反应详情

Ethyl 2-(6-amino-1H-indol-1-yl)acetate (intermediate B) (7.66 mmol, 1 equiv.) was dissolved in benzene (30 ml), and methyl 2-(bromo-methyl)-6-methylbenzoate (8.42 mol, 1.1 equiv.) and TEA (9.19 mmol, 1.2 equiv.) were added at 25° C. and the mixture was refluxed for 12 h. The reaction mixture was reduced under reduced pressure and the residue was taken up in dichloromethane (30 ml), washed with water and sat. NaCl solution (5 ml), dried over sodium sulfate and concentrated under reduced pressure. The crude product was purified by column chromatography (10% ethyl acetate in hexane). Yield: 64%

1. temperaturethe mixture was refluxed for 12 h
2. washwashed with water and sat. NaCl solution (5 ml)
3. dry with materialdried over sodium sulfate
4. concentrationconcentrated under reduced pressure
5. customThe crude product was purified by column chromatography (10% ethyl acetate in hexane)