Mechanochemical Strategies Applied to the Late‐Stage Modifications of Pharmaceutically Active Compounds

This review explores the potential of mechanochemistry in the late-stage modification of active pharmaceutical ingredients (APIs), offering a comprehensive analysis of methods designed to transform structurally complex molecular scaffolds by examining the scope, efficiency, and mechanistic aspects of these approaches. To further assist researchers, we provide a detailed table summarizing the discussed APIs, their respective modifications, and any necessary prefunctionalizations. This resource should provide a practical guide for selecting suitable substrates to evaluate the pharmaceutical relevance of existing and novel (mechano)chemical methods.