Patent ID: 6828120
Filing Date: 2004-12-07
Classification: C07J,C12P

Abstract:
A process for the preparation of 11&bgr;,17&agr;,21-trihydroxy-6&agr;-methylpregna-1,4-diene-3,20-dione 21-acetate (VI) which comprises:(1) contacting 17&agr;-hydroxy-6&agr;-methylpregn-4-ene-3,20-dione 17-acetate (I) with a &Dgr;1-dehydrogenase to produce 17&agr;-hydroxy-6&agr;-methylpregna-1,4-diene-3,20-dione 17 acetate (II); (2) contacting 17&agr;-hydroxy-6&agr;-methylpregna-1,4-diene-3,20-dione 17 acetate (II) with a 11&bgr;-hydroxylase to produce 11&bgr;,17&agr;-dihydroxy-6&agr;-methylpregna-1,4-diene-3,20-dione 17-acetate (III); (3) hydrolyzing the 11&bgr;,17&agr;-dihydroxy-6&agr;-methylpregna-1,4-diene-3,20-dione 17-acetate (III) to produce11&bgr;,17&agr;-dihydroxy-6&agr;-methylpregna-1,4-diene-3,20-dione (IV); (4) contacting 11&bgr;,17&agr;-dihydroxy-6&agr;-methylpregna-1,4-diene-3,20-dione (IV) with iodine, a catalyst, a mild base to produce 11&bgr;,17&agr;-dihydroxy-21-diiodo-6&agr;-methylpregna-1,4-diene-3,20-dione (V) and (5) contacting 11&bgr;,17&agr;-dihydroxy-21-diiodo-6&agr;-methylpregna-1,4-diene-3,20-dione (V) with a salt of acetic acid.