反应详情

温度

70 °C

In a sealed tube 3-(7-aminoimidazo[1,2-a]pyrimidin-2-yl)phenol hydrobromide (800 mg, 2.6 mmol) was combined with DMF (4.0 ml) to give a light brown solution. 1-Bromo-2-fluoroethane (476 mg, 3.75 mmol) dissolved in DMF (4.0 ml) and Cs2CO3 (1.62 g, 4.97 mmol) were added. The reaction mixture was stirred 23 h at 70° C. H2O (50 ml) was added to the reaction mixture and the product was extracted with EtOAc (3×40 ml). After drying over MgSO4, filtration and concentration in vacuum, the crude product (orange oil) was purified by flash chromatography (50 g SiO2—NH2 cartridge, eluent: CH2Cl2 to CH2Cl2/MeOH 95:5) to yield the title compound (150 mg, 21%).

1. customto give a light brown solution
2. extractionthe product was extracted with EtOAc (3×40 ml)
3. dry with materialAfter drying over MgSO4, filtration and concentration in vacuum
4. customthe crude product (orange oil) was purified by flash chromatography (50 g SiO2—NH2 cartridge, eluent: CH2Cl2 to CH2Cl2/MeOH 95:5)