反应详情

温度

150 °C

N-chlorosuccinimide (32.9 mg, 0.25 mmol) was added to a stirred solution of 6-(4-fluoro-phenyl)-2-phenoxymethyl-6H-imidazo[1,2-c]pyrimidin-5-one (75 mg, 0.22 mmol) in DMF (3.5 mL). The mixture was stirred at 150° C. for 15 minutes under microwave irradiation. The solvent was evaporated in vacuo and 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 DIPE to yield 3-chloro-6-(4-fluoro-phenyl)-2-phenoxymethyl-6H-imidazo[1,2-c]pyrimidin-5-one (46 mg, 56% yield) as a white solid. 1H NMR (400 MHz, CDCl3) 8 ppm 5.12 (s, 2H), 6.62 (d, J=7.9 Hz, 1H), 6.98 (tt, J=7.4, 0.9 Hz, 1H), 7.03-7.07 (m, 2H), 7.06 (d, J=7.6 Hz, 1H), 7.17-7.25 (m, 2H), 7.27-7.34 (m, 2H), 7.35-7.43 (m, 2H).

1. customThe solvent was 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 DIPE