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

被引:442
作者
Debets, Marjoke F. [1 ]
van Berkel, Sander S. [1 ]
Schoffelen, Sanne [1 ]
Rutjes, Floris P. J. T. [1 ]
van Hest, Jan C. M. [1 ]
van Delft, Floris L. [1 ]
机构
[1] Radboud Univ Nijmegen, Inst Mol & Mat, NL-6525 AJ Nijmegen, Netherlands
关键词
FREE TRIAZOLE FORMATION; FREE CLICK CHEMISTRY; PROTEIN PEGYLATION; POLYMER; STRATEGIES; LIGATION; PEPTIDE; TOOL;
D O I
10.1039/b917797c
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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.
引用
收藏
页码:97 / 99
页数:3
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