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
DOI:
10.1021/acs.orglett.1c00580
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.
Comment
The palladium-catalyzed olefination proceeds for various oxazolone-containing peptides.
Moreover, this method can be applied to macrocyclization.
