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

Johanna Templ, Lars Borchardt

2025Angewandte Chemie International Edition23 citationsDOIOpen Access PDF

Abstract

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.

Topics & Concepts

Scope (computer science)Computer scienceRelevance (law)Biochemical engineeringMechanochemistryResource (disambiguation)NanotechnologyEngineeringMaterials scienceLawComputer networkProgramming languagePolitical sciencePlant-based Medicinal ResearchCrystallography and molecular interactionsSynthesis and Reactivity of Heterocycles