反应详情

温度

160 °C

A solution of 2-bromo-8-(4-chloro-phenyl)-6-cyclopropyl-[1,2,4]triazolo[1,5-a]pyridine (50 mg, 0.14 mmol), 1-(6-methyl-pyrimidin-4-yl)-piperidin-4-ylamine (see example 94a, 23 mg, 0.12 mmol) and sodium phenoxide (21 mg, 0.2 mmol) in dry 1,4-dioxane (3 mL) in a sealed tube was purged with argon for 10 minutes. Pd2(dba)3.CHCl3 (8 mg, 0.01 mmol) and xanthphos (2 mg) were added to the solution and stirred at 160° C. for 15 hours. The reaction mixture was cooled to room temperature and water (10 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 dichloromethane/methanol as eluent. The title compound was obtained as a light brown solid (5 mg, 8%).

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