反应详情

PyBrOP™ (17.3 g) was added to a stirred mixture of 3-methanesulphonyl benzoic acid (7.35 g), 4-piperidone hydrochloride (5 g) and Hunig's base (25 ml) in dichloromethane (250 ml) with stirring at RT. The mixture was stirred overnight then washed with saturated NaHCO3 solution (200 ml) and then with saturated brine (200 ml). The organic layer was evaporated and the resulting residue purified by column chromatography (silica, 1:1 ethyl acetate: dichloromethane) to give the product as a thick oil (9.6 g; MS: APCI+(M+H) 282).

1. stirringThe mixture was stirred overnight
2. washthen washed with saturated NaHCO3 solution (200 ml)
3. customThe organic layer was evaporated
4. customthe resulting residue purified by column chromatography (silica, 1:1 ethyl acetate: dichloromethane)