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Literature DB >> 21057601

The [F]2-Fluoro-1,3-thiazolyl Moiety - an Easily-Accessible Structural Motif for Prospective Molecular Imaging Radiotracers.

Fabrice G Siméon¹, Matthew T Wendahl, Victor W Pike.

Abstract

2-Fluoro-1,3-thiazoles were rapidly and efficiently labeled with no-carrier-added fluorine-18 (t(1/2) = 109.7 min) by treatment of readily prepared 2-halo precursors with cyclotron-produced [(18)F]fluoride ion. The [(18)F]2-fluoro-1,3-thiazolyl moiety constitutes a new and easily-labeled structural motif for prospective molecular imaging radiotracers.

Entities: Chemical Disease Gene Species

Year: 2010 PMID： 21057601 PMCID： PMC2967737 DOI： 10.1016/j.tetlet.2010.09.037

Source DB: PubMed Journal: Tetrahedron Lett ISSN： 0040-4039 Impact factor: 2.415

16 in total

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2. Palladium-mediated fluorination of arylboronic acids.

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3. Fast and high-yield microreactor syntheses of ortho-substituted [(18)F]fluoroarenes from reactions of [(18)F]fluoride ion with diaryliodonium salts.

Authors: Joong-Hyun Chun; Shuiyu Lu; Yong-Sok Lee; Victor W Pike
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4. In vitro microsomal metabolic studies on a selective mGluR5 antagonist MTEP: characterization of in vitro metabolites and identification of a novel thiazole ring opening aldehyde metabolite.

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Review 5. Recent advances in non-competitive mGlu5 receptor antagonists and their potential therapeutic applications.

Authors: Abdelmalik Slassi; Methvin Isaac; Louise Edwards; Alexander Minidis; David Wensbo; Jan Mattsson; Karolina Nilsson; Patrick Raboisson; Donald McLeod; Thomas M Stormann; Lance G Hammerland; Edwin Johnson
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6. Metal-mediated inhibition of Escherichia coli methionine aminopeptidase: structure-activity relationships and development of a novel scoring function for metal-ligand interactions.

Authors: Rolf Schiffmann; Alexander Neugebauer; Christian D Klein
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7. Efficient and regioselective halogenations of 2-amino-1,3-thiazoles with copper salts.

Authors: Fabrice G Siméon; Matthew T Wendahl; Victor W Pike
Journal: J Org Chem Date: 2009-03-20 Impact factor: 4.354

8. Discovery of [18F]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide: a melanoma positron emission tomography imaging radiotracer with high tumor to body contrast ratio and rapid renal clearance.

Authors: Ivan Greguric; Stephen R Taylor; Delphine Denoyer; Patrice Ballantyne; Paula Berghofer; Peter Roselt; Tien Q Pham; Filomena Mattner; Thomas Bourdier; Oliver C Neels; Donna S Dorow; Christian Loc'h; Rodney J Hicks; Andrew Katsifis
Journal: J Med Chem Date: 2009-09-10 Impact factor: 7.446

Review 9. PET radiotracers: crossing the blood-brain barrier and surviving metabolism.

Authors: Victor W Pike
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10. Formation of ArF from LPdAr(F): catalytic conversion of aryl triflates to aryl fluorides.

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4 in total

1. Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.

Authors: Fabrice G Siméon; Matthew T Wendahl; Victor W Pike
Journal: J Med Chem Date: 2011-01-05 Impact factor: 7.446