反应详情

To a solution of 4-(4-fluorophenyl)-1,2,3,6-tetrahydropyridine (1.96 g, 13.7 mmol) in acetone (30 mL) was added 1,3-propane sultone (1.74 g, 14.5 mmol). The mixture was stirred at reflux overnight. Only a small amount of compound precipitated. The resulting suspension was cooled to room temperature with stiffing and a larger amount of solid precipitated. The suspension was heated with the addition of a small amount of MeOH until complete dissolution of the solid. The resulting solution was stirred at reflux for a few minutes and was cooled to room temperature with stiffing. The solid was collected by filtration, washed with MeOH and dried in vacuo. This allowed the isolation of compound F, 1.33 g (32%).

1. temperatureat reflux overnight
2. customOnly a small amount of compound precipitated
3. customa larger amount of solid precipitated
4. temperatureThe suspension was heated with the addition of a small amount of MeOH until complete dissolution of the solid
5. stirringThe resulting solution was stirred
6. temperatureat reflux for a few minutes
7. temperaturewas cooled to room temperature with stiffing
8. filtrationThe solid was collected by filtration
9. washwashed with MeOH
10. customdried in vacuo