Literature DB >> 15678189

Synthesis of 18F-labelled cyclooxygenase-2 (COX-2) inhibitors via Stille reaction with 4-[18F]fluoroiodobenzene as radiotracers for positron emission tomography (PET).

Frank R Wüst1, Aileen Höhne, Peter Metz.   

Abstract

The Stille reaction with 4-[(18)F]fluoroiodobenzene as a novel approach for the synthesis of radiotracers for monitoring COX-2 expression by means of PET has been developed. Optimized reaction conditions were elaborated by screening of various catalyst systems and solvents. By using optimized reaction conditions (18)F-labelled COX-2 inhibitors [(18)F]-5 and [(18)F]-13 could be obtained in radiochemical yields of up to 94% and 68%, respectively, based upon 4-[(18)F]fluoroiodobenzene.

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Year:  2004        PMID： 15678189     DOI： 10.1039/b412871k

Source DB:  PubMed          Journal:  Org Biomol Chem        ISSN： 1477-0520            Impact factor:   3.876


  6 in total

Review 1.  Radiosyntheses using fluorine-18: the art and science of late stage fluorination.

Authors:  Erin L Cole; Megan N Stewart; Ryan Littich; Raphael Hoareau; Peter J H Scott
Journal:  Curr Top Med Chem       Date:  2014       Impact factor: 3.295

Review 2.  Cyclooxygenases as Potential PET Imaging Biomarkers to Explore Neuroinflammation in Dementia.

Authors:  Bruny V Kenou; Lester S Manly; Sara B Rubovits; Somachukwu A Umeozulu; Maia G Van Buskirk; Andrea S Zhang; Victor W Pike; Paolo Zanotti-Fregonara; Ioline D Henter; Robert B Innis
Journal:  J Nucl Med       Date:  2022-06       Impact factor: 11.082

Review 3.  Nuclear imaging of neuroinflammation: a comprehensive review of [11C]PK11195 challengers.

Authors:  Fabien Chauveau; Hervé Boutin; Nadja Van Camp; Frédéric Dollé; Bertrand Tavitian
Journal:  Eur J Nucl Med Mol Imaging       Date:  2008-10-01       Impact factor: 9.236

4.  2-Carbaborane-3-phenyl-1H-indoles--synthesis via McMurry reaction and cyclooxygenase (COX) inhibition activity.

Authors:  Markus Laube; Wilma Neumann; Matthias Scholz; Peter Lönnecke; Brenda Crews; Lawrence J Marnett; Jens Pietzsch; Torsten Kniess; Evamarie Hey-Hawkins
Journal:  ChemMedChem       Date:  2013-01-09       Impact factor: 3.466

5.  Discovery of Furanone-Based Radiopharmaceuticals for Diagnostic Targeting of COX-1 in Ovarian Cancer.

Authors:  Md Jashim Uddin; Andrew J Wilson; Brenda C Crews; Paola Malerba; Md Imam Uddin; Philip J Kingsley; Kebreab Ghebreselasie; Cristina K Daniel; Michael L Nickels; Mohammed N Tantawy; Elma Jashim; H Charles Manning; Dineo Khabele; Lawrence J Marnett
Journal:  ACS Omega       Date:  2019-05-24

Review 6.  Small Molecule Radiopharmaceuticals - A Review of Current Approaches.

Authors:  Shubhra Chaturvedi; Anil K Mishra
Journal:  Front Med (Lausanne)       Date:  2016-02-23
  6 in total

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