反应详情

温度

90 °C

4-Bromo-2-fluoro-3-trifluoromethylaniline (5.0 g, 19.4 mmol), cyclopropylboronic acid (2.16 g, 25.2 mmol), K3PO4 (14.4 g, 67.8 mmol) and tricyclohexyl phosphine (0.54 g, 1.9 mmol) are dissolved in toluene (80 mL) and water (4 mL). The solution is degassed with N2, heated to 90° C., and Pd(OAc)2 (0.22 g, 1.0 mmol) is added. The reaction is heated at 90° C. for 5 hours, cooled, diluted with Et2O, filtered, washed with brine, dried (Na2SO4) and concentrated in vacuo. The residue is purified by column chromatography (EtOAc/hexanes) to give 4-cyclopropyl-2-fluoro-3-trifluoromethylaniline.

1. customThe solution is degassed with N2
2. temperatureThe reaction is heated at 90° C. for 5 hours
3. temperaturecooled
4. filtrationfiltered
5. washwashed with brine
6. dry with materialdried (Na2SO4)
7. concentrationconcentrated in vacuo
8. customThe residue is purified by column chromatography (EtOAc/hexanes)