Late‐Stage Functionalisation of Pyridine‐Containing Bioactive Molecules: Recent Strategies and Perspectives

Late‐Stage Functionalisation (LSF) is an innovative technique that has been successfully applied to the C−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. Mind the gap! A practical guide to navigate through the complex network of selective late‐stage functionalisations of pyridine‐containing biomolecules.