盐酸帕洛诺司琼的合成  

Synthesis of Palonosetron Hydrochloride

作　　者：姜大炜[1] 王磊[2] 黄乐群[2] 

机构地区：[1]江苏第二师范学院生命科学与化学学院,江苏南京210013 [2]南京大学医学院,江苏南京211102

出　　处：《江苏教育学院学报（自然科学版）》2013年第5期19-22,92,共4页Journal of Jiangsu Institute of Education(Social Science)

摘　　要：通过文献查询,结合试验条件,确定了一条合成盐酸帕洛司琼的可行路线:以1-萘甲酸为起始原料,经多步反应制备出产品——盐酸帕洛诺司琼.对每一步反应的产物用1HNMR进行了表征,确定了目标产物的结构与文献一致,最终产物的光学纯度经HPLC测定,达到99.5%.对其部分工艺条件进行了适当的改进,优化了部分反应条件,产品结晶的回收率较高,达80%以上.本合成工艺原料易得,生产成本低,操作简单,反应条件温和,适合工业化生产.产品质量符合原料药要求,为工业化生产提供了可能的技术途径.By referring to the related literature and applying comparative analysis,a feasible method to synthesize palonosetron hydrochloride is put forward in this article. Palonosetron hydrochloride is formed from 1-naphthoic acid after poly-step reactions and the products of each step are characterized by 1HNMR. The result shows that the optical purity reaches 99. 5% determined by HPLC. After improving some technological conditions and optimizing part of reaction conditions,their recovery rate of crystallization arrives at more than 80%. The synthetic process,due to its low cost,simple operation,mild reactive conditions and qualified product quality,can be applied to industrial production.

关 键 词：盐酸帕洛诺司琼 合成 氢化 

分 类 号：O626.3[理学—有机化学]