反应详情

1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)piperidine-4-carboxylic acid (365 mg, 0.920 mmol), 1-hydroxybenzotriazole (249 mg, 1.839 mmol) and EDCI (353 mg, 1.839 mmol) were dissolved in DCM (Volume: 3.0 ml). The suspension was stirred at room temperature for 10 minutes where it turned clear. Hunig'sBase (0.321 ml, 1.839 mmol) and pyridin-3-ylmethanamine (199 mg, 1.839 mmol) were added. The reaction was stirred at room temperature overnight. Solid precipitate formed overnight. The reaction was concentrated and triturated with ethyl acetate to afford product as a white solid. (Yield: 315 mg, white solid) 1H-NMR (400 MHz, DMSO-d6) 8.46, 8.40, 7.70-7.60, 7.54, 7.40-7.29, 7.21, 7.13-7.05, 6.73, 5.49, 4.38, 4.30, 4.04, 2.95, 2.47-2.39, 1.71, 1.42

1. stirringThe reaction was stirred at room temperature overnight
2. customSolid precipitate formed overnight
3. concentrationThe reaction was concentrated
4. customtriturated with ethyl acetate
5. customto afford product as a white solid