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Synfacts 2020; 16(02): 0229
DOI: 10.1055/s-0039-1691428
Peptide Chemistry
© Georg Thieme Verlag Stuttgart · New York

Stereoselective Macrocyclization of Peptides in CyClick Chemistry

Contributor(s):
Hisashi Yamamoto
,
Wataru Muramatsu
Adebomi V, Cohen RD, Wills R, Chavers HA. H, Martin GE, Raj M. * Auburn University, USA
CyClick Chemistry for the Synthesis of Cyclic Peptides.

Angew. Chem. Int. Ed. 2019;
58: 19073-19080
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Further Information

Publication History

Publication Date:
21 January 2020 (online)

 
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Key words

click chemistry - peptides - macrocycles - stereoselectivity

Significance

The pharmaceutical industry’s interest in peptide therapeutics is increasing owing to their low toxicities, high specificities towards targeted proteins, and so on. The authors describe a stereoselective macrocyclization of peptides through click chemistry.


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Comment

This DMAP-mediated intermolecular cyclization gives the desired cyclic peptides in moderate to high yields without the formation of linear oligopeptides through intramolecular reactions.


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