反应详情

温度

85 °C

1-(2-Fluoroethyl)piperazine diTFA salt (464 mg, 1.29 mmol), (prepared as described for the starting material in Example 27), was dissolved in acetonitrile (3.5 ml). Potassium carbonate (889 mg, 6.44 mmol) and 2-bromoethanol (95 μl, 1.34 mmol) were added and the mixture heated to 85° C. and left overnight. More bromoethanol (95 μl, 1.34 mmol) was added and the reaction mixture heated at 85° C. for a further 2 hours. The reaction mixture was cooled, filtered and concentrated. The residue was purified by column chromatography eluting with methylene chloride/methanol (saturated with ammonia) (92/8) to give 2-[4-(2-fluoroethyl)piperazin-1-yl]ethanol (151 mg, 66%).

1. temperaturethe reaction mixture heated at 85° C. for a further 2 hours
2. temperatureThe reaction mixture was cooled
3. filtrationfiltered
4. concentrationconcentrated
5. customThe residue was purified by column chromatography
6. washeluting with methylene chloride/methanol (saturated with ammonia) (92/8)