意地被CO、
O、S或NR3′置换和/或一个CH-CH-单元任意地被C=C-单元
置换,并且R5如上所定义;X是式VIII基团,
-CR8R9-(CR10R11)p- (VIII)R8、R9、R10和R11相同或不同,并且彼此独立地如对R7所定
义,或者是卤素或硝基,而且其中R8和R9、或者R10和R11
通过形成氧代基可以一起为O,或者R10和R11可以一起形成=N-OR3基团,或者R7和R8一起形成(C2-C5)-亚烷基,R7和R10一起形成(C1-C4)-
亚烷基或者R8和R10一起形成(C3-C6)-亚烷基,其中在每
种情况下,CH2-基团任意地被CO、O、S或NR3′置换和/或
一个CH-CH-单元任意地被C=C-单元置换,并且这些不
涉及与此环连接的基团如上所定义;和p是1、2或3。
3.按照权利要求2的用途,其中R1和R2相同或不同,并且它们彼此独立地为(C1-C12)-烷基,
(C3-C12)-环烷基,(C3-C12)-环烷基-(C1-C4)-烷基,(C6-
C12)-芳基,(C6-C12)-芳基-(C1-C4)-烷基,(C1-C8)-杂芳
基,(C1-C8)-杂芳基-(C1-C4)-烷基,氰基,硝基,卤素,
-COR3,-COOR3,-CONR3R4,
-OR3,-OCOR3,-OCOOR3,-OCO-NR3R4,-SR3,-SOR3,-SO2R3,
-SO2-OR3,-SO2NR3R4,-NR3R4,-NR3-SO2R4,-NR3-COR4或
-SiR3 3,其中,在前七个基团中,任选地满足对这些基团所定义的b)、c)、e)、g)和h)以及下列条件中的至少一个条件:a)如果含有1个不在环上的CH-CH-单元,则其被CH=CH-单元置
换,d)在非环部分的碳原子上存在的氢原子被最多三个相同或不
同的取代基置换,这些取代基是氰基,硝基,卤素,
-COR3,-COOR3,-CONR3R4,-OR3,-OCOR3,
-OCOOR3,-O-CO-NR3R4,-SR3,-SOR3,-SO2R3,-SO2-OR3,
-SO2-NR3R4,-NR3R4,-NR3-COR4,和-SiR3 3f)在环碳原子上存在的氢原子被最多3个相同或不同的取代基
R3(R3不是氢)和在d)中给出的取代基置换,R3和R4相同或不同,并且它们彼此独立地为(C1-C12)-烷基,
(C3-C8)-环烷基,(C3-C8)-环烷基-(C1-C4)-烷基,(C6-
C12)-芳基,(C6-C12)-芳基-(C1-C4)-烷基,(C1-C8)-杂芳
基或(C1-C8)-杂芳基-(C1-C4)-烷基,其中,在后七个基团
中,任选地满足对这些基团所定义的b)、c)、e)、g)和h)
以及下列条件中的至少一个条件:a)如果含有1个不在环上的CH-CH-单元,则其被CH=CH-单元置
换,d)在非环部分的碳原子上存在的氢原子被最多三个相同或不
同的取代基置换,这些取代基是氰基,硝基,卤素,
-COR3’,-COOR3’,-CONR3’ 2,-OR3’,-OCOR3’,-OCOOR3’,-O-CO-NR3’,-SR3’,-SOR3’,-SO2R3’,-SO2-OR3’,-SO2-NR3’ 2,-NR3’ 2,-NR3’-COR3’和-Si(R3’)3,f)在环碳原子上存在的氢原子被最多3个相同或不同的取代基
R3′(R3′不是氢)和在d)中给出的取代基置换,R3′和B如权利要求2所定义;R5是氢,(C1-C12)-烷基,(C3-C12)-环烷基,(C3-C12)-环烷基-
(C1-C4)-烷基,(C6-C12)-芳基,(C6-C12)-芳基-(C1-C4)-烷
基,(C1-C8)-杂芳基,(C1-C8)-杂芳基-(C1-C4)-烷基,氰
基,-COR3,-COOR3,-CONR3R4或-SiR3 3,并且R3和R4如上
所定义,其中第2-8个所述基团中任意地满足至少一个对
基团R1和R2所述的条件a)-h);R6是氢或者如对R1所定义,因此当R5=氢时,R6不通过O-、S-
或N-原子连接,或者R5和R6一起形成权利要求2所定义的环;R7是氢或者除硝基和卤素之外的如对R1的定义,或者R5和R7一起形成权利要求2所定义的环;R6和R7一起形成权利要求2所定义的环;X如权利要求2所定义;R8、R9、R10和R11相同或不同,并且彼此独立地如对R7所定
义,或者是卤素,而且其中R8和R9、或者R10和R11通过形
成氧代基可以一起为O,或者R10和R11可以一起形成=N-OR3基团,或者R7+R8、R7+R10或者R8+R10一起形成权利要求2所定义的
