反应详情

温度

80 °C

(4-[(Cyclopropylamino)carbonyl]-1-{4-[(ethylamino)carbonyl]phenyl}-1H-1,2,3-triazol-5-yl)propyl methanesulfonate (218 mg, 0.5 mmol) obtained in Example 1201a), potassium carbonate (69 mg, 0.5 mmol, 1.0 eq.) and 2,2-difluoroethanol (0.5 ml) were suspended in acetonitrile (3 ml) and the mixture was stirred at 80° C. for 8 hr. The reaction mixture was concentrated, and chloroform (10 ml) and water (10 ml) were added to the residue. After partitioning, the organic layer was dried over anhydrous sodium sulfate, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column (hexane/ethyl acetate=1/1 to ethyl acetate) to give the title compound as a white powder (50 mg, 24%).

1. concentrationThe reaction mixture was concentrated
2. additionchloroform (10 ml) and water (10 ml) were added to the residue
3. customAfter partitioning
4. dry with materialthe organic layer was dried over anhydrous sodium sulfate
5. customthe solvent was evaporated under reduced pressure
6. customThe residue was purified by silica gel column (hexane/ethyl acetate=1/1 to ethyl acetate)