法莫替丁合成工艺改进
Improved Synthesis Process of Famotidine
王亮1
作者信息
- 1. 上海市汇伦医药股份有限公司,上海 201100
- 折叠
摘要
采用脒基硫脲和1,3-二氯丙酮环合反应制得2-(4-(氯甲基)噻唑-2-基)胍基盐酸盐,再与硫脲反应制得(S)-((2-胍基-4-噻唑基)甲基)异硫脲二盐酸盐,最后与N-硫酰胺基-3-氯丙脒盐酸盐反应生成法莫替丁.采用一锅法制备关键中间体2-(4-(氯甲基)噻唑-2-基)胍基盐酸盐,单步反应收率达到95％以上,合成法莫替丁的总收率达到60％,大大降低了法莫替丁的生产成本.
Abstract
(S)-(2-Guanidino-4-thiazolyl)methylisothiourea dihydrochloride was synthesized by reacting 1,3-dichloro-acetone with amidinothiourea in the acetone and reacting 2-(4-(chloromethyl)thiazol-2-yl)guanidine hydrochloride with thiourea.Finally,it reacts with N-thiamide-3-chlorpropamidine hydrochloride to form famotidine.In this process,the key intermediate 2-(4-(chloromethyl)thiazol-2-yl)guanidine hydrochloride is prepared by one-pot method.The yield of this reaction can reach more than 95％,and the total yield of synthetic famotidine can reach 60％,which great-ly reduces the production cost of Famotidine.
关键词
脒基硫脲/(S)-((2-胍基-4-噻唑基)甲基)异硫脲二盐酸盐/一锅法合成Key words
amidine thiourea/2-(4-(chloromethyl)thiazol-2-yl)guanidine hydrochloride/onepot synthesis引用本文复制引用
出版年
2024
NETL
NSTL
万方数据