Synthesis
Step 1: Synthesis of N-methylpyrimidin-2-amine
To a solution of 2-chloropyrimidine (1 g, 8.7 mmol) in methanol (10 mL) was slowly added a methanolic solution of 2Methylamine (13.2 mL, 26.2 mmol) followed by potassium carbonate (2.5 g, 18 mmol). The reaction flask was sealed and the reaction was stirred at 80 °C overnight. Upon completion of the reaction, the mixture was cooled to room temperature and concentrated by rotary evaporator to remove volatile solvents. The residue was extracted by liquid-liquid partition with distilled water and dichloromethane. The organic layer was separated, dried over anhydrous sodium sulfate, filtered and concentrated to give 2-methylaminopyrimidine (290 mg, 30% yield) as a brown oil.
References
[1] Bulletin of the Chemical Society of Japan, 1998, vol. 71, # 8, p. 1973 - 1991
[2] Journal of Medicinal Chemistry, 2013, vol. 56, # 17, p. 6626 - 6637
[3] Molecules, 2004, vol. 9, # 7, p. 520 - 526
[4] Patent: WO2011/71716, 2011, A1. Location in patent: Page/Page column 99
[5] Journal of the American Chemical Society, 1954, vol. 76, p. 1065,1067
