反应详情

To 2-fluoro-6-(trifluoromethyl)benzylamine 4a (51.5 g, 0.267 mmol) in a flask, urea (64 g, 1.07 mmol), HCl (conc., 30.9 mmol, 0.374 mmol) and water (111 mL) were added. The mixture was refluxed for 6 hours. The mixture was cooled to ambient temperature, further cooled with ice and filtered to give a yellow solid. Recrystallization with 400 mL of EtOAc gave 4b as a white solid (46.2 g, 0.196 mmol). MS (CI) m/z 237.0 (MH+).

1. temperatureThe mixture was refluxed for 6 hours
2. temperaturefurther cooled with ice
3. filtrationfiltered
4. customto give a yellow solid
5. customRecrystallization with 400 mL of EtOAc