反应详情

After (E)-3-(4-benzyloxy-3,5-difluoro-phenyl)-acrylic acid ethyl ester (2.5 g, 7.85 mmol) obtained in Step C of Preparation Example 2 was dissolved in THF (10 mL), diazomethane solution (94 mL, 23.55 mmol, 0.25M ether) was added thereto. After the reactant was cooled to 0˜5° C., palladium(II) acetate (0.29 g, 1.30 mmol) was added slowly thereto, and the mixture was stirred at room temperature for 5 hours. After the termination of the reaction, the reactant was added with water and then extracted. The organic layer was concentrated under reduced pressure and the residue was purified by column chromatography (eluent EtOAc/Hex=1/10) to obtain the title compound (2.27 g, 87%).

1. temperatureAfter the reactant was cooled to 0˜5° C.
2. customAfter the termination of the reaction
3. extractionextracted
4. concentrationThe organic layer was concentrated under reduced pressure
5. customthe residue was purified by column chromatography (eluent EtOAc/Hex=1/10)