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One-pot synthesis of high molar activity 6-[18F]fluoro-l-DOPA by Cu-mediated fluorination of a BPin precursor.
Mossine, Andrew V; Tanzey, Sean S; Brooks, Allen F; Makaravage, Katarina J; Ichiishi, Naoko; Miller, Jason M; Henderson, Bradford D; Skaddan, Marc B; Sanford, Melanie S; Scott, Peter J H.
Afiliação
  • 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.
Org Biomol Chem ; 17(38): 8701-8705, 2019 10 14.
Article em En | MEDLINE | ID: mdl-31536095
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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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos Radiofarmacêuticos / Cobre Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos Radiofarmacêuticos / Cobre Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article