Late-Stage Functionalisation (LSF) is an innovative technique that has been successfully applied to the CÀ H diversification of pharmaceuticals. However, LSF of the pyridine ring in drug-like molecules is often unselective. As a result, a mixture of structurally related products is obtained, thus making the purification tedious and time-consuming. This review shines a light on recent strategies addressing the selectivity issue in the LSF of complex natural products or drugs containing the pyridine moiety. Specifically, we have reviewed the efforts reported both in academia and industries with the hope of providing a guide for the LSF of elaborated pyridines.

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The Front Cover Cover illustrates how the pyridine ring of the antihistamine loratadine can be selectively functionalised at the ortho‐, meta‐, or para‐position (each of them activated by a thunder). Indeed, the selective functionalisation of this N‐heterocycle is often problematic, thus a lighthouse guides the chemists through the late‐stage functionalisations of pyridine‐containing biomolecules. More information can be found in the Review by V. Fasano et al.