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Radiosynthesis of [18F]PBR111, a selective radioligand for imaging the translocator protein (18 kDa) with PET

✍ Scribed by Frédéric Dollé; Françoise Hinnen; Annelaure Damont; Bertrand Kuhnast; Christopher Fookes; Tien Pham; Bertrand Tavitian; Andrew Katsifis

Publisher
John Wiley and Sons
Year
2008
Tongue
French
Weight
137 KB
Volume
51
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

PBR111 (2‐(6‐chloro‐2‐(4‐(3‐fluoropropoxy)phenyl)imidazo[1,2‐a]pyridin‐3‐yl)‐N,N‐diethylacetamide) is a novel, reported, high‐affinity and selective ligand for the translocator protein (18 kDa). PBR111 has been labelled with fluorine‐18 (half‐life: 109.8 min) using our Zymate‐XP robotic system. The process involves (A) a simple one‐step tosyloxy‐for‐fluorine nucleophilic aliphatic substitution (performed at 165°C for 5 min in DMSO using K[^18^F]F‐Kryptofix^®^222 and 6.8–7.6 µmol of the corresponding tosylate as precursor for labelling) followed by (B) C‐18 PrepSep cartridge pre‐purification and (C) semi‐preparative HPLC purification on a Waters Symmetry^®^ C‐18. Up to 4.8 GBq (130 mCi) of [^18^F]PBR111 could be obtained with specific radioactivities ranging from 74 to 148 GBq/µmol (2–4 Ci/µmol) in 75–80 min (HPLC purification and SepPak^®^‐based formulation included), starting from a 37.0 GBq (1.0 Ci) [^18^F]fluoride batch. Overall non‐decay‐corrected isolated yields were 8–13% (13–21% decay‐corrected). Copyright © 2008 John Wiley & Sons, Ltd.

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