反应详情

Reflux a mixture of 1-benzyl-2,4,5-tribromoimidazole (1.043 g, 2.42 mmol), 2,4-difluorophenyl boronic acid (0.682 g, 4.32 mmol), palladium acetate (0.027 g, 0.12 mmol), R(+)-2,2′-bis(di-p-tolyl-phosphino)1,1′-binaphthyl (0.098 g, 0.14 mmol), 2 M sodium carbonate (3.6 mL, 4.83 mmol), methanol (3.6 mL) and toluene (36 mL) for 18 hours. Cool to ambient temperature and dilute with ethyl acetate. Wash with saturated sodium carbonate, saturated sodium chloride, dry with magnesium sulfate and purify the residue on silica gel eluting with hexane/ethyl acetate mixtures to provide 1-benzyl-4,5-dibromo-2-(2,4-difluoro-phenyl)-1H-imidazole (0.39 g). MS(ES+): m/z=461.1 (M+H)+

1. temperatureReflux
2. washWash with saturated sodium carbonate, saturated sodium chloride
3. dry with materialdry with magnesium sulfate
4. custompurify the residue on silica gel eluting with hexane/ethyl acetate