反应详情

温度

130 °C

2-Cyclopentyl-N-(2-bromo-6-trifluoromethyl-4-morpholin-4-yl-phenyl)-acetamide (1b, 15 mg), 3-pyridylboronic acid (21 mg), aqueous potassium carbonate (5 M, 90 μL) and palladium(II) acetate (1 mg) were mixed in acetone (2 mL) and heated to 130° C. for 20 minutes in a sealed microwave process vial. The reaction mixture was filtered through silica (500 mg), concentrated in vacuo, redissolved in dimethyl sulfoxide (0.5 mL) and subjected to preparative LC-MS purification to furnish 2.7 mg (18% yield) of the title compound as a colorless oil. LC-MS (m/z) 434 (MH+); tR=1.89, (UV, ELSD) 99%, 99%.

1. filtrationThe reaction mixture was filtered through silica (500 mg)
2. concentrationconcentrated in vacuo
3. dissolutionredissolved in dimethyl sulfoxide (0.5 mL)
4. customsubjected to preparative LC-MS purification