Microwave-assisted three-component synthesis of 7-aryl-2-alkylthio-4,7-dihydro-1,2,4-triazolo[1,5-a]-pyrimidine-6-carboxamides and their selective reduction

J Comb Chem. 2006 May-Jun;8(3):427-34. doi: 10.1021/cc060021a.

Abstract

Multicomponent reactions (MCRs) and microwave-assisted organic synthesis (MAOS) have been used as key methods for the synthesis of fused dihydropyrimidine derivatives. The three-component condensation of 3-amino-5-alkylthio-1,2,4-triazoles with aromatic aldehydes and acetoacetamides under microwave irradiation was developed as a rapid and efficient solution-phase method for the high-yielding preparation of 7-aryl-2-alkylthio-4,7-dihydro-1,2,4-triazolo[1,5-a]pyrimidine-6-carboxamide libraries. In addition, the selective reduction of the formed dihydrotriazolopyrimidines to trans-trans-2-alkylthio-7-aryl-4,5,6,7-tetrahydro-1,2,4-triazolo[1,5-a]pyrimidine-6-carboxamides was established. The described synthetic protocols provide rapid access to novel and diversely substituted dihydroazolopyrimidine libraries.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetamides / chemistry
  • Aldehydes / chemistry
  • Amides / chemical synthesis*
  • Carboxylic Acids / chemistry*
  • Chemistry, Pharmaceutical
  • Combinatorial Chemistry Techniques
  • Microwaves*
  • Molecular Structure
  • Oxidation-Reduction
  • Pyrimidines / chemistry*
  • Stereoisomerism
  • Sulfhydryl Compounds / chemistry*
  • Triazoles / chemistry*

Substances

  • 1,2,4-triazolo(1,5-c)pyrimidine
  • Acetamides
  • Aldehydes
  • Amides
  • Carboxylic Acids
  • Pyrimidines
  • Sulfhydryl Compounds
  • Triazoles