A Two-Step Synthesis of 2-Spiropiperidines

Samuel D. Griggs, Nathan Thompson, Daniel T. Tape, Marie Fabre, Paul A. Clarke*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


A general two-step synthesis of 2-spiropiperidines has been developed. δ-Amino-β-ketoesters can be reacted with cyclic ketones to generate 2-spiropiperidines in good to excellent yields. The 2-spiropiperidines formed occupy an under-explored region of 3D-chemical space and are novel scaffolds for use in drug discovery programs. These 2-spiropiperidines can be further functionalised to generate small highly sp3-rich structures, which exhibit an excellent likeness to lead-molecules in drug discovery.

Original languageEnglish
Pages (from-to)9262-9265
Number of pages4
JournalChemistry : A European Journal
Issue number39
Early online date31 May 2017
Publication statusPublished - 12 Jul 2017

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© 2017 Wiley‐VCH Verlag GmbH & Co. KGaA, Weinheim. This is an author-produced version of the published paper. Uploaded in accordance with the publisher’s self-archiving policy. Further copying may not be permitted; contact the publisher for details


  • Maitland–Japp
  • medicinal chemistry
  • piperidine
  • scaffolds
  • spirocyclic

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