PROCESS FOR THE PREPARATION OF OXINDOLES AND ORTHO-SUBSTITUTED ANILINES AND THEIR USE AS INTERMEDIATES FOR SYNTHESES
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF OXINDOLES AND ORTHO-SUBSTITUTED ANILINES AND THEIR USE AS INTERMEDIATES FOR SYNTHESES 有权
    制备氧化物和取代的苯胺的方法及其作为合成中间体的使用

    公开(公告)号:US20130281711A1

    公开(公告)日:2013-10-24

    申请号:US13915898

    申请日:2013-06-12

    CPC classification number: C07D209/34 C07C323/58

    Abstract: The present invention relates to processes for the preparation of oxindoles and ortho-substituted anilines and their use as intermediates for syntheses. The invention further relates to a process for the preparation of compounds of formula (4): where a mixture of an aniline (compound of formula Q) is reacted with a thioether (compound of formula W): in the presence of a chlorinating agent and an organic solvent at a reaction temperature in the range above −65° C.In a subsequent process, this compound is further reacted in the presence of an acid catalyst to give the indole of formula (7) or the oxindole of formula (8):

    Abstract translation: 本发明涉及制备羟吲哚和邻位取代苯胺的方法及其作为合成中间体的用途。 本发明还涉及制备式(4)化合物的方法:其中苯胺(式Q化合物)的混合物与硫醚(式W化合物)反应:在氯化剂和 在随后的方法中,该化合物在酸催化剂的存在下进一步反应,得到式(7)的吲哚或式(8)的羟吲哚, :

    Process for the preparation of oxindoles and ortho-substituted anilines and their use as intermediates for syntheses
    3.
    发明授权
    Process for the preparation of oxindoles and ortho-substituted anilines and their use as intermediates for syntheses 有权
    制备羟吲哚和邻位取代苯胺的方法及其作为合成中间体的用途

    公开(公告)号:US09242934B2

    公开(公告)日:2016-01-26

    申请号:US13915898

    申请日:2013-06-12

    CPC classification number: C07D209/34 C07C323/58

    Abstract: The present invention relates to processes for the preparation of oxindoles and ortho-substituted anilines and their use as intermediates for syntheses. The invention further relates to a process for the preparation of compounds of formula (4): where a mixture of an aniline (compound of formula Q) is reacted with a thioether (compound of formula W): in the presence of a chlorinating agent and an organic solvent at a reaction temperature in the range above −65° C. In a subsequent process, this compound is further reacted in the presence of an acid catalyst to give the indole of formula (7) or the oxindole of formula (8):

    Abstract translation: 本发明涉及制备羟吲哚和邻位取代苯胺的方法及其作为合成中间体的用途。 本发明还涉及制备式(4)化合物的方法:其中苯胺(式Q化合物)的混合物与硫醚(式W化合物)反应:在氯化剂和 在随后的方法中,该化合物在酸催化剂的存在下进一步反应,得到式(7)的吲哚或式(8)的羟吲哚, :

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