Enantioselective organocatalysis using SOMO activation

Science. 2007 Apr 27;316(5824):582-5. Epub 2007 Mar 29.

Abstract

The asymmetric α-addition of relatively nonpolar hydrocarbon substrates, such as allyl and aryl groups, to aldehydes and ketones remains a largely unsolved problem in organic synthesis, despite the wide potential utility of direct routes to such products. We reasoned that well-established chiral amine catalysis, which activates aldehydes toward electrophile addition by enamine formation, could be expanded to this important reaction class by applying a single-electron oxidant to create a transient radical species from the enamine. We demonstrated the concept of singly occupied molecular orbital (SOMO) activation with a highly selective α-allylation of aldehydes, and we here present preliminary results for enantioselective heteroarylations and cyclization/halogenation cascades.

Publication types

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

MeSH terms

  • Aldehydes / chemistry*
  • Amines / chemistry
  • Catalysis*
  • Cyclization
  • Halogens / chemistry
  • Molecular Structure
  • Organic Chemicals / chemistry*
  • Oxidation-Reduction
  • Stereoisomerism*

Substances

  • Aldehydes
  • Amines
  • Halogens
  • Organic Chemicals