Outputs (2)

Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery (2017)
Journal Article
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, https://doi.org/10.1016/j.bmc.2017.12.012

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 co... Read More about Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery.

C–H insertion as a key step to spiro-oxetanes, scaffolds for drug discovery (2017)
Journal Article
Nicolle, S. M., Nortcliffe, A., Bartrum, H. E., Lewis, W., Hayes, C. J., & Moody, C. J. (in press). C–H insertion as a key step to spiro-oxetanes, scaffolds for drug discovery. Chemistry - A European Journal, https://doi.org/10.1002/chem.201703746

A new route to spiro-oxetanes, potential scaffolds for drug discovery, is described. The route is based on the selective 1,4-C–H insertion reactions of metallocarbenes, generated from simple carbonyl precursors in flow or batch mode, to give spiro-β-... Read More about C–H insertion as a key step to spiro-oxetanes, scaffolds for drug discovery.