反应详情

温度

80 °C

A mixture of 7-chloro-imidazo[1,2-a]pyridine (15.0 g, 98.6 mmol), 4-fluorophenylboronic acid (16.55 g, 118.3 mmol), potassium carbonate (81.5 g, 590 mmol) in toluene-methanol-ethanol-water (1:1:1:1, 800 mL) was degassed with N2 and then bis(tri-tert-butylphosphine)palladium(0) (400 mg) added. The mixture was degassed and then heated to 80° C. for 18 h. The mixture was cooled to ambient, transferred to a separating funnel and the layers separated. The organic portion was reduced under reduced pressure and the residue extracted with dichloromethane. The dichloromethane extracts were washed with water, dried (MgSO4), filtered and concentrated under reduced pressure to afford 17.3 g (83%) of the title compound. 1H NMR (400 MHz, CDCl3) δ 8.22 (1H, d), 7.87 (1H, s), 7.71 (1H, s), 7.69-7.58 (3H, m), 7.20 (2H, t), 7.11 (1H, d).

1. customwas degassed with N2
2. additionbis(tri-tert-butylphosphine)palladium(0) (400 mg) added
3. customThe mixture was degassed
4. temperatureThe mixture was cooled
5. customtransferred to a separating funnel
6. customthe layers separated
7. extractionthe residue extracted with dichloromethane
8. washThe dichloromethane extracts were washed with water
9. dry with materialdried (MgSO4)
10. filtrationfiltered
11. concentrationconcentrated under reduced pressure