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\begin{document}

\title{Ruthenium-mediated \textsuperscript{18}F-fluorination~ of a new CB1R
tracer {[}\textsuperscript{18}F{]}FPATPP}



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


\vspace{-1em}



  
  \date{May 26, 2024}


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\selectlanguage{english}
\begin{figure}[H]
\begin{center}
\includegraphics[width=0.70\columnwidth]{figures/CAFACHEM1/CAFACHEM1}

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\end{figure}

\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}
\begin{figure}[H]
\begin{center}
\includegraphics[width=0.70\columnwidth]{figures/GE-Healthcare-PET-Chemistry-Systems-Banner---CAFACHEM/GE-Healthcare-PET-Chemistry-Systems-Banner---CAFACHEM}

\end{center}
\end{figure}

\par\null

\textbf{Authors: Noora Rajala}, Salla Lahdenpohja, Olof Solin and Anna
K. Kirjavainen \textbf{}

Radiopharmaceutical Chemistry Laboratory, Turku PET Centre, University
of Turku, Turku, Finland

\par\null

\textbf{Background}

Transition metal mediated \textsuperscript{18}F-fluorination have been
widely studied and the most recently published approach is
ruthenium-mediated \textsuperscript{18}F-deoxyfluorination.{[}1{]}

\par\null

\textbf{Aims}

We applied Ru- mediated \textsuperscript{18}F-deoxyfluorination to
produce a new cannabinoid subtype 1 specific radiotracer
{[}\textsuperscript{18}F{]}FPATPP
((3\emph{R},5\emph{R})-5-(3-{[}\textsuperscript{18}F{]}fluorophenyl)-3-(((\emph{R})-1-phenylethyl)amino)-1-(4-(trifluoromethyl)phenyl)pyrrolidin-2-one).
Our aim was to optimise the synthesis conditions and we utilised solid
phase extraction (SPE) or azeotropic distillation for
{[}\textsuperscript{18}F{]}fluoride activation.

\par\null

\textbf{Methods}

Previously described Ru-mediated labelling method (Fig. 1) was
followed{[}1{]}. In the SPE method, Ru-phenol complex was used to elute
{[}\textsuperscript{18}F{]}fluoride from an anion exchange cartridge.
The subsequent reaction was conducted at 100\selectlanguage{ngerman}°C to 160°C for 10 to 30
min. In the azeotropic distillation method, subsequent reaction was
conducted at 160°C.

\par\null

\textbf{Results and Conclusion}

The optimised conditions for the radiofluorination were 30 min in 160 °C
by using SPE method for {[}\textsuperscript{18}F{]}fluoride activation.
At 100°C no reaction occurred. Increasing the temperature from 130°C to
160°C increased the radiochemical yield of
{[}\textsuperscript{18}F{]}FPATPP from 20 to 50\% (based on HPLC
analysis of crude reaction mixture).

\par\null

\textbf{References}

\textbf{1.} Beyzavi MH et al. \textsuperscript{18}F-Deoxyfluorination of
Phenols via Ru \selectlanguage{greek}π-\selectlanguage{english}Complexes, \emph{ACS Cent. Sci.} 2017;3(9):944-948.

\par\null\selectlanguage{english}
\begin{figure}[H]
\begin{center}
\includegraphics[width=0.70\columnwidth]{figures/5-rajala/5-rajala}

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\end{figure}\selectlanguage{english}
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\includegraphics[width=0.70\columnwidth]{figures/CAFACHEM/CAFACHEM}

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\end{figure}

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