NOVEL PROCESS FOR PREPARING 17.BETA.-SUBSTITUTED 4-AZAANDROSTANE DERIVATIVES

摘要

The invention relates to a novel process for preparing 17.beta.-substituted 4-azaandrostane derivatives of general formula (I) wherein R represents hydrogen or a C1-3alkyl group; R1 represents a carboxamido group mono- or disubstituted by C1-8alkyl group(s); or a free carboxyl group; or a carboxyl group esterified with a C1-5 alcohol; and the ~ bond line represents a single or double bond; as well as their salts. The process comprises reacting a 17-halogeno-4-azaandrostene derivative of general formula (II) wherein R and the ~ bond line are as defined above, and X is chlorine, bromine or iodine, with a primary or secondary alkylamine or a C1-5 alcohol, in dimethylformamide or dimethylsulfoxide medium in the presence of a palladium(II) salt and phosphines or a palladium(II) complex and a tertiary amine base in carbon monoxide atmosphere at a temperature between 35.degree.C and 80.degree.C, then, if desired, transforming an obtained compound of general formula (I) to another compound of general formula (I) by hydrogenation, hydrolysis or salt forming reaction.