Boost your Research with our Original Cyclopropanes

Our Unique Building Blocks to Perform Far and Wide
15 February 2021
Oleg Lukin
Senior Research Scientist

Small, lipophilic, and conformationally-constrained substituted cyclopropane rings are finding increasingly sophisticated use in pharmaceuticals.1 Unlike the monosubstituted ring, di- and tri-substituted cyclopropane rings can give rise to crucial stereochemical features.2 For instance, introducing a cyclopropane ring as a conformational constraint into a flexible peptide ligand can provide a preorganized pseudo peptide having significantly higher activity.3

Combining a substituted cyclopropane fragment with other privileged substructures (mainly heterocycles) has been successfully adopted in drug design. Presently, a number of both approved drugs and experimental drug candidates contain the cyclopropane as a scaffold to link the functional substructures with other privileged ligands in a spatially well-defined fashion. For instance, antiplatelet agent Ticarelor 1, shown in Figure 1, has the trans-disubstituted cyclopropane bridging pharmacologically active difluorophenyl and heterocyclic fragments.

Recently discovered highly selective histamine H3 receptor agonist 2 (Fig. 1) contains a cis-disubstituted cyclopropane ring that connects privileged imidazole moiety and 2-aminoethyl group.4 Compounds 35 and 46 are examples of potent and specific enzyme inhibitors in which the functional substructures are connected through tri- and tetrasubstituted cyclopropane rings, respectively.

 Some biologically active molecules containing the cyclopropane moiety.

Figure 1. Some biologically active molecules containing the cyclopropane moiety.

A representative set of cyclopropane derivatives available from Life Chemicals is provided below. To explore the full data set, please, send your request to


  1. (a) Lamberth, C. Tetrahedron 2019, 75, 4365-4383. (b) Salaün, J. Top. Curr. Chem. 2000, 207, 1-67.
  2. Marson, C. M. Chem. Soc. Rev. 2011, 40, 5514.
  3. Reichelt, A.; Martin, S. F. Acc. Chem. Res. 2006, 39, 433.
  4. Kazuta, Y. et al. J. Med. Chem. 2003, 46, 1980.
  5. Guay, D. et al. Bioorg. Med. Chem. Lett. 2009, 19, 5392.
  6. Shiozaki, M. et al. Bioorg. Med. Chem. Lett. 2009, 19, 6213.
15 February 2021, 14:45 Oleg Lukin Building Blocks

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