反应详情

Reflux a mixture of 1-benzyl-4-bromo-5-(3,5-difluoro-phenyl)-2-(2,4-difluoro-phenyl)-imidazole (0.061 g, 0.13 mmol), 1-isopropylsulfonyl-2-amino-benzimidazole-6-boronic acid (0.113 g, 0.40 mmol) (described in preparation 56), trans-dichlorobis(triphenylphosphine) palladium (II) (0.009 g, 0.013 mmol), 2 M sodium carbonate (0.20 mL) and 1,2-dimethoxyethane (5 mL) for 18 hours. Cool to ambient temperature, dilute with ethyl acetate and wash with saturated sodium bicarbonate, saturated sodium chloride, dry with magnesium sulfate, filter and remove solvents under reduced pressure. Purify on silica gel with dichloromethane/methanol mixtures to provide the title compound (0.084 g). MS(ES+): m/z=620.1 (M+H)+

1. temperatureReflux
2. washwash with saturated sodium bicarbonate, saturated sodium chloride
3. dry with materialdry with magnesium sulfate
4. filtrationfilter
5. customremove solvents under reduced pressure
6. customPurify on silica gel with dichloromethane/methanol