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 ...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.展开更多
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)+4 种基金Chinese Academy of Sciences (Strategic Priority Research Program,No.XDB20000000International Partner Program,No.121731KYSB20190039Key Research Program of Frontier Sciences,No.QYZDB-SSW-SLH040)Science and Technology Commission of Shanghai Municipality (No.17XD1404600)K.C.Wong Education Foundation。
文摘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.
