49573-85-5Relevant academic research and scientific papers
Copper-catalysed C-H functionalisation gives access to 2-aminobenzimidazoles
Clark, Peter R.,Williams, Glynn D.,Tomkinson, Nicholas C. O.
, p. 7943 - 7955 (2019)
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.
