反应详情

温度

-78 °C

To a solution of (S)-methyl 2-(4-fluorophenyl)-7-methoxy-3-(2-methylpyrrolidin-1-yl)quinoxaline-6-carboxylate (200 mg, 0.51 mmol) in dichloromethane (80 ml) was added BBr3 (2.0 ml) dropwise with stirring at −78° C., and the reaction was allowed to proceed for 40 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 (S)-methyl 2-(4-fluorophenyl)-7-hydroxy-3-(2-methylpyrrolidin-1-yl)quinoxaline-6-carboxylate as a yellow solid (150 mg, 78%).

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)