Ball-Milling Strategy for Epimerization-Free Peptide Synthesis

Key words

ball milling - epimerization - peptide synthesis - mechanochemistry

Significance

Because of the large demand for peptides in various fields, chemists are actively searching for highly efficient and epimerization-free methods for peptide synthesis. The authors have developed a method involving ball milling for synthesizing peptides in high yields and with minimal epimerization.

Comment

The developed ball-milling strategy for coupling in which peptide fragments containing highly epimerization-prone and hindered amino acids at the C-terminus actively participate in the reaction to afford the desired peptides in high yields with excellent purity. This method requires a very small amount of solvent.