Literature DB >> 21987078

A simple, rapid procedure for nucleophilic radiosynthesis of aliphatic [18F]trifluoromethyl groups.

Patrick J Riss1, Franklin I Aigbirhio.   

Abstract

A procedure for the radiosynthesis of aliphatic [(18)F]trifluoromethyl groups by reacting 1,1-difluorovinyl precursors with [(18)F]fluoride ions, resulting in the equivalent of direct nucleophilic addition of H[(18)F]F, has been developed. A variety of (18)F-labelled model compounds were then obtained and two potential [(18)F]radiotracers were synthesised by a two step process starting from 1,1-difluorovin-2-yl 4-toluenesulfonate. The method is widely applicable for the synthesis of novel radiotracers in high radiochemical yields and good specific activity. This journal is © The Royal Society of Chemistry 2011

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Year:  2011        PMID: 21987078     DOI: 10.1039/c1cc15342k

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


  19 in total

1.  3-Substituted 1,5-Diaryl-1 H-1,2,4-triazoles as Prospective PET Radioligands for Imaging Brain COX-1 in Monkey. Part 2: Selection and Evaluation of [11C]PS13 for Quantitative Imaging.

Authors:  Stal Shrestha; Prachi Singh; Michelle Y Cortes-Salva; Kimberly J Jenko; Masamichi Ikawa; Min-Jeong Kim; Masato Kobayashi; Cheryl L Morse; Robert L Gladding; Jeih-San Liow; Sami S Zoghbi; Masahiro Fujita; Robert B Innis; Victor W Pike
Journal:  ACS Chem Neurosci       Date:  2018-06-13       Impact factor: 4.418

2.  Synthesis and evaluation of C-11, F-18 and I-125 small molecule radioligands for detecting oxytocin receptors.

Authors:  Aaron L Smith; Sara M Freeman; Jeffery S Stehouwer; Kiyoshi Inoue; Ronald J Voll; Larry J Young; Mark M Goodman
Journal:  Bioorg Med Chem       Date:  2012-02-25       Impact factor: 3.641

Review 3.  Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging.

Authors:  Victor W Pike
Journal:  Curr Med Chem       Date:  2016       Impact factor: 4.530

4.  Base mediated deprotection strategies for trifluoroethyl (TFE) ethers, a new alcohol protecting group.

Authors:  Qingliang Yang; Jon T Njardarson
Journal:  Tetrahedron Lett       Date:  2013-12-18       Impact factor: 2.415

Review 5.  Chemistry for Positron Emission Tomography: Recent Advances in 11 C-, 18 F-, 13 N-, and 15 O-Labeling Reactions.

Authors:  Xiaoyun Deng; Jian Rong; Lu Wang; Neil Vasdev; Lei Zhang; Lee Josephson; Steven H Liang
Journal:  Angew Chem Int Ed Engl       Date:  2019-01-14       Impact factor: 15.336

Review 6.  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

7.  Late-stage [18F]Fluorination: New Solutions to Old Problems.

Authors:  Allen F Brooks; Joseph J Topczewski; Naoko Ichiishi; Melanie S Sanford; Peter J H Scott
Journal:  Chem Sci       Date:  2014-12-01       Impact factor: 9.825

8.  High affinity radiopharmaceuticals based upon lansoprazole for PET imaging of aggregated tau in Alzheimer's disease and progressive supranuclear palsy: synthesis, preclinical evaluation, and lead selection.

Authors:  Maria V Fawaz; Allen F Brooks; Melissa E Rodnick; Garrett M Carpenter; Xia Shao; Timothy J Desmond; Phillip Sherman; Carole A Quesada; Brian G Hockley; Michael R Kilbourn; Roger L Albin; Kirk A Frey; Peter J H Scott
Journal:  ACS Chem Neurosci       Date:  2014-06-16       Impact factor: 4.418

9.  Synthesis of [18F]PS13 and Evaluation as a PET Radioligand for Cyclooxygenase-1 in Monkey.

Authors:  Carlotta Taddei; Cheryl L Morse; Min-Jeong Kim; Jeih-San Liow; Jose Montero Santamaria; Andrea Zhang; Lester S Manly; Paolo Zanotti-Fregonara; Robert L Gladding; Sami S Zoghbi; Robert B Innis; Victor W Pike
Journal:  ACS Chem Neurosci       Date:  2021-01-25       Impact factor: 5.780

10.  Evaluating N-difluoromethyltriazolium triflate as a precursor for the synthesis of high molar activity [18 F]fluoroform.

Authors:  Anna Pees; Maria J W D Vosjan; Jin Young Chai; Hyojin Cha; Dae Yoon Chi; Albert D Windhorst; Danielle J Vugts
Journal:  J Labelled Comp Radiopharm       Date:  2021-09-20       Impact factor: 1.949

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