反应详情

温度

80 °C

2-(2-tert-Butoxycarbonyl-3-oxo-butyryl)-pyrrolidine-1-carboxylic acid benzyl ester (9.74 g, 25.0 mmol) was dissolved toluene (40 mL) and was washed with 1N HCl (2×50 mL). To the resulting solution was added p-toluenesulfonic acid monohydrate (1.00 g, 5.00 mmol) and the solution was heated under nitrogen to 80° C. for 4 hours. The dark mixture was allowed to cool and was washed with water (3×100 mL). The organic layer was concentrated to give 6.87 g (95%) of 2-(3-oxo-butyryl)-pyrrolidine-1-carboxylic acid benzyl ester as an amber oil. The product was used directly in the subsequent step without further purification. [M+H]+ 290.03.

1. washwas washed with 1N HCl (2×50 mL)
2. temperatureto cool
3. washwas washed with water (3×100 mL)
4. concentrationThe organic layer was concentrated