反应详情

温度

100 °C

To a solution of 5-bromo-3-(5-isopropyl-[1,3,4]oxadiazol-2-yl)-pyridin-2-ylamine (250 mg, 0.883 mmol) in dioxane (15 mL) and water (7 mL) were added K2CO3 (365 mg, 2.649 mmol), indole-5-boronic acid (156 mg, 0.971 mmol) in a sealed tube. The reaction mixture was degassed by N2 for 20 min, then Pd(PPh3)4 (102 mg, 0.088 mmol) was added and stirred for 18 h at 100° C. Water (20 mL) was added and extracted with ethyl acetate (3×20 mL) and the organic layer was washed with brine, dried over anhydrous sodium sulphate, and concentrated under reduced pressure. Crude product was purified by column chromatography using 100-200 mesh silica gel compound eluted with 40% ethyl acetate in petroleum ether to afford the title compound as a yellow solid.

1. customThe reaction mixture was degassed by N2 for 20 min
2. extractionextracted with ethyl acetate (3×20 mL)
3. washthe organic layer was washed with brine
4. dry with materialdried over anhydrous sodium sulphate
5. concentrationconcentrated under reduced pressure
6. customCrude product was purified by column chromatography
7. washeluted with 40% ethyl acetate in petroleum ether