反应详情

A mixture of 4.0 g of 4-benzyl-5-bromo-2-pyridyl trifluoromethanesulfonate, 1.8 g of (3R,4R)-3,4-dihydroxypyrrolidine acetate, 3 ml of 1,8-diazabicyclo[5.4.0]-7-undecene and 5 ml of tetrahydrofuran was heated under stirring for 3 hours in an oil bath kept at 70° C. in a nitrogen atmosphere. After cooling as it was, the reaction 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 10% methanol/ethyl acetate, to give 1.67 g of the target compound.

1. temperaturewas heated
2. customkept at 70° C. in a nitrogen atmosphere
3. temperatureAfter cooling as it
4. extractionthe reaction mixture was extracted with ethyl acetate-water
5. washThe organic phase was washed with water and brine
6. dry with materialdried over anhydrous magnesium sulfate
7. customevaporated
8. washeluted with 10% methanol/ethyl acetate