反应详情

温度

150 °C

A solution of 4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenylboronic acid (226 mg, 0.83 mmol), methyl 1-(3,5-difluoro-4-(trifluoromethylsulfonyloxy)phenyl)cyclopropanecarboxylate (Intermediate 28-2; 300 mg, 0.83 mmol), lithium chloride (70.6 mg, 1.67 mmol) and tripotassium phosphate (265 mg, 1.25 mmol) in butyronitrile (2 mL) was degassed for 10 minutes then put under vacuum and refilled with nitrogen before addition of (1,1′-bis(diphenylphosphino)ferrocene)-dichloropalladium(II) (DCM adduct) (137 mg, 0.17 mmol). The reaction mixture was heated in the microwave at 150° C. for 1 hours. The crude product was purified by flash silica chromatography, elution gradient 0 to 90% EtOAc in isohexane. Pure fractions were evaporated to dryness to afford methyl 1-(4′-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)-2,6-difluorobiphenyl-4-yl)cyclopropanecarboxylate (160 mg, 43.9%)

1. customThe crude product was purified by flash silica chromatography, elution gradient 0 to 90% EtOAc in isohexane
2. customPure fractions were evaporated to dryness