1-Substituted 2-Azaspiro[3.3]heptanes: Overlooked Motifs for Drug Discovery

Angew Chem Int Ed Engl. 2017 Jul 17;56(30):8865-8869. doi: 10.1002/anie.201703801. Epub 2017 Jun 19.

Abstract

The 2-substituted piperidine core is found in drugs (18 FDA-approved drugs), however, their spirocyclic analogues remain unknown. Described here is the synthesis of spirocyclic analogues for 2-substituted piperidines and a demonstration of their validation in drug discovery.

Keywords: drug discovery; heterocycles; small rings; spirocycles; synthetic methods.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aza Compounds / chemical synthesis*
  • Aza Compounds / chemistry
  • Drug Discovery*
  • Heptanes / chemical synthesis*
  • Heptanes / chemistry
  • Molecular Structure
  • Piperidines / chemistry*
  • Spiro Compounds / chemical synthesis*
  • Spiro Compounds / chemistry

Substances

  • Aza Compounds
  • Heptanes
  • Piperidines
  • Spiro Compounds