ArticleChemistry (Weinheim an der Bergstrasse, Germany)2026
Late-Stage Modification of Halotryptophan-Containing Peptides Via Negishi Cross-Coupling.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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1 citing paper in PubMed.
- Extracellularly Activatable Conjugates of RGD Peptidomimetics and Cryptophycin for αChemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
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Abstract
Late-stage functionalization of peptides provides powerful opportunities for the rapid diversification of bioactive sequences. Among the available strategies, Negishi cross-coupling represents a versatile and orthogonal method for the installation of alkyl substituents under mild conditions. We describe the applicability of Negishi cross-coupling to increasingly complex bromotryptophan-containing peptides. While conditions effective for bromo-l-tryptophan proved unsuitable for peptide substrates, leading to incomplete conversion and pronounced debromination, systematic optimization enabled efficient cross-coupling of the model tripeptide Ac-Ala-Trp(6-Br)-Gly-NH
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