反应详情

温度

90 °C

N-(5-Iodopyridin-2-yl)-2-(4-(2-methylpyridin-4-yl)phenyl)acetamide 65-2 (20 mg, 0.046 mmol), 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (13.5 mg, 0.07 mmol) and Pd(PPh3)4 (5 mg, 0.004 mmol) was mixed in toluene (3 mL)/ethanol (1 mL)/Na2CO3 (2M, 1 mL). The reaction mixture was stirred at 90° C. for 10 hours. The solvent was removed by rotary evaporation and the residue was dissolved in DMSO. The inorganic salt was removed by filtration. The crude product in DMSO was purified by reverse phase HPLC to give N-(5-(1H-pyrazol-4-yl)pyridin-2-yl)-2-(4-(2-methylpyridin-4-yl)phenyl)acetamide 65 as off-white solid. MS m/z 370.2 (M+1).

1. customThe solvent was removed by rotary evaporation
2. dissolutionthe residue was dissolved in DMSO
3. customThe inorganic salt was removed by filtration
4. customThe crude product in DMSO was purified by reverse phase HPLC