反应详情

3-(Trifluoromethyl)benzaldehyde (21.54 g, 124 mmol) was added to a solution of 4-bromo-3-(methyloxy)aniline (25 g, 124 mmol) in ethanol (300 mL) dropwise. The mixture was stirred at reflux for 1 h, and 2-oxobutanoic acid (12.63 g, 124 mmol) was added portionwise. The reaction mixture was stirred at reflux for additional 3 h, cooled to room temperature, and stirred overnight. The mixture was filtered to collect the precipitate, and the solid was washed with ethanol and dried to give 6-bromo-3-methyl-7-(methyloxy)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxylic acid (42.6 g, 78% yield). This material was used without further purification. MS (m/z) 442.0 (M+H+).

1. temperatureat reflux for 1 h
2. stirringThe reaction mixture was stirred
3. temperatureat reflux for additional 3 h
4. stirringstirred overnight
5. filtrationThe mixture was filtered
6. customto collect the precipitate
7. washthe solid was washed with ethanol
8. customdried