Formal C–H‐Azidation – Based Shortcut to Diazido Building Blocks for the Versatile Preparation of Photoaffinity Labeling Probes

Short synthetic routes to diazido building blocks with different connectable groups were established on the basis of the sequential iridium‐catalyzed C–H borylation and copper‐catalyzed azidation of 1,3‐disubstituted benzenes, followed by diverse azido‐friendly functional‐group transformations. These building blocks facilitate the rapid development of effective diazido photoaffinity labeling probes that are useful for the identification of unknown target biomolecules of bioactive compounds.