Cesium carbonate → HCID 53380231, compound

Participants

Reaction Conditions

Reaction Steps

4-(4,6-dichloropyrimidin-2-yl)morpholine (100 mg 0.43 mmol), pyridine-3-boronic acid (49 mg, 0.4 mmol), Cs2CO3 (280 mg, 0.86 mmol) and Pd(PPh3)2Cl2 (20 mg, 0.025 mmol) were combined in dioxane (3 ml) and water (1 ml). The reaction mixture was then heated by microwave at 120° C. for 20 min. Without purification (4-(3-cyclopropylureido)phenyl)boronic acid pinacol ester (130 mg, 0.43 mmol), Cs2CO3 (280 mg, 0.86 mmol) and Pd(PPh3)2Cl2 (20 mg, 0.025 mmol) were added and the reaction mixture was then heated by microwave at 120° C. for a further 20 min. The reaction mixture was partitioned between EtOAc and water. The organic layer was passed through a PTFE hydrophobic frit and the solvent removed in vacuo. Residual solid was triturated to give crude produect which was further purifed by prep LC/MS (low pH) to yield (9 mg, 5%).

Provenance & Evidence