Transformation of anionically activated trifluoromethyl groups to heterocycles under mild aqueous conditions

Org Lett. 2011 Apr 1;13(7):1804-7. doi: 10.1021/ol200326u. Epub 2011 Mar 7.

Abstract

The (hetero)aromatic trifluoromethyl group is present in many biologically active molecules and is generally considered to be chemically stable. In this paper, a convenient one-step synthesis of C-C linked aryl-heterocycles or heteroaryl-heterocycles in good to excellent yields via the reaction of anionically activated trifluoromethyl groups with amino nucleophiles containing a second NH, OH, or SH nucleophile in 1 N sodium hydroxide is reported. The method has high functional group tolerability and is potentially useful in parallel synthesis.

MeSH terms

  • Anions / chemistry
  • Fluorine Compounds / chemistry*
  • Heterocyclic Compounds / chemistry*
  • Methylation
  • Molecular Structure
  • Stereoisomerism

Substances

  • Anions
  • Fluorine Compounds
  • Heterocyclic Compounds