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

Abstract

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, one-pot 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.