9-烯丙基-10-羟基喜树碱的合成

The Synthesis of 9-allyl-10-hydroxy Camptothecin

以10-羟基喜树碱为原料,经醚化反应先合成10-烯丙氧基喜树碱,再经克莱森重排反应得到9-烯丙基-10-羟基喜树碱的初产品。通过对醚化反应时间和温度进行研究,得到了较佳的反应条件,初产品总收率为39.8%,并经过LC/MS,1HNMR进行结构确证,产品纯度达到95%以上,为9-烯丙基-10-羟基喜树碱的合成提供了简便高效的合成方法。

Preparation of 9-allyl-10-hydroxy camptothecin by 10-hydroxy camptothecin （HCPT） through etherification and Claeson rearrangement reaction was studied in this paper. The conditions of etherification reaction such as temperature, time were examined. The optical conditions were experimentally selected and the total yield of 9-allyl-10-hydroxy camptothecin is 39.8% with 95% purity. An effective method with mild conditions, is provided for the synthesis of arrays of 9-allyl-10-hydroxy camptothecin.