Trimethyl siloxane steroid intermediates
    5.
    发明授权
    Trimethyl siloxane steroid intermediates 失效
    三甲基硅氧烷类固醇中间体

    公开(公告)号:US4036831A

    公开(公告)日:1977-07-19

    申请号:US626059

    申请日:1975-10-28

    摘要: A procedure for converting steroids characterized by presence of an 11.beta.OH group into potent corticoids having one or more substituents, such as 6.alpha.F, 16.alpha., 17.alpha.-hydroxy or isopropylidene dioxy, 16.alpha. or 16.beta. methyl, .DELTA..sup.1,4 ; by reacting the 11.beta.-hydroxy steroid with trichloromethyl siloxane steroid, thereby rendering the normally sensitive 11 substituent inert to the series of reactions which thereafter incorporate one or more of the desired above listed substituents into the steroid molecule. The siloxy group is then hydrolyzed to regenerate the 11.beta.-hydroxy substituent.Many of the trimethyl siloxy steroids are novel compounds.The siloxane may be selectively cleaved by reaction of the finely divided steroid with 40-60% aqueous HF.

    摘要翻译: 将以11β-OH基团存在为特征的类固醇的方法转化为具有一个或多个取代基的有效皮质激素,例如6αF,16α,17α-羟基或异亚丙基二氧基,16α或16β甲基,DELTA 1, 4; 通过使11β-羟基类固醇与三氯甲基硅氧烷类固醇反应,从而使通常灵敏的11个取代基对一系列反应是惰性的,其后将一个或多个所需的上述取代基并入类固醇分子。 然后将甲硅烷氧基水解以再生11β-羟基取代基。