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Simultaneous Cyclization and Derivatization of Peptides Using Cyclopentenediones

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journal contribution
posted on 17.02.2017, 17:37 by Omar Brun, Lewis J. Archibald, Jordi Agramunt, Enrique Pedroso, Anna Grandas
Unprotected linear peptides containing N-terminal cysteines and another cysteine residue can be simultaneously cyclized and derivatized using 2,2-disubstituted cyclopentenediones. High yields of cyclic peptide conjugates may be obtained in short reaction times using only a slight excess of the cyclopentenedione moiety under TEMPO catalysis and in the presence of LiCl.