Medicinal chemistry is an interdisciplinary science at the interface of chemistry, chemical biology, pharmacology, and medicine, playing a fundamental role in drug discovery. Advances in science and technology such as synthesis machines, activity prediction models, and automated screening facilities are offering a fertile ground of interest in both academia and pharmaceutical industries in the development of innovative approaches that can address some of the current limitations of medicinal chemistry. In this chapter, recent developments toward flow-based strategies and their impact on lead identification and optimization are highlighted. Starting from concepts and equipment, representative examples that showcase the integration of continuous-flow synthesis with downstream operations and bioassays, as well as the latest developments in end-to-end machinery platforms as a whole discovery circuit, are illustrated.
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