A unified lead-oriented synthesis of over fifty molecular scaffolds

作者: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
来源:Organic and Biomolecular Chemistry, 2015, 13(3): 859-865.
DOI:10.1039/c4ob02287d

摘要

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.

  • 出版日期2015