反应详情

温度

125 °C

A mixture of 5-fluoroisatin (702 mg, 4.25 mmol) and 1-(2-chloro-4-(morpholinomethyl)phenyl)ethanone (1.08 g, 4.25 mmol) (preparation 17) was prepared in EtOH/water (1:1) (10 ml) and then KOH (2.38 g, 42.49 mmol) was added and the resulting mixture heated under microwave irradiation at mw, 125° C. for 20 mins. The mixture was then diluted with water (10 ml) acidified to pH3 with 2M aqueous HCl, stirred for 16 h at room temperature and the resulting precipitate filtered, washed with water (2×10 ml) and concentrated under reduced pressure to afford 2-(2-chloro-4-(morpholinomethyl)phenyl)-6-fluoroquinoline-4-carboxylic acid as an orange solid (503 mg, 1.25 mmol, 30%).

1. filtrationthe resulting precipitate filtered
2. washwashed with water (2×10 ml)
3. concentrationconcentrated under reduced pressure