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Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery

Geary, Gemma C.; Nortcliffe, Andrew; Pearce, Christopher A.; Hamza, Daniel; Jones, Geraint; Moody, Christopher J.

Authors

Gemma C. Geary

Andrew Nortcliffe

Christopher A. Pearce

Daniel Hamza

Geraint Jones

Christopher J. Moody



Abstract

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.

Journal Article Type Article
Journal Bioorganic & Medicinal Chemistry
Electronic ISSN 0968-0896
Publisher Elsevier
Peer Reviewed Peer Reviewed
APA6 Citation Geary, G. C., Nortcliffe, A., Pearce, C. A., Hamza, D., Jones, G., & Moody, C. J. (in press). Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery. Bioorganic and Medicinal Chemistry, doi:10.1016/j.bmc.2017.12.012
DOI https://doi.org/10.1016/j.bmc.2017.12.012
Publisher URL https://www.sciencedirect.com/science/article/pii/S0968089617321880?via%3Dihub
Copyright Statement Copyright information regarding this work can be found at the following address: http://creativecommons.org/licenses/by-nc-nd/4.0

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Chris Moody Densely functionalised spirocclic.pdf (722 Kb)
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Copyright Statement
Copyright information regarding this work can be found at the following address: http://creativecommons.org/licenses/by-nc-nd/4.0





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