An Efficient Fmoc‐SPPS Approach for the Generation of Thioester Peptide Precursors for Use in Native Chemical Ligation

Abstract

Intramolecular activation of C-terminal peptides: Mildly activated N-acylurea peptides are readily formed on the solid support following chain assembly, avoiding over-activation of the C-terminus. The utility of these peptides is demonstrated by the native chemical ligation of unprotected peptides (see scheme; R=amino acid side chain).