反应详情

A solution of 4-[(3,4-dichloro-6-fluorophenyl)amino]-6-nitroquinazoline (1.09 mmol) in 18 ml 9:1 ethanol:water and 11 ml iso-propylalcohol was heated to reflux temperature. 250 μl hydrazine hydrate and 0.5 ml Raney®Nickel (in water) were added thereafter. After 30 minutes, additional 50 μl of hydrazine hydrate was added, and the reflux was maintained for 20 minutes. Filtration, evaporation and silica gel chromatography (using 90% CH2Cl2/10% MeOH as elute) gave 4-[(3,4-dichloro-6-fluorophenyl)amino]-6-aminoquinazoline (compound 2) in 75% yield.

1. temperatureto reflux temperature
2. temperaturethe reflux was maintained for 20 minutes
3. filtrationFiltration, evaporation and silica gel chromatography (using 90% CH2Cl2/10% MeOH as elute)