Abstract

Flow chemistry is one of the most prominent enabling technologies that has greatly shaped the way chemists’ approach organic synthesis. Specifically, in drug discovery, the advantages of flow techniques over batch procedures allow the rapid and efficient assembly of compound libraries to be tested for biological properties. The aim of the present review is to comment on some representative examples from the last five years of literature that highlight how flow procedures are becoming of increasing importance for the synthesis of biologically-relevant molecules.

Highlights

  • In the past decade, enabling technologies, i.e., all the methodologies that can speed-up chemical processes as well as simplify work-up procedures have greatly influenced the approach of chemists toward the development of new synthetic protocols [1,2,3,4]

  • A plethora of articles and reviews well-documented how many chemical processes could benefit from running reactions in flow [5,6,7,8,9]. This approach has demonstrated to be superior to batch protocols in every case where heat transfer and mixing are important, hazardous or sensitive materials are handled, and high temperatures/pressures are required. This technology is considered a green synthetic approach as it often delivers better product yields than those derived from batch protocols, and it allows easier product purification leading to minimum waste production [10,11,12]

  • In the drug discovery field, the need for novel molecules with drug-like structures to be used for high-throughput screening required enabling technologies for their production; in this context, flow chemistry represents the ideal tool for generating compound libraries in a fast and automated fashion [13]

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Summary

Introduction

In the past decade, enabling technologies, i.e., all the methodologies that can speed-up chemical processes as well as simplify work-up procedures have greatly influenced the approach of chemists toward the development of new synthetic protocols [1,2,3,4]. A plethora of articles and reviews well-documented how many chemical processes could benefit from running reactions in flow [5,6,7,8,9] This approach has demonstrated to be superior to batch protocols in every case where heat transfer and mixing are important, hazardous or sensitive materials are handled, and high temperatures/pressures are required. Fromliterature this green metric, it was possible to calculation and comparison the batch protocol and other processes values From this evaluate the beneficial effect oftothe flow methodology that allowed obtaining. 11 (Scheme corresponding epoxides 11 (Scheme 4a) [27]

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