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采用易得的原料、简单的化学方法和方便的操作,设计了新的合成路线,制备了拓扑替康药物报批中的三种相关杂质。分别由拓扑替康盐酸盐(1)经游离、酯水解开环反应制备得到了拓扑替康羧酸钠盐(2),由拓扑替康(11)经正丙醇取代反应制备得到9-丙氧甲基-10-羟基喜树碱(4),以及由10-羟基喜树碱(5)经羟甲基化反应制备得到9-羟甲基-10-羟基喜树碱(3)。
Using readily available raw materials, simple chemical methods and convenient operation, a new synthetic route was designed and three related impurities in the application of topotecan were prepared. The topotecan carboxylic acid sodium salt (2) was prepared from the topotecan hydrochloride (1) via free, ester hydrolysis and ring-opening reaction. The topotecan carboxylic acid sodium salt was prepared from topotecan (11) Hydroxycamptothecin (4), and 9-hydroxymethyl-10-hydroxycamptothecin (3) by hydroxymethylation from 10-hydroxycamptothecin (5).