(1-苯乙基哌啶-4-基)苯胺的制备  

Preparation of(1-Phenethylpiperidin-4-yl)aniline

作　　者：谌志华 曾海峰[2] 梁姗姗[2] 聂海艳[2] 虞心红[2] 

机构地区：[1]上海奥奇医药科技有限公司,上海200032 [2]华东理工大学药学院上海市新药设计重点实验室,上海200237

出　　处：《中国医药工业杂志》2013年第5期438-439,共2页Chinese Journal of Pharmaceuticals

基　　金：国家自然科学基金资助项目(NSFC-20972051);上海市科委科技支撑项目(12431900900;12431900902;11DZ2260600)

摘　　要：（1-苯乙基哌啶-4-基）苯胺（1）是合成阿片类镇痛药芬太尼（fentanyl）的重要中间体。（1-Phenethylpiperidin-4-yl）aniline was prepared from 13-phenylethanamine and methyl acrylate by Michael addition, Dieckmann condensation and hydrolysis in acid condition to give N-phenylethyl-4-piperidone, which was subjected to reductive amination with aniline and hydrogen catalysed by Raney Ni in an overall yield of 77.7 %.

关 键 词：苯胺 哌啶 制备 中间体 芬太尼 镇痛药 

分 类 号：O626.322[理学—有机化学]