反应详情

Ethyl 2-((4-fluorophenyl)(methyl)amino)-2-phenylacetate (I5) (0.59 g, 2.05 mmol) was dissolved in a mixture THF (10 ml) and water (10 ml), and lithium hydroxide hydrate (0.26 g, 6.14 mmol) was added. The reaction was stirred at room temperature for 3.5 hours and then at 70° C. for 24 hours. 3N HCl was added till pH was about 1, and the mixture was evaporated. Water (15 ml) was added, and the residue was triturated obtaining a pale brown suspension that was filtered on a buckner funnel washing with water and then with acetonitrile. The solid was dried under vacuum at 40° C. overnight to obtain intermediate I6 (0.44 g, 72% yield).

1. additionwas added
2. waitat 70° C. for 24 hours
3. customthe mixture was evaporated
4. additionWater (15 ml) was added
5. customthe residue was triturated
6. customobtaining a pale brown suspension that
7. filtrationwas filtered on a buckner funnel
8. washwashing with water
9. customThe solid was dried under vacuum at 40° C. overnight
10. customto obtain intermediate I6 (0.44 g, 72% yield)