4-(1-PIPERAZINYL)-6-(TRIFLUOROMETHYL)PYRIMIDINE synthesis

Yield:845616-55-9 56.6%

Reaction Conditions:

with triethylamine in DMF (N,N-dimethyl-formamide) at 100; for 5 h;

Steps:

28.B

A solution of 4-chloro-6-(trifluoromethyl)pyrimidine (1.0 g, 5.48 mmol), piperazine (2.36 g, 27.4 mmol), and triethylamine (2.29 mL, 16.4 mmol) in DMF (20 mL) was stirred at 100° C. for 5 h. The reaction solution was diluted with water and extracted with ethyl acetate three times, dried with sodium sulfate, filtered, and concentrated in vacuo. The crude residue was purified by flash column chromatography (10% MeOH/5% Et₃N/EtOAc) to yield the desired product (720 mg, 56.6%). LCMS calculated for C₉H₁₂F₃N₄: (M+1) 233.1; found 233.1.

References:

US2006/4018,2006,A1 Location in patent:Page/Page column 40