环,并且这些不涉及与此环连接的基团如上定义;和p如权利要求2所定义。
4.按照权利要求2或3的用途,其中R1和R2相同或不同,并且它们彼此独立地为(C1-C12)-烷基,
(C2-C12)-链烯基,(C2-C12)-链炔基,(C6-C12)-芳基,(C7-
C13)-芳烷基,(C1-C12)-烷氧基,(C2-C12)-链烯氧基,
(C2-C12)-链炔氧基,(C1-C12)-烷硫基,(C6-C12)-芳氧
基,(C7-C13)-芳烷氧基,(C7-C13)-芳烷硫基,(C6-C12)-
芳硫基,杂芳基,杂芳基-(C1-C4)-烷基,杂芳氧基,杂芳
基-(C1-C4)-烷氧基,杂芳基-(C1-C4)-烷硫基,杂芳氧基-
(C1-C4)-烷基,其中杂环芳基各自具有最多8个碳原子和最
多4个选自N、S和O的相同或不同的杂原子,(C3-C12)-环烷
基,(C3-C12)-环烷氧基,(C3-C12)-环烯基,(C3-C12)-环
烯氧基, -CN,
OH,NO2,F,Cl,Br,I,-COOR3,-COR3,-OCOR3,
-CONR3R4,-R3COR4,-NR3R4,-SO2NR3R4,-NR3SO2R4,
-NR3COR4,-SiR3 3,-SO2R3或-SO3R3,
其中,前23个基团任意地如权利要求2或3所述被取代,和R3和R4具有权利要求2或3所给出的含义;R5和R6彼此独立地为氢,(C1-C12)-烷基,(C2-C12)-链烯基,
(C2-C12)-链炔基,(C6-C12)-芳基,(C7-C12)-芳烷基,(C7-
C12)-芳氧烷基,杂芳基,杂芳基-(C1-C4)-烷基,杂芳氧
基-(C1-C4)-烷基,其中杂环芳基各自具有最多8个碳原子
和最多4个选自N、S和O的相同或不同的杂原子,(C3-C12)-
环烷基,(C3-C12)-环烯基,-COOR3,-COR3,-CONR3R4或-SiR3 3,其中,第2-12个所述基团任意地如权利要求2或3所
述被取代,或者R5与R6可以一起形成饱和或不饱和的5-、6-、7-或8-元环,R3和R4的含义同上,并且当R5不是氢
时,R6也可以是(C1-C6)-烷氧基、(C1-C6)-卤代烷氧基、
苯氧基、CN、-NR3R4、-NR3SO2R4或-NR3COR4;R7为氢,(C1-C6)-烷基,(C2-C6)-链烯基,(C2-C6)-链炔基,
(C6-C12)-芳基,(C7-C12)-烷芳基,(C1-C6)-烷氧基,(C2-
C6)-链烯氧基,(C3-C6)-链炔氧基,(C6-C12)-芳氧基,
(C7-C13)-烷芳氧基,杂芳基,杂芳基-(C1-C4)-烷基,杂
芳氧基,杂芳基-(C1-C4)-烷氧基,其中杂环芳基各自具有
最多8个碳原子和最多4个选自N、S和O的相同或不同的杂
原子,(C3-C8)-环烷基,(C3-C8)-环烷氧基,(C3-C8)-环烯
基,(C3-C8)-环烯氧基,-OH,-COOR3,-COR3,-OCOR3,
-CONR3R4,-NR3COR4,-SiR3 3或NR3R4,其中,第2-19个所述
基团任意地如权利要求2或3中所述被取代,R3和R4的含义
同上,或者R7与R5或R6形成饱和或不饱和的5-或6-元环部
分;R8、R9、R10和R11相同或不同,并且彼此独立地为F、Cl、
Br、I、CN或具有与R7相同的定义,或者R7+R8、R7+R10
或者R8+R10一起形成饱和或不饱和的5-、6-、7-或8-元
环的部分,并且剩余的基团和可变基团如权利要求2或3所
定义。
5.按照权利要求2-4中任何一项的用途,其中,R1和R2相同或不同,并且它们彼此独立地为(C1-C6)-烷基,(C2-
C6)-链烯基,(C3-C6)-链炔基,(C3-C7)-环烷基,(C3-C7)-
环烯基,(C3-C6)-烷氧基,苄氧基,(C1-C6)-烷硫基,苯
基,苯氧基,苯硫基,(C2-C6)-链烯氧基,(C3-C6)-链炔
氧基,(C7-C13)-苯基烷氧基,(C7-C13)-苯基烷硫基,(C1-
C6)-卤代烷基,(C1-C6)-卤代烷氧基,(C2-C6)-卤代烯氧
基,(C3-C6)-卤代炔氧基,特别是氟代烷基和氟代烷氧
基,(C3-C7)-环烷氧基,(C3-C7)-环烯氧基,(C1-C6)-卤代
烷硫基,(C2-C6)-卤代链烯硫基,(C3-C7)-卤代环烷基,
(C3-C7)-卤代环烯基,(C3-C7)-卤代环烷氧基,(C3-C7)-卤
代环烯氧基,(C3-C7)-卤代环烷硫基,特别是氟代烷硫
基,CN,OH,NO2,F,Cl,Br,I,CO2R3,OCOR3,COR3,
