反应详情

To a solution of 4-(1-(2,4-difluorophenoxy)ethyl)benzoic acid (127 mg, 0.5 mmol) in dichloromethane (80 mL) was added N-hydroxybenzotriazole (101.25 mg, 0.75 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (144 mg, 0.75 mmol) and triethylamine (151 mg, 1.5 mm ol). then the 3-(aminomethyl)-4,6-dimethylpyridin-2-ol (76 mg, 0.5 mmol) was added, the solution was stirred at room temperature for 12 hours, water was added and washed 3 times, the organic layer was evaporated and the residue was purified by column chromatography (silica gel, dichloromethane/methanol=20:1) to give 4-(1-(2,4-difluorophenoxy)ethyl)-N-((2-hydroxy-4,6-dimethylpyridin-3-yl)methyl)benzamide (78 mg, 38%).

1. washwashed 3 times
2. customthe organic layer was evaporated
3. customthe residue was purified by column chromatography (silica gel, dichloromethane/methanol=20:1)