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 3-pyridinamine (0.48 g, 5.13 mmol) were added to a solution of 2-{[(3,4-difluorophenyl)methyl]oxy}-5-formylbenzoic acid (may be prepared as described in Description 101; 1 g, 3.42 mmol) in N,N-dimethylformamide (25 ml), and the mixture was stirred at room temperature. The N,N-dimethylformamide was evaporated under reduced pressure and the residue was diluted with ethyl acetate (100 ml). The organic layer was 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 yellow solid. 1.19 g.

1. customThe N,N-dimethylformamide was evaporated under reduced pressure
2. additionthe residue was diluted with ethyl acetate (100 ml)
3. washThe organic layer was 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