期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 57, 期 42, 页码 13912-13916出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201807953
关键词
C-H activation; cyclic peptides; macrocycles; macrocyclization; palladium catalysis
资金
- 1000-Youth Talents Plan, NSF of China [21778030]
- NSF of Jiangsu Province [BK20160640]
- Fundamental Research Funds for the Central Universities [14380138, 14380131]
C-H activation methods for peptide macrocyclization have the potential to provide peptidomimetics and cyclic peptides with expanded structural diversity. Now, a highly versatile peptide macrocyclization strategy via late-stage palladium-catalyzed delta-C(sp(2))-H olefination of phenylalanine residues has been developed. This method utilizes peptide backbone amides as internal directing groups and allows facile macrocyclization of peptides in the N-to-C direction. Combined with the previously developed beta-C(sp(3))-H arylation method for peptide macrocyclization in the C-to-N direction, a pair of palladium-catalyzed reactions were obtained that are directionally orthogonal, and the first example of one-pot synthesis of bicyclic peptides via Pd-catalyzed beta-C(sp(3))-H and delta-C(sp(2))-H activation is demonstrated.
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