反应详情

To a solution of benzyl 4-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (1.0 g, 3.7 mmol) in CH2Cl2 (10 mL) at RT was added MsCl (0.29 mL, 3.7 mmol) and TEA (1.04 mL, 7.5 mmol). The reaction mixture was stirred at RT for 5 min, and partitioned between EtOAc and H2O. The organic layer was dried over Na2SO4, filtered, concentrated and purified on silica gel (10:1 to 1:2 hexanes:EtOAc) to give benzyl 4-fluoro-4-{[(methylsulfonyl)oxy]methyl}piperidine-1-carboxylate.

1. custompartitioned between EtOAc and H2O
2. dry with materialThe organic layer was dried over Na2SO4
3. filtrationfiltered
4. concentrationconcentrated
5. custompurified on silica gel (10:1 to 1:2 hexanes:EtOAc)