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Synfacts 2021; 17(07): 0825
DOI: 10.1055/s-0040-1706227
Peptide Chemistry

Palladium-Catalyzed Olefination of Oxazole-Containing Peptides

Contributor(s):
Hisashi Yamamoto
,
Tomohiro Hattori
Liu S, Cai C, Bai Z, Sheng W, Tan J, *, Wang H. * Chongqing Normal University and Nanjing University, P. R. of China
Late-Stage Macrocyclization of Bioactive Peptides with Internal Oxazole Motifs via Palladium-Catalyzed C–H Olefination.

Org. Lett. 2021;
23: 2933-2937
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Key words

palladium catalysis - oxazoles - C–H bond activation - macrocyclization - olefination

Significance

Late-stage functionalization of peptides has enormous potential for drug discovery. The authors have developed a palladium-catalyzed C(sp2)–H olefination at the aromatic ring of oxazole-containing peptides.


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Comment

The palladium-catalyzed olefination proceeds for various oxazolone-containing peptides. Moreover, this method can be applied to macrocyclization.


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Publication History

Article published online:
17 June 2021

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