PRACTICAL SYNTHESIS OF FULLY-SUBSTITUTED PEPTIDE THIAZOLES

Abstract The synthesis of optically active 2,4,5-substituted 1,3-thiazoles (peptide thiazoles) is described. Both the chirality and the set of side chain functionality in this fully-substituted scaffold are derived from a combination of two amino acids and one organometallic reagent. Preliminary results, with two specific examples, highlight the potential of this strategy for the preparation of a diverse set of building blocks.