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用于生物正交点击反应的水溶性配体
三(3-羟丙基三唑甲基)胺(THPTA)是一种水溶性配体,通过三炔丙基胺和3—叠氮基-1-丙醇的点击反应(= Hüisgen 1,3-偶极环加成反应)合成1)。在铜离子存在的条件下,THPTA可用于Cu-催化的炔烃-叠氮化物环化反应(CuAAC),即生命系统中一种典型的无干扰生物正交反应,并且形成的铜配合物可以加速CuAAC进程2)。THPTA的参与的CuAAC不仅适用于亲水性聚合物的修饰3)和含一个叠氮基的多肽的生物偶联4),还可用于活细胞表面代谢吸收的叠氮或炔烃标签的快速标记5)。
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- 4)Synthesis of Cyclic Peptide Disulfide–PHPMA Conjugates via Sequential Active Ester Aminolysis and CuAAC Coupling
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- b) Labeling Live Cells by Copper-Catalyzed Alkyne−Azide Click Chemistry
- V. Hong, N. F. Steinmetz, M. Manchester, M. G. Finn, Bioconjugate Chem. 2010, 21, 1912.
- D. C. Kennedy, C. S. McKay, M. C. B. Legault, D. C. Danielson, J. A. Blake, A. F. Pegoraro, A. Stolow, Z. Mester, J. P. Pezacki, J. Am. Chem. Soc. 2011, 133, 17993.