反应详情

To a mixture of 1.15 g of WSC and 8 ml of pyridine, 1.43 g of 3-tert-butoxycarbonylamino isonicotinic acid was added and stirred at room temperature for 15 minutes. To the reaction mixture, 1.06 g of 2-amino-4-(trifluoromethyl)phenol was added and stirred while heating at 60° C. for two hours. Thereafter, the mixture reaction was cooled to room temperature, and then concentrated under reduced pressure. Water was added to the residue, followed by extraction with ethyl acetate twice. The combined organic layers were washed with a saturated sodium chloride solution, dried over anhydrous sodium sulfate, and then concentrated under reduced pressure to give 1.79 g of 3-tert-butoxycarbonylamino-N-[2-hydroxy-5-(trifluoromethyl)phenyl]isonicotinamide.

1. additionwas added
2. stirringstirred
3. temperaturewhile heating at 60° C. for two hours
4. customThereafter, the mixture reaction
5. temperaturewas cooled to room temperature
6. concentrationconcentrated under reduced pressure
7. additionWater was added to the residue
8. extractionfollowed by extraction with ethyl acetate twice
9. washThe combined organic layers were washed with a saturated sodium chloride solution
10. dry with materialdried over anhydrous sodium sulfate
11. concentrationconcentrated under reduced pressure