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Solid‐Phase Parallel Synthesis of Functionalised Medium‐to‐Large Cyclic Peptidomimetics through Three‐Component Coupling Driven by Aziridine Aldehyde Dimers |
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| Authors: | Dr. Adam P. Treder Dr. Jennifer L. Hickey Marie‐Claude J. Tremblay Dr. Serge Zaretsky Dr. Conor C. G. Scully Dr. John Mancuso Annie Doucet Prof. Andrei K. Yudin Prof. Eric Marsault |
| Affiliation: | 1. Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, 3001, 12e av nord Sherbrooke (QC) J1H 5N4 (Canada);2. Davenport Research Laboratories, Department of Chemistry, University of Toronto, 80 St. George Street, Toronto (ON) M5S 3H6 (Canada) |
| 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. |
| Keywords: | drug discovery macrocycles peptides small ring systems solid‐phase synthesis |