发明名称 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)-lH-3- indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5- trifluoromethoxy-lH-indazole-S-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic a-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.
申请公布号 CA2740311(A1) 申请公布日期 2010.04.22
申请号 CA20092740311 申请日期 2009.10.06
申请人 F. HOFFMANN-LA ROCHE AG 发明人 CLEARY, THOMAS P.;JI, YAOHUI;RAWALPALLY, THIMMA
分类号 C07D231/56;C07D453/02 主分类号 C07D231/56
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