反应详情

To a solution of 4-(4-chloropyrimidin-2-yl)morpholine (80 mg, 0.40 mmol) and (4-(3-cyclopropylureido)phenyl)boronic acid pinacol ester (145 mg, 0.48 mmol) in dioxane (2 mL) was added Pd(PPh3)2Cl2 (14 mg, 0.02 mmol) and Cs2CO3 (2M aq solution, 0.3 mL). The reaction mixture was then heated to reflux for 16 h. The crude reaction mixture was then partitioned between water and EtOAc, the phases separated and the organic layer washed with aqueous NaHCO3 and brine, dried over magnesium sulfate, filtered and the solvent removed in vacuo. The residue was purified by flash chromatography (0-5% EtOAc/MeOH) to yield a white solid (7.8 mg, 6%).

1. temperatureThe reaction mixture was then heated
2. temperatureto reflux for 16 h
3. customThe crude reaction mixture
4. customwas then partitioned between water and EtOAc
5. customthe phases separated
6. washthe organic layer washed with aqueous NaHCO3 and brine
7. dry with materialdried over magnesium sulfate
8. filtrationfiltered
9. customthe solvent removed in vacuo
10. customThe residue was purified by flash chromatography (0-5% EtOAc/MeOH)