Iodine‐Promoted Sequential C(sp3)-H Functionalization Reactions: An Annulation Strategy for the Construction of 3‐Methylthio‐4‐arylmaleimides

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Abstract
A new process has been developed for the iodine‐promoted sequential C(sp3)H bond functionalization of methyl ketones and acetamides. This reaction represents a novel annulation strategy for the synthesis of 3‐(methylthio)‐4‐aryl‐1H‐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

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