Process for the preparation of fluorosteroids
    8.
    发明授权
    Process for the preparation of fluorosteroids 有权
    制备荧光素的方法

    公开(公告)号:US06794503B2

    公开(公告)日:2004-09-21

    申请号:US09858692

    申请日:2001-05-16

    IPC分类号: C07J7100

    CPC分类号: C07J71/0015

    摘要: Described herein is a process for the preparation of 6&agr;-fluorosteroids of formula (I), in which R is chosen from H, OH and an alkyl group with from 1 to 4 carbon atoms and R′ is a carboxyalkyl group with from 1 to 4 carbon atoms in the alkyl chain, comprising the selective fluorination at the 6&agr;-position by treatment of the compound of formula (III), wherein R and R′ are as defined above, with an electrophilic fluorinating agent.

    摘要翻译: 本文描述了制备式(I)的6α-荧光素的方法,其中R选自H,OH和具有1至4个碳原子的烷基,R'是具有1-4个碳原子的羧基烷基 包括通过用亲电氟化剂处理其中R和R'如上定义的式(III)化合物在6α-位置的选择性氟化。

    Process for the preparation of 17-acyl esters of 17.alpha.,
21-dihydroxysteroids of the pregnane series and novel products
    10.
    发明授权
    Process for the preparation of 17-acyl esters of 17.alpha., 21-dihydroxysteroids of the pregnane series and novel products 失效
    制备17 {60,孕烷系列和新产物{0-21-二羟基类固醇的17-酰基酯的方法

    公开(公告)号:US3998701A

    公开(公告)日:1976-12-21

    申请号:US529134

    申请日:1974-12-03

    摘要: A process is disclosed for making 17-monoesters of 17 .alpha., 21-dihydroxy steroids by acylating a 17 .alpha., 21-dihydroxy steroid phosphate and then subjecting the intermediate 17-acyloxy-21-phosphate to dephosphorylation using an acid phosphatase to achieve enzymatic hydrolysis. Several new 17-monoesters having an anti-inflammatory property are also disclosed.

    摘要翻译: 公开了通过酰化17α,21-二羟基类固醇磷酸酯然后使用酸性磷酸酶对中间体17-酰氧基-21-磷酸进行脱磷酸化来制备17α,21-二羟基类固醇的17-单酯以达到酶水解的方法 。 还公开了几种具有抗炎性质的新型17-单酯。