反应详情

温度

120 °C

A mixture of 4-(4-pyridinyl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinoline (250 mg, 0.75 mmol), 5-bromopyridine-3-sulfonamide (213 mg, 0.9 mmol), tetrakistriphenylphosphine palladium (0) (95 mg, 0.08 mmol), and saturated aqueous NaHCO3 (2.5 mL), and dioxane (5 mL)) was heated at 120° C. for 1 h and cooled to room temperature. The reaction mixture was filtered through Celite and the solvent was removed under reduced pressure. The crude product was purified by Gilson reverse phase HPLC (8-25% 6 min gradient 0.1% TFA in H2O/CH3CN) followed by neutralization with saturated aqueous NaHCO3 and extracted into EtOAc. Evaporation provided the title compound as an off white solid. (85 mg, 31%). ESMS [M+H]+=363.1

1. temperaturecooled to room temperature
2. filtrationThe reaction mixture was filtered through Celite
3. customthe solvent was removed under reduced pressure
4. customThe crude product was purified by Gilson reverse phase HPLC (8-25% 6 min gradient 0.1% TFA in H2O/CH3CN)
5. extractionextracted into EtOAc
6. customEvaporation