反应详情

To a solution of 1-{4-[(ethylamino)carbonyl]phenyl}-5-propyl-1H-1,2,3-triazole-4-carboxylic acid (0.40 g) obtained in Example 43b) in acetonitrile-DMF (7:2, 9 ml) were successively added cyclopropylamine (0.11 ml), triethylamine (0.22 ml), HOBt (0.24 g) and WSC (0.30 g), and the reaction mixture was stirred overnight at room temperature. The solvent was evaporated under reduced pressure, the residue was dissolved in ethyl acetate and washed with saturated aqueous sodium hydrogen carbonate solution. The organic layer was dried over anhydrous sodium 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) to give the title compound as a white powder (0.20 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 sodium 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)