反应详情

7-Amino-8,9-difluoro-2-methyl-6-oxo-1,2-dihydro-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acid (0.5 g) and 4-hydroxypiperidine (1.0 g) are suspended in N-methylpyrrolidone (5 ml), and the mixture is heated at 110°-120° C. for 5 hours. The reaction mixture is concentrated to dryness under reduced pressure, and to the residue is added ethanol. The resulting crystals are separated by filtration and recrystallized from N,N-dimethylformamide to give 7-amino-8-fluoro-9-(4-hydroxy-1-piperidyl)-2-methyl-6-oxo-1,2-dihydro-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acid (0.2 g) as yellow cubic crystals. m.p. 287°-292° C. (decomp.)

1. temperaturethe mixture is heated at 110°-120° C. for 5 hours
2. concentrationThe reaction mixture is concentrated to dryness under reduced pressure
3. additionto the residue is added ethanol
4. customThe resulting crystals are separated by filtration
5. customrecrystallized from N,N-dimethylformamide