反应详情

DAST (4.36 mL, 33 mmol) was added to a solution of (4-hydroxy-piperidin-1-yl)-acetonitrile (4.25 g, 30 mmol) in DCM (80 mL) at −30° C., the mixture was then stirred at rt for overnight. The reaction was cooled to −30° C. and quenched with methanol (10 mL) for 30 mins. The organic layer was then washed with NaHCO3 and dried. The residue was purified on a silica gel column to give 3 g (71%) of (4-fluoro-piperidin-1-yl)-acetonitrile.

1. temperatureThe reaction was cooled to −30° C.
2. customquenched with methanol (10 mL) for 30 mins
3. washThe organic layer was then washed with NaHCO3
4. customdried
5. customThe residue was purified on a silica gel column