Aza-dibenzocyclooctynes for fast and efficient enzyme PEGylation via copper-free (3+2) cycloaddition

A strained aza-dibenzocyclooctyne was prepared via a high-yielding synthetic route. Copper-free, strain-promoted click reaction with azides showed excellent kinetics, and a functionalised aza-cyclooctyne was applied in fast and efficient PEGylation of enzymes.

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Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2010-01, Vol.46 (1), p.97-99
Main Authors: Debets, Marjoke F, van Berkel, Sander S, Schoffelen, Sanne, Rutjes, Floris P J T, van Hest, Jan C M, van Delft, Floris L
Format: Article
Language:English
Subjects:
Aza Compounds - chemistry
Calbindins
Copper - chemistry
Cycloparaffins - chemistry
Kinetics
Polyethylene Glycols - chemistry
S100 Calcium Binding Protein G - chemistry
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Summary:A strained aza-dibenzocyclooctyne was prepared via a high-yielding synthetic route. Copper-free, strain-promoted click reaction with azides showed excellent kinetics, and a functionalised aza-cyclooctyne was applied in fast and efficient PEGylation of enzymes.
ISSN:1359-7345
1364-548X
DOI:10.1039/b917797c