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

Autor: Mossine AV; Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA. pjhscott@umich.edu., Tanzey SS; Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA. pjhscott@umich.edu and Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, USA., Brooks AF; Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA. pjhscott@umich.edu., Makaravage KJ; Department of Chemistry, University of Michigan, Ann Arbor, MI 48109, USA. mssanfor@umich.edu., Ichiishi N; Department of Chemistry, University of Michigan, Ann Arbor, MI 48109, USA. mssanfor@umich.edu., Miller JM; Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA. pjhscott@umich.edu and Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, USA., Henderson BD; Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA. pjhscott@umich.edu., Skaddan MB; AbbVie Translational Imaging, North Chicago, IL 60030, USA., Sanford MS; Department of Chemistry, University of Michigan, Ann Arbor, MI 48109, USA. mssanfor@umich.edu., Scott PJH; Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA. pjhscott@umich.edu and Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, USA.
Jazyk: angličtina
Zdroj: Organic & biomolecular chemistry [Org Biomol Chem] 2019 Oct 14; Vol. 17 (38), pp. 8701-8705. Date of Electronic Publication: 2019 Sep 19.
DOI: 10.1039/c9ob01758e
Abstrakt: A one-pot two-step synthesis of 6-[ 18 F]fluoro-l-DOPA ([ 18 F]FDOPA) has been developed involving Cu-mediated radiofluorination of a pinacol boronate ester precursor. The method is fully automated, provides [ 18 F]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.
Databáze: MEDLINE
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