158136-68-6Relevant articles and documents
NOVEL PROCESS FOR PREPARING 17 BETA-SUBSTITUTED 4-AZAANDROSTANE DERIVATIVES
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, (2008/06/13)
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; R 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 - &cir& _- &cir& _- &cir& _- &cir& _ 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 - &cir& _- &cir& _- &cir& _- &cir& _ 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 DEG C and 80 DEG 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.
17-halogeno-4-azaandrostene derivatives and process for the preparation thereof
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, (2008/06/13)
The invention relates to novel 4-azaandrostene intermediates of formula (I), STR1 wherein R is hydrogen or a C1-3 alkyl group; X is chlorine, bromine or iodine; and the ---- bond line is a single or double bond.