发明名称 Process of preparation of flumethasone 21-acetate, or flumethasone and its 17-carboxyl androsten analogue
摘要 A process for the preparation of high purity flumethasone in high yield involves C3 protecting 9,11beta-epoxy-17alpha,21-dihydroxy-16alpha-methylpregna-1,4-diene-3,20-dione,21-acetate, fluorinating at 6alpha, removing the C3 protecting group, fluorinating the 9,11-epoxy group. The resulting flumethasone 21-acetate is treated with the methanolic potassium hydroxide in the presence of an oxidation agent, causing a simultaneous hydrolyzation and degradative oxidation, resulting in the formation of 6alpha,9alpha-difluoro-11beta,17alpha-dihydroxy-16alpha-methyl-17beta-carboxy-androsta-1,4-diene-3-one in high yield. Flumethasone 21-acetate is alternatively hydrolyzed to yield flumethasone free alcohol.
申请公布号 US6528666(B1) 申请公布日期 2003.03.04
申请号 US20020162862 申请日期 2002.06.06
申请人 HORIONE LIMITED 发明人 VILLAX IVAN;MENDES ZITA
分类号 C07J3/00;C07J5/00;C07J71/00;C07J75/00;(IPC1-7):C07C50/22;C07D303/06 主分类号 C07J3/00
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