阿奇沙坦酯的合成工艺研究

Study on the synthetic technology of Azilsartan medoxomil

本文以3-硝基邻苯二甲酸-1-甲酯为起始原料,经羧基转为氨基、还原、环合、N-烷基化、缩合、闭环、水解、酯化共8步反应制得了降压药阿奇沙坦酯。所得目标化合物经元素分析、质谱、氢核磁共振确认,总收率达30%。

Azilsartan medoxomil was synthesized from methyl 3-nitrophthanoate by changing carboxylic group into amino group,re-duction,cyclization, N-alkylation with 2′-cyano-4-（ bromomethyl ） biphenyl, condensation, cyclization, hydrolysis, esterification in turn. The target compound was identified by elemental analysis,MS and 1 H-NMR,and the overall yield was 30%.