反应详情

温度

-78 °C

To a solution of methyl 2-(4-fluorophenyl)-3-(isopropyl(methyl)amino)-7-methoxyquinoxaline-6-carboxylate (500 mg, 1.31 mmol) in dichloromethane (80 mL) was added BBr3 (2.0 mL) dropwise with stirring at −78° C. for 30 minutes. The reaction was then quenched by the addition of water/ice. The resulting solution was extracted with dichloromethane (3×80 mL), and the organic layers combined, dried over anhydrous magnesium sulfate, and concentrated in vacuo to give the residue, which was purified via silica gel column chromatography (2% ethyl acetate in petroleum ether) to afford methyl 2-(4-fluorophenyl)-7-hydroxy-3-(isopropyl(methyl)amino)quinoxaline-6-carboxylate as a yellow solid (145 mg, 30%).

1. customThe reaction was then quenched by the addition of water/ice
2. extractionThe resulting solution was extracted with dichloromethane (3×80 mL)
3. dry with materialdried over anhydrous magnesium sulfate
4. concentrationconcentrated in vacuo
5. customto give the residue, which
6. customwas purified via silica gel column chromatography (2% ethyl acetate in petroleum ether)