反应详情

温度

0 °C

7-(Trifluoromethyl)-1,2,3,4-tetrahydroquinoline (440 mg, 2.2 mmol) was dissolved in DMF (10 mL) under N2 at room temperature. DIEA (284 mg, 2.2 mmol) was added, and the reaction solution was cooled to 0° C. 2,4-Dichloro-1,3,5-triazine was added, and reaction was stirred with gradual warming to RT. The reaction was quenched after 3 h with water, which caused a fine precipitate to form, which is not filterable. This mixture was extracted 3 times with EtOAc. The EtOAc extracts were then washed brine, combined, dried over Na2SO4, filtered, concentrated, and dried under high vacuum giving 1-(4-chloro-[1,3,5]triazin-2-yl)-7-trifluoromethyl-1,2,3,4-tetrahydro-quinoline (800 mg (>100%)) of a yellow oil that was used without further purification.

1. customreaction
2. temperaturewith gradual warming to RT
3. customThe reaction was quenched after 3 h with water, which
4. customto form
5. extractionThis mixture was extracted 3 times with EtOAc
6. dry with materialdried over Na2SO4
7. filtrationfiltered
8. concentrationconcentrated
9. customdried under high vacuum