反应详情

温度

25 °C

To a cold solution of [1-(2-hydroxy-propyl)-piperidin-4-yl]-carbamic acid tert-butyl ester (0.70 g, 2.7 mmol) in DCM (30 mL) was added DAST (1.1 mL, 8.1 mmol) and the mixture was stirred at 25° C. for 20 h. The reaction mixture was washed with saturated sodium bicarbonate solution, water, brine, dried over Na2SO4 and concentrated under reduced pressure to afford [1-(2-fluoro-propyl)-piperidin-4-yl]-carbamic acid tert-butyl ester (0.5 g, 70%). LCMS (Method G; ESI): RT=0.53 min; m+1=261.3. This was used without further purification below.

1. washThe reaction mixture was washed with saturated sodium bicarbonate solution, water, brine
2. dry with materialdried over Na2SO4
3. concentrationconcentrated under reduced pressure