Copper-Catalyzed Azide–Alkyne Click Chemistry for Bioconjugation

作者: Stanislav I. Presolski , Vu Phong Hong , M.G. Finn

DOI: 10.1002/9780470559277.CH110148

关键词: AlkyneAzideLigandCombinatorial chemistryBioconjugationChemistryCycloadditionReagentClick chemistryReducing agent

摘要: The copper‐catalyzed azide‐alkyne cycloaddition reaction is widely used for the connection of molecular entities of all sizes. A protocol is provided here for the process with biomolecules. Ascorbate is used as reducing agent to maintain the required cuprous oxidation state. Since these convenient conditions produce reactive oxygen species, five equivalents of a copper‐binding ligand are used with respect to metal. The ligand both accelerates the reaction and serves as a sacrificial reductant, protecting the biomolecules …

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