Thiazolium-catalyzed intermolecular Stetter reaction of linear and cyclic alkyl α-diketones

Org Biomol Chem. 2011 Dec 21;9(24):8437-44. doi: 10.1039/c1ob06480k. Epub 2011 Oct 26.

Abstract

An efficient method for the N-heterocyclic carbene (NHC)-catalyzed conjugate addition of acetyl anions to various α,β-unsaturated acceptors (Stetter reaction) has been optimized by using 2,3-butandione (biacetyl) as an alternative surrogate of acetaldehyde. The disclosed procedure proved to be compatible with microwave dielectric heating for reaction time reduction and with the use of different linear α-diketones as acyl anion donors (e.g. 3,4-hexanedione for propionyl anion additions). Moreover, the unprecedented umpolung reactivity of cyclic α-diketones in the atom economic nucleophilic acylation of chalcones is herein presented. Mechanistic aspects of the thiazolium-based catalysis involving linear and cyclic α-diketone substrates are also discussed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Ketones / chemical synthesis*
  • Ketones / chemistry
  • Molecular Structure
  • Thiazoles / chemistry*

Substances

  • Ketones
  • Thiazoles