盐酸阿罗洛尔的合成  

Synthesis of Arotinolol Hydrochloride

作　　者：刘洪彬[1] 唐珲[1] 杨丹[1] 吉庆刚[1] 

机构地区：[1]西南大学化学化工学院,重庆400715

出　　处：《中国医药工业杂志》2011年第9期641-644,共4页Chinese Journal of Pharmaceuticals

基　　金：中央高校基本科研业务费专项接金资助项目(XDJK2009C092);重庆市自然科学基金资助项目(CSTC2009BB5296)

摘　　要：噻吩经5步反应获得5-乙酰噻吩-2-羧酸,然后与氯化亚砜、氨水反应得到5-乙酰噻吩-2-甲酰胺,再与溴素及二硫代氨基甲酸铵反应生成5-(2-巯基-4-噻唑基)-2-噻吩甲酰胺,后者与环氧氯丙烷缩合后经叔丁胺开环,最后与盐酸成盐得到盐酸阿罗洛尔,总收率约6%。5-Acetylthiophene-2-carboxylic acid obtained through five-step reactions from thiophene was reacted with thionyl chloride and ammonia to give 5-acetylthiophene-2-formamide, then the latter was reacted with bromine and ammonium dithiocarbamate to produce 5-（2-mercapto-4-thiazolyl）-2-thiophene formamide, which reacted successively with epichlorohydrin, tert-butylamine and concentrated hydrochrolic acid to gain arotinolol hydrochloride with an overall yield of about 6 %.

关 键 词：盐酸阿罗洛尔 β-肾上腺素受体拮抗剂 合成 

分 类 号：R971.9[医药卫生—药品]