反应详情

2-(4-{[7-(benzyloxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)-N-(2,3-difluorophenyl)acetamide (836 mg, 1.60 mmol) was dissolved in trifluoroacetic acid (8 ml) and heated under reflux for 2.5 hours. The solution was concentrated and the residual oil was dissolved in methanol and neutralised with an aqueous solution of sodium bicarbonate. Water was added to the mixture and the solid recovered by filtration and dried in vacuo to yield N-(2,3-difluorophenyl)-2-{4-[(7-hydroxyquinazolin-4-yl)amino]-1H-pyrazol-1-yl}acetamide (633 mg, 100% yield):

1. temperatureheated
2. temperatureunder reflux for 2.5 hours
3. concentrationThe solution was concentrated
4. dissolutionthe residual oil was dissolved in methanol and neutralised with an aqueous solution of sodium bicarbonate
5. additionWater was added to the mixture
6. filtrationthe solid recovered by filtration
7. customdried in vacuo