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0 °C

4-Chloro-2,5-dimethyl-benzenesulfonyl chloride (1 g, 3.8 mmol) was added to a solution of ethyl 3-(piperidin-2-yl)propionic acid ethyl ester hydrochloride (1.1 g, 4.6 mmol) in dichloromethane (15 ml) while stirring, the mixture was cooled to 0° C., and triethylamine (1.6 ml, 11.5 mmol) was added dropwise over 15 min. The mixture was stirred for 4 h at 0° C., then diluted with dichloromethane, washed with water and saturated sodium chloride solution, dried over sodium sulfate and concentrated to small volume under vacuum. The crude product was purified with ethyl acetate/hexane (9:1) by column chromatography. Yield: 50%

1. stirringThe mixture was stirred for 4 h at 0° C.
2. washwashed with water and saturated sodium chloride solution
3. dry with materialdried over sodium sulfate
4. concentrationconcentrated to small volume under vacuum
5. customThe crude product was purified with ethyl acetate/hexane (9:1) by column chromatography