5-BROMO-4-CHLORO-6-TRIFLUOROMETHYLPYRIMIDINE synthesis

Yield:425392-76-3 100%

Reaction Conditions:

with trichlorophosphate at 110; for 3 h;

Steps:

4.I41

Example 141: Preparation of 5-bromo-4-chloro-6-trifluoromethyl-pyrimidine5-Bromo-6-trfluoromethyl-3H-pyrimidin-4-one (Example 140) (8.00 g, 32.9 mmol) was suspended in phosphorous oxychloride (6.00 g, 62.7 mmol). The mixture was heated at 11O⁰C for 3 hours. The reaction mixture was quenched by adding dropwise to hot water and the mixture was stirred until it had cooled to room temperature. The aqueous mixture was extracted with ethyl acetate. The organic extract was washed with water and brine, dried over magnesium sulfate and concentrated to give 5-bromo-4- chloro-6-trifluoromethyl-pyrimidine as viscous oil (8.50 g, 100% yield), which was used without further purification. ¹H-NMR (400 MHz₅ CDCl₃): 8.55 (s, IH, CH) ppm.

References:

WO2007/71900,2007,A1 Location in patent:Page/Page column 96