Eltoprazine can be obtained in a 3-step procedure starting from 5-nitrobenzodioxane (I): Catalytic hydrogenation of benzodioxane (I) results in the aniline hydrochloride (II) in high yieId. From the crude product obtained after treatment of (II) with bischloroethylamine dihydrochloride and subsequent crystallization from ethanol, pure eltoprazine hydrochloride is isolated.