反应详情

EDC (0.79 g, 4.11 mmol), HOBT (0.84 g, 5.48 mmol), N-ethylmorpholine (0.87 mL, 6.84 mmol) and 4-pyridazinamine (0.49 g, 5.13 mmol) were added to a solution of 2-{[(3,4-difluorophenyl)methyl]oxy}-5-formylbenzoic acid (may be prepared by Description 101; 1 g, 3.42 mmol) in N,N-dimethylformamide (DMF; 25 ml) and the mixture was stirred at room temperature. The DMF was evaporated under reduced pressure and the residue was diluted with ethyl acetate (100 ml) and the organic layer washed with saturated sodium hydrogencarbonate (2×50 ml) and water (2×50 ml). The organic layer was dried (MgSO4), filtered and evaporated under reduced pressure to yield the title compound as a dark yellow solid. 0.98 g.

1. customThe DMF was evaporated under reduced pressure
2. additionthe residue was diluted with ethyl acetate (100 ml)
3. washthe organic layer washed with saturated sodium hydrogencarbonate (2×50 ml) and water (2×50 ml)
4. dry with materialThe organic layer was dried (MgSO4)
5. filtrationfiltered
6. customevaporated under reduced pressure