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Wir präsentieren eine neue Spätphasenfunktionalisierung von kleinen Peptiden und Cyclopeptiden unter Verwendung leicht zugänglicher Iodtyrosin‐ oder Iodphenylalanin‐haltiger Peptide mittels Neghishi‐Kreuzkupplungen mit Aryl‐, Heteroaryl‐ und Alkylzinkpivalaten oder den jeweiligen Halogeniden. Computergestützte und In‐vitro‐Evaluierungen von Zellmembranpermeabilitätsparametern der modifizierten Cyclopeptide...
We report the first decarboxylative alkynylation of the C‐terminus of peptides starting from free carboxylic acids. The reaction is fast, metal‐free, and proceeds cleanly to afford alkynylated peptides with a broad tolerance for the C‐terminal amino acid. By the use of hypervalent iodine reagents, the introduction of a broad range of functional groups was successful. C‐terminal selectivity was achieved...
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