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A happy medium: the synthesis of medicinally important medium-sized rings: Via ring expansion

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Publication details

JournalChemical Science
DateAccepted/In press - 27 Feb 2020
DateE-pub ahead of print - 2 Mar 2020
DatePublished (current) - 21 Mar 2020
Issue number11
Number of pages6
Pages (from-to)2876-2881
Early online date2/03/20
Original languageEnglish


Medium-sized rings have much promise in medicinal chemistry, but are difficult to make using direct cyclisation methods. In this minireview, we highlight the value of ring expansion strategies to address this long-standing synthetic challenge. We have drawn on recent progress (post 2013) to highlight the key reaction design features that enable successful 'normal-to-medium' ring expansion for the synthesis of these medicinally important molecular frameworks, that are currently under-represented in compound screening collections and marketed drugs in view of their challenging syntheses.

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© The Royal Society of Chemistry 2020



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