反应详情

温度

80 °C

To a solution of 8-bromo-6-cyclopropyl-[1,2,4]triazolo[1,5-a]pyridin-2-ylamine (300 mg, 1.29 mmol) and 4-chlorophenyl boronic acid (463 mg, 2.96 mmol) in dioxane (15 mL) was added an aqueous solution of Na2CO3 (2 M, 2 mL) and degassed with argon for 5 minutes. PdCl2 (dppf)2.CH2Cl2 (30.34 mg, 0.04 mmol) was added and stirred at 80° C. for 90 minutes. The reaction mixture was cooled to room temperature and water (20 mL) was added. The aqueous phase was extracted with ethyl acetate, the combined organic phases were dried over sodium sulfate, the solvent was evaporated and the residue purified by silica gel chromatography using ethyl acetate/hexane as eluent. The title compound was obtained as an off white solid (252 mg, 75%).

1. customdegassed with argon for 5 minutes
2. temperatureThe reaction mixture was cooled to room temperature
3. extractionThe aqueous phase was extracted with ethyl acetate
4. dry with materialthe combined organic phases were dried over sodium sulfate
5. customthe solvent was evaporated
6. customthe residue purified by silica gel chromatography