莫吉司坦的合成  

Synthesis of Moguisteine

作　　者：赵蕊[1] 李玲[2] 丁一[2] 罗振福[2] 孙有光[1] 

机构地区：[1]天津理工大学化学化工学院,天津300191 [2]天津药物研究院化学制药部,天津300193

出　　处：《中国医药工业杂志》2011年第1期7-9,共3页Chinese Journal of Pharmaceuticals

摘　　要：愈创木酚与2-溴代乙醛缩二甲醇发生亲核取代,再与半胱胺盐酸盐缩合闭环得到2-[(2-甲氧基苯氧基)甲基]噻唑烷,最后与氯甲酰乙酸乙酯反应得到外周非麻醉性镇咳药莫吉司坦,总收率约71%。Moguisteine, a novel peripheral non-narcotic antitussive drug, was synthesized from guaiacol by nucleophilic substitution with 2-bromoacetaldehyde dimethyl acetal and cyclization with cysteamine hydrochloride to give 2- [ （2-methoxyphenoxy） methyl] thiazolidine, which was subjected to N-acylation with ethyl chloroformyl acetate. The overall yield was about 71% with purity of 99%.

关 键 词：莫吉司坦 外周非麻醉性镇咳药 合成 

分 类 号：R974.2[医药卫生—药品]