发明授权
US08354536B2 Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides 有权
在双环5-(三氟甲氧基)-1H-3-吲哚羧酸酰胺的合成中制备吲唑中间体的无重氮方法

  • 专利标题: Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides
  • 专利标题(中): 在双环5-(三氟甲氧基)-1H-3-吲哚羧酸酰胺的合成中制备吲唑中间体的无重氮方法
  • 申请号: US13528894
    申请日: 2012-06-21
  • 公开(公告)号: US08354536B2
    公开(公告)日: 2013-01-15
  • 发明人: Thomas ClearyYaohui JiThimma Rawalpally
  • 申请人: Thomas ClearyYaohui JiThimma Rawalpally
  • 申请人地址: US NJ Nutley
  • 专利权人: Hoffman-La Roche Inc.
  • 当前专利权人: Hoffman-La Roche Inc.
  • 当前专利权人地址: US NJ Nutley
  • 代理商 George W. Johnston; Patricia S. Rocha-Tramaloni; Kimberly J. Prior
  • 主分类号: C07D453/02
  • IPC分类号: C07D453/02 C07D241/38
Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides
摘要:
The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic α-7 receptor and are being studied for their use 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 compound (3) on scale up levels.
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