Solid-phase rhodium carbenoid reactions: an N-H insertion route to a diverse series of oxazoles

Org Lett. 2001 Jul 12;3(14):2173-6. doi: 10.1021/ol010075n.

Abstract

[reaction: see text] The solid-phase synthesis of a series of oxazoles is described. The key step in the construction of these molecules involves the rhodium-catalyzed decomposition of polymer-bound alpha-diazo-beta-ketoesters. These reactions are performed in the presence of primary amides and yield the corresponding N-H insertion products. Subsequent cyclodehydration of these alpha-(acylamino)-beta-ketoesters provides the corresponding resin-bound 2,5-disubstituted oxazoles, which are further elaborated during cleavage from the resin.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amines / chemical synthesis*
  • Amines / chemistry*
  • Catalysis
  • Chromatography, High Pressure Liquid
  • Cyclization
  • Models, Chemical
  • Molecular Structure
  • Oxazoles / chemical synthesis*
  • Oxazoles / chemistry*
  • Rhodium / chemistry*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Amines
  • Oxazoles
  • Rhodium