Condensation of phenytoin (I) with formaldehyde in the presence of K2CO3 provided (hydroxymethyl)phenytoin (II). This was then esterified with (1-piperidinyl)acetic acid (III) using either p-toluenesulfonyl chloride or N,N'-dicyclohexylcarbodiimide as the coupling agents. The title compound was finally isolated as the hydrochloride salt.