Modular C–H Functionalization Cascade of Aryl Iodides

We report the first example of ipso-borylation for the modular 1,2-bisfunctionalization of aryl iodides via C–H functionalization. The carbon–boron bond is used as a lynchpin to access ipso carbon–carbon, carbon–nitrogen, carbon–oxygen, and carbon–halogen (Cl, Br, I) bonds. The utility of our methodology is illustrated through quick, modular syntheses of the pharmaceuticals Abilify and Flunixin.