反应详情

3-[2-(Toluene-4-sulfonyloxy)-propionylamino]propionic acid methyl ester (307 mg) was dissolved in acetonitrile (5 mL). After addition of 1-methyl-3-(5-amino-4-chloro-2-fluorophenyl)-6-trifluoromethyl-1H-pyrimidin-2,4-dione (300 mg) and potassium carbonate (135 mg), the reaction mixture was heated for 6 hours under reflux without cooling. After cooling to room temperature, the reaction mixture was diluted with ethyl acetate (50 mL) and washed with water (50 mL). Thus obtained organic layer was dried with magnesium sulfate and concentrated. The concentrate was purified by silica gel column chromatography to give the target compound (170 mg).

1. temperaturethe reaction mixture was heated for 6 hours
2. temperatureunder reflux
3. temperaturewithout cooling
4. washwashed with water (50 mL)
5. dry with materialThus obtained organic layer was dried with magnesium sulfate
6. concentrationconcentrated
7. customThe concentrate was purified by silica gel column chromatography