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\begin{document}

\title{Comparison of~ two different precursors for efficient aromatic
\textsuperscript{18}F-fluorination of~ {[}\textsuperscript{18}F{]}BS224:
A novel TSPO-binding radiotracer~~~~~~~}



\author[1]{SRSTT Radiopharmaconnect}%
\affil[1]{Radiopharmaconnect}%


\vspace{-1em}



  
  \date{March 14, 2025}


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\href{https://www.srsweb.org/cafachem2020}{\textbf{CAFACHEM~2020}}
\textbf{} organizers are grateful for the support of
\textbf{\href{www.gehealthcare.co.uk/products/molecular-imaging/pet-radiopharmacy/chemistry--systems}{}\href{https://www.gehealthcare.co.uk/products/molecular-imaging/pet-radiopharmacy/chemistry--systems}{GE
Healthcare}}\selectlanguage{english}
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\par\null

\textbf{Authors: Sang Hee Lee\textsuperscript{1,2,3}}, Hyunho
An\textsuperscript{2}, Ji Hyeon Kim\textsuperscript{2}, Byung Chul
Lee\textsuperscript{2,3}, Sang Eun Kim\textsuperscript{1,2,3} \textbf{}

\textsuperscript{1}Department of Molecular and Biopharmaceutical
Sciences, Graduate School of Convergence Science and Technology, Seoul
National University, Suwon, South Korea

\textsuperscript{2}Department of Nuclear Medicine, Seoul National
University Bundang Hospital, Seongnam, South Korea

\textsuperscript{3}Center for Nanomolecular Imaging and Innovative Drug
Development, Advanced Institutes of Convergence Technology, Suwon, South
Korea

\textbf{Background}

TSPO PET imaging can provide the pathological information related to
neuroinflammatory brain disorders\textsuperscript{1}. Recently, we
developed a novel TSPO-binding radiotracer,
{[}\textsuperscript{18}F{]}BS224 which shows high TSPO-binding affinity,
a clearly visibility of the inflammatory lesion and less sensitivity to
TSPO polymorphism rs6971 in preclinical studies\textsuperscript{2}. ~

\par\null

\textbf{Aims}

High radiochemical yields and a reproducible synthesis of
{[}\textsuperscript{18}F{]}BS224 is urgently needed for clinical
studies. Therefore, we have synthesized two different precursors
(diaryliodonium tosylate and pinacol boronic ester forms) and attempted
to optimize the reaction conditions based on the reactivity in the
fluorine-18 incorporation environment using the automated module.

\textbf{Methods}

Radiosynthesis of {[}\textsuperscript{18}F{]}BS224 was performed by
using two different precursors (Figure). Fluorine-18 incorporation
condition from diaryliodonium tosylate or pinacol boronate ester
precursor were optimized in the presence of different PTC complexs,
solvents, temperatures and catalysts, respectively. \textbf{} The
obtained radiochemical yields of {[}\textsuperscript{18}F{]}BS224 were
measured by radio-TLC and ~semi-preparative HPLC.

\textbf{Results and Conclusion}

{[}\textsuperscript{18}F{]}BS224 was prepared in RCY 25\% and 63\% from
diaryliodonium tosylate and pinacol boronic ester precursor,
respectively, based on radio-TLC analysis. The condition (B) of
{[}\textsuperscript{18}F{]}BS224 resulted in RCY 39 \% (n=10) with high
A\textsubscript{M} (127 GBq/\selectlanguage{greek}µ\selectlanguage{english}mol) and RCY (\textgreater{}99 \%). The
reliable fully automated method for {[}\textsuperscript{18}F{]}BS224 is
ongoing.

\textbf{References}

\textbf{1.} Banati RB et al. PK (`peripheral benzodiazepine') -- binding
sites in the CNS indicate early and discrete brain lesions:
microautoradiographic detection of {[}\textsuperscript{3}H{]}PK 11195
binding to activated microglia. \emph{J Neurophysiol}. 1997;26:77-82

\textbf{2.} Owen DR et al. An 18-kDa Translocator Protein (TSPO)
Polymorphism Explains Differences in Binding Affinity of the PET
Radioligand PBR28. \emph{J Cerebr Blood F Met.} 2012;32:1-5\selectlanguage{english}
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