反应详情

Heat a mixture of 1-benzyl-2-methyl-5-bromo-1H-imidazole (4.71 g, 18.7 mmol), 2,4-difluorophenyl boronic acid (6.92 g, 43.8 mmol), bis(acetato)bis(triphenylphosphine)-palladium(II) (1.4 g, 1.875 mmol), 2N Na2CO3 (19 mL, 38 mmol), MeOH (19 mL) and 1,2-dimethoxyethane (120 mL) to reflux for 18 h. Cool to RT. Add water and EtOAc and separate the layers. Dry organic layer over MgSO4, filter, and concentrate. Purify the residue (silica gel chromatography, eluting with EtOAc:CH2Cl2 mixtures) to give the desired compound (3.59 g).

1. temperatureHeat
2. temperatureto reflux for 18 h
3. customAdd water and EtOAc and separate the layers
4. filtrationDry organic layer over MgSO4, filter
5. concentrationconcentrate
6. customPurify
7. washthe residue (silica gel chromatography, eluting with EtOAc:CH2Cl2 mixtures)