Solid-phase synthesis of oxazolones and other heterocycles via Wang resin-bound diazocarbonyls

Abstract

The preparation of Wang resin bound α-diazo-β-ketoesters is described. These highly useful intermediates were used for the synthesis of a series of heterocycle libraries, which were obtained from the resin using TFA cleavage. In addition, a novel route for the synthesis of oxazolones using an N-H insertion strategy is disclosed. © 2005 Elsevier Ltd. All rights reserved.