5α-还原酶抑制剂爱普列特的合成研究

摘要

Aim To improve the synthesis of epristeride,a potent human 5α-reductase inhibitor.Methods This synthesis starts from prognenolone,which is converted into epristeride in six synthetic steps in 45% overall yield by treatment of the key bromo diene intermediate.Results The synthesis has been employed to produce kilograms supplies of epristeride in high purity.Conclusions The synthesis is suitable for production on a large scale.%目的改善5α-还原酶抑制剂爱普列特的合成方法.方法通过引入一种溴化物关键性中间体,以3β-羟基-5-烯-孕甾-20-酮为原料,经6步反应合成了爱普列特,总产率为45%.结果 通过本路线已合成高纯度公斤级产品.结论 该法可应用于工业规模生产.