氨甲酰基苯肼盐酸盐的合成工艺研究  

Study on Synthetic Process of 4-hydrazinylbenzamide Hydrochloride

作　　者：周光华[1] 葛文[1] 罗明洪[1] 夏克坚[1] 

机构地区：[1]南昌师范学院化学系,江西南昌330032

出　　处：《广州化工》2017年第12期78-79,共2页GuangZhou Chemical Industry

基　　金：南昌师范学院博士基金项目(NSBSJJ2014023);南昌师范学院重点建设学科-应用化学(NSXK20141003)项目

摘　　要：取代苯肼盐酸盐是合成曲坦类药物(如氟伐曲坦、那拉曲坦、舒马曲坦以及阿莫曲坦等)的一类非常重要的中间体。本文中,我们对氟伐曲坦的一个重要中间体氨甲酰基苯肼盐酸盐的合成工艺进行了报道。以对硝基苯甲酰胺为原料,利用钴镁复合氧化物催化剂,在温和条件下催化氢转移还原制备得到芳胺,再经重氮化、保险粉还原得相应的肼盐,整个合成工艺产率高、纯度高、且环境友好,符合工业化生产。Derivatives of phenylhydrazine hydrochloride play an important role in synthesis of drug molecular such as frovatriptan, naratriptan, sumatriptan, almotriptan, and so on. The study on synthetic process of the key intermediate of frovatriptan phenylhydrazine hydrochloride was reported. With 4- nitrobenzamide as the starting material, reduced by catalyzed Co0-MgO under mild condition to afford the 4-aminobenzamide, after diazotization and sequentially reduced with sodium hydrosulfite, the key intermediate of frovatriptan phenylhydrazine hydrochloride was obtained in high purity, which was suitable for industrial production.

关 键 词：氟伐曲坦 苯肼盐酸盐 合成工艺 

分 类 号：O625.6[理学—有机化学]