螺内酯的合成  

Synthesis of Spironolactone

作　　者：王红霞[1] 叶景泉[1] 姜中兴[1] 

机构地区：[1]武汉大学化学与分子科学学院,湖北武汉430072

出　　处：《中国医药工业杂志》2005年第1期1-3,共3页Chinese Journal of Pharmaceuticals

摘　　要：雄烯二酮和原甲酸三乙酯反应后用碘化三甲基锍环氧化得到17β,20β-环氧-3-乙氧基-17α-孕甾-3,5-二烯,然后经与丙二酸二甲酯成内酯环、NBS溴化后脱溴化氢,与硫代乙酸加成制得利尿药螺内酯,总收率57%。Spironolactone was synthesized from 4-androstene-3,17-dione by condensation with HC(OEt)3, and subsequent epoxidation by Me3SI to give 17β,20β-epoxy-3-ethoxy-17α-pregnane-3,5-dien, which subjected to cyclization with dimethyl malonate, bromination, dehydrobromination and then addition with thioacetic acid with an overall yield of 57%.

关 键 词：螺内酯 利尿药 合成 

分 类 号：R986.1[医药卫生—药品]