反应详情

温度

95 °C

To a solution of methyl 3-(isopropyl(methyl)amino)-7-methoxy-2-(trifluoromethylsulfonyloxy)quinoxaline-6-carboxylate (2.5 g, crude) in dioxane (5.0 mL) and water (3 drops) was added (4-fluorophenyl)boronic acid (2.40 g, 17.15 mmol), Pd(PPh3)4 (320 mg, 0.28 mmol), and K3PO4 (3.58 g, 16.87 mmol) with stirring for 1.5 h at 95° C. under an atmosphere of nitrogen. The reaction mixture was concentrated in vacuo to give a residue, which was purified via silica gel column chromatography (1% ethyl acetate in petroleum ether) to afford methyl 2-(4-fluorophenyl)-3-(isopropyl(methyl)amino)-7-methoxyquinoxaline-6-carboxylate as a light yellow solid (0.9 g, 36% 2 steps).

1. concentrationThe reaction mixture was concentrated in vacuo
2. customto give a residue, which
3. customwas purified via silica gel column chromatography (1% ethyl acetate in petroleum ether)