9-二甲胺甲基-10-羟基喜树碱的合成

The Synthesis of 9-[(DimethylAmino)Methyl-10-Hydroxy Camptothecin

喜树碱是由植物衍生的抗癌药物，本文以它为母核，利用价廉易得的反应物料和简单可行的反应条件，对分子结构中的A环进行化学修饰，合成了新的拓扑异构酶Ⅰ抑制剂-9-二甲胺甲基-10-羟基喜树碱（SK＆F104864-A），其抗癌活性高于喜树碱和10-羟基喜树碱。

Camptothecin deriving from plant is an antitumor drug. As a new topoisomerase Ⅰ inhibitor,SK&F104864-A was synthesized by A-ring modification of Camptothecin in available material and simple reaction condition. It demonstrated higher antitumor activity than camptothech and 10-hydroxy-camptothecin.