Synthesis of 2‐Aryl‐1,3‐Cyclopentanediones through Catalytic Borylation as a Key Step

We describe a practical straightforward synthesis of 2‐aryl‐1,3‐cyclopentanediones from α‐iodoenones, via in situ palladium‐catalyzed cross‐coupling with hindered arylboronic acids followed by copper‐mediated β‐borylation and finishing with an oxidative work‐up. The sequential reactions are performed without intermediate isolation and the whole synthetic strategy might become of practical use for the major challenges that companies currently face in R&D in agrochemicals.