Login / Signup

Ruthenium(II)-Catalyzed Late-Stage Incorporation of N-Aryl Triazoles and Tetrazoles with Sulfonium Salts via C-H Activation.

Hendrik SimonAgnese ZangarelliTristan BauchHarry L Anderson
Published in: Angewandte Chemie (International ed. in English) (2024)
The late-stage functionalization of active pharmaceutical ingredients is a key challenge in medicinal chemistry. Furthermore, N-aryl triazoles and tetrazoles are important structural motifs with the potential to boost the activity of diverse drug molecules. Using easily accessible dibenzothiophenium salts for the ruthenium-catalyzed C-H arylation, these scaffolds were introduced into a variety of bioactive compounds. Our methodology uses cost-efficient ruthenium, KOAc as a mild base and gives access to a plethora of highly decorated triazole and tetrazole containing drug derivatives.
Keyphrases
  • room temperature
  • ionic liquid
  • adverse drug
  • drug induced
  • quantum dots
  • emergency department
  • tissue engineering
  • human health
  • risk assessment
  • drug discovery