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Dissolve 3-(2,6-dichloro-4-hydroxybenzyl)-1-(cis-2-methylcyclohexyl)pyrrolidin-2-one (1.0 g, 2.81 mmol) in DCM (100 mL) and cool to 0° C. under N2. Add DMAP (0.069 g, 0.56 mmol), Et3N (2.84 g, 28.01 mmol), and Tf2O (0.83 g, 2.95 mmol) at the same temperature. Stir the reaction for six hour and then add water (100 mL). Extract the aqueous layer with dichloromethane (3×100 mL). Combine the organic layers and dry with Na2SO4, filter, concentrate and purify by flash column chromatography (silica gel, 20-50% of EtOAc-Hexane) to give 1.2 g (88%) of the title compound as a colorless oil. 1H NMR (CDCl3) δ 7.28 (s, 2H), 4.02 (m, 1H), 3.46 (m, 2H), 3.38 (m, 1H), 3.02 (m, 1H), 2.91 (m, 1H), 2.35 (m, 1H), 2.02 (m, 1H), 1.31-1.87 (m, 9H), 0.92 (d, 3H).

1. customthe reaction for six hour
2. extractionExtract the aqueous layer with dichloromethane (3×100 mL)
3. dry with materialCombine the organic layers and dry with Na2SO4
4. filtrationfilter
5. concentrationconcentrate
6. custompurify by flash column chromatography (silica gel, 20-50% of EtOAc-Hexane)