苯乙酸衍生物,其制备方法和中间产品及含有它们的药剂技术

技术编号:71842 阅读:228 留言:0更新日期:2012-04-11 18:40
一种式Ⅰ的苯乙酸衍生物 *** Ⅰ 其中取代基和指数含义如下: X 是NOCH↓[3],CHOCH↓[3],CHCH↓[3]; Y 是O,NR; R↑[1],R 相互独立地为氢和C↓[1]-C↓[4]烷基; R↑[2] 是氰基,硝基,三氟甲基,卤素,C↓[1]-C↓[4]烷基和C↓[1]-C↓[4]烷氧基; m 是0,1或2,当m为2时,基团R↑[2]可能是不相同的; R↑[3] 是氢,氰基,C↓[1]-C↓[4]烷基,C↓[1]-C↓[4]卤代烷基,C↓[3]-C↓[6]环烷基; R↑[4],R↑[6] 相互独立地为氢,C↓[1]-C↓[10]烷基,C↓[3]-C↓[6]环烷基,C↓[2]-C↓[10]链烯基,C↓[2]-C↓[10]炔基,C↓[1]-C↓[10]烷基羰基,C↓[2]-C↓[10]链烯基羰基,C↓[3]-C↓[10]炔基羰基或C↓[1]-C↓[10]烷基磺酰基,这些基团可能被部分或完全卤化,或者连有1-3个下列基团:氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,卤素,C↓[1]-C↓[6]烷基,C↓[1]-C↓[6]卤代烷基,C↓[1]-C↓[6]烷基磺酰基,C↓[1]-C↓[6]烷基次硫酸基,C↓[1]-C↓[6]烷氧基,C↓[1]-C↓[6]卤代烷氧基,C↓[1]-C↓[6]烷氧羰基,C↓[1]-C↓[6]烷硫基,C↓[1]-C↓[6]烷基氨基,二-C↓[1]-C↓[6]烷基氨基,C↓[1]-C↓[6]烷基氨基羰基,二-C↓[1]-C↓[6]烷基氨基羰基,C↓[1]-C↓[6]烷基氨基硫代羰基,二-C↓[1]-C↓[6]烷基氨基硫代羰基,C↓[2]-C↓[6]链烯基,C↓[2]-C↓[6]链烯氧基,C↓[3]-C↓[6]环烷基,C↓[3]-C↓[6]环烷氧基,杂环基,杂环氧基,苄基,苄氧基,芳基,芳氧基,芳硫基,杂芳基,杂芳氧基和杂芳硫基,这些环状基团本身又可能被部分或完全卤化,或者连有1-3个下列基团:氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,卤素,C↓[1]-C↓[6]烷基,C↓[1]-C↓[6]卤代烷基,C↓[1]-C↓[6]烷基磺酰基,C↓[1]-C↓[6]烷基次硫酸基,C↓[3]-C↓[6]环烷基,C↓[1]-C↓[6]烷氧基,C↓[1]-C↓[6]卤代烷氧基,C↓[1]-C↓[6]烷氧羰基,C↓[1]-C↓[6]烷硫基,C↓[1]-C↓[6]烷基氨基,二-C↓[1]-C↓[6]烷基氨基,C↓[1]-C↓[6]烷基氨基羰基,二-C↓[1]…。(*该技术在2016年保护过期,可自由使用*)

Phenylacetic acid derivatives, process for their preparation, intermediates and pharmaceutical compositions containing them

