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Strategies for the synthesis of spiropiperidines – a review of the last 10 years

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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.

Graphical abstract: Strategies for the synthesis of spiropiperidines – a review of the last 10 years

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Publication details

The article was received on 29 May 2018, accepted on 03 Jul 2018 and first published on 04 Jul 2018


Article type: Review Article
DOI: 10.1039/C8OB01271G
Citation: Org. Biomol. Chem., 2018, Advance Article
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    Strategies for the synthesis of spiropiperidines – a review of the last 10 years

    S. D. Griggs, D. T. Tape and P. A. Clarke, Org. Biomol. Chem., 2018, Advance Article , DOI: 10.1039/C8OB01271G

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