Abrégé

The invention provides a process for preparing eplerenone, which comprises the following steps: (1) in the presence of a side reaction inhibitor, 17α-hydroxyl-3-oxo-γ-lactone-pregn-4,9(11)-diene-7α,21-dicarboxylic acid methyl ester IV is selectively expoxidized on double bond in trichloroacetonitrile, oxidant and phosphate buffer system in solution, to prepare crude eplerenone; (2) the crude eplerenone is recrystallized to yield pure eplerenone. High pure eplerenone can be obtained by the method of the present invention, the purity of eplerenone can reach 99.5% and the yield is as high as 87%. The method of the present invention is suitable for production on an industrial scale.

Classes IPC  ?

• C07J 21/00 - Stéroïdes normaux contenant du carbone, de l'hydrogène, un halogène, ou de l'oxygène ayant un hétérocycle contenant de l'oxygène condensé en spiro avec le squelette du cyclopenta[a]hydrophénanthrène

Abrégé

The invention provides a preparation method of magnesium tert-butylate with high purity, which is produced by the ester exchange reaction of magnesium lower alkoxide and tert-butanol ester under the condition of rectification or distillation. The magnesium tert-butylate of the invention has the purity of 92%-98%. The method of the present invention is simple, high yield, and easy to industrial production.

Classes IPC  ?

• C07C 29/68 - Préparation d'alcoolates métalliques
• C07C 31/30 - Alcoolates alcalins ou alcalino-terreux

Abrégé

A method for preparing S-fluoromethyl-6&agr;, 9&agr;-difluoro-11&bgr;-hydroxy-16&agr;-methyl-17&agr;-propionyloxy-3-oxoandrosta-1, 4-diene-17&bgr;-carbothioate (fluticasone propionate) was disclosed. The present method could be conduct simply and conveniently in mild conditions with high product purity, and be suitable for commercial process on a large scale.

Classes IPC  ?

• C07C 327/24 - Esters d'acides monothiocarboxyliques ayant des atomes de carbone de groupes thiocarboxyle estérifiés liés à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons
• C07C 327/02 - Acides monothiocarboxyliques
• C07J 31/00 - Stéroïdes normaux contenant un ou plusieurs atomes de soufre n'appartenant pas à un hétérocycle