反应详情

Methanesulfonyl chloride (2.7 ml) was dropwise added to a methylene chloride (200 ml) solution of tert-butyl 4-(3-hydroxypropyl)piperidine-1-carboxylate (8.00 g) and TEA (4.8 ml) at 0° C., followed by stirring overnight at room temperature. The reaction liquid was washed with aqueous saturated sodium hydrogencarbonate solution and saturated brine, then dried over anhydrous magnesium sulfate, and the solvent was evaporated. The residue was purified by silica gel column chromatography (eluent: EtOAc:hexane=1:3 (v/v)) to obtain tert-butyl 4-{3-[(methylsulfonyl)oxy]propyl}piperidine-1-carboxylate (10.1 g).

1. customThe reaction liquid
2. washwas washed with aqueous saturated sodium hydrogencarbonate solution and saturated brine
3. dry with materialdried over anhydrous magnesium sulfate
4. customthe solvent was evaporated
5. customThe residue was purified by silica gel column chromatography (eluent: EtOAc:hexane=1:3 (v/v))