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Strategies for the Synthesis of Spiropiperidines - A Review of the Last 10 Years
Research output: Contribution to journal › Review article
Author(s)
Department/unit(s)
Publication details
| Journal | Organic and Biomolecular Chemistry |
|---|---|
| Date | Accepted/In press - 3 Jul 2018 |
| Date | Published (current) - 4 Jul 2018 |
| Issue number | 36 |
| Volume | 16 |
| Number of pages | 14 |
| Pages (from-to) | 6620-6633 |
| Original language | English |
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.
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.
Bibliographical note
© 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
- Spirocycles, Piperidines, Medicinal chemistry
Research areas
Research outputs
Synthesis of highly substituted 2-spiropiperidines
Research output: Contribution to journal › Article
A Two-Step Synthesis of 2-Spiropiperidines
Research output: Contribution to journal › Article
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