Quetiapine → Quetiapine fumarate

Participants

Reaction Conditions

Reaction Steps

To a solution of quetiapine (VI) (82.5 g, 215 mmol) in ethanol (660 ml) there was added fumaric acid (12.49 g, 108 mmol) and the mixture was heated under reflux for 2 hours in an inert atmosphere. A precipitate out of the solution formed shortly after starting the heating. After cooling the mixture to 0° C., it was filtered, washed with ethanol (250 ml, 0° C.) and dried at reduced pressure to give quetiapine hemifumarate (77.4 g, 81%) as a crystalline white solid.

Provenance & Evidence