Radiochemical synthesis of 2'-[18F]-labelled and 3'-[18F]-labelled nucleosides for positron emission tomography imaging

J Labelled Comp Radiopharm. 2014 May 15;57(5):333-7. doi: 10.1002/jlcr.3197. Epub 2014 Apr 1.

Abstract

This review article considers 2'-labelled and 3'-labelled nucleosides, which are of great importance as positron emission tomography (PET) probes in clinical diagnostics and PET research. Although the radiochemical preparation of several [(18)F]-labelled nucleosides such as [(18)F]fluorothymidine or [(18)F](fluoroarabinofuranosyl)cytosine has been accomplished within the last two decades, a number of potentially interesting nucleoside-based biomarkers are not yet available for automated good manufacturing practice production due to the lack of fast and efficient synthetic methods for late-stage [(18)F]-introduction. In order to meet recent demands for new PET-based biomarkers in various clinical applications, appropriate precursors that can easily be fluorinated and deprotected need to be developed.

Keywords: [18F]-incorporation; late stage precursor; nucleoside analogues; radiosynthesis.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Contrast Media / chemical synthesis*
  • Fluorine Radioisotopes / chemistry*
  • Humans
  • Image Enhancement / methods
  • Isotope Labeling / methods
  • Molecular Imaging / methods
  • Nucleosides / chemistry*
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals / chemical synthesis

Substances

  • Contrast Media
  • Fluorine Radioisotopes
  • Nucleosides
  • Radiopharmaceuticals