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Copper Catalysis in Living Systems and In Situ Drug Synthesis

Research output: Contribution to journalArticle

Original languageEnglish
Pages (from-to)15662-15666
JournalAngewandte Chemie International Edition
Issue number50
Early online date15 Nov 2016
Publication statusPublished - 12 Dec 2016


Abstract: The copper catalyzed azide–alkyne cycloaddition
(CuAAC) reaction has proven to be a pivotal advance in chemical
ligation strategies with applications ranging from polymer fabrication
to bioconjugation. However, application in vivo has been limited by
the inherent toxicity of the copper catalyst. Here we report the
application of heterogeneous copper catalysts in azide–alkyne
cycloaddition chemistries in biological systems ranging from cells to
zebrafish, with chemistries spanning from fluorophore activation to
the first reported in situ generation of a triazole-containing anticancer
agent from two benign components, opening up many new avenues
of exploration of CuAAC chemistry.

ID: 31547283