发明申请
US20120259120A1 DIAZONIUM-FREE METHOD TO MAKE AN INDAZOLE INTERMEDIATE IN THE SYNTHESIS OF BICYCLIC 5-(TRIFLUORMETHOXY)-1H-3-INDAZOLECARBOXYLIC ACID AMIDES
有权
在双酚-5-（三氟甲基）-1H-3-异吲哚酸酰胺的合成中制备吲哚中间体的无氮方法
- 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）： 在双酚-5-（三氟甲基）-1H-3-异吲哚酸酰胺的合成中制备吲哚中间体的无氮方法
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申请号： US13528894申请日： 2012-06-21
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公开(公告)号： US20120259120A1公开(公告)日： 2012-10-11
- 发明人: Thomas Cleary , Yaohui Ji , Thimma Rawalpally
- 申请人： Thomas Cleary , Yaohui Ji , Thimma Rawalpally
- 主分类号： C07D231/56
- IPC分类号： C07D231/56 ; C07D453/02
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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