Issue 38, 2019

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

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

Article type
Communication
Submitted
09 Mha 2019
Accepted
17 Ndz 2019
First published
17 Ndz 2019

Org. Biomol. Chem., 2019,17, 8701-8705

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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