4-HYDROXY-2-(PYRAZIN-2-YL)-6-(TRIFLUOROMETHYL)PYRIMIDINE synthesis

Yield:438249-85-5 84%

Reaction Conditions:

with trichlorophosphate

Steps:

74.a 4-(3-Methoxyanilino)-2-(2-pyrazinyl)-6-(trifluoromethyl)pyrimidine

a. 4-Chloro-2-(2-pyrazinyl)-6-(trifluoromethyl)pyrimidine A mixture of 4-hydroxy-2-(2-pyrazinyl)-6-(trifluoromethyl)pyrimidine (2.0 g, 8.26 mmol) and phosphorus oxychloride (30 ml) was refluxed for 3 h. The mixture was cooled to room temperature and then rotary evaporated to dryness. The residual was purified by column chromatography and isolated as a tan solid (1.8 g, 84%). ¹H NMR (DMSO-d₆): 9.54 (d, J=1.5 Hz, 1H), 8.92 (dd, J=1.5, 2.4 Hz, 1H), 8.90 (d, J=2.4 Hz, 1H), 8.48 (s, 1H).

References:

US2003/69239,2003,A1