Phenylacetic acid derivatives of formula I a * * * 1 substituents and the index meaning is as follows: X NOCH: 3, CHOCH: 3, CHCH: 3; Y O, NR; R = 1, R and C independently for hydrogen: 1 C: 4 alkyl; R = 2 is three cyano, nitro, trifluoromethyl, halogen, C: 1 C: 4 and C: 1 alkyl - C: 4 alkoxy; m is 0, 1 or 2, when m is 2 when group R = 2 may not be the same; R = 3 is hydrogen, cyano group, C: 1 C: 4 C: 1 alkyl, C: 4 halogenated alkyl, C: 3 C: 6 naphthenic radical; R = 4 \uff0c\uff32\u2191\uff3b\uff16\uff3d \u76f8\u4e92\u72ec\u7acb\u5730\u4e3a\u6c22\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff11\uff10\uff3d\u70f7\u57fa\uff0c\uff23\u2193\uff3b\uff13\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u73af\u70f7\u57fa\uff0c\uff23\u2193\uff3b\uff12\uff3d\uff0d\uff23\u2193\uff3b\uff11\uff10\uff3d\u94fe\u70ef\u57fa\uff0c\uff23\u2193\uff3b\uff12\uff3d\uff0d\uff23\u2193\uff3b\uff11\uff10\uff3d\u7094\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff11\uff10\uff3d\u70f7\u57fa\u7fb0\u57fa\uff0c\uff23\u2193\uff3b\uff12\uff3d\uff0d\uff23\u2193\uff3b\uff11\uff10\uff3d\u94fe\u70ef\u57fa\u7fb0\u57fa\uff0c\uff23\u2193\uff3b\uff13\uff3d\uff0d\uff23\u2193\uff3b\uff11\uff10\uff3d\u7094\u57fa\u7fb0\u57fa\u6216\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff11\uff10\uff3d\u70f7\u57fa\u78fa\u9170\u57fa\uff0c\u8fd9\u4e9b\u57fa\u56e2\u53ef\u80fd\u88ab\u90e8\u5206\u6216\u5b8c\u5168\u5364\u5316\uff0c\u6216\u8005\u8fde\u6709\uff11\uff0d\uff13\u4e2a\u4e0b\u5217\u57fa\u56e2\uff1a\u6c30\u57fa\uff0c\u785d\u57fa\uff0c\u7f9f\u57fa\uff0c\u5def\u57fa\uff0c\u6c28\u57fa\uff0c\u7fa7\u57fa\uff0c\u6c28\u57fa\u7fb0\u57fa\uff0c\u6c28\u57fa\u786b\u4ee3\u7fb0\u57fa\uff0c\u5364\u7d20\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u5364\u4ee3\u70f7\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa \u78fa\u9170\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\u6b21\u786b\u9178\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u6c27\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u5364\u4ee3\u70f7\u6c27\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u6c27\u7fb0\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u786b\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\u6c28\u57fa\uff0c\u4e8c\uff0d\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\u6c28\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\u6c28\u57fa\u7fb0\u57fa\uff0c\u4e8c\uff0d\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\u6c28\u57fa\u7fb0\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\u6c28\u57fa\u786b\u4ee3\u7fb0\u57fa\uff0c\u4e8c\uff0d\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\u6c28\u57fa\u786b\u4ee3\u7fb0\u57fa\uff0c\uff23\u2193\uff3b\uff12\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u94fe\u70ef\u57fa\uff0c\uff23\u2193\uff3b\uff12\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u94fe\u70ef\u6c27\u57fa\uff0c\uff23\u2193\uff3b\uff13\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u73af\u70f7\u57fa\uff0c\uff23\u2193\uff3b\uff13 \uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u73af\u70f7\u6c27\u57fa\uff0c\u6742\u73af\u57fa\uff0c\u6742\u73af\u6c27\u57fa\uff0c\u82c4\u57fa\uff0c\u82c4\u6c27\u57fa\uff0c\u82b3\u57fa\uff0c\u82b3\u6c27\u57fa\uff0c\u82b3\u786b\u57fa\uff0c\u6742\u82b3\u57fa\uff0c\u6742\u82b3\u6c27\u57fa\u548c\u6742\u82b3\u786b\u57fa\uff0c\u8fd9\u4e9b\u73af\u72b6\u57fa\u56e2\u672c\u8eab\u53c8\u53ef\u80fd\u88ab\u90e8\u5206\u6216\u5b8c\u5168\u5364\u5316\uff0c\u6216\u8005\u8fde\u6709\uff11\uff0d\uff13\u4e2a\u4e0b\u5217\u57fa\u56e2\uff1a\u6c30\u57fa\uff0c\u785d\u57fa\uff0c\u7f9f\u57fa\uff0c\u5def\u57fa\uff0c\u6c28\u57fa\uff0c\u7fa7\u57fa\uff0c\u6c28\u57fa\u7fb0\u57fa\uff0c\u6c28\u57fa\u786b\u4ee3\u7fb0\u57fa\uff0c\u5364\u7d20\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u5364\u4ee3\u70f7\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\u78fa\u9170\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u57fa\u6b21\u786b\u9178\u57fa\uff0c\uff23\u2193\uff3b\uff13\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u73af\u70f7\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u6c27\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u5364\u4ee3\u70f7\u6c27\u57fa\uff0c\uff23\u2193\uff3b\uff11\uff3d\uff0d\uff23\u2193\uff3b\uff16\uff3d\u70f7\u6c27\u7fb0\u57fa\uff0c\uff23\u2193 1 - C: 6 thioialkyl, C: 1 C: 6 C: two amino alkyl, 1 - C: 6 amino alkyl, C: 1 C: 6 alkyl amino carbonyl, two - C: 1....

【技术实现步骤摘要】
本专利技术涉及式I的苯乙酸衍生物 其中的取代基和指数含义如下X 是NOCH3,CHOCH3,CHCH3;Y 是O,NR;R1,R 相互独立地为氢和C1-C4烷基;R2是氰基,硝基,三氟甲基,卤素,C1-C4烷基和C1-C4烷氧基;m 是0,1或2,当m为2时,基团R2可能是不相同的;R3是氢,氰基,C1-C4烷基,C1-C4卤代烷基,C3-C6环烷基;R4,R6相互独立地为氢,C1-C10烷基,C3-C6环烷基,C2-C10链烯基,C2-C10炔基,C1-C10烷基羰基,C2-C10链烯基羰基,C3-C10炔基羰基或C1-C10烷基磺酰基,这些基团可能被部分或完全卤化,或者连有1-3个下列基团氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,卤素,C1-C6烷基,C1-C6卤代烷基,C1-C6烷基磺酰基,C1-C6烷基次硫酸基(sulfoxyl),C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷氧羰基,C1-C6烷硫基,C1-C6烷基氨基,二-C1-C6烷基氨基,C1-C6烷基氨基羰基,二-C1-C6烷基氨基羰基,C1-C6烷基氨基硫代羰基,二-C1-C6烷基氨基硫代羰基本文档来自技高网...

