反应详情

温度

100 °C

After degassing with N2, a mixture of methyl 4-bromo-8-fluoro-7-methylquinoline-2-carboxylate (7-16, 650 mg, 2.18 mmol.), 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (544 mg, 2.62 mmol) Pd(dppf)Cl2—CH2Cl2 adduct (89 mg, 0.11 mmol), and K3PO4 (1388 mg, 6.54 mmol) in 1,4-dioxane (12.9 mL) and H2O (1.6 mL) was heated at 100° C. for 20 min under microwave condition. After cooling to room temperature, the reaction mixture was filtered and concentrated. The residue was purified by column chromatography on silica gel, eluting with EtOAc/Hexane (0-100%) to afford methyl 8-fluoro-7-methyl-4-(1-methyl-1H-pyrazol-4-yl)quinoline-2-carboxylate (7-17, 481 mg, 74%). LRMS m/z (M+H)+ 300.3 found, 300.1 require.

1. customAfter degassing with N2
2. temperatureAfter cooling to room temperature
3. filtrationthe reaction mixture was filtered
4. concentrationconcentrated
5. customThe residue was purified by column chromatography on silica gel
6. washeluting with EtOAc/Hexane (0-100%)