The perspective is focused on chemical transformations which are intended for scale-up, and the primary objective is data generation and not necessarily miniaturization to minimize material demand. In this review article, we aim to provide a comprehensive view of how HTE is being used in pharmaceutical companies for chemical transformations. A series of case studies are presented to exemplify state-of-the-art workflows developed within our laboratories. This review will deliver an overview of the latest best practices currently taking place within our teams in process chemistry by sharing frequently studied transformations, our perspective for the next several years in the field, and manual and automated tools to enable experimentation. The industry’s commitment to accelerating process development has led to rapid innovations in the HTE space. Today, most major pharmaceutical companies have created dedicated HTE groups within their process development teams, invested in automation technology to accelerate screening, or both. The past decade has also witnessed the extension of HTE principles toward the realm of small-molecule process chemistry. High-throughput experimentation (HTE) has revolutionized the pharmaceutical industry, most notably allowing for rapid screening of compound libraries against therapeutic targets.
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