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Benzamide derivatives are highly prevalent in biologically active compounds, including approved and investigational drugs of diverse mechanism of action. They have also been exploited as radiotracers for melanoma imaging and as chromophores for stereochemical studies by circular dichroism. Such a wide range of applications of benzamides makes late-stage modification of their structure a vibrant area of research. In this chapter, we review the state of the art in photocatalytic modifications of benzamides at their N-alkyl fragments. The protocols developed so far include such transformations as intramolecular cyclisation, annulation, intermolecular C–H arylation, alkylation and N-dehalogenation processes. We also indicate probable directions for further development in this area of research.

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