反应详情

EDC (122 mg, 0.64 mmol), 3-pyridinamine (59.9 mg, 0.64 mmol), HOBT (63.4 mg, 0.41 mmol) and diisopropylethylamine (0.11 ml, 0.64 mmol) were added to a solution of 2-{[(4-fluorophenyl)methyl]oxy}-5-(trifluoromethyl)benzoic acid (may be prepared as described in Description 119; 100 mg, 0.32 mmol) in N,N-dimethylformamide (5 ml) and the mixture was stirred at room temperature overnight. The mixture was then heated to 70° C. for 5 hours. The mixture was diluted with water (25 ml) and extracted with ethyl acetate (3×25 ml). The organics were combined, evaporated under reduced pressure on a buchi and the residue was purified using an MDAP to yield the title compound. 85 mg.

1. temperatureThe mixture was then heated to 70° C. for 5 hours
2. extractionextracted with ethyl acetate (3×25 ml)
3. customevaporated under reduced pressure on a buchi
4. customthe residue was purified