Levoprotiline (II) is the levorotatory R-enantiomer of oxaprotitine (I). It is obtained by resolution of oxaprotitine via its (-)-di-O,O'-p-toluoyl-L-tartaric acid salt, which is then cleaved with hydrogen chloride to levoprotiline hydrochloride (CGP-12 103 A). By an analogous procedure, using (+)-di-O,O'-p-toluoyl-D-tartaric acid, the dextrarotatory S-enantiomer, CGP 12 104 A (III), is gained from oxaprotiline.