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. 2013 Dec;56(14):736-40.
doi: 10.1002/jlcr.3098. Epub 2013 Jul 24.

A concise radiosynthesis of the tau radiopharmaceutical, [(18) F]T807

Timothy M Shoup  1 , Daniel L Yokell, Peter A Rice, Raul N Jackson, Eli Livni, Keith A Johnson, Thomas J Brady, Neil Vasdev
Affiliations

A concise radiosynthesis of the tau radiopharmaceutical, [(18) F]T807

Timothy M Shoup et al. J Labelled Comp Radiopharm. 2013 Dec.

Abstract

Fluorine-18 labeled 7-(6-fluoropyridin-3-yl)-5H-pyrido[4,3-b]indole ([(18) F]T807) is a potent and selective agent for imaging paired helical filaments of tau and is among the most promising PET radiopharmaceuticals for this target in early clinical trials. The present study reports a simplified one-step method for the synthesis of [(18) F]T807 that is broadly applicable for routine clinical production using a GE TRACERlab™ FXFN radiosynthesis module. Key facets of our optimized radiosynthesis include development and use of a more soluble protected precursor, tert-butyl 7-(6-nitropyridin-3-yl)-5H-pyrido[4,3-b]indole-5-carboxylate, as well as new HPLC separation conditions that enable a facile one-step synthesis. During the nucleophilic fluorinating reaction with potassium cryptand [(18) F]fluoride (K[(18) F]/K222 ) in DMSO at 130 °C over 10 min the precursor is concurrently deprotected. Formulated [(18) F]T807 was prepared in an uncorrected radiochemical yield of 14 ± 3%, with a specific activity of 216 ± 60 GBq/µmol (5837 ± 1621 mCi/µmol) at the end of synthesis (60 min; n = 3) and validated for human use. This methodology offers the advantage of faster synthesis in fewer steps, with simpler automation that we anticipate will facilitate widespread clinical use of [(18) F]T807.

Keywords: PET; T807; fluorine-18; tau.

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