Radiosynthesis of [18F]-fluorobenzoate-doxorubicin using acylation approach

Pardeep Kumar, Ankit Watts, Pratap Acharya, Ranju Bansal, Anchal Ghai, Amritjyot Kaur, Baljinder Singh

Research output: Contribution to journalArticlepeer-review

1 Scopus citations


Background: Previously, we have labeled doxorubicin with [99mTc] and evaluated its potential as a SPECT agent to detect cancer in tumor bearing mice. In this study, we sought to radiolabel doxorubicin with [18F] using acylation method. Methods: A quaternary salt of the precursor pentamethylbenzyl-4-(trimethylammonium trifluoromethanesulfonate) benzoate was synthesized and characterized by 1H-NMR. As a first step, 4-[18F]- fluorobenzoic acid (FBA) was synthesized from precursor. In second step, [18F]-FBA was further converted to its corresponding acyl form to radiolabel doxorubicin via acylation reaction. Results: The total reaction time for the synthesis of [18F]-fluorobenzoate-doxorubicin was about 60 minutes. The radiolabeling efficiency of the final product was estimated to be about 59.0% The radiochemical yield for the synthesis of [18F]-FBA and [18F]-fluorobenzoate-doxorubicin were 19.0-29.0% and 12.0-14.0% respectively. Conclusion: Radio synthesis of [18F]-fluorobenzoate-doxorubicin by acylation is a convenient method. However, further improvement in the labeling strategy is required to increase the radiolabeling efficiency and radio synthesis yield. Also, the radiolabeled product needs a detailed pre-clinical evaluation.

Original languageEnglish (US)
Pages (from-to)215-221
Number of pages7
JournalCurrent Radiopharmaceuticals
Issue number3
StatePublished - Dec 1 2016
Externally publishedYes


  • Acylation
  • Doxorubicin
  • Fluorine-18
  • PET
  • Radiolabeling
  • Radiosynthesis

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging
  • Pharmacology


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