Synthesis
General procedure for the synthesis of 6-ethyl-5-iodopyrimidine-2,4-diamine from 2,4-diamino-6-ethylpyrimidine: a suspension of 2,4-diamino-6-ethylpyrimidine (0.8750 g, 5.00 mmol) and iodine monochloride (0.40 mL, 7.50 mmol) was stirred for 2 h at room temperature in methanol (15 mL). Upon completion of the reaction, water (5 mL) was added and the pH was adjusted with 10% NaOH aqueous solution to 7. Subsequently, the reaction mixture was extracted with ethyl acetate (15 mL each time) three times, and the organic phases were combined and dried with anhydrous MgSO4. Finally, the solvent was removed by evaporation to afford the light brown solid product 6-ethyl-5-iodopyrimidine-2,4-diamine (1.1355 g, 86% yield).
References
[1] Patent: WO2017/52479, 2017, A1. Location in patent: Page/Page column 10
[2] Journal of Chemical Research - Part S, 2002, # 10, p. 482 - 484
[3] Bioorganic and Medicinal Chemistry, 2017, vol. 25, # 15, p. 3947 - 3963
