计划生育药物的合成——Ⅱ.苯甲孕酮及其衍生物的合成

SYNTHETIC STUDIES OF CONTRACETIVE DRUGS Ⅱ. THE SYNTHESIS OF 16α, 17α-DIHYDROXYPROGESTERONE ACETOPHENIDE

摘要: 本文报告以薯芋皂素降解物双烯醇酮乙酸酯(Ⅳ)为原料,通过高锰酸钾氧化、与苯乙酮缩合、水解和沃氏氧化等反应,合成了目的物(Ⅰ)。并且还合成了△⁶-苯甲孕酮(Ⅷ)和△^3,5-苯甲孕酮(X)等衍生物。

Abstract: The synthesis of 16α, 17α-dihydroxyprogesterone acetophenide (1) is reported. Starting from pregna-5,16-dien-3-ol-20-on, 3-acetate(Ⅳ), via potassium permanganate oxidation, condensation with acetophenone in presence of acid, followed by alkaline hydrolysis and Oppenauer oxdation, the object compound (1) was obtained. The △⁶-(Ⅵ) and △^3,5-3-deoxy-(Ⅹ) derivative were also synthesized.