2-AMINO-4-CHLORO-6-TRIFLUOROMETHYL-PYRIMIDINE

1513-69-5

16097-60-2

Example 15: Synthesis of 4-chloro-6-(trifluoromethyl)pyrimidin-2-amine (24) 2-Amino-6-(trifluoromethyl)pyrimidin-4-ol (200 mg, 1.1 mmol) was dissolved in a mixed solution of phosphorus oxychloride (POCl3, 3 eq., 0.3 mL, 3.3 mmol) and N,N-dimethylaniline (0.28 mL, 2 eq.). The reaction mixture was heated with stirring at 70 °C for 4 hours. Upon completion of the reaction, the mixture was slowly poured into an ice-water mixture to quench the reaction and the precipitated solid was collected by filtration to afford the target compound 24 in 59% yield. The product was identified by electrospray ionization mass spectrometry (ESI-MS), m/z 198 [M + H]+.