Iodine-Promoted Semmler-Wolff Reactions: Step-Economic Access to meta-Substituted Primary Anilines via Aromatization.

An atom- and step-economic access to an array of unprotected meta-substituted primary anilines was disclosed using the Semmler-Wolff reaction, promoted by molecular iodine. Therein, noble metal catalysts and inert atmosphere are unnecessary while the forcing reaction conditions and the lengthy synthesis can be avoided. The synthetic utility of this approach is evident in the de novo syntheses of three bioactive molecules with good total yields.