A simple and practical route for the asymmetric synthesis of (S)-4-(4-fluorophenyl)-1, 4, 5, 6- tetrahydro-6-oxo-3-pyridinecarboxylic acid (1) is presented. The procedure comprises catalytic desymmetrization of a meso-anhydride using a chiral thiourea organocatalyst, followed by selective formylation and cyclization.