Microbial hydroxylation of 16α,17α-dimethyl-17β-(l-oxopropyl)androsta-l,4-dien-3-one to rimexolone by Curvularia lunata AS 3.4381

A novel synthetic route to rimexolone, a corticosteroid for treatment of ocular inflammation without significant elevation of intraocular pressure, was described. An investigation has been undertaken of the microbial transformation of 16α,17α-dimethyl-17β-(l-oxopropyl)androsta-l,4-dien-3-one by microorganisms known to hydroxylate conventional steroids, using Curvularia lunata AS 3.4381 gave rimexolone, the product of 11β-hydroxylation, respectively. The target compound was characterized with reference substance rimexolone by TLC, HPLC, elemental analysis, MS, IR, and NMR.