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The benzamide moiety is among the most common structural fragments in pharmacologically relevant compounds. It is present in a variety of approved and investigational drugs of diverse mechanism of action, including antitumour agents,1,2  antiemetics,3  antipsychotic drugs and antidepressants,4  gastroprokinetic agents,5  antiparasitic and antiviral medications,6  platelet aggregation inhibitors,7  or recently inhibitors of SARS-CoV-2 replication8  (Fig. 1). Benzamide derivatives have also been utilised as radiotracers for melanoma imaging9,10  and applied as chromophores for cottonogenic derivatives of amines for stereochemical studies by circular dichroism.11  Such a wide range of application makes late-stage modification of their structure a vibrant area of research, with the potential to provide libraries of derivatives with unique properties.12,13 

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