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DMAPO/Boc2O‐Mediated One‐Pot Direct N‐Acylation of Sulfoximines with Carboxylic Acids

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The one-pot direct N-acylation of NH sulsoximines with carboxylic acids is described. The method can be performed under mild low-temperature reaction conditions and exhibits a wide substrate scope (> 60 examples). The present method is operationally simple, scalable, and practical; thus, it can find wide applications in both academic and industrial laboratories.


This report describes a general and simple method for the one-pot direct N-acylation of sulfoximines with carboxylic acids using the previously developed 4-(N,N-dimethylamino)pyridine N-oxide (DMAPO)/di-tert-butyl dicarbonate (Boc2O) system. The method can be performed under mild low-temperature reaction conditions and has a wide substrate scope. The present method is operationally simple, scalable, and practical; thus, it can find wide applications in both academic and industrial laboratories.

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