通过点击反应快速构建F-三唑基四嗪
Rapid Construction of F-Triazolyl-tetrazines through the Click Reaction.
作者信息
Yang Cheng, Lu Kai, Li Jie, Wu Haoxing, Chen Wei
机构信息
Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced Drug, and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Department of Radiology and Huaxi MR Research Center (HMRRC), Functional and Molecular Imaging Key Laboratory of Sichuan Province, and Frontiers Science Center for Disease Related Molecular Network West China Hospital, Sichuan University, Huaxi Research Building, 001 4th Keyuan Road, Chengdu 610041, China.
出版信息
J Org Chem. 2024 Oct 18;89(20):14673-14678. doi: 10.1021/acs.joc.4c00574. Epub 2024 Jun 14.
Due to the fast reaction rate, F-labeled tetrazines have been widely applied in positron emission tomography (PET) imaging in cancer research and drug discovery. In this work, several functional F-triazolyl-tetrazines were rapidly obtained through an optimized copper-catalyzed alkyene-azide cycloaddition reaction system in >99% radiochemical conversions. Notably, the commonly used F-labeled azides were isolated through cartridges and directly used for cycloadditions, which greatly simplified the labeling procedure. The assembled triazolyl-tetrazines demonstrated high stability and reaction kinetics, exhibiting considerable potential for the development of PET agents.
由于反应速率快，F 标记的四嗪已广泛应用于癌症研究和药物发现中的正电子发射断层扫描（PET）成像。在这项工作中，通过优化的铜催化炔烃-叠氮环加成反应体系，以>99%的放射化学转化率快速获得了几种功能性 F-三唑基四嗪。值得注意的是，常用的 F 标记叠氮化物通过柱分离得到并直接用于环加成反应，这大大简化了标记过程。组装的三唑基四嗪表现出高稳定性和反应动力学，在 PET 试剂开发方面具有相当大的潜力。
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