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Strategies for the Synthesis of Spiropiperidines - A Review of the Last 10 Years

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JournalOrganic and Biomolecular Chemistry
DateAccepted/In press - 3 Jul 2018
DatePublished (current) - 4 Jul 2018
Issue number36
Volume16
Number of pages14
Pages (from-to)6620-6633
Original languageEnglish

Abstract

Spiropiperidines have gained in popularity in drug discovery programmes as medicinal chemists explore new areas of
three-dimensional chemical space. This review focuses on the methodology used for the construction of 2-, 3- and 4-
spiropiperidines, covering the literature from the last 10 years. It classifies the synthesis of each of the types of
spiropiperidine by synthetic strategy: the formation of the spiro-ring on a preformed piperidine ring, and the formation of
the piperidine ring on a preformed carbo- or heterocyclic ring. While 3- and 4-spiropiperidines are predominantly
synthesised for drug discovery projects, 2-spiropiperidines are synthesised en route to natural products. The lack of 2-
spiropiperidines in drug discovery is presumably due to limited general procedures for their synthesis.

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© 2018, The Royal Society of Chemistry.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

  • Spirocycles, Piperidines, Medicinal chemistry

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