反应详情

7-Bromo-N-(5-(3,4-difluorobenzylcarbamoyl)-2-fluorophenyl)imidazo[1,2-a]pyridine-3-carboxamide (Intermediate 3A) (500 mg, 0.993 mmol), methyl 2-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate (306 mg, 1.093 mmol) and cesium carbonate (1295 mg, 3.97 mmol) in water (2 ml)/DME (5 ml) were mixed to give a suspension. The mixture was degassed with nitrogen and PdCl2(dppf).CH2Cl2 adduct (40.6 mg, 0.050 mmol) was added. The reaction mixture was heated using microwave radiation at 100° C. for 1 hr and partitioned between EtOAc and water. The organic portion was separated, dried (MgSO4) and concentrated in vacuo. The crude product was triturated with MeOH/diethyl ether to afford the title compound;

1. customto give a suspension
2. customThe mixture was degassed with nitrogen and PdCl2(dppf)
3. temperatureThe reaction mixture was heated
4. customat 100° C.
5. customfor 1 hr
6. custompartitioned between EtOAc and water
7. customThe organic portion was separated
8. dry with materialdried (MgSO4)
9. concentrationconcentrated in vacuo
10. customThe crude product was triturated with MeOH/diethyl ether