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.