A unified lead-oriented synthesis of over fifty molecular scaffoldsElectronic supplementary information (ESI) available. See DOI: 10.1039/c4ob02287d

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 minima...

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Main Authors Doveston, Richard G, Tosatti, Paolo, Dow, Mark, Foley, Daniel J, Li, Ho Yin, Campbell, Amanda J, House, David, Churcher, Ian, Marsden, Stephen P, Nelson, Adam
Format Journal Article
LanguageEnglish
Published 17.12.2014
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Summary: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. Sourcing large numbers of lead-like compounds is a major challenge; a unified synthetic approach enabled the efficient synthesis of 52 diverse lead-like molecular scaffolds from just 13 precursors.
Bibliography:10.1039/c4ob02287d
Electronic supplementary information (ESI) available. See DOI
ISSN:1477-0520
1477-0539
DOI:10.1039/c4ob02287d