Optimization of reaction conditions for synthesis of [18F]FMISO using stable [19F]F-

Cocevska, Maja (2023) Optimization of reaction conditions for synthesis of [18F]FMISO using stable [19F]F-. Journal of Research in Pharmacy. ISSN 2630-6344

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Abstract

The increasing number of fluorinated pharmaceuticals in pharmaceutical chemistry and fluorine
radiopharmaceuticals in radiochemistry highlights the importance of optimizing their synthesis processes.
[18F]Fluoromisonidazole ([18F]FMISO) radiopharmaceutical synthesized using aqueous [18F]F- and 1-(2'-nitro-1'-
imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulfonylpropanediol precursor (NITTP), is one such example. This
radiolabeled compound is used for imaging tumor hypoxia by positron emission tomography (PET). When working
with ionizing radiation, ensuring the operator's safety is crucial. As a result, the synthesis process for [18F]FMISO takes
place within automated modules in closed lead-shielded hot cells. This protective measure prohibits the collection of
control samples during the synthesis process. Our experiments involved utilizing the stable isotope [19F]F- instead of
[18F]F- to examine various aspects. These included analyzing the intermediate compound produced after the
fluorination reaction, assessing unhydrolyzed/hydrolyzed intermediates, and detecting unexpected or unknown
chemical impurities in both the unpurified and final purified products. HPLC analysis was employed to analyze the
collected samples. The results obtained from these experiments proved invaluable in addressing the challenge of
unwanted chemical impurities during the radiosynthesis of [18F]FMISO. They provided valuable insights that aided in
the further development of the synthesis process. Overall, this study demonstrates the significance of utilizing non�radioactive chemistry to optimize radiosynthesis, allowing for the safe and efficient production of [18F]FMISO without
the need for radiation exposure.
KEYWORDS: [18F]Fluoromisonidazole; [19F]F-; synthesis; fluorinated intermediate; impurity

Item Type:	Article
Subjects:	Medical and Health Sciences > Other medical sciences
Divisions:	Faculty of Medical Science
Depositing User:	Maja Cocevska
Date Deposited:	28 Nov 2023 08:37
Last Modified:	28 Nov 2023 08:37
URI:	https://eprints.ugd.edu.mk/id/eprint/32623

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