抗肿瘤新药伊立替康的合成研究

Improving Synthetic Method of Irinotecan

本文报道了抗肿瘤新药伊立替康的合成工艺。以喜树碱为原料合成了关键中间体 7 乙基 1 0 羟基喜树碱 (5 ) ,再以苄胺为原料经 7步反应合成哌啶基哌啶甲酰氯 (7) ,最后将两部分连接 ,制得伊立替康 ,总收率为 2 1 7%

In this paper,an improving preparation of irinotec an was reported.The key intermediate 7-ethyl-10-hydroxy-camptothecin(5) was sy nthesized from camptothecin as the starting material,then connected with chloroc arbonyl 4-piperidinopiperidine(7) to give Irinotecan.The total yield was about 21%.