A report of the automated radiosynthesis of the tau positron emission tomography radiopharmaceutical, [18F]-THK-5351

Ramesh Neelamegam, Daniel L. Yokell, Peter A. Rice, Shozo Furumoto, Yukitsuka Kudo, Nobuyuki Okamura, Georges El Fakhri

Research output: Contribution to journalArticle

2 Scopus citations

Abstract

The radiotracer, [18F]-THK-5351, is a highly selective and high-binding affinity PET imaging agent for aggregates of hyper-phosphorylated tau protein. Our report is a simplified 1-pot, 2-step radiosynthesis of [18F]-THK-5351. This report is broadly applicable for routine clinical production and multi-center trials on account of favorable half-life of flourine-18 and the use of a commercially available radiosynthesis module, the GE TRACERlab™ FXFN. First, the O-THP protected tosyl precursor underwent nucleophilic fluorinating reaction with potassium cryptand fluoride ([18F] fluoride (K[18F]/K222)) in Dimethyl sulfoxide at 110°C for 10 minutes followed by O-THP removal by using diluted hydrochloric acid (HCl) at same temperature. [18F]-THK-5351 was purified via semi-preparative high-performance liquid chromatography and formulated by using 10% EtOH, United States Pharmacopeia (USP) in 0.9% sodium chloride for injection, USP and an uncorrected radiochemical yield of 21 ± 3.5%, with a specific activity of 153.11 ± 25.9 GBq/μmol (4138 ± 700 mCi/μmol) at the end of synthesis (63 minutes; n = 3).

Original languageEnglish (US)
Pages (from-to)140-146
Number of pages7
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume60
Issue number2
DOIs
StatePublished - Feb 1 2017

Keywords

  • PET
  • THK-5351
  • Tau
  • fluorine-18

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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