反应详情

(5-Bromo-2-methylpentane-2-sulfonyl)benzene (5 g, 16.4 mmol), 3-hydroxypiperidine (2 g, 20 mmol) and potassium carbonate (4.5 g, 33 mmol) in acetonitrile (50 ml) were stirred at 50° C. for 18 hours. The cooled reaction mixture was partitioned between ethyl acetate and brine. The organic layer was dried (MgSO4) and concentrated in vacuo. The residue was purified by flash column chromatography on silica, eluting with 120:8:1 dichloromethane/methanol/ammonia, to give the title compound (5.2 g, 98%).

1. customThe cooled reaction mixture
2. customwas partitioned between ethyl acetate and brine
3. dry with materialThe organic layer was dried (MgSO4)
4. concentrationconcentrated in vacuo
5. customThe residue was purified by flash column chromatography on silica
6. washeluting with 120:8:1 dichloromethane/methanol/ammonia