反应详情

To a mixture of 3-amino-5-trifluoromethylpyridin-2-ol (0.75 g) and THF (5 ml), 2-ethylsulfanylbenzoic acid hydrochloride (0.93 g) was added under ice-cooling, heated to room temperature, and stirred for 2 hours. After the mixture was allowed to stand overnight, the mixture was heated to 50° C., and stirred with heating for 6 hours. To the mixture, sodium hydrogen carbonate (0.35 g) was added, and stirred with heating for further 2.5 hours. After the mixture was allowed to stand, water was poured thereinto, and the precipitated solid was collected by filtration. The obtained solid was washed with water, and dried to give 1.37 g of 2-ethylsulfanyl-N-(2-hydroxy-5-trifluoromethylpyridin-3-yl)-benzamide (Compound (1B)-506).

1. additionwas added under ice-
2. temperaturecooling
3. waitto stand overnight
4. temperaturethe mixture was heated to 50° C.
5. stirringstirred
6. temperaturewith heating for 6 hours
7. stirringstirred
8. temperaturewith heating for further 2.5 hours
9. filtrationthe precipitated solid was collected by filtration
10. washThe obtained solid was washed with water
11. customdried