反应详情

温度

0 °C

To a solution of (S)-2-[4-(2-fluoro-3-methoxy-phenoxy)-2-oxo-2,5-dihydro-pyrrol-1-yl]-4-methyl-pentanoic acid methyl ester (1.35 g, 3.83 mmol) in dichloromethane (20 mL) was added a boron tribromide in dichloromethane solution (1 M, 11.50 mL, 11.50 mmol) at 0° C. The resulting mixture was stirred at 0° C. for 2 h and then poured into ice water containing hydrochloric acid (2N, 30 mL). The organic phase was separated, washed with water and brine. The solvents were removed by evaporation and the residue purified by ISCO flash chromatography (Teledyne Isco RediSep Flash Column 50 g, 30% to 100% (9:1 dichloromethane:methanol)/hexanes) which afforded (S)-2-[4-(2-fluoro-3-hydroxy-phenoxy)-2-oxo-2,5-dihydro-pyrrol-1-yl]-4-methyl-pentanoic acid methyl ester (1.05 g, 81%) as a brown oil.

1. customThe organic phase was separated
2. washwashed with water and brine
3. customThe solvents were removed by evaporation
4. customthe residue purified by ISCO flash chromatography (Teledyne Isco RediSep Flash Column 50 g, 30% to 100% (9:1 dichloromethane:methanol)/hexanes) which