One-pot synthesis of high molar activity 6-[18F]fluoro-l-DOPA by Cu-mediated fluorination of a BPin precursor†
Andrew V.
Mossine, 
‡a
Sean S.
Tanzey,
ab
Allen F.
Brooks,
a
Katarina J.
Makaravage,
‡c
Naoko
Ichiishi,
‡c
Melanie S.
Sanford
*c
and
Peter J. H.
Scott
*ab
‡a
Sean S.
Tanzey,
ab
Allen F.
Brooks,
a
Katarina J.
Makaravage,
‡c
Naoko
Ichiishi,
‡c
Melanie S.
Sanford
*c
and
Peter J. H.
Scott
*ab
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.
![Graphical abstract: One-pot synthesis of high molar activity 6-[18F]fluoro-l-DOPA by Cu-mediated fluorination of a BPin precursor](/aa/Image/Get?imageInfo.ImageType=GA&imageInfo.ImageIdentifier.ManuscriptID=C9OB01758E&imageInfo.ImageIdentifier.Year=2019)
- This article is part of the themed collections: Celebrating our 2020 Prize and Award winners and Synthetic methodology in OBC
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