Synfacts 2021; 17(04): 0461
DOI: 10.1055/s-0040-1706153
Peptide Chemistry

Ball-Milling Strategy for Epimerization-Free Peptide Synthesis

Contributor(s):
Hisashi Yamamoto
,
Isai Ramakrishna
Yeboue Y, Jean M, Subra G, Martinez J, Lamaty F, *, Métro T.-X. * Univ Montpellier, France
Epimerization-Free C‑Term Activation of Peptide Fragments by Ball Milling.

Org. Lett. 2021;
23: 631-635
DOI: 10.1021/acs.orglett.0c03209.
 

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.


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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.


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Publication History

Article published online:
18 March 2021

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