ANTIMO GIOIELLO
Laboratory of Medicinal and Advanced Synthetic Chemistry (Lab MASC),
Department of Pharmaceutical Sciences, University of Perugia,
Perugia, Italy

Abstract

In the changing landscape of drug discovery, technological innovation in synthesis is playing a crucial role in the successful delivery of novel therapeutics and in the development of modern processes for chemical manufacturing. This review article is aimed to provide in a concise way insights and evidences into how integrated flow platforms can improve drug discovery from early stages to market production, with particular emphasis on the new opportunities and technological advances.

There is no doubt that the role and tasks of the synthetic medicinal chemist in drug discovery have changed over the last years (1). About 50 years ago, compounds were designed and individually synthesized in gram quantities to satisfy the request of material for testing in animal models. Given the restricted methods and tools available to assist with compound preparation and characterization, these syntheses were often time-consuming, risky and poorly efficient. The output encompassed few products per week and compound libraries for exploratory biological screening were very limited. These drawbacks when combined with the lack of knowledge about the target and disease rendered the process at early stage of drug discovery slower and based on the intuition and creativity of the medicinal chemist.
More recently, the advent of high-throughput screening (HTS) and computational modelling, and the crucial use of chemical probes for unravelling the function and therapeutic potential of unstudied biological targets, have changed the landscape and broadened the importance of chemical synthesis. Nowadays, synthetic methods need to be versatile to guarantee a fast access to chemic ...