Synthesis of Constrained Peptidomimetics via the Pictet-Spengler Reaction

Rico Petersen, Vitaly V. Komnatnyy, Thomas E. Nielsen

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Peptidomimetics offers a solution to the poor pharmacokinetic properties displayed by natural peptides, by providing pharmaceutically useful chemical structures with the ability to mimic the endogenous polyamide structure. This chapter gives an overview of the past decade’s developments in the field of Pictet-Spengler reactions for the synthesis of peptidomimetics, with an emphasis on the applications of constrained heterocycles in mimicry of peptide geometry and biology.
Original languageEnglish
Title of host publicationPeptidomimetics II
EditorsWilliam Lubell
Publication date2016
ISBN (Print)978-3-319-49123-3
ISBN (Electronic)978-3-319-49124-0
Publication statusPublished - 2016
SeriesTopics in Heterocyclic Chemistry


  • Drug discovery
  • Peptidomimetics
  • Pictet-Spengler reaction

Cite this

Petersen, R., Komnatnyy, V. V., & Nielsen, T. E. (2016). Synthesis of Constrained Peptidomimetics via the Pictet-Spengler Reaction. In W. Lubell (Ed.), Peptidomimetics II (Vol. 49, pp. 81-103). Springer. Topics in Heterocyclic Chemistry