盐酸托烷司琼合成工艺改进  

Improvment in the synthesis of tropisetron hydrochloride

作　　者：吴锋[1,2,3] 朱敏 杨俊[1,2,3] 陈敏 余小娟 张静 向红琳[4] 陈锋 

机构地区：[1]新乡医学院药学院,河南新乡453003 [2]湖南康普医药研究院,长沙410008 [3]康普药业股份有限公司,长沙410008 [4]湖南师范大学医学院,长沙410013

出　　处：《中南药学》2011年第1期8-11,共4页Central South Pharmacy

摘　　要：目的改进盐酸托烷司琼的合成工艺。方法本文以吲哚-3-甲酸为起始原料,酰氯化后与托品醇钠发生缩合反应,再与盐酸成盐,纯化制得高纯度盐酸托烷司琼。结果该合成工艺避免了采用易燃易爆的正丁基锂,增加了安全性,节约了成本,且提高了收率(>53%)。结论该方法在整个制备过程中,不用分离中间体,操作简便,该方法适合工业化生产。Objective To improve the synthesis of tropisetron hydrochlorride. Methods Tropisetron hydrochloride was synthesized from indol-3-carboxylic acid by chloride acetylation and condensed with tropic alcohol sodium, followed by salt formation with hydrochlororic acid. Results This synthetic process avoided using the inflammable and explosive n-butyllithium and therefore ensured security and cost reduction and improved yield. Conclusion The process without separating the intermediates is simple and suitable for industry production.

关 键 词：盐酸托烷司琼 合成工艺 改进 

分 类 号：R914[医药卫生—药物化学] R927[医药卫生—药学]