Process for the stereoselective synthesis of 5 - aza - ariloxi 5alfa androstan - 3 - onas, 16 16 Alpha and beta and replaced insustituidas, and intermediariosobtenidos in this process.

摘要

Process for the stereoselective synthesis of 5 - aza - ariloxi 5alfa androstan onas and 16betas 16alfa - 3 - substituted and insustituidas obtenidosen and intermediaries that process.Process for the formation of a metilsulfonato and Displacement nucleofilodel same proceeds without Secondary reaction with lafuncionalidad eno - lactam.In particular, a process for producing a compound with Structural formula (a), in which the dotted line is a enlacesimple or Double Bond; r1 is H or CH3 CH3 and H; r2es or ar is phenylInsustituido naphthyl or alkylated mono - or, or a ring heteroaromu00e1tico 5 or 6 which contains at least one member selected from the group consisting of Oxygen Atom in a ring,A Sulfur Atom delanillo, 1 - 4 denitrogeno Atoms or combinations thereof; where the heteroaromu00e1tico can also be merged with a benzo Ring or heteroaromu00e1tico,Produced by treating a compound of Structural formula (b) with RA - Oh and aprotico Cesium carbonate in a Polar Solvent selected from DMSO, DMF, nitromethane, Dioxane,THF and acetonitrile, where ar is as defined above.Compound having the Structural formula (b), where the line Points to a double Bond or a enlacesimple; r1 is H or CH3, R2 is H or CH3.Compound having the Structural formula (12), where the line of Staples is a Single Bond or a double Bond; r1 is H or CH3; R2 is H or CH3.