5β-雄甾-3-烯-17-酮的合成研究  

Synthesis of 5β-androst-3-en-17-one

作　　者：叶鹏[1] 杨波[2] 郭晓红[2] 刘秀娟[2] 柯贤炳[2] 

机构地区：[1]武汉大学人民医院药学部,武汉430060 [2]武汉生物工程学院,武汉430415

出　　处：《中南药学》2016年第9期957-959,共3页Central South Pharmacy

基　　金：武汉市高新技术产业科技创新团队计划项目(No.2015071704021617);国家自然科学基金资助项目(No.21102109)

摘　　要：目的研究重要甾类药物中间体5β-雄甾-3-烯-17-酮的合成。方法以去氢表雄酮为原料,经Oppenauer氧化、Clemmensen还原反应得到5β-雄甾-3-烯-17-酮,重点研究了还原反应中金属、酸、溶剂等反应条件对反应速率及反应产物中5β-构型比例的影响。结果成功获得5β-雄甾-3-烯-17-酮,总产率为72.1%。结论该工艺简单,反应快,产率高,环境友好。Objective To synthesize 5β-androstan-3-en-17-one as an important intermediate for steroidal drugs. Methods 5β-androstan-3-en-17-one was synthesized from dehydroepiandrosterone via Oppenauer oxidation and Clemmensen reduction. The effects of the metal, acid, and the solvent on the reduction product were de- termined. Results 5β-androstan-3-en-17-one was obtained with an overall yield of 72.1%. Conclusion The method is quick and convenient and environment friendly with high yield.

关 键 词：去氢表雄酮 5β-雄甾-3-烯-17-酮 Oppenauer氧化 Clemmensen还原 合成 

分 类 号：R914[医药卫生—药物化学]