NR3COR4,NR3R4,SO3R3,SO2NR3R4,杂芳基,杂芳氧基,
其中杂环芳基各自具有最多5个碳原子和最多3个选自N、S
和O的相同或不同的杂原子,并且R3和R4具有权利要求2、3
或4给出的含义;m=1-5;n=1-4;m′=2-5;和n′=2-4;R5和R6相同或不同,并且彼此独立地为氢,(C1-C6)-烷基,(C2-
C6)-链烯基,(C2-C6)-链炔基,(C3-C7)-环烷基,(C3-C7)-
环烯基,苯基,杂芳基,其中杂环芳基各自具有最多5个
碳原子和最多3个选自N、S和O的相同或不同的杂原子,
(C1-C6)-羟烷基,(C1-C6)-卤代烷基,(C2-C6)-卤代烯基,
COOR3,COR3,CONR3R4或-SiR3 3,并且当R5不是氢时,R6还
可以是(C1-C6)-烷氧基,苯氧基,(C1-C6)-卤代烷氧基,
CN、NR3R4或NR3COR4,或者R5与R6可以一起形成饱和或不饱
和的5-或6-元环,并且R3和R4具有权利要求2、3或4给出的
含义;R7为氢,(C1-C6)-烷基,(C2-C6)-链烯基,(C2-C6)-链炔基,苯
基,(C1-C6)-烷氧基,苯氧基,(C2-C6)-链烯氧基,(C3-
C6)-链炔氧基,(C3-C7)-环烯氧基,(C1-C6)-卤代烷基,
(C1-C6)-卤代烷氧基,OH,COOR3,COR3,OCOR3,
CONR3R4,NR3COR4,NR3R4或SiR3 3,或者R7与R5或R6形成饱
和或不饱和的5-或6-元环,并且R3和R4具有权利要求2、3
或4给出的含义;R8、R9、R10和R11相同或不同,并且彼此独立地为F、Cl、
Br、I或CN或具有与R7相同的定义,或者R7+R8或R7+R10
或者R8+R10可以是饱和或不饱和的5-或6-元环的组成部
分,并且剩余的基团和可变基团如权利要求2、3或4所定
义。
6.按照权利要求5的用途,其中R1是(C1-C6)-烷基,(C2-C6)-链烯基,(C3-C6)-链炔基,(C3-
C7)-环烷基,(C3-C7)-环烯基,苯基,(C1-C6)-卤代烷
基,(C2-C6)-卤代烯基,(C2-C6)-卤代炔基,(C1-C6)-卤代
烷氧基,(C2-C6)-卤代烯氧基,(C3-C6)-卤代炔氧基,
(C3-C7)-环烷氧基,(C1-C6)-卤代烷硫基,(C2-C6)-卤代链
烯硫基,(C3-C7)-卤代环烷基,(C3-C7)-卤代环烯基,
(C3-C7)-卤代环烷氧基,(C3-C7)-卤代环烯氧基,(C3-C7)-
卤代环烷硫基,CN,OH,NO2,F,Cl,Br,I,CO2R3,
OCOR3,COR3,NR3COR4,NR3R4,SO3R3,SO2NR3R4,杂芳
基,其中杂环芳基各自具有最多5个碳原子和最多3个选自
N、S和O的相同或不同的杂原子,并且R3和R4具有权利要求
2、3或4给出的含义。
7.按照权利要求5或6的用途,其中R2是(C1-C6)-烷基,(C2-C6)-链烯基,(C3-C6)-链炔基,(C3-
C7)-环烷基,(C3-C7)-环烯基,(C1-C6)-烷氧基,苄氧
基,(C1-C6)-烷硫基,苯氧基,苯硫基,(C2-C6)-链烯氧
基,(C3-C6)-链炔氧基,(C7-C13)-苯基烷氧基,(C7-C13)-
苯基烷硫基,(C1-C6)-卤代烷基,(C1-C6)-卤代烷氧基,
(C2-C6)-卤代烯氧基,(C3-C6)-卤代炔氧基,(C3-C7)-环烷
氧基,(C3-C7)-环烯氧基,(C1-C6)-卤代烷硫基,(C2-C6)-
卤代链烯硫基,(C3-C7)-卤代环烷基,(C3-C7)-卤代环烯
基,(C3-C7)-卤代环烷氧基,(C3-C7)-卤代环烯氧基,
(C3-C7)-卤代环烷硫基,CO2R3,OCOR3,COR3,NR3COR4,
NR3R4,杂芳氧基,其中杂环芳基各自具有最多5个碳原子
和最多3个选自N、S和O的相同或不同的杂原子,并且R3和
R4具有权利要求2、3或4给出的含义。
8.式I化合物其中X和R7如前述任一权利要求中所定义;B是被任意取代的羟基取代的亚甲基;A′是二烷氧基苯基,其中苯基还可以任意地被进一步取代;和A是被一个或多个选自卤素、氰基、硝基、任意取代的氨基、
任意取代的烷基、卤代烷氧基、芳基、杂环基的基团取代
的苯基,其中苯基可以任意地被进一步取代。
9.按照权利要求8的化合物,其中A是被一个或多个选自卤素、氰基、烷基、三氟甲基和卤代烷氧基的基团取代的苯基。
10.权利要求8或9的化合物用于抗真菌的用途。
