5α-雄甾烷-3,17-二酮的合成新工艺

New Synthetic Process of 5α-Androstane-3,17-dione

5α-雄甾烷-3,17-二酮是一种甾体类药物的中间体。以雄烯二酮(4-雄甾烯-3,17-二酮)为原料,经氰化、缩酮、催化氢化、水解可制备得到目标化合物,目标化合物5α-雄甾烷-3,17-二酮的质量总收率为78%(以雄烯二酮计)。本制备方法条件温和,操作简单,易于实现工业化生产。

5α-androstane-3,17-dione was an intermediate of steroid hormone drugs.Using androstenedione(4-androstene-3,17-dione)as raw material,the target compound 5α-androstane-3,17-dione was obtained through followed steps:17-position stereoselective addition of cyanide,3-position ketalization and 17-position hydrolysis reaction,hydrogenation of 5,6 double bond and 3-position hydrolysis reaction.The total yield of 5α-androstane-3,17-dione was 78%(based on androstenedione).This method had some advantages such as mild reacting conditions,convenient operation,high yield and easy to be industrialized.