反应详情

温度

80 °C

6-Bromo-4-chloro-3-methanesulfonyl-2-methyl-quinoline (compound of example D.1) (11.5 g, 34.4 mmol), morpholine (3.3 mL, 37.8 mmol) and N,N-diisopropyl ethyl amine (6.5 mL, 37.8 mmol) were heated at 100° C. in dry N,N-dimethylformamide (10 mL) for 30 min. The reaction mixture was evaporated to dryness, and the residue extracted with dichloromethane, 10% Na2CO3 and sat. NaCl. The crude product was stirred and heated at 80° C. in ethyl acetate (80 mL) for 10 min, the resulting suspension was cooled in ice, the crystals were filtered off and washed with little cold ethyl acetate. One obtained 10.8 g (81%) of white crystals. MS: m/z=385/387 (M+H).

1. customThe reaction mixture was evaporated to dryness
2. extractionthe residue extracted with dichloromethane, 10% Na2CO3 and sat. NaCl
3. temperaturethe resulting suspension was cooled in ice
4. filtrationthe crystals were filtered off
5. washwashed with little cold ethyl acetate