反应详情

温度

95 °C

A screw-cap vial was charged with 2,4-dichloro-5,7-difluoro-3-methylquinoline (600 mg, 2.42 mmol), 5-(methylthio)pyridin-3-ylboronic acid (429 mg, 2.54 mmol), dichlorobis(triphenylphosphine)palladium (II) (170 mg, 0.24 mmol), sodium carbonate (769 mg, 7.26 mmol), 1,4-dioxane (6.5 mL), and water (1.6 mL). The mixture was stirred at 95° C. for 2 h, then cooled to rt and partitioned between EtOAc and water. The organic layer was washed with brine, dried over magnesium sulfate, and cond. The crude product was purified by flash chromatography (silica gel, 0-30% EtOAc in hexanes), affording 4-chloro-5,7-difluoro-3-methyl-2-(5-(methylthio)pyridin-3-yl)quinoline. Mass Spectrum (ESI) m/e=337.0 (M+1).

1. temperaturecooled to rt
2. custompartitioned between EtOAc and water
3. washThe organic layer was washed with brine
4. dry with materialdried over magnesium sulfate, and cond
5. customThe crude product was purified by flash chromatography (silica gel, 0-30% EtOAc in hexanes)