Literature DB >> 27241832

Enhanced copper-mediated (18)F-fluorination of aryl boronic esters provides eight radiotracers for PET applications.

Sean Preshlock1, Samuel Calderwood1, Stefan Verhoog1, Matthew Tredwell1, Mickael Huiban2, Antje Hienzsch3, Stefan Gruber1, Thomas C Wilson1, Nicholas J Taylor1, Thomas Cailly4, Michael Schedler1, Thomas Lee Collier5, Jan Passchier2, René Smits3, Jan Mollitor3, Alexander Hoepping3, Marco Mueller3, Christophe Genicot6, Joël Mercier6, Véronique Gouverneur1.   

Abstract

[(18)F]FMTEB, [(18)F]FPEB, [(18)F]flumazenil, [(18)F]DAA1106, [(18)F]MFBG, [(18)F]FDOPA, [(18)F]FMT and [(18)F]FDA are prepared from the corresponding arylboronic esters and [(18)F]KF/K222 in the presence of Cu(OTf)2py4. The method was successfully applied using three radiosynthetic platforms, and up to 26 GBq of non-carrier added starting activity of (18)F-fluoride.

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Year:  2016        PMID： 27241832     DOI： 10.1039/c6cc03295h

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN： 1359-7345            Impact factor:   6.222


  42 in total

1.  Synthesis and in Vivo Evaluation of a Novel PET Radiotracer for Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) in Nonhuman Primates.

Authors:  Songye Li; Zhengxin Cai; Xiaoai Wu; Daniel Holden; Richard Pracitto; Michael Kapinos; Hong Gao; David Labaree; Nabeel Nabulsi; Richard E Carson; Yiyun Huang
Journal:  ACS Chem Neurosci       Date:  2018-11-16       Impact factor: 4.418

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

Authors:  Andrew V Mossine; Sean S Tanzey; Allen F Brooks; Katarina J Makaravage; Naoko Ichiishi; Jason M Miller; Bradford D Henderson; Marc B Skaddan; Melanie S Sanford; Peter J H Scott
Journal:  Org Biomol Chem       Date:  2019-09-19       Impact factor: 3.876

3.  Automated synthesis of PET radiotracers by copper-mediated 18 F-fluorination of organoborons: Importance of the order of addition and competing protodeborylation.

Authors:  Andrew V Mossine; Allen F Brooks; Vadim Bernard-Gauthier; Justin J Bailey; Naoko Ichiishi; Ralf Schirrmacher; Melanie S Sanford; Peter J H Scott
Journal:  J Labelled Comp Radiopharm       Date:  2018-02-02       Impact factor: 1.921

4.  (Radio)fluoroclick Reaction Enabled by a Hydrogen-Bonding Cluster.

Authors:  Xiaojun Zeng; Junling Li; Chin K Ng; Gerald B Hammond; Bo Xu
Journal:  Angew Chem Int Ed Engl       Date:  2018-02-13       Impact factor: 15.336

Review 5.  Fluorine-18 patents (2009-2015). Part 2: new radiochemistry.

Authors:  Andrew V Mossine; Stephen Thompson; Allen F Brooks; Alexandra R Sowa; Jason M Miller; Peter Jh Scott
Journal:  Pharm Pat Anal       Date:  2016-09

6.  GABAA Receptors in the Mongolian Gerbil: a PET Study Using [18F]Flumazenil to Determine Receptor Binding in Young and Old Animals.

Authors:  M Kessler; M Mamach; R Beutelmann; M Lukacevic; S Eilert; P Bascuñana; A Fasel; F M Bengel; J P Bankstahl; T L Ross; G M Klump; G Berding
Journal:  Mol Imaging Biol       Date:  2020-04       Impact factor: 3.488

7.  Comparison of high and low molar activity TSPO tracer [18F]F-DPA in a mouse model of Alzheimer's disease.

Authors:  Thomas Keller; Francisco R López-Picón; Anna Krzyczmonik; Sarita Forsback; Jatta S Takkinen; Johan Rajander; Simo Teperi; Frédéric Dollé; Juha O Rinne; Merja Haaparanta-Solin; Olof Solin
Journal:  J Cereb Blood Flow Metab       Date:  2019-05-29       Impact factor: 6.200

8.  Synthesis of [18 F]Fluoroarenes by Nucleophilic Radiofluorination of N-Arylsydnones.

Authors:  Maruthi Kumar Narayanam; Gaoyuan Ma; Pier Alexandre Champagne; Kendall N Houk; Jennifer M Murphy
Journal:  Angew Chem Int Ed Engl       Date:  2017-09-07       Impact factor: 15.336

9.  NHC-Copper Mediated Ligand-Directed Radiofluorination of Aryl Halides.

Authors:  Liam S Sharninghausen; Allen F Brooks; Wade P Winton; Katarina J Makaravage; Peter J H Scott; Melanie S Sanford
Journal:  J Am Chem Soc       Date:  2020-04-10       Impact factor: 15.419

10.  Radiosynthesis and Biodistribution of 18F-Linezolid in Mycobacterium tuberculosis-Infected Mice Using Positron Emission Tomography.

Authors:  Filipa Mota; Ravindra Jadhav; Camilo A Ruiz-Bedoya; Alvaro A Ordonez; Mariah H Klunk; Joel S Freundlich; Sanjay K Jain
Journal:  ACS Infect Dis       Date:  2020-04-09       Impact factor: 5.084
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