发明申请
US20110172428A1 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
- 专利标题: 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
- 专利标题(中): 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
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申请号: US12983906申请日: 2011-01-04
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公开(公告)号: US20110172428A1公开(公告)日: 2011-07-14
- 发明人: Shan-Ming Kuang , Pingsheng Zhang
- 申请人: Shan-Ming Kuang , Pingsheng Zhang
- 主分类号: C07D453/02
- 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.
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