Fully automated radiosynthesis of [1-(2-[18F]fluoroethyl),1H[1, 2,3]triazole 4-ethylene] triphenylphosphonium bromide as a potential positron emission tomography tracer for imaging apoptosis

Anna Haslop, Antony Gee, Christophe Plisson, Nicholas Long*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

23 Citations (Scopus)

Abstract

A novel phosphonium salt bearing a fluorine-18 labelled triazole has been designed as a potential imaging agent for apoptosis. The radiosynthesis of [1-(2-[18F]fluoroethyl),1H[1,2,3]triazole 4-ethylene] triphenylphosphonium bromide ([18F]MitoPhos-01) has been carried out on a fully automated system in a two-step reaction. Radiolabelling an ethyl azide and then carrying out a copper-mediated 1,3-cycloaddition reaction has allowed for total synthesis time to be slightly more than 1 h from aqueous [18F]fluoride. After purification by HPLC, the average radiochemical yield was determined to be 9% (not decay corrected); the specific activity was on average 70 GBq/μmol at the end of synthesis, and the radiochemical purity was >99%. A novel phosphonium salt bearing a fluorine-18 labelled triazole has been designed as a potential imaging agent for apoptosis. The radiosynthesis of [1-(2-[18F]fluoroethyl),1H[1,2,3]triazole 4-ethylene] triphenylphosphonium bromide ([18F]MitoPhos-01) has been carried out on a fully automated system in a two-step reaction, with the average radiochemical yield determined to be 9% (not decay corrected); the specific activity being around 70 GBq/μmol at the end of synthesis and the radiochemical purity above 99%.

Original languageEnglish
Pages (from-to)313-316
Number of pages4
JournalJOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
Volume56
Issue number6
DOIs
Publication statusPublished - 30 May 2013

Keywords

  • apoptosis imaging
  • automated synthesis
  • fluoride
  • phosphonium salts

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