Process for the preparation of 20-oxo, 17-alpha, 21 dihydroxy steroid derivatives and new intermediates thereof

摘要

Prepn. of 20-oxo,17 alpha ,21-dihydroxy steroid derivs. of formula (I) comprises (a) treating a steroid deriv. of formula (II) with a cyclic cpd. (IX); (b) treating with ArSHalo (X) in the presence of a base; (c) rearranging in the presence of a base; (d) epimerising; equilibrating with (VII); (e) cleaving the sulphur gp. using a thiophile to give (VIII); then (f) acid hydrolysis to give (I). R1 = H or 1-4C alkyl; R2 = 1-4C alkyl; rings A-D contg. one or more double bonds and are opt. substd. by OH or (opt. protected) ketone gps., halo, 1-4C alkyl, 1-4C alkoxy and/or 2-4C alkenyl and/or alkynyl; Ar = Ph opt. substd. by halo. Intermediates are new, excluding methyloestrone.