11.抗真菌组合物,该组合物含有杀真菌活性量的至少一种权利要求1-8中任何一项所定义的式I化合物和用于该用途的常规添加剂和辅剂。
12.植物保护组合物,该组合物含有杀真菌活性量的至少一种权利要求1-8中任何一项所定义的式I化合物和至少一种其它的活性成分,优选杀真菌剂、杀虫剂、干燥剂、杀菌剂、杀螨剂、杀线虫剂和除草剂,以及用于此用途的常规添加剂和辅剂。
13.用作木材防腐剂或涂料和增稠剂防腐剂、用于金属加工用的冷却润滑剂中、或者用于钻孔和切割油中的组合物,该组合物含有活性量的至少一种权利要求1-8中任何一项所定义的式I化合物以及用于此用途的常规添加剂和辅剂。
14.权利要求11-13中任何一项的组合物,该组合物含有至少一种表面活性剂。
15.权利要求1-8中任何一项所定义的化合物用作木材防腐剂或涂料和增稠剂防腐剂、用于金属加工用的冷却润滑剂中、或者用于钻孔和切割油中的用途。
16.抗植物致病真菌的方法,其特征在于向真菌上或植物上、或者真菌所侵袭的表面或底物上、或者向种子上施用杀真菌活性量的权利要求1-8中任何一项所定义的化合物。
17.木材防腐剂、涂料、增稠剂、金属加工用的冷却润滑剂、或钻孔和切割油,其中含有杀真菌活性量的权利要求1-8中任何一项所定义的化合物。
18.用杀真菌活性量的权利要求1-8中任何一项所定义的化合物处理的种子。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE4319887A DE4319887A1 (de) | 1993-06-16 | 1993-06-16 | Arylacetamide, Verfahren zu ihrer Herstellung, sie enthaltende Mittel und ihre Verwendung als Fungizide |
DEP4319887.2 | 1993-06-16 |
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Publication Number | Publication Date |
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CN1128019A true CN1128019A (zh) | 1996-07-31 |
Family
ID=6490422
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CN94192918.3A Pending CN1128019A (zh) | 1993-06-16 | 1994-06-14 | 芳基乙酰胺类化合物、其制备方法、含有这些化合物的组合物及其作为杀真菌剂的用途 |
Country Status (8)
Country | Link |
---|---|
EP (1) | EP0703899A1 (zh) |
JP (1) | JPH08511772A (zh) |
CN (1) | CN1128019A (zh) |
AU (1) | AU7123994A (zh) |
DE (1) | DE4319887A1 (zh) |
HU (1) | HUT73352A (zh) |
IL (1) | IL110037A0 (zh) |
WO (1) | WO1994029267A1 (zh) |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN100340541C (zh) * | 2001-11-16 | 2007-10-03 | 辛根塔参与股份公司 | α-羟基羧酸酰胺的制备方法 |
CN100482639C (zh) * | 2002-07-24 | 2009-04-29 | 辛根塔参与股份公司 | N-芳基-亚环烷基-α-羟基-和α-烷氧基乙酰胺类化合物 |
CN100509759C (zh) * | 2001-11-16 | 2009-07-08 | 辛根塔参与股份公司 | 新颖的α-氧或α-硫羧酸苯乙酰胺衍生物 |
CN103288669A (zh) * | 2013-07-01 | 2013-09-11 | 南开大学 | 一种阿卓乳酸酰胺衍生物及应用 |
CN111747873A (zh) * | 2019-03-29 | 2020-10-09 | 成都同心纵横生物医药有限公司 | 一种艾瑞昔布中间体及其制备方法和用途 |
