反应详情

1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)piperidine-4-carboxylic acid (317 mg, 0.799 mmol), 1-hydroxybenzotriazole (135 mg, 0.999 mmol), and EDC (191 mg, 0.999 mmol) were dissolved in 2.0 mL of DCM. The reaction was allowed to stir at room temperature for 10 minutes before adding (2,3-dihydrofuro[2,3-c]pyridin-3-yl)methanamine (100 mg, 0.666 mmol) as a DCM solution and Hunig'sBase (0.174 mL, 0.999 mmol). The reaction was allowed to stir at room temperature overnight. The reaction was diluted with water and ethyl acetate. The organic layer was washed with saturated sodium bicarbonate and saturated sodium chloride solution. It was dried over magnesium sulfate, filtered and concentrated. The crude material was triturated in ethyl acetate, filtered and concentrated to obtain white solid. (Yield: 176 mg, white solid) 1H-NMR (500 MHz, DMSO-d6) 8.13-8.04, 7.63, 7.55, 7.37-7.28, 7.22, 7.13-7.02, 6.72, 5.47, 4.59, 4.47-4.28, 4.13-3.85, 3.73-3.62, 3.17, 3.07-2.76, 2.41-2.31, 1.79-1.20

1. stirringto stir at room temperature overnight
2. washThe organic layer was washed with saturated sodium bicarbonate and saturated sodium chloride solution
3. dry with materialIt was dried over magnesium sulfate
4. filtrationfiltered
5. concentrationconcentrated
6. customThe crude material was triturated in ethyl acetate
7. filtrationfiltered
8. concentrationconcentrated
9. customto obtain white solid