盐酸倍他司汀及其关键中间体的合成综述  

Synthesis of betahistine hydrochloride and its key intermediates

作　　者：俞伟 颜国明 尹超 刘威 梁超茗 孙茂林 叶金星 YU Wei;YAN Guoming;YIN Chao;LIU Wei;LIANG Chaoming;SUN Maolin;YE Jinxing(Shanghai Zhongxi Sunve Pharmaceutical Co.,Ltd.,Shanghai 201419,China;Engineering Research Center of Pharmaceutical Process Chemistry,Ministry of Education,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China)

机构地区：[1]上海中西三维药业有限公司,上海201419 [2]华东理工大学药学院制药工程与过程化学教育部工程研究中心,上海200237

出　　处：《上海医药》2020年第9期75-79,共5页Shanghai Medical & Pharmaceutical Journal

摘　　要：盐酸倍他司汀是一种组胺H1受体激动剂,临床上用作血管扩张药,是目前在临床上治疗美尼尔氏综合症最常用的药物之一。本文综述了盐酸倍他司汀和其关键中间体2-羟乙基吡啶以及2-乙烯基吡啶的合成路线,根据原料和中间体不同,报道了5种盐酸倍他司汀的合成方法,根据原料和反应条件不同,总结了7种2-羟乙基吡啶的合成方案和8种2-乙烯基吡啶的合成方案。虽然技术和合成方案在不断优化,但目标产物盐酸倍他司汀的合成和产业化仍有很大发展空间。Betahistine hydrochloride is a histamine H1 receptor agonist that is clinically used as a vasodilator and is one of the most commonly used drugs for the treatment of Meniere’s syndrome.The synthesis routes of betahistine hydrochloride and its key intermediates,2-hydroxyethylpyridine and 2-vinylpyridine,were reviewed.Five synthetic methods of betahistine hydrochloride were reported so far depending on different raw materials and intermediates.The synthesis schemes of 7 kinds of 2-hydroxyethylpyridine and 8 kinds of 2-vinylpyridine were summarized based on the differences of starting materials and reaction conditions.Although the technical and synthetic schemes are continuously being optimized,there is still much room for the development and industrialization of the synthesis of the target product,betahistine hydrochloride.

关 键 词：盐酸倍他司汀 组胺H1受体激动剂 2-羟乙基吡啶 2-乙烯基吡啶 

分 类 号：O626.321[理学—有机化学] R972.4[理学—化学]