Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery.

Bioorg Med Chem

School of Chemistry, University of Nottingham, University Park, Nottingham NG7 2RD, UK. Electronic address:

Published: February 2018

A spirocyclic, sp-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.

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http://dx.doi.org/10.1016/j.bmc.2017.12.012DOI Listing

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