Toluene → Quetiapine fumarate

Participants

Reaction Conditions

Reaction Steps

A suspension of 1.62 g (0.014 mol) of fumaric acid in 100 ml of ethyl acetate is brought to the boil. At this temperature, 100 ml of a toluene solution containing 10.77 g (0.028 mol) of pure quetiapine base is added, and the reaction mixture is allowed to boil for about 5 minutes. During this period a crystalline product starts to precipitate, which is then cooled to ca. 20° C. and is stirred at this temperature for 60 minutes. After being sucked off and dried, approximately 12.28 g (0.028 mol) of quetiapine hemifumarate is obtained, i.e. 99% of the theory, having the HPLC purity 99.76%, and melting point 175.7° C.

Provenance & Evidence