Potassium Phosphate, Tribasic → HCID 86721251, compound

Participants

Reaction Steps

A solution of 2-(2-(5-bromo-1-tert-butyl-1H-pyrazol-4-yl)thiazol-4-yl)-N-((tetrahydro-2H-pyran-4-yl)methyl)acetamide (102 mg, 0.23 mmol), 4-cyanophenylboronic acid (50.9 mg, 0.35 mmol), tripotassium phosphate (98 mg, 0.46 mmol), S-Phos (7.59 mg, 0.02 mmol) and palladium(II) acetate (2.075 mg, 9.24 μmol) in toluene (1.5 ml) was stirred under an argon atmosphere at 90° C. for 20 hr. Water was added to the reaction solution, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine and dried, and the solvent was evaporated under reduced pressure. The residue was purified by NH-silica gel column chromatography (solvent gradient; 50% ethyl acetate/hexane→5% methanol/ethyl acetate) to give the title compound (60 mg, 0.129 mmol, 56.0%) as a white powder.

Provenance & Evidence