盐酸托烷司琼的合成改进

The Synthesis and Improvement of Tropisetron Hydrochloride

以吲哚 3-甲酸为起始原料 ,经酰氯化、与托品醇缩合等反应合成了盐酸托烷司琼。研究结果表明 ,酰氯化选用二氯亚砜 ,在 0℃下进行缩合并以二氯甲烷为溶剂时 ,产物的收率由传统方法的2 0 %上升到 5 0 % ,且工艺操作简单、安全 ,产物容易提纯 ,适于工业化生产。

Tropisetron hydrochloride was synthesized from indol-3-carboxylic acid by chloride acetylation and condensation with Tropic alcohol in an overall yield of 50% (the yield of literature was only 20%). Oxalyl chloride is replaced by thionyl chloride in chloride acetylation. The process was simple, the reaction conditions were mild, and the product was easily purified and suitable for scale-up production.