反应详情

Diethyl {[(4-methoxyphenyl)amino]methylene}malonate (63.5 g, 0.22 mol) was dissolved into POCl3 (300 mL, 3.0 mol), and the reaction mixture was heated at reflux for 16 h. After removal of solvent, toluene was added and the mixture was concentrated to remove remaining POCl3. The residue was diluted with DCM, washed with aqueous Na2CO3 and brine, dried over Na2SO4 and concentrated to give ethyl 4chloro-6methoxyquinoline-3-carboxylate (55.4 g, 96% yield) as a yellow solid which was used without further purification. LCMS: (FA) ES+ 266.1.

1. temperaturethe reaction mixture was heated
2. temperatureat reflux for 16 h
3. customAfter removal of solvent, toluene
4. additionwas added
5. concentrationthe mixture was concentrated
6. customto remove
7. additionThe residue was diluted with DCM
8. washwashed with aqueous Na2CO3 and brine
9. dry with materialdried over Na2SO4
10. concentrationconcentrated