反应详情

3-Methyl-4-isoxazolamine (38.0 mg, 0.28 mmol), 1-hydroxy-7-azabenzotriazole (30.7 mg, 0.23 mmol), EDC (43.3 mg, 0.23 mmol) and diisopropylethylamine (0.10 ml, 0.56 mmol) were added to a solution of 2-{[(4-fluorophenyl)methyl]oxy}-5-{1-[2-(4-morpholinyl)ethyl]-1H-pyrazol-4-yl}benzoic acid (may be prepared as described in Description 114; 80 mg, 0.19 mmol) in N,N-dimethylformamide (2 ml) and the reaction mixture was stirred at room temperature overnight. The DMF was removed on a buchi. The residue was taken up into ethyl acetate (50 ml) and washed with water (1×25 ml). The ethyl acetate layer was evaporated on a buchi under reduced pressure and the residue was purified using the MDAP. The solid obtained after concentrating the appropriate sample was taken up into ethyl acetate (50 ml) and washed with saturated bicarbonate (10 ml). The organic phase was dried (MgSO4) and evaporated to yield the title compound as a white solid. 15 mg.

1. customThe DMF was removed on a buchi
2. washwashed with water (1×25 ml)
3. customThe ethyl acetate layer was evaporated on a buchi under reduced pressure
4. customthe residue was purified
5. customThe solid obtained
6. concentrationafter concentrating the appropriate sample
7. washwashed with saturated bicarbonate (10 ml)
8. dry with materialThe organic phase was dried (MgSO4)
9. customevaporated