This thematic issue encompasses C–H bond functionalization reactions involving transition metal catalysis, photoredox catalysis, Lewis acid catalysis, as well as transition metal-free approaches. Next to the recent progress in this growing field, future directions for exploration and discovery will be highlighted.

In the past years, the field of synthetic organic chemistry (and particularly organometallic chemistry) has witnessed a tremendous growth in C–H bond functionalization reactions. This facilitates the efficient synthesis of numerous functionally dense biologically relevant molecules and natural products. Today, C–H bond functionalization has become a powerful tool for transforming inexpensive feedstock materials into complex molecular frameworks in an atom-economical and step-economical fashion, without requiring any halogenated or prefunctionalized precursors. The scope of such advantageous C–H bond functionalization reactions was further extended to remote C–H bond functionalization reactions. That way, manipulations can be achieved at the nonclassical sites of the substrates. Specifically, this involves either an undirected approach (chain walking functionalization) or directing-group-assisted strategies. Consequently, the design of novel synthetic paths involving C–H bond functionalization allows to bypass laborious multistep syntheses of target molecules in an eco-friendly way.

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