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---|---|---|---|---|
AU4265596A (en) * | 1994-12-06 | 1996-06-26 | Agrevo Uk Limited | Heterocyclyl substituted hydroxyacetamide derivatives as fongicides |
DE19512617A1 (de) * | 1995-04-05 | 1996-10-10 | Bayer Ag | Hydrazonoessigsäureamide |
DE19642863A1 (de) * | 1996-10-17 | 1998-04-23 | Bayer Ag | Amide |
FR2761986B1 (fr) * | 1997-04-09 | 1999-05-21 | Hoechst Schering Agrevo Sa | Nouveaux amides aromatiques, leur procede de preparation et leur application comme pesticides |
TW564244B (en) * | 1999-01-11 | 2003-12-01 | Novartis Ag | Novel propargylether derivatives |
GB0011944D0 (en) * | 2000-05-17 | 2000-07-05 | Novartis Ag | Organic compounds |
UA75093C2 (en) | 2000-10-06 | 2006-03-15 | Dimensional Pharm Inc | Aminopyridinyl-,aminoguanidinyl-, and alkoxyguanidinesubstituted phenylsubstituted phenylacetamides as protease inhibitors |
GB0127554D0 (en) * | 2001-11-16 | 2002-01-09 | Syngenta Participations Ag | Organic compounds |
GB0127557D0 (en) * | 2001-11-16 | 2002-01-09 | Syngenta Participations Ag | Organic compounds |
GB0223665D0 (en) * | 2002-10-10 | 2002-11-20 | Syngenta Participations Ag | Organic compounds |
WO2005068416A1 (ja) * | 2003-12-12 | 2005-07-28 | Sumitomo Chemical Company, Limited | アミド化合物及びそれを用いた植物病害の防除方法 |
US9120744B2 (en) | 2007-04-16 | 2015-09-01 | The Regents Of The University Of Michigan | Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism |
JP5793883B2 (ja) * | 2010-03-03 | 2015-10-14 | 住友化学株式会社 | 植物病害防除組成物及び植物病害防除方法 |
KR101629767B1 (ko) | 2012-07-04 | 2016-06-13 | 아구로카네쇼 가부시키가이샤 | 2-아미노니코틴산에스테르 유도체 및 이를 유효 성분으로 하는 살균제 |
CN105008323B (zh) * | 2012-10-31 | 2018-11-06 | 密歇根大学董事会 | 纤溶酶原激活物抑制因子-1抑制剂和其使用方法 |
AU2018307807B2 (en) | 2017-07-27 | 2024-05-02 | Eastern Michigan University | Plasminogen activator inhibitor-1 (PAI-1) inhibitor and method of use |
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---|---|---|---|---|
