1α-羟基去氢表雄酮的合成

Synthesis of 1α-Hydroxydehydroepiandrosterone

本文以1,4-雄烯二酮为起始原料,经羰基保护、溴代、异构化、羰基还原、环氧化、开环及脱保护7步反应以28.3%的总收率合成1α-羟基去氢表雄酮。该方法具有高效经济、技术可行、安全环保等优点,为1α-羟基去氢表雄酮的规模生产及维生素D类药物合成研究奠定理论基础。

1α-hydroxydehydroepiandrosterone was prepared from androsta-1,4-diene-3,17-dione through seven steps such as protection of carbonyl group, bromination, deconjugation, reduction, epoxidation, ring-opening and deprotection, with an overall yield of 28.3%. The method has the advantages of high efficiency and economy, technical feasibility, safety and environmentally benign, and lays a foundation for industrialized production of 1α- hydroxydehydroepiandrosterone and research of vitamin D drugs.