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Issue 12, 2012
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Emac – a comparative index for the assessment of macrocyclization efficiency

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Abstract

Macrocycle-based drug design represents an exciting new frontier in drug discovery, and consequently there is considerable interest in methodologies for the efficient construction of macrocyclic motifs. However, typical high-dilution macrocyclization conditions are inefficient and impractical in a pharmaceutical setting from cost, capacity and green chemistry perspectives. This critical review reports the results of a comprehensive literature survey of recent macrocyclization reactions and proposes a macrocyclization efficiency index, Emac, which takes into account both reaction yield and concentration. Analysis and discussion of the literature dataset using this novel metric are presented, along with selected examples of high and low efficiency macrocyclizations.

Graphical abstract: Emac – a comparative index for the assessment of macrocyclization efficiency

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Publication details

The article was received on 30 Jun 2012, accepted on 24 Aug 2012 and first published on 29 Aug 2012


Article type: Review Article
DOI: 10.1039/C2MD20176C
Med. Chem. Commun., 2012,3, 1489-1495

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    Emac – a comparative index for the assessment of macrocyclization efficiency

    J. C. Collins and K. James, Med. Chem. Commun., 2012, 3, 1489
    DOI: 10.1039/C2MD20176C

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