Method of manufacturing stereoisomers of buprenorphine and analogues thereof

    公开(公告)号:US10035807B2

    公开(公告)日:2018-07-31

    申请号:US15557311

    申请日:2016-03-11

    申请人: SIEGFRIED AG

    IPC分类号: C07D489/12

    摘要: The present invention relates to a method of preparing a compound of Formula II-a′ or Formula II-b′, wherein RI represents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms;RII represents a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; RIII represents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms or a linear, branched and/or cyclic alkoxy group having 1 to 10 carbon atoms; RIV represents hydrogen or a linear, branched and/or cyclic alkyl group having 1 to 10 carbon atoms or an optionally substituted aryl or alkylaryl group having 6 to 40 carbon atom or acetyl or silyl or a protective group; and RV represents hydrogen or a methyl group; wherein RI and RII are different from each other.

    MORPHINAN DERIVATIVES AND PREPARATION METHODS THEREOF
    8.
    发明申请
    MORPHINAN DERIVATIVES AND PREPARATION METHODS THEREOF 失效
    莫宁衍生物及其制备方法

    公开(公告)号:US20110112297A1

    公开(公告)日:2011-05-12

    申请号:US13000200

    申请日:2009-06-19

    IPC分类号: C07D489/08 C07F7/18

    CPC分类号: C07D489/08 C07D489/09

    摘要: The present invention relates to morphinan derivatives and preparation methods thereof, especially to ketal hydroxyl protected compounds of morphinan derivatives and preparation method thereof, and to a method for preparing corresponding alkylated morphinan derivatives by using the ketal hydroxyl protected compounds as intermediates, and more especially to a ketal hydroxyl protected compound of methylnaltrexone as intermediate for preparing methylnaltrexone and a method for preparing methylnaltrexone through said intermediate.

    摘要翻译: 本发明涉及吗啡喃衍生物及其制备方法,尤其涉及缩酮羟基保护的吗啡喃衍生物化合物及其制备方法,以及通过使用缩酮羟基保护的化合物作为中间体制备相应的烷基化吗啡喃衍生物的方法,更具体地涉及 作为制备甲基纳曲酮的中间体的甲基纳曲酮的缩酮羟基保护的化合物和通过所述中间体制备甲基纳曲酮的方法。