Invention Grant
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
- Patent Title: Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides
- Patent Title (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
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Application No.: US13528894Application Date: 2012-06-21
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Publication No.: US08354536B2Publication Date: 2013-01-15
- Inventor: Thomas Cleary , Yaohui Ji , Thimma Rawalpally
- Applicant: Thomas Cleary , Yaohui Ji , Thimma Rawalpally
- Applicant Address: US NJ Nutley
- Assignee: Hoffman-La Roche Inc.
- Current Assignee: Hoffman-La Roche Inc.
- Current Assignee Address: US NJ Nutley
- Agent George W. Johnston; Patricia S. Rocha-Tramaloni; Kimberly J. Prior
- Main IPC: C07D453/02
- IPC: C07D453/02 ; C07D241/38

Abstract:
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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