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Synfacts 2019; 15(02): 0203
DOI: 10.1055/s-0037-1611960
Peptide Chemistry
© Georg Thieme Verlag Stuttgart · New York

Native Chemical Ligation by Microflow Chemistry

Contributor(s):
Hisashi Yamamoto
,
Takahiro Sawano
Ollivier N, Toupy T, Hartkoorn RC, Desmet R, Monbaliu J.-CM. * Melnyk O. * Université de Lille, France and University of Liège, Belgium
Accelerated Microfluidic Native Chemical Ligation at Difficult Amino Acids toward Cyclic Peptides.

Nat. Commun. 2018;
9: 2847
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Further Information

Publication History

Publication Date:
18 January 2019 (online)

 
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Key words

native chemical ligation - cyclic peptides - microflow reaction - flow synthesis - thioesters

Significance

The authors reported a fast and highly efficient intramolecular cyclization of peptides with native chemical ligation under homogeneous microfluidic conditions, in which the formation of highly active S-{2-[(2-sulfanylethyl)amino]ethyl} peptidyl thioesters is a key step.


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Comment

This scale-independent microfluidic native chemical ligation proceeds rapidly, even for difficult junctions, and realizes an expedient preparation of bioactive macrocyclic peptides.


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