Process for the stereospecific synthesis of indole derivatives
    5.
    发明授权
    Process for the stereospecific synthesis of indole derivatives 失效
    吲哚衍生物的立体有择合成方法

    公开(公告)号:US4806655A

    公开(公告)日:1989-02-21

    申请号:US67273

    申请日:1987-06-29

    CPC分类号: C07D413/06 C07D209/16

    摘要: The present invention relates to a process for the stereo-specific synthesis of indole derivatives of formula: ##STR1## which consists in using 3-tosyloxy-1,2-O-isopropylidenepropane-1,2-diol (II) in an optically pure form in order to introduce the asymetric carbon C* of compound (I). Compound (II) is condensed with a suitable primary amine in order to prepare an oxazolidinone and condensation with a suitable phenol, and the oxazolidinone ring is then opened to form an indole compound (I).

    摘要翻译: 本发明涉及立体特异性合成下式的吲哚衍生物的方法:其中包括使用3-甲苯磺酰氧基-1,2-邻 - 异丙基丙烷-1,2-二醇( II)以光学纯的形式引入化合物(I)的不对称碳C *。 化合物(II)与合适的伯胺缩合以制备恶唑烷酮并与合适的苯酚缩合,然后将恶唑烷酮环打开以形成吲哚化合物(I)。