【技术保护点】

【技术特征摘要】
1.一种式I的苯乙酸衍生物其中取代基和指数含义如下X 是NOCH3,CHOCH3,CHCH3;Y 是O,NR;R1,R 相互独立地为氢和C1-C4烷基;R2是氰基,硝基,三氟甲基,卤素,C1-C4烷基和C1-C4烷氧基;m 是0,1或2,当m为2时,基团R2可能是不相同的;R3是氢,氰基,C1-C4烷基,C1-C4卤代烷基,C3-C6环烷基;R4,R6相互独立地为氢,C1-C10烷基,C3-C6环烷基,C2-C10链烯基,C2-C10炔基,C1-C10烷基羰基,C2-C10链烯基羰基,C3-C10炔基羰基或C1-C10烷基磺酰基,这些基团可能被部分或完全卤化,或者连有1-3个下列基团氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,卤素,C1-C6烷基,C1-C6卤代烷基,C1-C6烷基磺酰基,C1-C6烷基次硫酸基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷氧羰基,C1-C6烷硫基,C1-C6烷基氨基,二-C1-C6烷基氨基,C1-C6烷基氨基羰基,二-C1-C6烷基氨基羰基,C1-C6烷基氨基硫代羰基,二-C1-C6烷基氨基硫代羰基,C2-C6链烯基,C2-C6链烯氧基,C3-C6环烷基,C3-C6环烷氧基,杂环基,杂环氧基,苄基,苄氧基,芳基,芳氧基,芳硫基,杂芳基,杂芳氧基和杂芳硫基,这些环状基团本身又可能被部分或完全卤化,或者连有1-3个下列基团氰基,硝基,羟基,巯基,氨基,羰基,氨基羰基,氨基硫代羰基,卤素,C1-C6烷基,C1-C6卤代烷基,C1-C6烷基磺酰基,C1-C6烷基次硫酸基,C3-C6环烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷氧羰基,C1-C6烷硫基,C1-C6烷基氨基,二-C1-C6烷基氨基,C1-C6烷基氨基羰基,二-C1-C6烷基氨基羰基,C1-C6烷基氨基硫代羰基,二-C1-C6烷基氨基硫代羰基,C2-C6链烯基,C2-C6链烯氧基,苄基,苄氧基,芳基,芳氧基,芳硫基,杂芳基,杂芳氧基,杂芳硫基或C(=NOR7)-An-R8;芳基,芳基羰基,芳基磺酰基,杂芳基,杂芳基羰基或杂芳基磺酰基,这些基团可能被部分或完全卤化,或者连有1-3个下列基团氰基,硝基,羟基,巯基,氨基,羰基,氨基羰基,氨基硫代羰基,卤素,C1-C6烷基,C1-C6卤代烷基,C1-C6烷基羰基,C1-C6烷基磺酰基,C1-C6烷基次硫酸基,C3-C6环烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷氧羰基,C1-C6烷硫基,C1-C6烷基氨基,二-C1-C6烷基氨基,C1-C6烷基氨基羰基,二-C1-C6烷基氨基羰基,C1-C6烷基氨基硫代羰基,二-C1-C6烷基氨基硫代羰基,C2-C6链烯基,C2-C6链烯氧基,苄基,苄氧基,芳基,芳氧基,杂芳基,杂芳氧基或C(=NOR7)-An-R8;R5是氢,C1-C6烷基,C2-C6链烯基,C2-C6炔基,这些烃基可能被部分或完全卤化,或者连有1-3个下列基团氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,卤素,C1-C6烷基氨基羰基,二-C1-C6烷基氨基羰基,C1-C6烷基氨基硫代羰基,二-C1-C6烷基氨基硫代羰基,C1-C6烷基磺酰基,C1-C6烷基次硫酸基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷氧羰基,C1-C6烷硫基,C1-C6烷基氨基,二-C1-C6烷基氨基,C2-C6链烯氧基,C3-C6环烷基,C3-C6环烷氧基,杂环...

【专利技术属性】
技术研发人员:T·格罗特H·巴耶R·穆勒H·萨特尔R·克里斯特恩V·哈里斯G·洛恩茨E·阿墨尔曼S·斯特拉斯曼
申请(专利权)人:巴斯福股份公司
类型:发明
国别省市:

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