Cryptate mediated nucleophilic 18F-fluorination without azeotropic drying

Nuklearmedizin. 2012;51(1):1-8. doi: 10.3413/Nukmed-0425-11-08. Epub 2011 Oct 11.

Abstract

The radiosynthesis of the vast majority of 18F-labeled tracers rely on azeotropic drying of [18F]fluoride and subsequent cryptate mediated introduction of [18F]fluoride by nucleophilic substitution. THE AIM of this study was to develop a method for simplification of this process, based on preparation of reactive [K(+) is a subset of 2.2.2]18F(-) by solvent drying of [18F]fluoride adsorbed onto an anion exchange resin.

Methods: Aqueous [18F]fluoride (0.5-1 ml) obtained from the 18O(p,n)18F nuclear reaction was trapped on a strong anion-exchange (SAX) cartridge. After washing the cartridge with dry CH3CN, [18F]fluoride was eluted with an anhydrous solution of [K(+) is a subset of 2.2.2]OH(-) in CH3CN and directly used for nucleophilic fluorination reactions.

Results: [18F]Fluoride from target water was quantitatively retained by the SAX cartridge, and water-free [18F]fluoride recovered in an overall yield of 92±5% (n = 10). [18F]Fluoride obtained by this procedure led to radiochemical yields of 70-90% for [18F]FDG, [18F]FET, [18F]FLT, [18F]FAZA and [18F]Fallypride.

Conclusion: SAX-resin adsorbed [18F]fluoride can be dried with non-aqueous solvents and eluted with [K(+) is a subset of 2.2.2]OH(-) in CH3CN. The reactivity of [K(+) is a subset of 2.2.2]F(-) generated by the new method is comparable to that of [18F]fluoride obtained by azeotropic drying. The described procedure facilitates the automated production of 18F-radiopharmaceuticals in general, and may also simplify the use of microfluidic devices for 18F-radiotracer production.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Crown Ethers / chemistry*
  • Desiccation / methods
  • Fluorine Radioisotopes / chemistry*
  • Fluorine Radioisotopes / isolation & purification*
  • Isotope Labeling / methods
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / isolation & purification*

Substances

  • Crown Ethers
  • Fluorine Radioisotopes
  • Radiopharmaceuticals