化学研究与应用
化學研究與應用
화학연구여응용
CHEMICAL RESEARCH AND APPLICATION
2014年
3期
413-417
,共5页
贾景雨%马帅%杜伟宏%赵俊%李少华%曹胜华
賈景雨%馬帥%杜偉宏%趙俊%李少華%曹勝華
가경우%마수%두위굉%조준%리소화%조성화
阿奇沙坦酯%降压药%合成
阿奇沙坦酯%降壓藥%閤成
아기사탄지%강압약%합성
Azilsartan medoxomil%hypotensor%synthesis
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%。
本文以3-硝基鄰苯二甲痠-1-甲酯為起始原料，經羧基轉為氨基、還原、環閤、N-烷基化、縮閤、閉環、水解、酯化共8步反應製得瞭降壓藥阿奇沙坦酯。所得目標化閤物經元素分析、質譜、氫覈磁共振確認，總收率達30%。
본문이3-초기린분이갑산-1-갑지위기시원료，경최기전위안기、환원、배합、N-완기화、축합、폐배、수해、지화공8보반응제득료강압약아기사탄지。소득목표화합물경원소분석、질보、경핵자공진학인，총수솔체30%。
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%.
