Process for the preparation of 1,5-naphthyridine-3-carboxyamides by direct ester amidation
    1.
    发明申请
    Process for the preparation of 1,5-naphthyridine-3-carboxyamides by direct ester amidation 审中-公开
    通过直接酯酰胺化制备1,5-萘啶-3-羧酰胺的方法

    公开(公告)号:US20050038065A1

    公开(公告)日:2005-02-17

    申请号:US10856161

    申请日:2004-05-28

    CPC分类号: C07D471/04

    摘要: A new route for the preparation of substituted 1,5-naphthyridine-3-carboxyamides, useful in the diagnosis and treatment of anxiety, Downs Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness, is provided. These compounds may be readily prepared by heating the corresponding 1,5-naphthyridine-3-carboxylic acid ester with a primary amine in a polar solvent such as dimethylformamide or dimethylsulfoxide.

    摘要翻译: 提供了一种制备用于诊断和治疗焦虑症,唐氏综合症,睡眠,认知和发作障碍以及用苯二氮卓类药物过量并提高警觉性的取代的1,5-二氮杂萘-3-羧酰胺的新途径 。 这些化合物可以通过在极性溶剂如二甲基甲酰胺或二甲基亚砜中用伯胺加热相应的1,5-二氮杂萘-3-羧酸酯来容易地制备。