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Issue 28, 2016
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Modern advances in heterocyclic chemistry in drug discovery

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New advances in synthetic methodologies that allow rapid access to a wide variety of functionalized heterocyclic compounds are of critical importance to the medicinal chemist as it provides the ability to expand the available drug-like chemical space and drive more efficient delivery of drug discovery programs. Furthermore, the development of robust synthetic routes that can readily generate bulk quantities of a desired compound help to accelerate the drug development process. While established synthetic methodologies are commonly utilized during the course of a drug discovery program, the development of innovative heterocyclic syntheses that allow for different bond forming strategies are having a significant impact in the pharmaceutical industry. This review will focus on recent applications of new methodologies in C–H activation, photoredox chemistry, borrowing hydrogen catalysis, multicomponent reactions, regio- and stereoselective syntheses, as well as other new, innovative general syntheses for the formation and functionalization of heterocycles that have helped drive project delivery. Additionally, the importance and value of collaborations between industry and academia in shaping the development of innovative synthetic approaches to functionalized heterocycles that are of greatest interest to the pharmaceutical industry will be highlighted.

Graphical abstract: Modern advances in heterocyclic chemistry in drug discovery

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Publication details

The article was received on 29 Apr 2016, accepted on 02 Jun 2016 and first published on 10 Jun 2016

Article type: Review Article
DOI: 10.1039/C6OB00936K
Org. Biomol. Chem., 2016,14, 6611-6637

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    Modern advances in heterocyclic chemistry in drug discovery

    A. P. Taylor, R. P. Robinson, Y. M. Fobian, D. C. Blakemore, L. H. Jones and O. Fadeyi, Org. Biomol. Chem., 2016, 14, 6611
    DOI: 10.1039/C6OB00936K

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