反应详情

To a solution of (S)-2-amino-6-((1-butyrylpiperidin-3-yl)methoxy)benzonitrile (Example 1b, 9.2 g, 30.53 mmol) in DMA (60 mL) was added sulfamoyl chloride (Example 1f, 10.54 g, 91.58 mmol) at room temperature under nitrogen. The reaction mixture was stirred at room temperature under nitrogen overnight then concentrated under reduced pressure, diluted with EtOAc, successively washed with NaHCO3, water and brine, dried over Na2SO4, filtered and the solvent was removed under reduced pressure to give the title compound as colorless gel (9.5 g) in 82% yield. MS 381 (MH+).

1. concentrationthen concentrated under reduced pressure
2. additiondiluted with EtOAc
3. washsuccessively washed with NaHCO3, water and brine
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. customthe solvent was removed under reduced pressure