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

作者：Neelamegam Ramesh; Yokell Daniel L^*; Rice Peter A; Furumoto Shozo; Kudo Yukitsuka; Okamura Nobuyuki; El Fakhri Georges

来源：Journal of Labelled Compounds and Radiopharmaceuticals, 2017, 60(2): 140-146.

DOI：10.1002/jlcr.3482

• fluorine-18
• PET
• Tau
• THK-5351

The radiotracer, [F-18]-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 [F-18]-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 T FXFN. First, the O-THP protected tosyl precursor underwent nucleophilic fluorinating reaction with potassium cryptand fluoride ([F-18] fluoride (K[F-18]/K222)) in Dimethyl sulfoxide at 110 degrees C for 10 minutes followed by O-THP removal by using diluted hydrochloric acid (HCl) at same temperature. [F-18]-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/mu mol (4138 +/- 700 mCi/mu mol) at the end of synthesis (63 minutes; n = 3).

• 出版日期2017-2