反应详情

温度

80 °C

To a solution of 6-chloro-5-fluoroindole (1.8 g, 10.8 mmol) and Ac2O (10 mL) in AcOH (30 mL) was added L-serine (2.2 g, 20.9 mmol), the mixture was heated to 80° C. After TLC indicated the reaction was complete, the mixture was cooled to 0° C., neutralized to pH 11, and washed with MTBE. The aqueous phase was acidified to pH 2 and extracted with EtOAc. The combined organic layers were washed with water and brine, dried with Na2SO4, filtered, and concentrated. The residue was purified with chromatography (Petroleum ether/EtOAc 1:1) to give 2-acetylamino-3-(6-chloro-5-fluoro-1H-indol-3-yl)-proprionic acid as a light yellow solid (1.2 g, 37% yield).

1. temperaturethe mixture was cooled to 0° C.
2. washwashed with MTBE
3. extractionextracted with EtOAc
4. washThe combined organic layers were washed with water and brine
5. dry with materialdried with Na2SO4
6. filtrationfiltered
7. concentrationconcentrated
8. customThe residue was purified with chromatography (Petroleum ether/EtOAc 1:1)