盐酸帕洛诺司琼的合成

Synthesis of Palonosetron Hydrochloride

合成新型5-HT3受体阻滞剂。以(S)-1,2,3,4-四氢-1-萘甲酸为起始原料,经酰化、缩合、还原、环合、成盐等反应合成盐酸帕洛诺司琼,总收率达36.2%。该法工艺操作简便,反应条件温和,适合工业化生产。

Palonosetron hydrochloride,a novel 5-HT3 receptor antagonist was prepared from （S）-1,2,3,4-tetrahydro-1-Naphthalenecarboxylic acid via a series of steps including chlorination,condensation,reduction,cyclization and saponification. The overall yield was 36.2%. The process has simple operation and mild reactive conditions, it＇s suitable for industrial production.