Iodine‐Promoted Sequential C(<i>sp</i>³)H Functionalization Reactions: An Annulation Strategy for the Construction of 3‐Methylthio‐4‐arylmaleimides

Abstract

Abstract A new process has been developed for the iodine‐promoted sequential C( sp 3 )H bond functionalization of methyl ketones and acetamides. This reaction represents a novel annulation strategy for the synthesis of 3‐(methylthio)‐4‐aryl‐1 H ‐pyrrole‐2,5‐diones, and involves an α‐ketoimide as the key intermediate. Furthermore, DMSO was converted to DMS in situ , which served as the methylthiolation reagent in the reaction. This protocol constitutes an efficient and convenient method for the methylthiolation of substrates bearing a wide range of functional groups. magnified image