Esterification of L-alpha-glycerophosphorylcholine (I) with docosahexaenoic acid (II) by means of DCC affords diester (III), which is regioselectively converted to mono-ester (IV) by phospholipase A2-catalyzed hydrolysis. Finally, acylation of (IV) with methotrexate (V) in the presence of DCC gives rise to the title compound.