反应详情

To a stirred suspension of NaH (40% oil dispersion, 19 mg) in THF (6 ml) was added a solution of 1-(2-cyclopropyl-3-methylimidazo[1,2-a]pyridin-6-yl)-4-hydroxypyridin-2 (1H)-one (75 mg) in THF (1 ml) at 0° C., and then the mixture was stirred at room temperature for 30 min. 2,4-Difluorobenzyl bromide (67 mg) in THF (0.5 ml) was added, and the resulting mixture was stirred at room temperature for further 3 h followed by heating at reflux for 6 h. The reaction mixture was then cooled to room temperature and quenched with ice-water. The mixture was extracted with DCM, and the extract was washed with brine, dried over Na2SO4 and concentrated in vacuo. The crude product was purified by silica gel column chromatography (MeOH/DCM) to give the title compound (38 mg) as an off-white solid.

1. stirringthe resulting mixture was stirred at room temperature for further 3 h
2. temperatureby heating
3. temperatureat reflux for 6 h
4. temperatureThe reaction mixture was then cooled to room temperature
5. customquenched with ice-water
6. extractionThe mixture was extracted with DCM
7. washthe extract was washed with brine
8. dry with materialdried over Na2SO4
9. concentrationconcentrated in vacuo
10. customThe crude product was purified by silica gel column chromatography (MeOH/DCM)