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
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United States of America Patent
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Issued Date -
Jul 14, 2011
app pub date -
Jan 4, 2011
filing date -
Jan 12, 2010
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Abandoned
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Abstract
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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