DMAPO/Boc₂O-Mediated One-Pot Direct N-Acylation of Oxazolidinones with Carboxylic Acids

Abstract

This report describes a general and simple method for the one-pot direct N-acylation of oxazolidinones with carboxylic acids using our previously developed 4-(N,N-dimethylamino)pyridine N-oxide (DMAPO)/di-tert-butyl dicarbonate (Boc₂O) system. This method employs mild reaction conditions and provides N-acyl oxazolidinones in high yields, which can then be used in various asymmetric transformations. As the present method is operationally simple, scalable, and practical, it should find wide applications in asymmetric syntheses of natural products and pharmaceuticals.

Keywords

Acylation - N-oxides - Oxazolidinones - Carboxylic acids - Synthetic methods - Chiral auxiliaries

Publication History

Received: 31 July 2025

Accepted after revision: 14 September 2025

Accepted Manuscript online:
14 September 2025

Article published online:
02 October 2025

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