Innovative Organic Synthesis Approaches in Drug Design and Development

Dear Colleagues, 

The development of novel therapeutics is increasingly dependent on innovative, efficient and sustainable organic synthesis strategies. While traditional methods are foundational to medicinal chemistry, they often involve lengthy synthetic sequences, limited atom economy and extensive use of toxic reagents or volatile organic solvents. To address these challenges, the field is shifting towards methodologies that combine chemical innovation with the principles of green chemistry. This approach fosters safer, cleaner and more resource-efficient drug discovery pipelines. This Special Issue showcases recent advances in synthetic methodologies that directly impact drug design and development. Topics of interest include transition-metal catalysis, Lewis Acid catalysis, photoredox and electrochemical transformations, organocatalysis, multicomponent reactions, flow chemistry and hybrid molecule approaches, combining different activation modes through various different pharmacophore motifs in a single organic structure. Particular emphasis will be placed on methodologies that expand accessible chemical spaces, enable the late-stage functionalization of bioactive molecules and provide higher levels of efficiency, selectivity and scalability. A central theme will be the adoption of non-traditional solvents and environmentally benign reaction conditions. Using ionic liquids, deep eutectic solvents, supercritical fluids and water as alternative media is one way to reduce the ecological footprint of pharmaceutical synthesis. In addition, the adoption of microwave-assisted solvent-free reactions provide a green approach to synthesizing a new bioactive compound. Combined with advances in automation, miniaturization and computationally guided reaction design, these approaches have the potential to transform drug discovery into an innovative process that is aligned with sustainability goals. Through a collection of original research articles, reviews and perspectives, this Special Issue will provide a comprehensive overview of how novel synthetic strategies are reshaping the design and development of therapeutic agents, offering new opportunities for innovation at the interface between synthetic chemistry and sustainable drug discovery and enhancing the biological activity of novel synthesized drugs. 

Dr. Antonio Jiritano
Dr. Vincenzo Algieri
Guest Editors

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