New metabolites from fungal biotransformation of an oral contraceptive agent: Methyloestrenolone

► Methyloestrenolone (1) is an oral contraceptive. ► First report of the fungal biotransformation of methyloestrenolone (1). ► Fermentation of 1 with fungus produced eleven metabolites 2-12. ► Six metabolites (2-5, 11 and 12) were found to be new. ► An efficient method to synthesize libraries of new oral contraceptive.