反应详情

温度

120 °C

To a solution of methyl 2-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate (259 mg, 1.308 mmol), 3-bromo-5-(tetrahydro-2H-pyran-4-yl)pyrazin-2-amine (225 mg, 0.872 mmol), and PdCl2(dppf) (64 mg, 0.087 mmol) was added DME (6.5 mL) and 2 M Na2CO3 solution (3.2 mL). The reaction mixture was heated at the microwave synthesizer (120° C., 10 min). The reaction mixture was worked up with EtOAc. The organic layer was washed with water and brine, dried over anhydrous sodium sulfate, filtered off, and concentrated in vacuo. The crude product was purified by flash chromatography (gradient EtOAc in heptane) to yield the desired product (192 mg, 67%). LCMS (m/z): 332.2 (MH+), 0.63 min.

1. washThe organic layer was washed with water and brine
2. dry with materialdried over anhydrous sodium sulfate
3. filtrationfiltered off
4. concentrationconcentrated in vacuo
5. customThe crude product was purified by flash chromatography (gradient EtOAc in heptane)