반응 #678980

반응 방정식

2-amino-4,6-difluoro-benzamide

pyridine-4-carbaldehyde

sodium hydrogen sulfite

p-toluenesulfonic acid

→

5,7-difluoro-2-pyridin-4-yl-3H-quinazolin-4-one

용매

N,N-dimethylacetamide

반응 조건

후처리

1. 1
   기타The solvent was evaporated in vacuo, water
2. 2
   workup.ADDITIONwas added
3. 3
   여과the precipitated solid was filtered off

실험 절차

To a stirred solution of 2-amino-4,6-difluoro-benzamide (0.50 g, 2.9 mmol) and pyridine-4-carbaldehyde (0.35 g, 3.2 mmol) in N,N-dimethylacetamide (10 mL) were added sodium hydrogen sulfite (0.63 g, 3.5 mmol) and p-toluenesulfonic acid (0.06 g, 0.3 mmol); the reaction mixture was stirred at 115° C. for 16 hours. The solvent was evaporated in vacuo, water was added, and the precipitated solid was filtered off to obtain 5,7-difluoro-2-pyridin-4-yl-3H-quinazolin-4-one as a yellow solid, which was used in the next step without further purification. Yield: 0.4 g (53%).

출처