WO2010043515 diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides

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Scaffold: indazole

Biological target:

Nicotinic alpha-7 receptor 

Activity:

Agonist

Steps Conditions Reactions
a Amderlite FPC22H resine / HC(OEt)3 / EtOH Ketone protection 
b tBuOK / NMP Hydrazine synthesis
c

1. 1N NaOH / H2O / THF

2. 2M AcOH / H2O / THF / ACN


d HBTU / DMAP / DIEA / DMF Amide synthesis (HBTU coupling)