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法莫替丁合成工艺改进

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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.
Improved Synthesis Process of Famotidine
(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.

amidine thiourea2-(4-(chloromethyl)thiazol-2-yl)guanidine hydrochlorideonepot synthesis

王亮

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上海市汇伦医药股份有限公司,上海 201100

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

2024

10.3969/j.issn.1008-553X.2024.01.025

安徽化工
安徽省化工研究院

安徽化工

影响因子：0.229
ISSN：1008-553X
年,卷(期)：2024.50(1)
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