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, the review highlights protocols capable of effectively modifying structurally complex molecular scaffolds. To further assist researchers, we provide a detailed table summarizing the discussed APIs, their respective modifications, and any necessary pre-functionalizations. This resource should provide a practical guide for selecting suitable substrates to evaluate the pharmaceutical relevance of existing and novel (mechano)chemical methods.