Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides
US8232412B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Oct 9, 2009 |
| Grant date | Jul 31, 2012 |
| Priority date | — |
| Expiry date | Dec 31, 2030 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D231/56
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.