反应详情

To a solution of commercially available (1R,2S)-2-amino-3-fluoro-1-(4-iodophenyl)propan-1-ol (5.0 g, 20.0 mmol) in methanol (100 mL) is added triethylamine (9.56 mL, 67.8 mmol) and ethyldichloroacetate (6.22 mL, 50.8 mmol) and the mixture heated to reflux for 16 hours. After allowing to cool to room temperature, the solvent is removed under reduced pressure and the resultant oil purified by column chromatography eluting from neat heptanes to 80% ethylacetate/heptanes to give the title compound (5.94 g). m/z (Cl) M+H 405.

1. temperaturethe mixture heated
2. temperatureto reflux for 16 hours
3. customthe solvent is removed under reduced pressure
4. customthe resultant oil purified by column chromatography
5. washeluting from neat heptanes to 80% ethylacetate/heptanes