Derivatization based on tetrazine scaffolds:synthesis of tetrazine derivatives and their biomedical applications  

作　　者：Hongbao Sun Qinghe Xue Chang Zhang Haoxing Wu Ping Feng 

机构地区：[1]Huaxi MR Research Center(HMRRC),Department of Radiology,Frontiers Science Center for Disease-related Molecular Network,National Clinical Research Center for Geriatrics,Functional and Molecular Imaging Key Laboratory of Sichuan Province,West China Hospital,Sichuan University,Chengdu 610041,China [2]Clinical Trial Center,West China Hospital of Sichuan University,Chengdu 610041,China

出　　处：《Organic Chemistry Frontiers》2022年第2期481-498,共18页有机化学前沿（英文）

基　　金：supported by the National Natural Science Foundation of China(21801178,21977075);the 1.3.5 project for disciplines of excellence,West China Hospital,Sichuan University;Post-Doctor Research Project,West China Hospital,Sichuan University(No.2019HXBH009).

摘　　要：Bioorthogonal chemistry is widely used in biological systems and has been trialed in patients,attracting a lot of attention in this century.Tetrazine-based bioorthogonal reactions are essential in chemical biology applications,including cellular labeling,live-cell imaging,diagnosis,drug release,and oncotherapy,due to their tunable rapid reaction kinetics and unique fluorogenic characteristics.However,the scope of de novo tetrazine synthesis is restricted due to the limited supply of commercial starting materials.Therefore,derivatization based on tetrazine scaffolds has been used to synthesize various tetrazine derivatives to enhance the applications of tetrazine bioorthogonal reactions.Herein,the recent advances in tetrazine scaffold-based derivatizations,including tetrazine skeletons,aromatic substituents and alkyl substituents of tetrazines,have been summarized.The advantages and limitations of the derivatization methods and applications of the developed tetrazine derivatives in bioorthogonal chemistry have also been highlighted.

关 键 词：materials. SYNTHESIS SUBSTITUENT 

分 类 号：O62[理学—有机化学]