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Review
. 2022 Feb:180:110032.
doi: 10.1016/j.apradiso.2021.110032. Epub 2021 Nov 18.

An automated radiosynthesis of [18F]DPA-714 on a commercially available radiosynthesizer, Elixys Flex/Chem

Katelyenn S McCauley  1 , Justin H Wilde  1 , Sophia M Bufalino  2 , Kiel D Neumann  3
Affiliations
Review

An automated radiosynthesis of [18F]DPA-714 on a commercially available radiosynthesizer, Elixys Flex/Chem

Katelyenn S McCauley et al. Appl Radiat Isot. 2022 Feb.

Abstract

[18F]DPA-714 is a radiotracer specific to the translocator protein (TSPO) and is useful for in vivo Positron Emission Tomography imaging studies. In this report, we have developed an automated radiosynthesis of [18F]DPA-714 on a commercially-available radiosynthesis platform, which comports with USP <823> guidelines. The wide availability of the radiosynthesis module and ease of dissemination of the production sequence will facilitate preclinical and clinical research of TSPO-related pathology.

Keywords: Automation; F-18; Fluorine-18; Positron emission tomography; Radiochemistry; Radiosynthesis.

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Conflict of interest statement

Declaration of competing interest

The authors declare no competing interests.

Figures

Figure 1.
Figure 1.
Reagents and consumables needed to complete the radiosynthesis of [18F]DPA-714 on the Elixys Flex/Chem™.
Figure 2
Figure 2. Influence of Time on Activity Yields of [18F]DPA-714.
All reactions were performed at 100 °C on the Elixys Flex/Chem module. All activity yields are reported as an average (n=3).
Figure 3
Figure 3. Influence of Temperature on Activity Yields of [18F]DPA-714.
All reactions were performed for 15 minutes on the Elixys Flex/Chem module. All activity yields are reported as an average (n=3).
Scheme 1.
Scheme 1.. Synthetic organic route to the radiochemical precursor of [18F]DPA-714.
The hypothesized formation of the elimination side product observed during the production of 8 is highlighted (lower right).
Scheme 2.
Scheme 2.
Radiochemical Synthesis of [18F]DPA-714.
See this image and copyright information in PMC

References

    1. Arlicot N, Vercouillie J, Ribeiro M-J, Tauber C, Venel Y, Baulieu J-L, Maia S, Corcia P, Stabin MG, Reynolds A, Kassiou M, & Guilloteau D (2012). Initial evaluation in healthy humans of [18F]DPA-714, a potential PET biomarker for neuroinflammation. Nuclear Medicine and Biology, 39(4), 570–578. 10.1016/j.nucmedbio.2011.10.012 - DOI - PubMed
    1. Banister SD, Wilkinson SM, Hanani R, Reynolds AJ, Hibbs DE, & Kassiou M (2012). A practical, multigram synthesis of the 2-(2-(4-alkoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide (DPA) class of high affinity translocator protein (TSPO) ligands. Tetrahedron Letters, 53(29), 3780–3783. 10.1016/j.tetlet.2012.05.044 - DOI
    1. Block ML, Zecca L, & Hong J-S (2007). Microglia-mediated neurotoxicity: uncovering the molecular mechanisms. Nature Reviews Neuroscience, 8(1), 57–69. 10.1038/nrn2038 - DOI - PubMed
    1. Chauveau F, Boutin H, Camp NV, Dollé F, & Tavitian B (2008). Nuclear imaging of neuroinflammation: a comprehensive review of [11C]PK11195 challengers. European Journal of Nuclear Medicine and Molecular Imaging, 35(12), 2304–2319. 10.1007/s00259-008-0908-9 - DOI - PubMed
    1. Chauveau F, Camp NV, Dollé F, Kuhnast B, Hinnen F, Damont A, Boutin H, James M, Kassiou M, & Tavitian B (2009). Comparative Evaluation of the Translocator Protein Radioligands 11C-DPA-713, 18F-DPA-714, and 11C-PK11195 in a Rat Model of Acute Neuroinflammation. Journal of Nuclear Medicine, 50(3), 468–476. 10.2967/jnumed.108.058669 - DOI - PubMed

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