An overview of late-stage functionalization in today's drug discovery.

Clicks: 371
ID: 26452
2019
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Ranked #5 of 25 articles by views in expert opinion on drug discovery

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Abstract
: Late-stage functionalization (LSF) can introduce important chemical groups in the very last steps of the synthesis. LSF has the potential to speed up the preparation of novel chemical entities and diverse chemical libraries and have a major impact on drug discovery. Functional group tolerance and mild conditions allows access to new molecules not easily accessible by conventional approaches without the need for laborious chemical synthesis. : A historical overview of late-stage functionalization and its applicability to drug discovery is provided. Pioneering methodologies that laid the foundations for the field are briefly covered and archetypal examples of their application to drug discovery are discussed. Novel methodologies reported in the past few years mainly stemming from the recent renaissances of photoredox catalysis and radical chemistry are reviewed and their application to drug discovery considered. : It is envisioned that late-stage functionalization will improve the efficiency and efficacy of drug discovery. There is evidence of the widespread uptake of LSF by the medicinal chemistry community and it is expected that the recent and continuing endeavors of many academic laboratories and pharmaceutical companies will soon have an impact on drug development.
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moir2019anexpert Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Moir, Michael;Danon, Jonathan J;Reekie, Tristan A;Kassiou, Michael;
Journal expert opinion on drug discovery
Year 2019
DOI
10.1080/17460441.2019.1653850
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Keywords Keywords not found

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