Synthesis of the Antimalarial Peptide Aldehyde, a Precursor of Kozupeptin A, Utilizing a Designed Hydrophobic Anchor Molecule

This Letter describes an efficient method of synthesizing highly bioactive peptide aldehydes without any concern about epimerization by liquid-phase peptide synthesis through the use of newly designed hydrophobic anchor molecules. Peptide elongation reactions effectively proceeded in less polar solvents, and direct crystallization by the addition of polar solvents enabled easy purification. This method also represents a new concept for the efficient synthesis of peptide derivatives. The development of new antimalarial drug candidates will be accelerated using this methodology.