反应详情

温度

80 °C

A mixture of DME (3.0 mL) and 1 M aqueous Na2CO3 (0.88 mL) was degassed by bubbling in Argon for 10 minutes. The mixture was transferred via syringe to a vial containing 6-((6-bromo-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)quinoline (100 mg, 0.29 mmol), 2-fluorophenylboronic acid (45 mg, 0.32 mmol) and Pd(dppf)2Cl2.CH2Cl2 (6.2 mg, 0.01 mmol). The vial was capped and heated to 80° C. for 3.5 hours. The crude reaction mixture was diluted with dichloromethane then washed with water. The dichloromethane was dried over Na2SO4, filtered and concentrated by rotary evaporation. The residue was purified by column chromatography using gradient elution with ethyl acetate and dichloromethane to afford 6-((6-(2-fluorophenyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)quinoline (77 mg, 74%).

1. customwas degassed
2. customby bubbling in Argon for 10 minutes
3. customThe mixture was transferred via syringe
4. customThe vial was capped
5. customThe crude reaction mixture
6. washthen washed with water
7. dry with materialThe dichloromethane was dried over Na2SO4
8. filtrationfiltered
9. concentrationconcentrated by rotary evaporation
10. customThe residue was purified by column chromatography
11. washelution with ethyl acetate and dichloromethane