S-美托洛尔的不对称合成  

Asymmetric synthesis of S-metoprolol

作　　者：纪德华[1] 姚军[1] 贾永辉[1] 张显[1] 耿建宁[1] 

机构地区：[1]河北科技大学化学与制药工程学院,河北石家庄050018

出　　处：《现代化工》2008年第11期58-59,共2页Modern Chemical Industry

摘　　要：介绍了一种不对称合成选择性β-受体阻断剂S-美托洛尔的方法,以R-表氯醇为手性原料直接与对羟基苯乙醇反应,经过碘甲烷的烷基化,最后与异丙胺作用得S-美托洛尔,总收率79.6%,光学纯度达97%。The asymmetric synthesis of S-metoprolol, a selective β-blocker inhibitor with clinical extensive use, is presented in this paper. Firstly R- epichlorohydrin is used as chiral reagent to directly react with p- hydroxyphenylethanol, and after the alkylation by iodomethane and then reaction with isopropylamine, S-metoprolol can be synthesized in a total yield of 79.6% with an e.e. % higher than 97%.

关 键 词：S-美托洛尔 R-表氯醇 不对称合成 

分 类 号：TQ463[化学工程—制药化工]