1-alkyl-3-aminoindazoles
    10.
    发明授权
    1-alkyl-3-aminoindazoles 有权
    1-烷基-3-氨基吲唑

    公开(公告)号:US07799930B2

    公开(公告)日:2010-09-21

    申请号:US12368869

    申请日:2009-02-10

    IPC分类号: C07D231/56

    CPC分类号: C07D231/56

    摘要: Methods of making 1-alkylindazoles are described. The methods involve reacting a 2-alkylaminobenzonitrile with a nitrosating agent followed by reduction-cyclization of the resulting nitrosamine to form a 1-alkyl-3-aminoindazole. The 1-alkyl-3-aminoindazole can be deaminated to form a 1-alkylindazole which ultimately can be used to form desired indazoles which are preferably pharmaceutically active products. The process of the present invention further permits the formation of enantiomerically enriched or pure indazoles such as aminoalkyl indazoles.

    摘要翻译: 描述制备1-烷基吲唑的方法。 所述方法包括使2-烷基氨基苄腈与亚硝化剂反应,然后还原环化所得亚硝胺以形成1-烷基-3-氨基吲唑。 1-烷基-3-氨基吲唑可以脱氨基以形成1-烷基吲唑,其最终可以用于形成优选药物活性产物的所需吲唑。 本发明的方法还允许形成对映体富集或纯的吲唑如氨基烷基吲唑。