Enantioselective organocatalytic α-fluorination of cyclic ketones

J Am Chem Soc. 2011 Feb 16;133(6):1738-41. doi: 10.1021/ja111163u. Epub 2011 Jan 19.

Abstract

The first highly enantioselective α-fluorination of ketones using organocatalysis has been accomplished. The long-standing problem of enantioselective ketone α-fluorination via enamine activation has been overcome via high-throughput evaluation of a new library of amine catalysts. The optimal system, a primary amine functionalized Cinchona alkaloid, allows the direct and asymmetric α-fluorination of a variety of carbo- and heterocyclic substrates. Furthermore, this protocol also provides diastereo-, regio-, and chemoselective catalyst control in fluorinations involving complex carbonyl systems.

Publication types

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

MeSH terms

  • Catalysis
  • Halogenation*
  • Ketones / chemistry*
  • Stereoisomerism
  • Substrate Specificity

Substances

  • Ketones