Highlighting the versatility of the tracerlab synthesis modules. Part 1: fully automated production of [¹⁸F]labelled radiopharmaceuticals using a Tracerlab FX_FN

Abstract

The field of radiochemistry is moving towards exclusive use of automated synthesis modules for production of clinical radiopharmaceutical doses. Such a move comes with many advantages, but also presents radiochemists with the challenge of re-configuring synthesis modules for production of radiopharmaceuticals that require non-conventional radiochemistry whilst maintaining full automation. This review showcases the versatility of the Tracerlab FXFN synthesis module by presenting simple, fully automated methods for producing [18F]FLT, [18F]FAZA, [18F]MPPF, [18F]FEOBV, [18F]sodium fluoride, [18F]fluorocholine and [18F]SFB.

In Vivo Imaging of Human Cholinergic Nerve Terminals with (–)-5-18F-Fluoroethoxybenzovesamicol: Biodistribution, Dosimetry, and Tracer Kinetic Analyses

“…Structural brain MR imaging was performed before PET. 18 F-FEOBV was prepared as described previously (8). The average yield of 18 F-FEOBV was 5,400 MBq (146 mCi) (;9% non-decaycorrected yield), and average specific activity was 166 TBq/mmol (4,500 Ci/mmol).…”

Automated electrophilic radiosynthesis of [18F]FBPA using a modified nucleophilic GE TRACERlab FXFDG

“…We produced [ 18 F]F 2 gas by using the 18 (Nickles et al, 1984;Solin and Bergman, 1986). For the automated synthesis of [ 18 F]FBPA we used a custommodified commercially available automated synthesis module for nucleophilic [ 18 F]fluorinations (TRACERlab™ FX FDG , GE Healthcare), which is similar to the TRACERlab™ FX N synthesis module, which has been shown to be a versatile synthesis platform for the production of a range of different 18 F-labelled radiopharmaceuticals (Shao et al, 2011). The nucleophilic synthesis module contains two reactors (reactor 1 and 2, Fig.…”

Radiosyntheses using Fluorine-18: The Art and Science of Late Stage Fluorination

“…18 ). Examples include [ 18 F]fluoroethoxybenzovesamicol ([ 18 F]FEOBV), a radioligand for the vesicular acetylcholine transporter (Scheme 12a) [102], and [ 18 F]fallypride for imaging the D2/D3 receptors [103]. However, many precursors do contain functional groups that require protection, typically using standard protecting groups from the organic chemistry literature (Boc, Fmoc etc.).…”

“…This reaction however suffers from low radiochemical yields, and so alternative precursors (e.g. Boc-Boc-Nosyl 21 ) have been designed, which contain a secondary nosylate leaving group, rather than the cyclic precursor, and provide higher yields of [ 18 F]FLT (Scheme 13b) [102]. A range of other radiopharmaceuticals for oncological imaging have been developed including [ 18 F]fluoroethyl tyrosine ([ 18 F]FET), and 2-nitroimidazoles such as [ 18 F]fluoroazomycin arabinoside ([ 18 F]FAZA), [ 18 F]fluoromisonidazole ([ 18 F]FMISO) and [ 18 F]flortanidazole ([ 18 F]HX4) for imaging of tumor hypoxia that are all prepared using similar chemistry.…”