反应详情

94 mg of N-iodosuccinic acid imide was added little by little to 5.0 ml of an N,N-dimethylformamide solution containing 104 mg of 2-benzyl-6-[(3R,4R)-3,4-difluoropyrrolidine-1-yl]pyridine under ice-cooling, followed by stirring overnight as it was. Water was added to the reaction solution and the mixture was extracted with ethyl acetate. The organic phase was washed with an aqueous sodium thiosulfate solution, water and brine, and the solvent was removed. The residue was subjected to NH-silica gel (Fuji Silicia) column chromatography and eluted with hexane/ethyl acetate (10:1), to give 152 mg of the target compound.

1. temperaturecooling
2. extractionthe mixture was extracted with ethyl acetate
3. washThe organic phase was washed with an aqueous sodium thiosulfate solution, water and brine
4. customthe solvent was removed
5. washeluted with hexane/ethyl acetate (10:1)