反应详情

温度

70 °C

4-(aminomethyl)phenol (2.4 g) white solid and iPr2NEt (5.0 g) were added into a solution of methyl 4-(4-chloro-6-(2,2,2-trifluoroethoxy)-1,3,5-triazin-2-ylamino)benzoate (7.0 g) in THF (150 mL). The mixture was heated at 70° C. for 16 hours. After cooling, the mixture was charged with 250 mL of EtOAc. The resulting solution was washed with water (2×50 mL) and brine (30 mL). The organic layer was dried over MgSO4 and concentrated under vacuum to give a residue which was recrystallized in EtOAc to give 6.54 g of methyl 4-(4-(4-hydroxybenzylamino)-6-(2,2,2-trifluoroethoxy)-1,3,5-triazin-2-ylamino)benzoate.

1. temperatureAfter cooling
2. washThe resulting solution was washed with water (2×50 mL) and brine (30 mL)
3. dry with materialThe organic layer was dried over MgSO4
4. concentrationconcentrated under vacuum
5. customto give a residue which
6. customwas recrystallized in EtOAc