Process for the preparation of abiraterone and abiraterone acetate

摘要

Process for the preparation of 3beta - hidroxiandrost - 5:16 - dien - 17 - il - trifluorometanosulfonato or 3beta - acetoxiandrost - 516 - dien - 17 - il - trifluorometanosulfonato (ii) comprising the reaction of DHEA or DHEA acetate (iii) with bis (trifluorometanosulfonimida) of General formula (TF) AR, n 2 and a baseThe ar is an optionally substituted Aromatic radical, according to the scheme of reaction (see formula): * * * * followed by the reaction of transformation of 3beta - hidroxiandrost - 516 - dien - 17 - il - trifluorometanosulfonato or 3beta - acetoxiandrost - 5:16 - dien - 17 - il - trifluorometanosulfonato (ii), respectively, Abiraterone acetate Abiraterone or (i)By reacting the mixture resulting from the reaction with Diethyl (pyridyl) borane in the presence of a catalyst of PALLADIUM (ii) According to the following Pattern: * * * * (see formula) in which XIs Hydrogen or an acyl radical CH3 - CO, characterized in that the base is selected from Lithium diisopropylamide, Tri SEC butiroborohidruro trisec - butiroborohidruro Lithium, potassiumTert butu00f3xico sodium and potassium tert butoxide.