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.
出处
《中南药学》
CAS
2011年第1期8-11,共4页
Central South Pharmacy
关键词
盐酸托烷司琼
合成工艺
改进
tropisetron hydrochlotide
synthesis
improvement
