A catalytic one-step synthesis of peptide thioacids: the synthesis of leuprorelin via iterative peptide-fragment coupling reactions.

A catalytic one-step synthesis of peptide thioacids: the synthesis of leuprorelin via iterative peptide-fragment coupling reactions.
Chem Commun (Camb). 2018 Oct 12;:
Authors: Matsumoto T, Sasamoto K, Hirano R, Oisaki K, Kanai M
Abstract
A catalytic one-step synthesis of peptide thioacids was developed. The oxygen-sulfur atom exchange reaction converted the carboxy group at the C-terminus of the peptides into a thiocarboxy group with suppressed epimerization. This method was successfully applied to the synthesis of the peptide drug leuprorelin via an iterative fragment-coupling protocol.
PMID: 30310900 [PubMed - as supplied by publisher]

Source: Chemical Communications - October 12, 2018 Category: Chemistry Authors: Matsumoto T, Sasamoto K, Hirano R, Oisaki K, Kanai M Tags: Chem Commun (Camb) Source Type: research