Electrochemical chemoselective thiocarbamylation of late-stage Tyr-containing drugs and peptides  

作　　者：Wan-Jie Wei Xin-Yu Wang Hai-Tao Tang Fei-Hu Cui Yun-Qi Wu Ying-Ming Pan 

机构地区：[1]State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources,Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources(Ministry of Education of China),Collaborative Innovation Center for Guangxi Ethnic Medicine,School of Chemistry and Pharmaceutical Sciences,Guangxi Normal University,Guilin 541004,China

出　　处：《Science China Chemistry》2024年第10期3382-3388,共7页中国科学（化学英文版）

基　　金：supported by the Guangxi Science and Technology Base and Talent Project(High level Innovative Talents and Team Training)(Guike AD23026094);the Guangxi Natural Science Foundation of China(2021GXNSFFA220005);the National Natural Science Foundation of China(22161008,22061003);the Innovation and Entrepreneurship Training Programme for University Students(202310602013)。

摘　　要：The synthesis and modification of peptides occupy a unique position in the field of drug development,and the functionalization of amino acids is a valuable strategy as an alternative to peptide modification.Currently,the development of tyrosine(Tyr)as a target amino acid is a major challenge in the field of chemistry.Herein,we report an electrochemical radical coupling reaction of labeling tyrosine-containing active drugs and peptides with thiocarbamate derivatives for the first time.This tri-component,onepot reaction can be performed smoothly under simple,gentle,and clean electrochemical conditions and is suitable for the functionalization of various Tyr-containing drug molecular derivatives and peptides.

关 键 词：TYROSINE electrochemical radical coupling chemical modification PEPTIDES 

分 类 号：O621.25[理学—有机化学] TQ460.1[理学—化学]