Ethanol → 2-(2-Chloro-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (4'-acetylamino-biphenyl-4-yl)-amide

Participants

Reaction Conditions

Reaction Steps

In a 4 ml vial was added 22.3 mg (0.125 mmol) of (4-acetylaminophenyl)boronic acid, 11 mg (0.025 mmol) of N-(4-bromophenyl)-1-(2-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide, 200 μL of a saturated CsCO3 solution of ethanol and 10 μg of DAPCy. The vial was sealed and heated to 60° C. overnight. The crude product was dissolved up in 200 μL of DMSO and injected directly on a reverse phase LCMS preparative instrument. The relevant fraction was collected dried to afford 2-(2-Chloro-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (4′-acetylamino-biphenyl-4-yl)-amide (4.3 mg, 0.0086 mmol: 34% yield as an off white solid. MS (ESI) m/z 499 [M+H]+.

Provenance & Evidence