反应详情

温度

120 °C

To a solution of 2-fluoro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine (500 mg, 2.242 mmol) was added PdCl2(dppf) (68.3 mg, 0.093 mmol), 4-bromo-1-methylpyridin-2(1H)-one (351 mg, 1.868 mmol), 2M Na2CO3 (4.1 mL) and DME (8.3 mL) at room temperature. The reaction mixture was heated at microwave synthesizer for 10 min at 120° C. The reaction mixture was extracted with EtOAc. The organic layers were washed with water and brine, dried over anhydrous Na2SO4, filtered off, and concentrated in vacuo. The crude 6-fluoro-1′-methyl-[3,4′-bipyridin]-2′(1′H)-one was purified by flash chromatography (gradient EtOAc in DCM). LCMS (m/z): 205.2 (MH+), 0.47 min.

1. extractionThe reaction mixture was extracted with EtOAc
2. washThe organic layers were washed with water and brine
3. dry with materialdried over anhydrous Na2SO4
4. filtrationfiltered off
5. concentrationconcentrated in vacuo
6. customThe crude 6-fluoro-1′-methyl-[3,4′-bipyridin]-2′(1′H)-one was purified by flash chromatography (gradient EtOAc in DCM)
7. custom205.2 (MH+), 0.47 min.