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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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Supplementary files

Article information


Submitted
28 Oct 2014
Accepted
29 Oct 2014
First published
18 Nov 2014

This article is Open Access

Org. Biomol. Chem., 2015,13, 859-865
Article type
Paper
Author version available

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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