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Solid-Phase Parallel Synthesis of Functionalised Medium-to-Large Cyclic Peptidomimetics through Three-Component Coupling Driven by Aziridine Aldehyde Dimers.

Authors :
Treder AP
Hickey JL
Tremblay MC
Zaretsky S
Scully CC
Mancuso J
Doucet A
Yudin AK
Marsault E
Source :
Chemistry (Weinheim an der Bergstrasse, Germany) [Chemistry] 2015 Jun 15; Vol. 21 (25), pp. 9249-55. Date of Electronic Publication: 2015 May 26.
Publication Year :
2015

Abstract

The first solid-phase parallel synthesis of macrocyclic peptides using three-component coupling driven by aziridine aldehyde dimers is described. The method supports the synthesis of 9- to 18-membered aziridine-containing macrocycles, which are then functionalized by nucleophilic opening of the aziridine ring. This constitutes a robust approach for the rapid parallel synthesis of macrocyclic peptides.<br /> (© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Details

Language :
English
ISSN :
1521-3765
Volume :
21
Issue :
25
Database :
MEDLINE
Journal :
Chemistry (Weinheim an der Bergstrasse, Germany)
Publication Type :
Academic Journal
Accession number :
26014974
Full Text :
https://doi.org/10.1002/chem.201500068