反应详情

温度

130 °C

The mixture of N-(5-amino-2-cyclopropyl-4-fluorophenyl)acetamide (54.2 mg, 0.26 mmol), 5-chloro-7-(oxetan-3-ylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile (50.0 mg, 0.20 mmol), cesium carbonate (196 mg, 0.60 mmol), Pd2(dba)3 (18.34 mg, 0.02 mmol) and di-tert-butyl(2',4',6'-triisopropylbiphenyl-2-yl)phosphine (17.01 mg, 0.04 mmol) sealed with microwave vial was degassed and refilled with argon 3 times. Then the degassed dioxane (4 mL) was added. The resulting solution was heated at 130°C for 30 mins in microwave. After removed all the solvents, the crude residue was purified by chromatography (100% EtOAc to 3% MeOH in EtOAc). N-(5-(3-cyano-7-(oxetan-3-ylamino)pyrazolo[1,5-a]pyrimidin-5-ylamino)-2-cyclopropyl-4-fluorophenyl)acetamide (10.00 mg, 11.85 %) was obtained.