Expeditious and scalable preparation of a Li-Thiele reagent for amine-based bioconjugation  

作　　者：Jiacheng Li Yuyong Ma Xiang Zhang Xin Cao Hegui Gong Ang Li 

机构地区：[1]Department of Chemistry,Shanghai University,Shanghai 200444,China [2]State Key Laboratory of Bioorganic and Natural Products Chemistry,Center for Excellence in Molecular Synthesis,Shanghai Institute of Organic Chemistry,University of Chinese Academy of Sciences,Chinese Academy of Sciences.Shanghai 200032,China

出　　处：《Chinese Chemical Letters》2021年第2期700-702,共3页中国化学快报（英文版）

基　　金：supported by Ministry of Science and Technology (National Key Research and Development Program of China,No.2018YFA0901900);the National Natural Science Foundation of China (Nos.21931014,21525209, 21621002,21772225,and 21761142003);Chinese Academy of Sciences (Strategic Priority Research Program,No.XDB20000000;International Partner Program,No.121731KYSB20190039;Key Research Program of Frontier Sciences,No.QYZDB-SSW-SLH040);Science and Technology Commission of Shanghai Municipality (No.17XD1404600);K.C.Wong Education Foundation。

摘　　要：Chemoselective amine bioco njugation has long been a challenge for native protein modification.Inspired by Thiele’s seminal discovery,Li and co-workers recently developed an orto-phthalaldehyde(OPA)based reagent for labeling the amino group of a protein.Here we report an expeditious and scalable synthesis of a Li-Thiele reagent featuring an arene construction strategy.The reagent contains an alkyne side chain as a handle for secondary modification.

关 键 词：Amine-based bioconjugation Li-Thiele reagent Arene synthesis ORTHO-PHTHALALDEHYDE 

分 类 号：TQ464[化学工程—制药化工]