Rh(III)-Catalyzed directed C-H carbenoid coupling reveals aromatic bisphosphonates inhibiting metallo- and Serine-beta-lactamases

We report the highly efficient and scalable Rh(III)-catalyzed C-H coupling of arenes with diazo-methylene-diphosphonates to give structurally diverse aromatic bisphosphonates in good to excellent yields. These bisphosphonates are one of the very few classes of inhibitors acting against the mechanistically distinct metallo-beta-lactamases and serine-beta-lactamases and thus represent good starting points for the development of broad spectrum beta-lactamase inhibitors.