反应详情

温度

70 °C

To 5-bromo-7-azaindole (1, 1.04 g, 5.28 mmol) in 1.00 M potassium carbonate in water (15.8 mL) and tetrahydrofuran (50.0 mL) were added 1-methyl-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyrazole (108, 1.65 g, 7.92 mmol), Tetrakis(triphenylphosphine)-palladium(0) (0.305 mg, 0.26 mmol) and tetra-n-butylammonium iodide (0.20 g, 0.53 mmol). The reaction mixture was stirred at 70° C. overnight. The reaction mixture was poured into water and the organic layer was washed with brine, dried over sodium sulfate, and concentrated. The residue was purified with silica gel column chromatography eluting with 25% ethyl acetate in hexane to provide a light yellow solid (109, 670 mg, 64.0%). MS (ESI) [M+H+]+=199.4.

1. washthe organic layer was washed with brine
2. dry with materialdried over sodium sulfate
3. concentrationconcentrated
4. customThe residue was purified with silica gel column chromatography
5. washeluting with 25% ethyl acetate in hexane
6. customto provide a light yellow solid (109, 670 mg, 64.0%)