反应详情

2.55 g sodium periodate and 0.4 mg ruthenium (III) chloride hydrate were added to 60 mL solution mixture (carbon tetrachloride/acetonitrile/water=1:1:2) of 1.5 g t-butyl 4-(4-trifluoromethylsulfanyl-phenoxy)piperidine-1-carboxylate (compound in Production Example 454) with stirring under ice-cooling, and the mixture was stirred at room temperature for 1 hour. Water and a sodium bicarbonate solution were added thereto, and the reaction solution was extracted with ethyl acetate, dried over sodium sulfate and purified by silica gel chromatography (hexane/ethyl acetate) to give 1.3 g t-butyl 4-(4-trifluoromethylsulfonylphenoxy)piperidine-1-carboxylate. 2 mL solution of 4 N hydrogen chloride in ethyl acetate was added thereto and left for 1 hour. The solvent was removed, and the precipitated crystals were washed with ethyl acetate/ether to give 965 mg of the title compound as colorless crystals.

1. temperaturecooling
2. stirringthe mixture was stirred at room temperature for 1 hour
3. extractionthe reaction solution was extracted with ethyl acetate
4. dry with materialdried over sodium sulfate
5. custompurified by silica gel chromatography (hexane/ethyl acetate)