反应详情

Potassium carbonate (800 mg, 5.8 mmol) followed by potassium iodide (30 mg, 0.2 mmol) and morpholine (500 μl, 5.7 mmol) were added to a solution of 5-(2-chloroacetyl)oxindole (1.05 g, 5 mmol), (J. Med. Chem. 1991, 1860), in DMF (20 ml) and the mixture was stirred for 1 hour at ambient temperature. The solvent was removed by evaporation and the residue was purified by reverse phase column chromatography on a Diaion (trade mark of Mitsubishi) HP20SS resin column, eluting with water/methanol (a gradient from 100/0 to 30/70). The purified product was then purified by chromatography on silica eluting with methylene chloride/methanol (95/5) to give 5-(2-morpholinoacetyl)oxindole (673 mg, 51%).

1. customThe solvent was removed by evaporation
2. customthe residue was purified by reverse phase column chromatography on a Diaion (trade mark of Mitsubishi) HP20SS resin column
3. washeluting with water/methanol (a gradient from 100/0 to 30/70)
4. customThe purified product was then purified by chromatography on silica eluting with methylene chloride/methanol (95/5)