Acetone → Quetiapine fumarate

Participants

Reaction Conditions

Reaction Steps

0.65 g (0.006 mol) of fumaric acid is suspended in a solution of 25 ml of acetone and 5 ml of water, the solution is brought to the boil, and 25 ml of a toluene solution containing 4.5 g (0.012 mol) of pure quetiapine base is added. The solution is refluxed for approximately 5 minutes and then cooled to a temperature of 0 to 5° C., at which crystals start to precipitate. It is stirred at this temperature for 90 minutes. After being sucked off and dried, 3.8 g (0.009 mol) of quetiapine hemifumarate is obtained, i.e. 64.5% of the theory, having the HPLC purity 99.82%, and melting point 172° C.

Provenance & Evidence