摘要
目的改善5a-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。
Aim To improve the synthesis of epristeride, a potent human 5a-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.
出处
《中国药物化学杂志》
CAS
CSCD
2003年第5期276-279,共4页
Chinese Journal of Medicinal Chemistry
基金
Project of National Scientific Foundation of China(96-902-01-01)
