首页> 外国专利> Method for preparing 17amp;agr;-acetoxy-11amp;bgr;-(4-N, N- dimethylaminophyl)-19-Norpregna-4,9-diene-3, 20-dione, intermediates useful in the method, and methods for the preparation of such intermediates

Method for preparing 17amp;agr;-acetoxy-11amp;bgr;-(4-N, N- dimethylaminophyl)-19-Norpregna-4,9-diene-3, 20-dione, intermediates useful in the method, and methods for the preparation of such intermediates

机译:制备17α-乙酰氧基-11b-(4-N,N-二甲基氨基)-19-去甲孕烯-4,9-二烯-3,20-二酮的方法,在该方法中有用的中间体以及制备该方法的方法中间体

摘要

Methods for the preparation of the 19-norprogesterone of formula I ##STR1## and its intermediates, in crystalline and amorphous forms are disclosed. The process is performed by (1) protecting the hydroxyl group of a compound of formula II ##STR2## (2) reacting the protected compound with an alkali or alkaline earth metal anion radical, (3) hydrolyzing the resulting compound, (4) ketalizing the carbonyl groups, (5) epoxidizing the compound, (6) opening the epoxide ring and introducing an N,N, dimethylamino-phenyl functional group into the axial position of C.sub.11, (7) deketalizing and dehydrating the resulting compound, and (8) acetylating to provide 17&agr;-acetoxy-11&bgr;-(4-N,N- dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione (I).
机译:公开了以结晶和无定形形式制备式I的19-去孕酮及其中间体的方法。该方法是通过以下步骤进行的:(1)保护式II化合物的羟基(2)使受保护的化合物与碱金属或碱土金属阴离子自由基反应,(3)水解所得化合物,(4 )缩酮化羰基,(5)环氧化该化合物,(6)打开环氧化物环并将N,N,二甲基氨基-苯基官能团引入C.sub.11的轴向位置,(7)使缩酮脱水和脱水得到的化合物,和(8)乙酰化,得到17α-乙酰氧基-11b-(4-N,N-二甲基氨基苯基)-19-去甲戊烯-4,9-二烯-3,20-二酮(I)。

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