Synthesis of [d-Pyrenylalanine4,4′]gramicidin S by Solid-Phase-Synthesis and Cyclization-Cleavage Method with Oxime Resin

Abstract
Cyclic decapeptide [D-pyrenylalanine4,4′]gramicidin S has been efficiently synthesized via stepwise solid-phase-synthesis and cyclization-cleavage with the Kaiser’s oxime resin in 45% total yield. This analog showed the similar conformation to the natural gramicidin S in MeOH. The pyrene ring introduced into the peptide is a useful fluorescent probe for the study of the mechanism of the antimicrobial activity.

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