An effective and general method for the highly regioselective synthesis of 1-phenylpyrazoles from beta-enaminoketoesters, tandem Blaise-acylation adducts

Org Biomol Chem. 2009 Mar 21;7(6):1132-6. doi: 10.1039/b820324e. Epub 2009 Jan 26.

Abstract

An effective and general route for the regioselective synthesis of 1-phenylpyrazoles has been developed from beta-enaminoketoesters prepared by tandem Blaise-acylation. This method is applicable to a very broad range of substrates, generating a diverse set of 3-aryl-5-alkyl, 3-alkyl-5-aryl, 3,5-diaryl, and 3,5-dialkyl substituted pyrazoles regioselectively. The dichotomous regioselective synthesis of isotopically discriminated 3-CD(3)-5-CH(3) and 3-CH(3)-5-CD(3) substituted pyrazoles showcases the power of this protocol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acylation
  • Crystallography, X-Ray
  • Esters / chemistry*
  • Ketones / chemistry*
  • Models, Molecular
  • Molecular Structure
  • Nitriles / chemistry
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / chemistry
  • Stereoisomerism

Substances

  • Esters
  • Ketones
  • Nitriles
  • Pyrazoles