A facile synthesis of precursor for the σ-1 receptor PET radioligand [18F]FTC-146 and its radiofluorination

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22330%2F24%3A43927969" target="_blank" >RIV/60461373:22330/24:43927969 - isvavai.cz</a>
Alternative codes found
RIV/60461373:22340/24:43927969
Result on the web
<a href="https://analyticalsciencejournals.onlinelibrary.wiley.com/doi/full/10.1002/jlcr.4081" target="_blank" >https://analyticalsciencejournals.onlinelibrary.wiley.com/doi/full/10.1002/jlcr.4081</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/jlcr.4081" target="_blank" >10.1002/jlcr.4081</a>

Result language
angličtina
Original language name
A facile synthesis of precursor for the σ-1 receptor PET radioligand [18F]FTC-146 and its radiofluorination
Original language description
The sigma-1 receptor is a non-opioid transmembrane protein involved in various human pathologies including neurodegenerative diseases, inflammation, and cancer. The previously published ligand [F-18]FTC-146 is among the most promising tools for sigma-1 molecular imaging by positron emission tomography (PET), with a potential for application in clinical diagnostics and research. However, the published six- or four-step synthesis of the tosyl ester precursor for its radiosynthesis is complicated and time-consuming. Herein, we present a simple one-step precursor synthesis followed by a one-step fluorine-18 labeling procedure that streamlines the preparation of [F-18]FTC-146. Instead of a tosyl-based precursor, we developed a one-step synthesis of the precursor analog AM-16 containing a chloride leaving group for the S(N)2 reaction with F-18-fluoride. F-18-fluorination of AM-16 led to a moderate decay-corrected radiochemical yield (RCY = 7.5%) with molar activity (A(m)) of 45.9 GBq/mu mol. Further optimization of this procedure should enable routine radiopharmaceutical production of this promising PET tracer.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10401 - Organic chemistry

Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2024
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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