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

摘要

The straightforward C-terminal modification of peptides assembled on a solid support remains a significant challenge in peptide and protein chemistry.In particular,C-terminal thioester peptides are important intermediates for the generation of active esters,amides and hydrazides and are an essential component of many synthetic strategies for protein synthesis.Currently,the most effective approach for the synthesis of peptidyl thioesters is the in situ neutralization protocol for tert-butoxycarbonyl solid-phase peptide synthesis(Boc-SPPS)using thioester linkers.