富马酸奈拉西坦的合成  

Synthesis of Nebracetam Fumarate

作　　者：蒋勇[1] 黄国生[1] 

机构地区：[1]兰州大学应用有机国家重点实验室,甘肃兰州730000

出　　处：《中国医药工业杂志》2008年第6期404-406,共3页Chinese Journal of Pharmaceuticals

摘　　要：衣康酸二甲酯和苄胺经Michael加成、分子内环合得到1-苄基-5-氧代吡咯烷-3-羧酸甲酯,再经硼氢化钠还原、氯化、叠氮化、常压Pd/C催化氢化后成盐制得富马酸奈拉西坦,总收率约48%。Nebracetam fumarate was synthesized form itaconic acid dimethyl ester and benzylamine via Michael addition and intramolecular cyclization to give 1-benzyl-5-oxopyrrolidine-3-carboxylic acid methyl ester, which was subjected to reduction, chlorination, azidation, hydrogenation and salt formation with an over all yield of about 48 %.

关 键 词：富马酸奈拉西坦 益智药 合成 

分 类 号：R971.91[医药卫生—药品]