Decarboxylative benzylations of alkynes and ketones

J Am Chem Soc. 2010 Jul 14;132(27):9280-2. doi: 10.1021/ja1035557.

Abstract

Benzyl esters of propiolic and beta-keto acids undergo catalytic decarboxylative coupling when treated with appropriate palladium catalysts. Such decarboxylative couplings allow the benzylation of alkynes without the use of strong bases and/or organometallics. This allows the synthesis of sensitive benzylic alkynes that are prone to undergo isomerizations under basic conditions. Additionally, decarboxylation facilitates the site-specific benzylation of diketones and ketoesters under mild, base-free conditions. Ultimately, the methodology described expands our ability to cross-couple medicinally relevant heterocycles.

Publication types

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

MeSH terms

  • Alkynes / chemistry*
  • Benzene / chemistry*
  • Cross-Linking Reagents
  • Decarboxylation
  • Heterocyclic Compounds / chemistry
  • Ketones / chemistry*

Substances

  • Alkynes
  • Cross-Linking Reagents
  • Heterocyclic Compounds
  • Ketones
  • Benzene