Hydrochloric Acid → Fexofenadine Hydrochloride

Participants

Reaction Conditions

Reaction Steps

In a 500 mL four-neck flask equipped with mechanical agitator, a thermometer and a condenser, a suspension of 2-(4-(1-hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (VI) (9 g, 17.9 mmol) in ethyl acetate (90 mL) was heated to 40° C. Then 30.36% aqueous hydrochloric acid (2 g, 20 mmol) was dropped to the mixture and the final solution was stirred at 40° C. for 1 hour and at room temperature overnight. The crystallized solid was filtered, washed with ethyl acetate and dried under vacuum at 50° C., to give 8.5 g of polymorph φ of Fexofenadine hydrochloride, as a white solid. Yield: 88%.

Provenance & Evidence