943006-45-9

Part C: 4,6-Dichloro-5-fluoro-2-methylpyrimidine (1.55 g, 8.56 mmol), ammonium hydroxide solution (35%, 10.0 mL, 257 mmol) and methanol (1.00 mL) were mixed in a sealed tube and the reaction was heated for 2 hours at 70 °C. After completion of the reaction, the mixture was cooled to room temperature and precipitate was precipitated. The reaction mixture was diluted by adding water (about 10 mL) and stirring was continued for 30 minutes. The solid product was collected by diafiltration, washed with water and dried in air to afford 4-amino-6-chloro-5-fluoro-2-methylpyrimidine (845 mg, 61% yield) as a brown solid.LC-MS (m/z): 162,164 ([M+H]+).

[1] Journal of Medicinal Chemistry, 2012, vol. 55, # 11, p. 5188 - 5219
[2] Patent: WO2007/75852, 2007, A2. Location in patent: Page/Page column 32
[3] Patent: US2007/197523, 2007, A1. Location in patent: Page/Page column 7-8