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A Two-Step Synthesis of 2-Spiropiperidines

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Published copy (DOI)


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


Publication details

JournalChemistry : A European Journal
DateAccepted/In press - 31 May 2017
DateE-pub ahead of print - 31 May 2017
DatePublished (current) - 12 Jul 2017
Issue number39
Number of pages4
Pages (from-to)9262-9265
Early online date31/05/17
Original languageEnglish


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.

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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

    Research areas

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


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