Isotope chemistry; a useful tool in the drug discovery arsenal

Bioorg Med Chem Lett. 2015 Jan 15;25(2):167-71. doi: 10.1016/j.bmcl.2014.11.051. Epub 2014 Nov 26.


As Medicinal Chemists are responsible for the synthesis and optimization of compounds, they often provide intermediates for use by isotope chemistry. Nevertheless, there is generally an incomplete understanding of the critical factors involved in the labeling of compounds. The remit of an Isotope Chemistry group varies from company to company, but often includes the synthesis of compounds labeled with radioisotopes, especially H-3 and C-14 and occasionally I-125, and stable isotopes, especially H-2, C-13, and N-15. Often the remit will also include the synthesis of drug metabolites. The methods used to prepare radiolabeled compounds by Isotope Chemists have been reviewed relatively recently. However, the organization and utilization of Isotope Chemistry has not been discussed recently and will be reviewed herein.

Keywords: C-14; Isotope chemistry; Isotopic labeling; Tritium.

Publication types

  • Review

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical / methods*
  • Drug Discovery / methods*
  • Humans
  • Isotope Labeling / methods*
  • Isotopes / analysis
  • Isotopes / chemistry*


  • Isotopes