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

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 Noxide (DMAPO)/di-tert-butyl dicarbonate (Boc 2 O) 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.

Publication History

Received: 31 July 2025

Accepted after revision: 14 September 2025

Accepted Manuscript online:
14 September 2025