123846-86-6Relevant articles and documents
An efficient and easily-accessible ligand for Cu(i)-catalyzed azide-alkyne cycloaddition bioconjugation
Guo, Yuan-Yang,Zhang, Bo,Wang, Luying,Huang, Shenlong,Wang, Shilei,You, Yanbo,Zhu, Gongming,Zhu, Anlian,Geng, Mingwei,Li, Lingjun
supporting information, p. 14401 - 14403 (2020/12/01)
A novel ligand (6) for copper-catalyzed azide-alkyne cycloaddition (CuAAC) in bioconjugation has been developed. Both in vitro and in vivo experiments indicate that 6 is more efficient and less cytotoxic than the canonical CuAAC ligands. Besides, 6 is easily accessible and can be prepared at gram scale. Our study reveals that 6 might be an ideal CuAAC ligand for bioconjugations.
Synthesis method of new ligand for efficient catalysis of CuAAC reaction
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Paragraph 0013; 0014; 0015, (2018/03/28)
Belonging to the technical field of synthesis of functional structural molecules, the invention discloses a synthesis method of a new ligand for efficient catalysis of CuAAC reaction. The key point ofthe technical scheme adopted by the invention lies in that: the synthesis method of the new ligand for efficient catalysis of CuAAC reaction includes: firstly synthesizing glycine methyl ester diyne,then taking glycine methyl ester diyne, an azido compound, K2CO3 and copper iodide as the raw materials, using acetonitrile and water as the solvent, carrying out stirring reaction at room temperature, and performing post-treatment at the end of reaction, thus obtaining the new ligand glycine methyl ester 1, 2, 3-ditriazole ring opening compound. The invention provides a variety of novel, efficient and easily available ligand catalysts for click reaction, as a ligand, the compound synthesized by the method provided by the invention has obvious effect of accelerating reaction and has a very practical application.
Preparation method of 1,2,3-bis-triazole ligands and application of 1,2,3-bis-triazole ligands in CuAAC reaction
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Paragraph 0006; 0008; 0015, (2018/02/04)
The invention discloses a preparation method of 1,2,3-bis-triazole ligands and an application of the 1,2,3-bis-triazole ligands in a CuAAC reaction. With cheap and easily available glycine methyl ester hydrochloride as a base raw material, and through derivation and conversion of functional groups, a diyne compound with glycine as a structure is obtained; then under a condition of room temperature and with organic azide as a raw material and copper iodide as a catalyst, 1,2,3-bis-triazole seven-membered-ring compounds are synthesized; and with the bis-triazole compounds and derivatives thereof as substrates, a series of methods for synthesis of the 1,2,3-bis-triazole derivatives are developed. A variety of novel, highly efficient, simple and easily available ligand catalysts are provided for a click reaction, and the 1,2,3-bis-triazole ligands have obvious effect on accelerating the reaction when used as the ligands and have quite practical application.
