57356-66-8

110-91-8

1722-12-9

57356-66-8

GENERAL STEPS: The Buchwald-Hartwig amination reaction was carried out in a CEM Discover microwave reaction apparatus. To a 10 mL PTFE reaction tube, 1.0 mmol of 2-chloropyrimidine, 3.0 mmol of morpholine, 2.0 mmol of base, 0.05 mmol of palladium(II) acetate, 0.10 mmol of ligand LHX and 2.0 mL of solvent were added sequentially. The reaction mixture was subjected to microwave radiation set at a power of 150 W and a temperature of 100 °C for a specified time and then cooled to room temperature. The reaction mixture was extracted with ether three times, the organic phases were combined, washed with water, dried with anhydrous magnesium sulfate and concentrated under reduced pressure to remove the solvent. The crude product was purified by silica gel column chromatography to afford the target compound 4-(pyrimidin-2-yl)morpholine.