Enantiopure quaternary alpha-trifluoromethyl-alpha-alkoxyaldehydes from L-tartaric acid derived ketoamides

J Org Chem. 2008 Oct 17;73(20):7990-5. doi: 10.1021/jo8013403. Epub 2008 Sep 25.

Abstract

The diastereoselective nucleophilic trifluoromethylation of a range of ketoamides derived from L-tartaric acid has been studied. TMSCF3 in the presence of a catalytic amount of K2CO3 in DMF has been identified as the conditions leading to the highest diastereoselectivities. A sequential one-pot reaction trifluoromethylation-etherification of the trifluoromethylcarbinol has been developed. Only one further one-pot reaction, ketal hydrolysis-oxidative cleavage, led to the final alpha-trifluoromethylated alpha-alkoxyaldehydes. This procedure was applied to the preparation of a series of enantiopure aryl, heteroaryl, and alkyl alpha-trifluoromethyl-alpha-alkoxyaldehydes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemical synthesis
  • Aldehydes / chemistry*
  • Alkylation
  • Amides / chemistry*
  • Catalysis
  • Dimethylformamide / chemistry
  • Hydrocarbons, Fluorinated / chemistry*
  • Ketones / chemistry*
  • Magnetic Resonance Spectroscopy
  • Silanes / chemistry*
  • Stereoisomerism
  • Tartrates / chemistry*

Substances

  • Aldehydes
  • Amides
  • Hydrocarbons, Fluorinated
  • Ketones
  • Silanes
  • Tartrates
  • Dimethylformamide
  • trimethyl(trifluoromethyl)silane
  • tartaric acid