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Molecular Imaging and Biology

, Volume 16, Issue 1, pp 28–35 | Cite as

Fully Automated Radiosynthesis of 2-[18F]Fludarabine for PET Imaging of Low-Grade Lymphoma

  • Stéphane Guillouet
  • Delphine Patin
  • Olivier Tirel
  • Jérôme Delamare
  • Fabienne Gourand
  • Jean Bernard Deloye
  • Michel Leporrier
  • Louisa BarréEmail author
Research Article

Abstract

Purpose

An efficient and fully automated radiosynthesis of 2-[18F]fluoro-9-β-d-arabinofuranosyl-adenine (2-[18F]fludarabine, [18F]-5) based on a GE TRACERlab™ FX-FN module has been developed.

Procedures

A 2-nitro purine derivative 3 was developed as precursor for labeling with fluorine-18. The radiosynthesis of [18F]-5 was performed in two steps in a single reactor with an intermediary purification on Sep-Pak® silica which involved the addition of a three-way valve on the original module. After hydrolysis, [18F]-5 was purified by semi-preparative high-pressure liquid chromatography (HPLC) and a quality control was established.

Results

The labeling precursor 3 was obtained in 45 % overall yield. Nucleophilic substitution with K18F/K2.2.2 afforded protected 2-[18F]fludarabine ([18F]-4) in 73 ± 4 % , radiochemical yield (decay corrected to the end of bombardment (EOB)) and based on the initial [18F]F activity. An aqueous ammonia/methanol solution was used for the deprotection reaction and gave the desired [18F]-5 in 67 ± 3 % yield after 20 min at 70 °C based on HPLC profile.

Conclusions

The process afforded pure 2-[18F]fludarabine in 48 ± 3 % yield (decay corrected to the EOB) in 85 min, with a specific activity of 310 ± 72 GBq/μmol at the end of synthesis (EOS) and a radiochemical purity up to 99 %.

Key words

F-18 labeling 2-[18F]Fludarabine Automated radiosynthesis PET Nucleoside Lymphoma 

Notes

Acknowledgments

This work has been in part supported by a grant from the French National Agency for Research called “Investissements d’Avenir” no. ANR-11-LABEX-0018-01, the Commissariat à l’énergie atomique et aux énergies alternatives (CEA) and the Région Basse Normandie. The authors wish to thank Dr. Eric T. MacKenzie for his helpful comments and discussion.

Conflict of Interest

The authors declare that they have no conflict of interest.

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Copyright information

© World Molecular Imaging Society 2013

Authors and Affiliations

  • Stéphane Guillouet
    • 1
    • 2
    • 3
  • Delphine Patin
    • 1
    • 2
    • 3
    • 4
  • Olivier Tirel
    • 1
    • 2
    • 3
  • Jérôme Delamare
    • 1
    • 2
    • 3
  • Fabienne Gourand
    • 1
    • 2
    • 3
  • Jean Bernard Deloye
    • 4
  • Michel Leporrier
    • 1
    • 2
    • 3
  • Louisa Barré
    • 1
    • 2
    • 3
    Email author
  1. 1.CEA, I2BM, LDM-TEP, UMR 6301 ISTCTCaenFrance
  2. 2.CNRS, UMR 6301 ISTCT, LDM-TEPCaen CedexFrance
  3. 3.Université de Caen Basse-Normandie, UMR 6301 ISTCT, LDM-TEPCaenFrance
  4. 4.Laboratoires CYCLOPHARMASaint BeauzireFrance

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