GB2104065B (en) * | 1981-06-04 | 1985-11-06 | Ciba Geigy Ag | Heterocyclyl-substituted mandelic acid compounds and mandelonitriles and their use for combating microorganisms |
JPS5832853A (ja) * | 1981-08-18 | 1983-02-25 | Idemitsu Kosan Co Ltd | N−(α,α−ジアルキルベンジル)フエニルアセトアミド誘導体の製造方法 |
US4518789A (en) * | 1982-06-30 | 1985-05-21 | Yu Ruey J | Phenyl alpha-acyloxyacetamide derivatives and their therapeutic use |
-
1993
- 1993-06-16 DE DE4319887A patent/DE4319887A1/de not_active Withdrawn
-
1994
- 1994-06-14 WO PCT/EP1994/001938 patent/WO1994029267A1/en not_active Application Discontinuation
- 1994-06-14 CN CN94192918.3A patent/CN1128019A/zh active Pending
- 1994-06-14 JP JP7501348A patent/JPH08511772A/ja active Pending
- 1994-06-14 HU HU9503609A patent/HUT73352A/hu unknown
- 1994-06-14 EP EP94920452A patent/EP0703899A1/en not_active Withdrawn
- 1994-06-14 AU AU71239/94A patent/AU7123994A/en not_active Abandoned
- 1994-06-16 IL IL11003794A patent/IL110037A0/xx unknown
Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN100340541C (zh) * | 2001-11-16 | 2007-10-03 | 辛根塔参与股份公司 | α-羟基羧酸酰胺的制备方法 |
CN100509759C (zh) * | 2001-11-16 | 2009-07-08 | 辛根塔参与股份公司 | 新颖的α-氧或α-硫羧酸苯乙酰胺衍生物 |
CN100482639C (zh) * | 2002-07-24 | 2009-04-29 | 辛根塔参与股份公司 | N-芳基-亚环烷基-α-羟基-和α-烷氧基乙酰胺类化合物 |
CN103288669A (zh) * | 2013-07-01 | 2013-09-11 | 南开大学 | 一种阿卓乳酸酰胺衍生物及应用 |
CN103288669B (zh) * | 2013-07-01 | 2015-06-24 | 南开大学 | 一种阿卓乳酸酰胺衍生物及应用 |
CN111747873A (zh) * | 2019-03-29 | 2020-10-09 | 成都同心纵横生物医药有限公司 | 一种艾瑞昔布中间体及其制备方法和用途 |
CN111747873B (zh) * | 2019-03-29 | 2022-04-08 | 成都同心纵横生物医药有限公司 | 一种艾瑞昔布中间体及其制备方法和用途 |
Also Published As
Publication number | Publication date |
---|---|
HUT73352A (en) | 1996-07-29 |
HU9503609D0 (en) | 1996-02-28 |
AU7123994A (en) | 1995-01-03 |
JPH08511772A (ja) | 1996-12-10 |
WO1994029267A1 (en) | 1994-12-22 |
IL110037A0 (en) | 1994-10-07 |
EP0703899A1 (en) | 1996-04-03 |
DE4319887A1 (de) | 1994-12-22 |
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