Regioselective N-2 arylation of indazoles

    公开(公告)号:US10815214B2

    公开(公告)日:2020-10-27

    申请号:US16576133

    申请日:2019-09-19

    IPC分类号: C07D401/10

    摘要: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.

    REGIOSELECTIVE N-2 ARYLATION OF INDAZOLES
    2.
    发明申请

    公开(公告)号:US20200010449A1

    公开(公告)日:2020-01-09

    申请号:US16576133

    申请日:2019-09-19

    IPC分类号: C07D401/10

    摘要: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.