Copper-catalysed C-H functionalisation gives access to 2-aminobenzimidazoles

Peter R. Clark, Glynn D. Williams, Nicholas C. O. Tomkinson

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)
8 Downloads (Pure)


This paper describes the development, optimisation and exemplification of a copper-catalysed C–H functionalisation to form pharmaceutically relevant 2-aminobenzimidazoles from aryl-guanidines. High throughput screening was used as a tool to identify a catalytically active copper source, DoE was used for reaction optimisation and a range of aryl-guanidines were prepared and exposed to the optimum conditions to afford a range of 2-aminobenzimidazoles in moderate to good yields. The methodology has been applied to the synthesis of Emedastine, a marketed anti-histamine pharmaceutical compound, with the key cyclisation step performed on a gram-scale.
Original languageEnglish
Pages (from-to)7943-7955
Number of pages13
JournalOrganic and Biomolecular Chemistry
Issue number34
Early online date13 Aug 2019
Publication statusPublished - 14 Sep 2019


  • optimisation
  • development
  • 2-aminobenzimidazoles
  • copper-catalysed C–H functionalisation


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