摘要
本文报道了合成甲地孕酮的简便方法,即以17α-乙酰氧基-黄体酮(3)为原料,将其烯醇醚(4)经Mannich反应,或将△^(3,5)-3,17α-二乙酰氧基-黄体酮(2)与二乙氧基甲烷反应,生成6-次甲基-17α-乙酰氧基-黄体酮(5),然后将5用钯/碳酸钙作催化剂转位得目的物甲地孕酮(6b),总收率分别为56%和50%(均以17α-羟基-黄体酮(1)为起始物)。
A Simple synthetic route for megestrol acetate (6b) is reported.The keyintermediate C_6-methylene steroid (5) may be obtained either from enol ether (4) of 17a-acetoxy-progesterone (3) by Mannich reaction,or from △^(3,5)-3.17a-diacetoxy-progesterone(2) by treatment with C_2H_5OCH_2OC_2H_5.Then 5 is isomerized with Pd/CaCO_3 in the pre-sence of cyclohexene and sodium acetate to obtain 6b.The overall yield of route 17a-hy-droxy-progesterone 1→2→3→4→5→6b is 56% and of route 1→2→5→6b is 50%.
出处
《有机化学》
SCIE
CAS
1983年第6期451-453,共3页
Chinese Journal of Organic Chemistry
关键词
甲地孕酮
合成
孕激素
避孕药
megestrol acetate
synthesis
progestin
contraceptive.
