反应详情

温度

65 °C

tert-Butyl 6-bromo-8-nitro-2-oxo-1,2,3,4-tetrahydroquinolin-3-ylcarbamate (628 g) was added to ethanol (3.1 L), and the mixture was heated at 65° C. To the mixture, 10% Pd—C (water content: 53%) (67.1 g) and ammonium formate (1.03 kg) were sequentially added, and the resultant mixture was stirred for 10 minutes under heating and reflux. Tetrahydrofuran (2.5 L) was added to the reaction mixture so as to dissolve the precipitates, and undissolved matter was removed through filtration with Celite. The filtrate was concentrated under reduced pressure, and water was added to the residue. The formed precipitates were recovered through filtration. The thus-obtained solid was dried, whereby the title compound (418 g) was yielded as a powdery compound.

1. temperatureunder heating
2. temperaturereflux
3. dissolutionto dissolve the precipitates, and undissolved matter
4. customwas removed through filtration with Celite
5. concentrationThe filtrate was concentrated under reduced pressure, and water
6. additionwas added to the residue
7. customThe formed precipitates
8. filtrationwere recovered through filtration
9. customThe thus-obtained solid was dried