反应详情

温度

90 °C

Phenol (40 mg, 0.24 mmol) was added to a stirred suspension of 2-chloromethyl-6-(4-fluoro-phenyl)-6H-imidazo[1,2-c]pyrimidin-5-one (0.107 g, 0.38 mmol) and K2CO3 (0.160 g, 1.15 mmol) in ACN (3 mL). The mixture was stirred at 90° C. for 16 hours and then the solvents were evaporated in vacuo. The crude product was purified by flash column chromatography (silica; AcOEt in DCM with a gradient of 0/100 to 20/80). The desired fractions were collected and the solvents evaporated in vacuo. The product was triturated with diethyl ether to yield 6-(4-fluoro-phenyl)-2-phenoxymethyl-6H-imidazo[1,2-c]pyrimidin-5-one (0.12 g, 90% yield) as a white solid. 1H NMR (500 MHz, CDCl3) δ ppm 5.20 (s, 2H), 6.70 (d, J=7.8 Hz, 1H), 6.98 (t, J=7.2 Hz, 1H), 7.03 (d, J=8.1 Hz, 2H), 7.12 (d, J=7.8 Hz, 1H), 7.19-7.25 (m, 2H), 7.27-7.34 (m, 2H), 7.38-7.45 (m, 2H), 7.83 (s, 1H).

1. customthe solvents were evaporated in vacuo
2. customThe crude product was purified by flash column chromatography (silica
3. customThe desired fractions were collected
4. customthe solvents evaporated in vacuo
5. customThe product was triturated with diethyl ether