盐酸帕洛诺司琼中间体的合成

Synthesis of the Chemical Intermediate of Palonosetron Hydrochloride

研究了双(三氯甲基)碳酸酯替代传统氯代试剂合成盐酸帕洛诺司琼中间体的新工艺路线。以1-萘甲酸为起始原料,经还原,氯化,酰胺化,手性拆分,得到盐酸帕洛诺司琼中间体,该工艺具有生产安全,环境友好,操作简单等优点,反应总收率为26.8%。

The bis（trichloromethyl）carbonate replaced the traditional chlorination reagent to synthesize of the chemical intermediate of palonosetron hydrochloride. The chemical intermediate of palonosetron hydrochloride was synthesized from α-naphthoic acid via reduction, chlorination, amidation and chiral resolution. The advantages of this procedure are simple, safe and environmentally friendly. The total yield was 26.8%。