反应详情

A mixture of ethyl-2-(2-chloro-5-{[(tert-butoxycarbonyl)-amino]-methyl}-phenylamino)-6-(2,2-difluoro-ethoxy)-1-methyl-1H-benzimidazole-5-carboxylate (1.35 g; 2.50 mmol), NaOH (4 mL; 2 M aq; 8 mmol) and 1,4-dioxane (15 mL) was refluxed for 3 h. After cooling to rt the mixture was acidified to pH ˜5-6 and extracted with EtOAc. The organic extracts were dried over Na2SO4, filtered and concentrated. The residue was washed with Et2O to give the sub-title compound. Yield: 1.12 g (88%).

1. temperaturewas refluxed for 3 h
2. extractionextracted with EtOAc
3. dry with materialThe organic extracts were dried over Na2SO4
4. filtrationfiltered
5. concentrationconcentrated
6. washThe residue was washed with Et2O