反应详情

温度

120 °C

To a solution of 5-bromopyrimidin-2-amine (2.1 g, 0.012 mol) in 1,4-dioxane (30 mL) was added (4-bromo-3-fluorophenyl)boronic acid (2.0 g, 0.0091 mol), potassium phosphate (6.4 g, 0.030 mol) and tetrakis(triphenylphosphine)palladium (700 mg, 0.6 mmol), water (5 mL). The solution was degassed with N2, and heated at 120° C. for 4 h. The mixture was cooled to RT, poured into water, and extracted with EtOAc. The combined organic layers were washed with brine, dried with MgSO4, filtered, and concentrated. The residue was purified by chromatography on silica gel with EtOAc in CH2Cl2 (0-30%) to afford the desired compound. LCMS: (M+H)=267.9.

1. customThe solution was degassed with N2
2. temperatureThe mixture was cooled to RT
3. additionpoured into water
4. extractionextracted with EtOAc
5. washThe combined organic layers were washed with brine
6. dry with materialdried with MgSO4
7. filtrationfiltered
8. concentrationconcentrated
9. customThe residue was purified by chromatography on silica gel with EtOAc in CH2Cl2 (0-30%)