Pyrophosphoric acid → 2-Cyclopropyl-4-(4'-fluorophenyl)quinoline-3-carbonitrile

Participants

Reaction Steps

Into a glass flask having an internal volume of 10 mL, equipped with a stirring apparatus, a thermometer, a reflux condenser and a Dean-Stark apparatus, 5 mL of diisopropyl ether was put in an atmosphere of nitrogen, and 0.82 g (4.6 mmol) of pyrophosphoric acid, 0.29 g (2.5 mmol) of 3-cyclopropyl-3-oxopropanenitrile and 0.50 g (2.3 mmol) of 2-amino-4′-fluorobenzophenone were added thereto with stirring at room temperature. Then, the temperature was raised to 70° C., and reaction was carried out for 3 hours. After completion of the reaction, the reaction liquid was cooled to room temperature, and analyzed by high performance liquid chromatography (absolute quantitative analysis), whereupon 0.60 g (yield: 91%) of 2-cyclopropyl-4-(4′-fluorophenyl)quinoline-3-carbonitrile was formed.

Provenance & Evidence