反应详情

温度

90 °C

N-(3-Bromo-5-(trifluoromethyl)phenyl)methanesulfonamide (1.33 g, 4.06 mmol), bis(pinacolato)diboron (4.12 g, 16.22 mmol), potassium acetate (2 g, 20.38 mmol), bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex (500 mg, 0.61 mmol) and 1,1′-bis(diphenylphosphino)ferrocene (340 mg, 0.61 mmol) were suspended in dioxane (35 ml) and stirred at 90° C. for 48 h. After evaporation of the solvent under reduced pressure, ethyl acetate (100 ml) was added to the residue and the precipitated salts were eliminated by filtration. The solvent was evaporated under reduced pressure to give 6.39 g (100% yield) of the title compound as a mixture of (3-(methylsulfonamido)-5-(trifluoromethyl)phenyl)boronic acid and N-(3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5-(trifluoromethyl)phenyl)methanesulfonamide that was used in next step without further purification. (1:1). Estimated Purity: 24%

1. customAfter evaporation of the solvent under reduced pressure, ethyl acetate (100 ml)
2. additionwas added to the residue
3. filtrationthe precipitated salts were eliminated by filtration
4. customThe solvent was evaporated under reduced pressure