反应详情

温度

115 °C

The mixture of 3-(3-bromo-4-fluorophenyl)propanimidamide hydrochloride (5.0 g, 19.38 mmol), potassium carbonate (9.37 g, 67.8 mmol) and ethyl 2-formyl-3-(5-pyrimidinyl)propanoate (4.03 g, 20.35 mmol) in toluene (100 mL) was stirred at 115° C. for 2.5 h. After cooling, the mixture was diluted with water, then extracted with DCM (50 mL×2). The combined organic phase was concentrated to give the crude title compound as a light yellow solid (6.0 g, 77% yield). The crude was used without further purification. LCMS: rt=1.20 min, [M+H+]=389

1. temperatureAfter cooling
2. extractionextracted with DCM (50 mL×2)
3. concentrationThe combined organic phase was concentrated