反应详情

温度

95 °C

A mixture of 6.4 g 6-bromo-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one (31.3 mmol), 12.4 g 4-(trifluoromethoxy)phenyl boronic acid (60.0 mmol), 12.4 g potassium carbonate (90.0 mmol), and 1.1 g Pd(dppf)Cl2 in 200 mL degassed 2:1:1 toluene:isopropanol:water was heated at 95° C. in sealed vessel. After 3 days, the aqueous layer was decanted and the organic concentrated. The residue was triturated with ethyl acetate to provide 6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one as a dark grey solid. m/z (ESI)=226.2 [M+H]+. 1H NMR (δ, d6-DMSO, 400 MHz) 12.55 (s, 1H), 8.07 (s, 1H), 7.82 (d, 2H), 7.56 (dd, 1H), 7.43 (d, 2H), 7.33 (d, 1H)

1. customdegassed 2:1:1 toluene
2. customthe aqueous layer was decanted
3. customThe residue was triturated with ethyl acetate