3137 104 Automated radiosynthesis of no - carrier - added 4 - [ 18 F ] fl uoroiodobenzene : a versatile building block in 18 F radiochemistry
نویسنده
چکیده
4-[F]Fluoroiodobenzene ([F]FIB) is a versatile building block in F radiochemistry used in various transition metalmediated C–C and C–N cross-coupling reactions and [F]fluoroarylation reactions. Various synthesis routes have been described for the preparation of [F]FIB. However, to date, no automated synthesis of [F]FIB has been reported to allow access to larger amounts of [F]FIB in high radiochemical and chemical purity. Herein, we describe an automated synthesis of no-carrier-added [F]FIB on a GE TRACERlabTM FX automated synthesis unit starting from commercially available (4-iodophenyl)diphenylsulfonium triflate as the labelling precursor. [F]FIB was prepared in high radiochemical yields of 89 ±10% (decay-corrected, n=7) within 60min, including HPLC purification. The radiochemical purity exceeded 95%, and specific activity was greater than 40GBq/μmol. Typically, from an experiment, 6.4 GBq of [F]FIB could be obtained starting from 10.4GBq of [F]fluoride. Copyright © 2013 John Wiley & Sons, Ltd.
منابع مشابه
Synthesis of no-carrier-added 4-[18F]fluorophenol from 4-benzyloxyphenyl-(2-thienyl)iodonium bromide.
4-[(18)F]Fluorophenol is a versatile synthon for the synthesis of more complex radiopharmaceuticals bearing a 4-[(18)F]fluorophenoxy moiety. In order to prepare 4-[(18)F]fluorophenol in no-carrier-added (n.c.a.) form only a nucleophilic labelling method starting from [(18)F]fluoride is suitable. In this paper a new, two step radiosynthesis starting from 4-benzyloxyphenyl-(2-thienyl)iodonium bro...
متن کاملFluorine-18 Radiochemistry, Labeling Strategies and Synthetic Routes
Fluorine-18 is the most frequently used radioisotope in positron emission tomography (PET) radiopharmaceuticals in both clinical and preclinical research. Its physical and nuclear characteristics (97% β(+) decay, 109.7 min half-life, 635 keV positron energy), along with high specific activity and ease of large scale production, make it an attractive nuclide for radiochemical labeling and molecu...
متن کامل18 F-click labeling and preclinical evaluation of a new 18 F-folate for PET imaging
BACKGROUND The folate receptor (FR) is a well-established target for tumor imaging and therapy. To date, only a few 18 F-folate conjugates via 18 F-prosthetic group labeling for positron emission tomography (PET) imaging have been developed. To some extent, they all lack the optimal balance between efficient radiochemistry and favorable in vivo characteristics. METHODS A new clickable olate p...
متن کاملSynthesis of a Potent Aminopyridine-Based nNOS-Inhibitor by Two Recent No-Carrier-Added (18)F-Labelling Methods.
Nitric oxide (NO), an important multifunctional signaling molecule, is produced by three isoforms of NO-synthase (NOS) and has been associated with neurodegenerative disorders. Selective inhibitors of the subtypes iNOS (inducible) or nNOS (neuronal) are of great interest for decoding neurodestructive key factors, and (18)F-labelled analogues would allow investigating the NOS-function by molecul...
متن کاملHighlighting the Versatility of the Tracerlab Synthesis Modules. Part 1: Fully Automated Production of [F]Labelled Radiopharmaceuticals using a Tracerlab FX(FN).
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 ...
متن کامل