反应详情

Add cyclobutanone (0.738 mL; 9.89 mmol) to a stirred mixture of 3-(2-(diethoxyphosphoryl)-acetyl)pyrrolidine-1-carboxylic acid tert butyl ester (3.14 g, 8.99 mmol) and potassium hydroxide (656 mg, 11.7 mmol) in ethanol (45 mL) kept under nitrogen at 5° C. Warm to room temperature and stir for 3 hours. Concentrate under reduced pressure and subject the residue to silica gel chromatography, eluting with 20% ethyl acetate in hexanes to afford 0.85 g (36%) of the crude desired compound, which is used in the next step without further purification.

1. customkept under nitrogen at 5° C
2. concentrationConcentrate under reduced pressure
3. washeluting with 20% ethyl acetate in hexanes