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. 2019 Oct 14;17(38):8701-8705.
doi: 10.1039/c9ob01758e. Epub 2019 Sep 19.

One-pot synthesis of high molar activity 6-[18F]fluoro-l-DOPA by Cu-mediated fluorination of a BPin precursor

Andrew V Mossine  1 , Sean S Tanzey  2 , Allen F Brooks  1 , Katarina J Makaravage  3 , Naoko Ichiishi  3 , Jason M Miller  2 , Bradford D Henderson  1 , Marc B Skaddan  4 , Melanie S Sanford  3 , Peter J H Scott  2
Affiliations

One-pot synthesis of high molar activity 6-[18F]fluoro-l-DOPA by Cu-mediated fluorination of a BPin precursor

Andrew V Mossine et al. Org Biomol Chem. .

Abstract

A one-pot two-step synthesis of 6-[18F]fluoro-l-DOPA ([18F]FDOPA) has been developed involving Cu-mediated radiofluorination of a pinacol boronate ester precursor. The method is fully automated, provides [18F]FDOPA in good activity yield (104 ± 16 mCi, 6 ± 1%), excellent radiochemical purity (>99%) and high molar activity (3799 ± 2087 Ci mmol-1), n = 3, and has been validated to produce the radiotracer for human use.

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Conflict of interest statement

Conflicts of interest

There are no conflicts to declare.

Figures

Fig. 1
Fig. 1
Radiosyntheses of [18F]FDOPA and motivation for this work. a based on [18F]F2 in reactor; b doses not reformulated for clinical use.
See this image and copyright information in PMC

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