反应详情

温度

0 °C

3-Hydroxy-Cbz-(R)-pyrrolidine (13.7 g, 0.06 mol) was dissolved in CH2Cl2 (250 mL) and cooled to 0° C. p-Toluenesulfonyl chloride (14.16 g, 0.07 mol), and triethylamine (20.7 mL, 0.15 mol) were added and the resulting solution was stirred for 4 h at 0° C. The solution was washed with 1 M HCl, saturated NaHCO3, and brine. The organic solution was dried over MgSO4 and concentrated. The crude product was purified by column chromatography eluting with ethyl acetate/hexanes (3/1, v/v) to afford 20.4 g (88% yield) of the desired product as an oil.

1. additionwere added
2. washThe solution was washed with 1 M HCl, saturated NaHCO3, and brine
3. dry with materialThe organic solution was dried over MgSO4
4. concentrationconcentrated
5. customThe crude product was purified by column chromatography
6. washeluting with ethyl acetate/hexanes (3/1