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DOI: 10.1055/a-2601-4723
One-Pot Peptide Synthesis under Neutral Conditions Using Triphenyl Phosphite
Triphenyl Phosphite-Mediated One-Pot Peptide-Bond Formation under Neutral Reaction Conditions.
Org. Lett. 2025;
27: 3742-3746
DOI: 10.1021/acs.orglett.5c00904
Significance
Over the years, there has been an evolution of synthetic strategies to access peptides with newer methods aiming to combat the limitations of pre-existing and conventional methods such as low atom economy and optical purity. Developing new methods for liquid-phase peptide synthesis using especially easily accessible and cheap coupling reagents in a more compact neutral synthetic protocol is highly recommended. The authors have herein showcased that goal using triphenyl phosphite.
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Comment
A variety of dipeptides and tripeptides were prepared in excellent yields using triphenyl phosphite as the coupling reagent under the standard neutral conditions from their respective amino acids and dipeptides. Some of the tripeptides are precursors for some endogenous opioids such as Leu-enkephalin, thus demonstrating the potential of this strategy in accessing some biologically important and synthetically useful peptides.
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Publication History
Article published online:
23 June 2025
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