C-H activation reactions as useful tools for medicinal chemists

In recent years, there has been an exponential rise in the number of reports describing synthetic methods that utilize catalytic sp³ and sp² C-H bond activation. Many have emerged as powerful synthetic tools for accessing biologically active motifs. Indeed, application to C-C and C-heteroatom bond formation, provides new directives for the construction of new pharmaceutical entities. Herein, we highlight some recent novel C-H activation processes that exemplify the utility of these transformations in medicinal chemistry.