反应详情

温度

125 °C

N-(2-Bromo-4,6-dimethyl-phenyl)-2-(4-fluoro-phenyl)-acetamide (1c, 15.1 mg), 3-aminobenzeneboronic acid (30.8 mg), aqueous potassium carbonate (5 M, 90 uL) and palladium(II) acetate (1 mg) were mixed in acetone (2 mL) and heated to 125° C. for 15 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 14.9 mg (95% yield) of the title compound as an oil. LC-MS (m/z) 349 (MH+); tR=1.92, (UV, ELSD) 98%, 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