Direct incorporation of [18F] into Aliphatic Systems: A promising Mn-catalysed Labelling Technique for PET Imaging

Curr Radiopharm. 2021;14(2):101-106. doi: 10.2174/1874471013666200907115026.

Abstract

Background: One of the challenges in positron emission tomography (PET) is labelling complex aliphatic molecules.

Objective: This study aimed to develop a method of metal-catalysed radiofluorination that is site-selective and works in moderate to good yields under facile conditions.

Methods: Herein, we report on the optimisation of an aliphatic C-H to C-18F bond transformation catalysed by a Mn(porphyrin) complex.

Results: The successful oxidation of 11 aliphatic molecules, including progesterone, is reported. Radiochemical Incorporations (RCIs) up to 69% were achieved within 60 min without the need for pre-activation or special equipment.

Conclusion: The method features mild conditions (60 °C) and promises to constitute a valuable approach to labelling of biomolecules and drug substances.

Keywords: PET; [18F]-Fluoride; aliphatic labelling; imaging; mn-Catalysed; nucleophilic fluorination; porphyrin; tracer synthesis.

Publication types

  • Review

MeSH terms

  • Fluorine Radioisotopes / chemistry*
  • Humans
  • Manganese / chemistry*
  • Positron-Emission Tomography*
  • Radiochemistry
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Structure-Activity Relationship

Substances

  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Manganese