2-Methoxy-6-oxo-1,4,5,6-tetrahydropyridine-3-carbonitriles: versatile starting materials for the synthesis of libraries with diverse heterocyclic scaffolds

J Comb Chem. 2005 May-Jun;7(3):436-48. doi: 10.1021/cc049828y.

Abstract

Heterocyclic demonstration libraries for agrochemical screening were prepared from the common intermediates 2-methoxy-6-oxo-1,4,5,6-tetrahydropyridine-3-carbonitriles (1), using standard solution-phase techniques. A total of 18 screening libraries were prepared in good to excellent yields. Several members of these libraries were active in the first level of agrochemical screening, especially in the fungicide screen.

MeSH terms

  • Chemistry, Pharmaceutical*
  • Combinatorial Chemistry Techniques*
  • Cyclization
  • Drug Evaluation, Preclinical
  • Fungicides, Industrial / analysis
  • Fungicides, Industrial / pharmacology
  • Heterocyclic Compounds / chemical synthesis*
  • Molecular Weight
  • Nitriles / chemistry*
  • Pyridones / chemistry*
  • Stereoisomerism

Substances

  • Fungicides, Industrial
  • Heterocyclic Compounds
  • Nitriles
  • Pyridones