反应详情

To a solution of 1-(4-aminophenyl)-N-cyclopropyl-5-propyl-1H-1,2,3-triazole-4-carboxamide (0.29 g) obtained in Example 1d) in acetonitrile (10 ml) were successively added methoxyacetic acid (0.08 ml), triethylamine (0.17 ml), HOBt (0.18 g) and WSC (0.23 g), and the mixture was stirred overnight at room temperature. The solvent was evaporated under reduced pressure, and the residue was dissolved in ethyl acetate and washed with saturated aqueous sodium hydrogen carbonate solution. The organic layer was dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column (ethyl acetate/hexane=1/1 to ethyl acetate), and the obtained product was recrystallized from ethanol-water to give the title compound as colorless needle crystals (0.16 g, 44%).

1. customThe solvent was evaporated under reduced pressure
2. dissolutionthe residue was dissolved in ethyl acetate
3. washwashed with saturated aqueous sodium hydrogen carbonate solution
4. dry with materialThe organic layer was dried over anhydrous magnesium sulfate
5. customthe solvent was evaporated under reduced pressure
6. customThe residue was purified by silica gel column (ethyl acetate/hexane=1/1 to ethyl acetate)
7. customthe obtained product was recrystallized from ethanol-water