Phosphatidylinositol bearing arachidonoyl group at sn-2 position was synthesized through preparation of protected myo-inositol, chemoenzymatic synthesis of an optically active lysophosphatidylcholine, introduction of an optically active sn-2 hydroxyl group, phospholipase D-assisted synthesis of a phosphatidic acid, and trisopropylbenzene sulfonylchloride assisted eaterification of the acid with the protected myo-inositol; as a final step.