Synthesis of Cyclophane-Braced Peptide Macrocycles
A General Strategy for Synthesis of Cyclophane-Braced Peptide Macrocycles via Palladium-Catalysed Intramolecular sp3 C–H Arylation.
Nat. Chem. 2018;
15 February 2019 (online)
New efficient methods for the intramolecular cyclization of peptides are important in terms of the development of drugs based on cyclic peptides. The authors report a powerful method for constructing new types of peptide macrocycles through palladium-catalyzed, aminoquinoline-directed, intramolecular C(sp3)–H arylation reactions.
The cyclization of readily accessible linear peptide precursors selectively proceeds at side chains of either aromatic or modified nonaromatic amino acids units to provide a variety of cyclophane-braced peptide macrocycles containing small-sized cyclophanes.