反应详情

2-(5-Trifluoromethyl-pyridin-2-yl)-benzoic acid (325 mg, 1.05 mmol) was dissolved in 15 ml of thionyl chloride, and the mixture heated at 60 C. After 4 h, the volatiles were removed under vacuum, the residue combined with 7-amino-quinoline-3-carboxylic acid ethyl ester (100 mg, 0.46 mmol), dissolved in 1,2-dichloroethane (15 ml), and diisopropylethylamine (300 mg, 2.31 mmol) added. After heating at reflux for 48 h, the reaction mixture was washed with 1N HCl, dried (magnesium sulfate), filtered, and concentrated under vacuum. The resulting residue was purified by silica gel chromatography eluting with 50% ethyl acetate in hexanes to provide 180 mg (85%) of the title compound.

1. temperaturethe mixture heated at 60 C
2. customthe volatiles were removed under vacuum
3. temperatureAfter heating
4. temperatureat reflux for 48 h
5. washthe reaction mixture was washed with 1N HCl
6. dry with materialdried (magnesium sulfate)
7. filtrationfiltered
8. concentrationconcentrated under vacuum
9. customThe resulting residue was purified by silica gel chromatography
10. washeluting with 50% ethyl acetate in hexanes