反应详情

A mixture of 550 mg of 4-benzyl-5-bromo-2-pyridyl trifluoromethanesulfonate (Production Example 1), 600 mg of 4-hydroxypiperidine hydrochloride, 1 ml of triethylamine and 2 ml of N,N-dimethylformamide was heated under stirring for 3 hours in an oil bath kept at 100° 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 50% ethyl acetate/hexane, to give 270 mg of the target compound.

1. temperaturewas heated
2. customkept at 100° 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 50% ethyl acetate/hexane