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

Angew Chem Int Ed Engl. 2024 Apr 15:e202402060. doi: 10.1002/anie.202402060. Online ahead of print.ABSTRACTThe 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.PMID:38618872 | DOI:10.1002/anie.202402060

Source: Angewandte Chemie - April 15, 2024 Category: Chemistry Authors: Hendrik Simon Agnese Zangarelli Tristan Bauch Lutz Ackermann Source Type: research