Patent ID: 7872135
Filing Date: 2011-01-18
Classification: C07J,Y02P

Abstract:
1. A process for preparing 17β-substituted 4-azaandrost-1-en-3-one compounds of the general formula (I): where R is hydroxyl, optionally substituted, linear or branched (C R R —NR characterized in that (A) protecting groups are introduced into the 3-keto-4-aza moiety (lactam moiety) of a compound of the general formula (II): so that a compound of the general formula (III) is formed: where R R Y is —[C(R R n is an integer of 1 to 4; and where, in the case that R is hydroxyl, it has optionally reacted with a protecting group; (B) the compound obtained [in step (A)] is reacted in the presence (i) of a dehydrogenation catalyst selected from the group comprising catalytically active Pd(0) compounds, the tris(dibenzylidineacetone)dipalladium-chloroform complex and Pd(II) compounds. said Pd(II) compounds being selected from the group consisting of PdCl phosphino)ethane], Pd(dppe)Cl (C) the protecting groups R