Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery

Publication date: 15 February 2018
Source:Bioorganic & Medicinal Chemistry, Volume 26, Issue 4
Author(s): Gemma C. Geary, Andrew Nortcliffe, Christopher A. Pearce, Daniel Hamza, Geraint Jones, Christopher J. Moody
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.

Graphical abstract

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