反应详情

To a solution of (2R, 4S)-4-(4-methoxyphenyl)-5-oxopyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester (305 mg, 0.91 mmol), diisopropylethylamine (0.35 mL, 2.0 mmol) and O-benzylhydroxylamine hydrochloride (160 mg, 1.0 mmol) in methylene chloride (20 mL) was added (benztriazol-1-yloxy)tris(dimethylamino)phosphonium hexafluoroborate (443 mg, 1.0 mmol). The reaction was stirred at room temperature overnight. After dilution with methylene chloride, the mixture was washed with aqueous saturated sodium bicarbonate solution, water and brine. The solution was dried over magnesium sulfate and concentrated to a white solid from which the title compound (294 mg, 73%) was isolated by flash chromatography eluting with 25% hexane in ethyl acetate.

1. washAfter dilution with methylene chloride, the mixture was washed with aqueous saturated sodium bicarbonate solution, water and brine
2. dry with materialThe solution was dried over magnesium sulfate
3. concentrationconcentrated to a white solid from which the title compound (294 mg, 73%)
4. customwas isolated by flash chromatography
5. washeluting with 25% hexane in ethyl acetate