| 摘要 |
PURPOSE: A process for the preparation of 17-esters of 9 α,21-dihalo-pregnane-11β,17α-diol-20-ones is provided which is especially suitable for the preparation of anti-inflammatory steroids, Mometasone Furoate which is useful for the treatment of inflammatory diseases CONSTITUTION: 17-esters of 9α,21-dihalo-pregnane-11β,17α-diol-20-ones is prepared by the steps of: (1) reacting a 9β,11β-epoxy-pregnane-17α,21-diol-20-one with an axles of an organic sulfonyl halide, in the presence of a trialkylamine and an inert organic solvent to form the 21-sulfonate ester, and then adding to the reaction mixture an alcohol in an amount substantially equivalent to the excess of sulfonyl halide, to yield a 9β,11β-epoxy-21-halo-pregnane-17α-ol-20-one; (2) reacting the resulting 9β,11β -epoxy-21-halo-pregnane-17α-ol-20-one with an anhydride, chloride, or bromide of a carboxyl acid in the presence of a trialkylamine, to form the 17-ester of the 9β,11β -epoxy-21-halo-pregnane-17α-ol-20-one; and (3) reacting the resulting 9β,11β -epoxy-21-halo-pregnane-17α-ol-20-one 17-ester with aqueous hydrogen halide in the presence of an inert organic solvent to form the 17-ester of the 9 α,21-dihalo-pregnane-11β,17α-diol-20-ones.
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