Iron-Catalyzed C–H Alkylamination of Tyrosine Derivatives

An efficient method for the direct alkylamination of tyrosine derivatives via iron-catalyzed C–H amination has been developed. The method, using O-benzoyl-N,N-dialkylhydroxylamines as aminating agents, provides various C-amino-functionalized tyrosine derivatives in up to 77% yield. The utility of this method is showcased by its application to the direct introduction of drug molecules into tyrosine, facilitating access to structurally diverse amino-functionalized tyrosine derivatives.