Iron-catalysed C–H ortho-arylation of edaravone, a promising monoamine oxidase-B inhibitor

Abstract

Edaravone is a neuroactive drug that is currently used in the treatment of stroke patients and shows promise against a range of neurodegenerative processes including amyotrophic lateral sclerosis, Parkinson's disease and Alzheimer's disease. We show that iron-catalysed C–H functionalisation of edaravone and its derivatives can be exploited to generate a small library of 21 arylated edaravones, while the results of a preliminary computational binding study of these derivatives predicts that they should all bind more strongly in the active site of monoamine oxidase-B than edaravone.