期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 16, 期 36, 页码 6620-6633出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c8ob01271g
关键词
-
资金
- Department of Chemistry, University of York
- GlaxoSmithKline
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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