METHODS FOR THE PREPARATION OF INDAZOLE-3-CARBOXYLIC ACID AND N-(S)-1-AZABICYCLO[2.2.2]OCT-3-YL-1H-INDAZOLE-3-CARBOXAMIDE HYDROCHLORIDE SALT
    11.
    发明申请
    METHODS FOR THE PREPARATION OF INDAZOLE-3-CARBOXYLIC ACID AND N-(S)-1-AZABICYCLO[2.2.2]OCT-3-YL-1H-INDAZOLE-3-CARBOXAMIDE HYDROCHLORIDE SALT 审中-公开
    用于制备吲哚-3-羧酸和N-(S)-1-氮杂双环[2.2.2] OCT-3-YL-1H-吲唑-3-羧酰胺盐酸盐的方法

    公开(公告)号:US20110172428A1

    公开(公告)日:2011-07-14

    申请号:US12983906

    申请日:2011-01-04

    IPC分类号: C07D453/02 C07D231/56

    摘要: The present invention provides novel methods for preparing indazole-3-carboxylic acid 2, a key starting material for the manufacture of agonists or partial agonists of the nicotinic α-7 receptor, such as N—(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 13. Nicotinic α-7 receptor agonists and partial agonists are being useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing indazole-3-carboxylic acid on scaled-up levels.

    摘要翻译: 本发明提供了制备吲唑-3-羧酸2的新方法,该吲唑-3-羧酸是用于制备烟碱型α-7受体的激动剂或部分激动剂的关键起始物质,例如N-(S)-1-氮杂双环[2.2。 2]辛-3-基-1H-吲唑-3-甲酰胺盐酸盐13.烟碱型α-7受体激动剂和部分激动剂可用于治疗与缺陷或功能异常的烟碱乙酰胆碱受体(特别是脑部)相关的疾病状况 ,例如用于治疗阿尔茨海默病和精神分裂症,以及其他精神和神经障碍。 本方法可用于按比例放大水平制备吲唑-3-羧酸。