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Synfacts 2019; 15(03): 0317
DOI: 10.1055/s-0037-1611466
DOI: 10.1055/s-0037-1611466
Peptide Chemistry
Synthesis of Cyclophane-Braced Peptide Macrocycles
Zhang X,
Lu G,
Sun M,
Mahankali M,
Ma Y,
Zhang M,
Hua W,
Hu Y,
Wang Q,
Chen J,
He G.
*
Qi X.
*
Shen W.
*
Liu P.
*
Chen G.
* Nankai University, Tianjin and National Institute of Biological Sciences, Beijing, P. R. of China; University of Pittsburgh, California Institute for Biomedical Research, La Jolla, and The Pennsylvania State University, University Park, USA
A General Strategy for Synthesis of Cyclophane-Braced Peptide Macrocycles via Palladium-Catalysed Intramolecular sp3 C–H Arylation.
Nat. Chem. 2018;
10: 540-548
A General Strategy for Synthesis of Cyclophane-Braced Peptide Macrocycles via Palladium-Catalysed Intramolecular sp3 C–H Arylation.
Nat. Chem. 2018;
10: 540-548
Weitere Informationen
Publikationsverlauf
Publikationsdatum:
15. Februar 2019 (online)
![](https://www.thieme-connect.de/media/synfacts/201903/i_h004_s1_10-1055_s-0037-1611466.gif)
Significance
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.
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Comment
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.
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![](https://www.thieme-connect.de/media/synfacts/201903/i_h004_s1_10-1055_s-0037-1611466.gif)