阿奇沙坦酯的合成工艺研究  

Study on the synthetic technology of Azilsartan medoxomil

作　　者：贾景雨[1] 马帅[1] 杜伟宏[1] 赵俊[1] 李少华[1] 曹胜华[1] 

机构地区：[1]中国医药集团总公司四川抗菌素工业研究所,四川成都60052

出　　处：《化学研究与应用》2014年第3期413-417,共5页Chemical Research and Application

摘　　要：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%.

关 键 词：阿奇沙坦酯 降压药 合成 

分 类 号：R914.5[医药卫生—药物化学]