Nishad, Chandra ShekharHaldar, Krishna KantaBanerjee, Biplab2024-01-212024-08-132024-01-212024-08-132022-08-1722326310.1021/acs.joc.2c01292http://10.2.3.109/handle/32116/3249We report a mild and efficient metal-free one-pot procedure for the synthesis of N-sulfonyl amidines via the direct reaction of sulfonamides with secondary amines without using any additives. A wide range of substrates with variety of functional groups is well tolerated under the reaction conditions. Preliminary mechanistic studies indicate that the secondary amine plays a dual role as a C1 source of the amidine group and an aminating agent. Synthetic utility of this method is shown in the late-stage functionalization of drug molecules on the gram scale. � 2022 American Chemical Society.en-USAmidesAminesSulfur compoundsamidineaminefunctional groupsulfonamideBond formationDirect reactionsDual roleMechanistic studiesMetal freeOne-pot proceduresReaction conditionsSecondary aminesSulphonamidesSynthetic utilityArticlecontrolled studyone pot synthesissynthesisAdditivesArticlehttps://pubs.acs.org/doi/10.1021/acs.joc.2c01292