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Issue 38, 2019

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

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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

Supplementary files

Article information


Submitted
09 Aug 2019
Accepted
17 Sep 2019
First published
17 Sep 2019

Org. Biomol. Chem., 2019,17, 8701-8705
Article type
Communication
Author version available

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

A. V. Mossine, S. S. Tanzey, A. F. Brooks, K. J. Makaravage, N. Ichiishi, J. M. Miller, B. D. Henderson, M. B. Skaddan, M. S. Sanford and P. J. H. Scott, Org. Biomol. Chem., 2019, 17, 8701 DOI: 10.1039/C9OB01758E

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