反应详情

To a solution of 3-(1H-Pyrrolo[2,3-b]pyridin-4-ylamino)-thiophene-2-carboxylic acid (2-amino-ethyl)-amide (40 mg, 0.12 mmol) and diisopropylethylamine (0.1 mL, 0.59 mmol) in methylene chloride (1.0 mL) was added benzoyl chloride (15 uL, 0.13 mmol) and stirred at room temperature for 30 min. The crude reaction was purified by ISCO Companion (silica, (silica, 0-5% methanol, methylene chloride, 1% ammonium hydroxide) to afford 3-(1H-Pyrrolo[2,3-b]pyridin-4-ylamino)-thiophene-2-carboxylic acid (2-benzoylamino-ethyl)-amide (48 mg, 48%). LCMS (ESI) 406 (M+H) 1H NMR (400 MHz, DMSO-d6) δ ppm 11.51 (1H, br. s.) 10.36 (1H, s) 8.55 (1H, s) 8.24 (1H, br. s.) 8.00 (1H, d, J=5.27 Hz) 7.73-7.85 (3H, m) 7.43-7.52 (2H, m) 7.35-7.42 (2H, m) 7.28 (1H, d, J=3.32 Hz) 6.82 (1H, d, J=5.47 Hz) 6.40 (1H, d, J=3.51 Hz) 3.39-3.45 (4H, m)

1. customThe crude reaction
2. customwas purified by ISCO Companion (silica, (silica, 0-5% methanol, methylene chloride, 1% ammonium hydroxide)