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Synthesis of Diverse (11)C-Labeled PET Radiotracers via Direct Incorporation of [(11)C]CO2.
Mossine, Andrew V; Brooks, Allen F; Jackson, Isaac M; Quesada, Carole A; Sherman, Phillip; Cole, Erin L; Donnelly, David J; Scott, Peter J H; Shao, Xia.
Afiliación
  • Mossine AV; Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Brooks AF; Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Jackson IM; Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Quesada CA; Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Sherman P; Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Cole EL; Discovery Chemistry Platforms, PET Radiochemical Synthesis, Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08648, United States.
  • Donnelly DJ; Discovery Chemistry Platforms, PET Radiochemical Synthesis, Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08648, United States.
  • Scott PJ; Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Shao X; The Interdepartmental Program in Medicinal Chemistry, The University of Michigan , Ann Arbor, Michigan 48109, United States.
Bioconjug Chem ; 27(5): 1382-9, 2016 05 18.
Article en En | MEDLINE | ID: mdl-27043721
Three new positron emission tomography (PET) radiotracers of interest to our functional neuroimaging and translational oncology programs have been prepared through new developments in [(11)C]CO2 fixation chemistry. [(11)C]QZ (glutaminyl cyclase) was prepared via a tandem trapping of [(11)C]CO2/intramolecular cyclization; [(11)C]tideglusib (glycogen synthase kinase-3) was synthesized through a tandem trapping of [(11)C]CO2 followed by an intermolecular cycloaddition between a [(11)C]isocyanate and an isothiocyanate to form the 1,2,4-thiadiazolidine-3,5-dione core; [(11)C]ibrutinib (Bruton's tyrosine kinase) was synthesized through a HATU peptide coupling of an amino precursor with [(11)C]acrylic acid (generated from [(11)C]CO2 fixation with vinylmagnesium bromide). All radiochemical syntheses are fully automated on commercial radiochemical synthesis modules and provide radiotracers in 1-5% radiochemical yield (noncorrected, based upon [(11)C]CO2). All three radiotracers have advanced to rodent imaging studies and preliminary PET imaging results are also reported.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dióxido de Carbono / Radioisótopos de Carbono / Tomografía de Emisión de Positrones Límite: Animals Idioma: En Revista: Bioconjug Chem Asunto de la revista: BIOQUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dióxido de Carbono / Radioisótopos de Carbono / Tomografía de Emisión de Positrones Límite: Animals Idioma: En Revista: Bioconjug Chem Asunto de la revista: BIOQUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos