反应详情

To a solution of ethyl 2-amino-5-(2,6-difluorophenyl)-1,3-thiazole-4-carboxylate in THF was slowly added dropwise tert-butyl nitrate under heating under reflux. After completion of dropwise addition, it was further stirred at the same temperature for 4 hours. The reaction mixture was cooled to room temperature, followed by addition of water and extraction with EtOAc. The organic layer was washed with brine, dried, and then concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane:EtOAc=9:1-7:3) to obtain ethyl 5-(2,6-difluorophenyl)-1,3-thiazole-4-carboxylate as a yellow oily substance.

1. temperatureunder heating
2. temperatureunder reflux
3. additionAfter completion of dropwise addition, it
4. washThe organic layer was washed with brine
5. customdried
6. concentrationconcentrated under reduced pressure
7. customThe residue was purified by silica gel column chromatography (hexane:EtOAc=9:1-7:3)