反应详情

温度

70 °C

6-Bromo-3-(chloro-difluoro-methyl)-[1,2,4]triazolo[4,3-a]pyridine (2.76 g, 9.8 mmol), 4-trifluoromethoxyphenyl boronic acid (2.5 g, 12.1 mmol), dppfPdCl2 (1,1′-bis(diphenylphosphino)ferrocene palladium dichloride) (350 mg, 0.5 mmol), and potassium carbonate (2.76 g, 20 mmol) were suspended in degassed toluene (20 mL), degassed isopropanol (10 mL) and degassed water (10 mL) under an atmosphere of nitrogen. The reaction mixture was heated at 70° C. for 1 hour before being cooled to room temperature. The aqueous phase was discarded and the organic phase was concentrated and purified by flash chromatography (rf=0.5 in 1:1 hexanes/ethyl acetate) to give 3-(chloro-difluoro-methyl)-6-(4-trifluoromethoxy-phenyl)[1,2,4]triazolo[4,3-a]pyridine as a pale orange powder.

1. customdegassed isopropanol (10 mL)
2. customdegassed water (10 mL) under an atmosphere of nitrogen
3. temperaturebefore being cooled to room temperature
4. concentrationthe organic phase was concentrated
5. custompurified by flash chromatography (rf=0.5 in 1:1 hexanes/ethyl acetate)