Self-Purified Solid-Phase Synthesis of Peptide Thioesters

Significance

A cyclization-thiolysis sequence was developed for the synthesis of peptide thio­esters with self-purification. Thus, linker 1 was installed to polymer-supported peptide sulfone amides 2 to give 3, which were converted into 6 via macrocyclization. Thiolysis of 6 gave non-cyclic truncation byproducts that were hence washed away. Only the full-length peptide thio­esters 8 were detached from 7 as pure forms in the final step.