反应详情

温度

0 °C

5-Methoxy-1-(4-methoxyphenyl)-1-H-indole (50 mg, 0.2 mmol), prepared by the method of example 1C, is dissolved in 1 mL of CH2Cl2 at 0° C. Et2AlCl (300 μL, 1M in hexanes, 0.3 mmol) is then added. After stirring at 0° C. for 30 min, a solution of acetyl chloride (22 mL, 0.3 mmol) in 1 mL of CH2Cl2 is added dropwise. This is stirred at 0° C. for a further 90 min. The reaction mixture is quenched with H2O and is extracted with CH2Cl2 and concentrated in vacuo. Purification by column chromatography on silica gel EtOAc/CH2Cl2 (5/95) yields the title compound as a white solid (42 mg, 71%).

1. stirringThis is stirred at 0° C. for a further 90 min
2. customThe reaction mixture is quenched with H2O
3. extractionis extracted with CH2Cl2
4. concentrationconcentrated in vacuo
5. customPurification by column chromatography on silica gel EtOAc/CH2Cl2 (5/95)