富马酸奈拉西坦的合成

Synthesis of Nebracetam Fumarate

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 %.