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1. 发明授权

US4151169A Process for preparing substituted 1,2,4-triazole derivatives 失效
标题翻译：制备取代的1,2,4-三唑衍生物的方法
公开(公告)号：US4151169A
公开(公告)日：1979-04-24
申请号：US921911
申请日：1978-07-03
申请人： Amedeo O. Sale , Giorgio Pifferi , Pietro Consonni , Alberto Diena , Bonaccorso R. Del Turco
发明人： Amedeo O. Sale , Giorgio Pifferi , Pietro Consonni , Alberto Diena , Bonaccorso R. Del Turco
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： New 1-alkyl-3,5-disubstituted-1,2,4-triazole derivatives of following formula I ##STR1## wherein R may represent phenyl; phenyl substituted by a radical selected from (C.sub.1-4)alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec.-butyl, isobutyl or tert.-butyl, (C.sub.1-4)alkoxy, e.g. methoxy, ethoxy, propoxy, butoxy, isobutyloxy or tert.-butoxy, fluoro, chloro, bromo, nitro, amino, cyano, carbamoyl, carboxy, hydroxymethyl, methylenedioxy and trifluoromethyl; dichlorophenyl; dimethoxyphenyl; 3,4,5-trimethoxyphenyl;R.sub.1 may represent phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl as above defined, (C.sub.1-4)alkoxy as above defined, fluoro, chloro, bromo, hydroxymethyl, (C.sub.2-4)aliphatic acyloxymethyl, e.g. acetoxymethyl, propionyloxymethyl or butyryloxymethyl, carbamoyloxymethyl, bromomethyl and dimethylaminomethyl; dimethylphenyl; dimethoxyphenyl; phenyl contemporaneously substituted by o-hydroxymethyl and chloro;R.sub.2 represents a (C.sub.1-4)alkyl group as above defined; with the proviso that R and R.sub.1 cannot simultaneously represent phenyl;With the further proviso that, when R is phenyl, R.sub.1 cannot be p-chlorophenyl; and processes for their preparation.The compound of the invention have CNS depressant utility. They are especially useful as sedatives and hypnotics. Some of the compounds of the invention are also useful as anxiety relieving means.
摘要翻译：新的下式I的1-烷基-3,5-二取代-1,2,4-三唑衍生物其中R可以表示苯基; 被选自（C 1-4）烷基的基团取代的苯基，例如甲基，乙基，丙基，异丙基，丁基，仲丁基，异丁基或叔丁基，（C 1-4）烷氧基。甲氧基，乙氧基，丙氧基，丁氧基，异丁氧基或叔丁氧基，氟，氯，溴，硝基，氨基，氰基，氨基甲酰基，羧基，羟甲基，亚甲二氧基和三氟甲基; 二氯苯; 二甲氧基苯基; 3,4,5-三甲氧基苯基; R 1可以表示苯基，被选自上述定义的（C 1-4）烷基的基团取代的苯基，如上所定义的（C 1-4）烷氧基，氟，氯，溴，羟甲基，（C 2-4）脂族酰氧基甲基，乙酰氧基甲基，丙酰氧基甲基或丁酰氧基甲基，氨基甲酰氧基甲基，溴甲基和二甲基氨基甲基; 二甲基苯基; 二甲氧基苯基; 同时由邻羟甲基和氯取代的苯基; R2表示如上定义的（C 1-4）烷基; 条件是R和R1不能同时表示苯基; 另外，当R是苯基时，R 1不能是对氯苯基; 及其制备方法。

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