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Issue 3, 2015
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A unified lead-oriented synthesis of over fifty molecular scaffolds

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Abstract

Controlling the properties of lead molecules is critical in drug discovery, but sourcing large numbers of lead-like compounds for screening collections is a major challenge. A unified synthetic approach is described that enabled the synthesis of 52 diverse lead-like molecular scaffolds from a minimal set of 13 precursors. The divergent approach exploited a suite of robust, functional group-tolerant transformations. Crucially, after derivatisation, these scaffolds would target significant lead-like chemical space, and complement commercially-available compounds.

Graphical abstract: A unified lead-oriented synthesis of over fifty molecular scaffolds

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Publication details

The article was received on 28 Oct 2014, accepted on 29 Oct 2014 and first published on 18 Nov 2014


Article type: Paper
DOI: 10.1039/C4OB02287D
Citation: Org. Biomol. Chem., 2015,13, 859-865
  • Open access: Creative Commons BY license
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    A unified lead-oriented synthesis of over fifty molecular scaffolds

    R. G. Doveston, P. Tosatti, M. Dow, D. J. Foley, H. Y. Li, A. J. Campbell, D. House, I. Churcher, S. P. Marsden and A. Nelson, Org. Biomol. Chem., 2015, 13, 859
    DOI: 10.1039/C4OB02287D

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