To a solution of 5-bromo-2-chloropyrimidine (4 g, 20.68 mmol) in acetonitrile (40 mL) was sequentially added 2-methoxyethylamine (5.5 mL, 63 mmol) and potassium carbonate (14 g, 100 mmol). The reaction mixture was heated and stirred at 100 °C for 6 hours. After completion of the reaction, the solvent was removed by concentration under reduced pressure. The residue was diluted with distilled water (30 mL) and subsequently extracted with dichloromethane (50 mL x 3). The organic layers were combined, dried with anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The crude product was purified by silica gel column chromatography with the eluent of petroleum ether/ethyl acetate (v/v=9/1) to afford the colorless oily target compound 5-bromo-N-(2-methoxyethyl)pyrimidin-2-amine (4.43 g, 92.3% yield). m/z MS (ESI, cation): 233.2 [M+H]+.
