反应详情

A mixture of 1-(2-dimethylamino-ethyl)-1H-indazol-6-ylamine (484 mg, 2 mmol), 4-benzyloxy-phenylacetic acid (200 mg, 2 mmol), ethyldimethylpropylcarbodiimide hydrochloride (460 mg, 2.4 mmol), N-hydroxybenzotriazole (324 mg, 2.4 mmol), and N-methyl morpholine (513 mg, 4.8 mmol) in DMF (15 mL) was stirred at room temperature for 6 hours and concentrated under reduced pressure The residue was purified by flash chromatography (Silica gel, ethyl acetate/triethylamine, 30/1) to provide the title compound as a pale yellow solid (95%). 1H NMR (300 MHz, DMSO-d6) ppm 2.15 (s, 6H), 2.66 (t, J=6.44, 2H), 3.60 (s, 2H), 4.35 (t, J=6.44, 2H), 5.09 (s, 2H), 6.98 (d, J=8.82, 2H), 7.14 (m, 1H), 7.25–7.45 (m, 6H), 7.65 (m, 1H), 7.94 (m, 1H), 7.94 (s, 1H), 7.95 (s, 1H), 8.12 (s, 1H); MS (DCI/NH3) m/z 429 [M+H]+.

1. concentrationconcentrated under reduced pressure The residue
2. customwas purified by flash chromatography (Silica gel, ethyl acetate/triethylamine, 30/1)