Synthesis of a novel series of N-pyrandione substituted amino acids and their esters 3 via a condensation reaction between pyrandione and amino acid or their derivatives in excess ethyl orthoformate without solvent is described. The stereochemistry of 3 has been discussed. Synthesis of a novel series of N-pyrandione substituted amino acids and their esters 3 via a condensation reaction between pyrandione and amino acid or their derivatives in excess ethyl orthoformate without solvent is described. The stereochemistry of 3 has been discussed.