反应详情

A mixture of 113.5 g (2.45 mole) of 99% formic acid and 200 ml of formaldehyde (36.5% w/v) is added, under stirring and by cooling at 15°-20° C., to a solution of 100 g (0.49 mole) of 3-amino-6,7-dimethoxyquinoline (prepared according to J. Med. Chem., 22, 1005, 1979) in 400 ml of N,N-dimethylformamide. The thus obtained mixture is refluxed for 6 hours, then water is added, the pH is adjusted to 10 with 40% NaOH and the mixture is extracted with ethyl acetate.

1. additionis added
2. temperatureThe thus obtained mixture is refluxed for 6 hours
3. extractionthe mixture is extracted with ethyl acetate