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%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2005年第1期1-3,共3页
Chinese Journal of Pharmaceuticals
关键词
螺内酯
利尿药
合成
spironolactone
hydragog
synthesis
