A facile and rapid automated synthesis of 3'-deoxy-3'-[(18)F]fluorothymidine

Appl Radiat Isot. 2010 Sep;68(9):1734-9. doi: 10.1016/j.apradiso.2010.04.010. Epub 2010 Apr 28.

Abstract

Aim: To develop a simplified and fully automated synthesis procedure of 3'-deoxy-3'-[(18)F]fluorothymidine ([(18)F]FLT) using PET-MF-2V-IT-I synthesis module.

Methods: Synthesis of [(18)F]FLT was performed using PET-MF-2V-IT-I synthesis module by one-pot two-step reaction procedure, including nucleophilic fluorination of 3-N-t-butoxycarbonyl-1-[5'-O-(4,4'-dimethoxy triphenylmethyl)-2'-deoxy-3'-O-(4-nitrobenzenesulfonyl)-beta-d-threopentofuranosyl]thymine (15mg) as the precursor molecule with [(18)F]fluoride, and subsequent hydrolysis of the protecting group with 1.0M HCl at the same reaction vessel and purification with SEP PAK cartridges instead of the HPLC system.

Results: The automated synthesis of [(18)F]FLT with SEP PAK purification gave corrected radiochemical yield of 23.2+/-2.6% (n=6, uncorrected yield: 16-22%) and radiochemical purity of >97% within the total synthesis time of 35min.

Conclusion: The fully one-pot automated synthesis procedure with SEP PAK purification can be applied to the fully automated synthesis of [(18)F]FLT using commercial [(18)F]FDG synthesis module.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Dideoxynucleosides / chemistry*
  • Dideoxynucleosides / isolation & purification*
  • Isotope Labeling / methods
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / isolation & purification*
  • Robotics / methods*

Substances

  • Dideoxynucleosides
  • Radiopharmaceuticals
  • alovudine