反应详情

1-Benzyl-3-(3,5-dichlorophenyl)-4-(methylsulfonyl)-3-(trifluoromethyl)pyrrolidine (2.00 g, 95% purity, 4.13 mmol) was dissolved in toluene (40 mL) under a nitrogen atmosphere and sodium carbonate (1.31 g, 12.4 mmol) was added. The reaction mixture was heated to reflux for 150 minutes and cooled to room temperature. Water (20 mL) was added, the mixture stirred for 5 minutes and the phases separated. The water phase was extracted with toluene (20 mL) and solvent of the combined organic phases was evaporated under vacuum. The crude material was dissolved in warm n-heptane and after standing and cooling the forming crystals were filtered off to yield 1-benzyl-3-(3,5-dichlorophenyl)-3-(trifluoromethyl)-2,3-dihydro-1H-pyrrole (972 mg, 95% purity, 60% yield).

1. temperatureThe reaction mixture was heated
2. temperatureto reflux for 150 minutes
3. customthe phases separated
4. extractionThe water phase was extracted with toluene (20 mL) and solvent of the combined organic phases
5. customwas evaporated under vacuum
6. dissolutionThe crude material was dissolved in warm n-heptane
7. temperaturecooling the forming crystals
8. filtrationwere filtered off