Acetonitrile → N-(4-((2-amino-3-chloropyridin-4-yl)oxy)-2,5-difluorophenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide

Participants

Reaction Conditions

Reaction Steps

To a suspension of 3-chloro-4-(4-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamido)-2,5-difluorophenoxy)picolinamide (310 mg, 0.60 mmol) in EtOAc (6.0 mL), CH3CN (6.0 mL) and H2O (3.0 mL) at 0° C. was added iodobenzene diacetate (234 mg, 0.72 mmol). After stirring at 0° C. for 30 minutes, the mixture was allowed warm up to rt and stirred for 4 hours. The mixture was concentrated in vacuo and the residue was purified by a silica gel column chromatography (MeOH/DCM (v/v)=1/70) to give the title compound as a pale yellow solid (200 mg, 69%).

Provenance & Evidence