In a world where budgets and head counts are increasingly constrained and environmental impact scrutinized, new automated laboratory capabilities spanning from organic synthesis, analytical chemistry, through mechanical, chemical, and electrical engineering to robotics, computer science, and information technologies, are finding use as transformative methods for facilitating faster and better drug discovery operations as well as accelerated development of patient‐centric treatments and personalized medical applications. A significant challenge for life sciences researchers is gaining rapid access to probe molecules to query biological targets or pathways identified through various screening activities. Additional challenges include the ability to quickly and interactively optimize molecules identified as hits from screening activities. In the past two decades, the race has been on to build an automated laboratory to address gaps in organic synthesis and thereby supporting biological and drug discovery research by providing rapid access to a synthetic chemistry resource that is both cost‐effective and robust. This review focuses on concepts and approaches that have already been introduced in the automated synthesis world and also innovative technologies that could radically change small and large molecules research and, thus, have far‐reaching implications in the intelligent automation drug discovery world in the near future.
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