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