Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery

Gold catalysed rearrangement of a propargylic alcohol leads to densely finctionaised spirocyclic oxetane-piperidine scaffolds for drug discovery. [Display omitted] A spirocyclic, sp3-atom rich oxetane-containing scaffold was synthesised in just two steps via a gold catalysed propargylic alcohol rear...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2018-02, Vol.26 (4), p.791-797
Main Authors: Geary, Gemma C., Nortcliffe, Andrew, Pearce, Christopher A., Hamza, Daniel, Jones, Geraint, Moody, Christopher J.
Format: Article
Language:English
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Summary:Gold catalysed rearrangement of a propargylic alcohol leads to densely finctionaised spirocyclic oxetane-piperidine scaffolds for drug discovery. [Display omitted] A spirocyclic, sp3-atom rich oxetane-containing scaffold was synthesised in just two steps via a gold catalysed propargylic alcohol rearrangement. The key gold cyclisation can be undertaken on a 40 g scale allowing the preparation of 419 lead-like compounds based on the scaffold for the European Lead Factory.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2017.12.012