反应详情

温度

95 °C

To a solution of 3-iodoaniline in DME (40 mL) and water (20 mL), was added para-trifluoromethylphenyl boronic acid (2.6 g, 13.7 mmol) and sodium carbonate (2.5 g, 23.6 mmol). The apparatus was flushed with nitrogen prior to the addition of tetrakis (triphenylphosphine) palladium (0) (0.312 g, 0.27 mmol). The reaction mixture was stirred at 95° C. for 17 h under nitrogen, then allowed to cool to rt and the solvents removed in vacuo. The residue was partitioned between EtOAc (2×75 mL) and water (75 mL). The organic solution was dried (MgSO4) and the solvent was removed in vacuo. Purification by Biotage™ chromatography (90 g Silica column) eluted with 1:4 EtOAc:cyclohexane afforded the title compound as a white solid (1.33 g).

1. customThe apparatus was flushed with nitrogen
2. temperatureto cool to rt
3. customthe solvents removed in vacuo
4. customThe residue was partitioned between EtOAc (2×75 mL) and water (75 mL)
5. dry with materialThe organic solution was dried (MgSO4)
6. customthe solvent was removed in vacuo
7. customPurification by Biotage™ chromatography (90 g Silica column)
8. washeluted with 1:4 EtOAc