反应详情

Under stirring in an ice bath, 2.5 g of N-iodosuccinimide was added little by little to a mixture of 3.11 g of 2-benzyl-6-[(3R,4R)-3-hydroxy-4-methoxypyrrolidine-1-yl]pyridine and 10 ml of N,N-dimethylformamide, followed by stirring as it was overnight. Sodium sulfite was added thereto and the mixture was extracted with ethyl acetate-water. The organic phase was washed with water and brine, dried over anhydrous magnesium sulfate and evaporated. The residue was subjected to silica gel column chromatography and eluted with 30% ethyl acetate/hexane, to give 4.19 g of the target compound.

1. stirringby stirring as it
2. extractionthe mixture was extracted with ethyl acetate-water
3. washThe organic phase was washed with water and brine
4. dry with materialdried over anhydrous magnesium sulfate
5. customevaporated
6. washeluted with 30% ethyl acetate/hexane