Iodine‐Promoted Oxidative Cross‐Coupling of Unprotected Anilines with Methyl Ketones: A Site‐Selective Direct C—H Bond Functionalization to C4‐Dicarbonylation of Anilines.

An unprecedented direct dual C–H bond functionalization of unprotected anilines and methyl ketones has been demonstrated. It is the first example of iodine-promoted highly chemo- and site-selective oxidative C–H/C–H cross-coupling of anilines and methyl ketones to furnish the C4-dicarbonylation of anilines in moderate to good yields. Moreover, coproduct HI acted as a catalyst in the reaction. The salient feature of this approach is unprecedented C–H functionalization rather than N–H functionalization of unprotected anilines.