Academic literature on the topic 'Late stage fluorination'

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Journal articles on the topic "Late stage fluorination"

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Tang, Pingping, Takeru Furuya, and Tobias Ritter. "Silver-Catalyzed Late-Stage Fluorination." Journal of the American Chemical Society 132, no. 34 (September 2010): 12150–54. http://dx.doi.org/10.1021/ja105834t.

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Campbell, Michael G., and Tobias Ritter. "Late-Stage Fluorination: From Fundamentals to Application." Organic Process Research & Development 18, no. 4 (March 11, 2014): 474–80. http://dx.doi.org/10.1021/op400349g.

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Abele, Stefan, and Hans-Jürgen Federsel. "Invited Academic Review on Late-Stage Fluorination." Organic Process Research & Development 18, no. 4 (March 11, 2014): 473. http://dx.doi.org/10.1021/op5000539.

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Brooks, Allen F., Joseph J. Topczewski, Naoko Ichiishi, Melanie S. Sanford, and Peter J. H. Scott. "Late-stage [18F]fluorination: new solutions to old problems." Chem. Sci. 5, no. 12 (2014): 4545–53. http://dx.doi.org/10.1039/c4sc02099e.

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Wu, Qiuzi, Yang-Jie Mao, Kun Zhou, Shuang Wang, Lei Chen, Zhen-Yuan Xu, Shao-Jie Lou, and Dan-Qian Xu. "Pd-Catalysed direct C(sp2)–H fluorination of aromatic ketones: concise access to anacetrapib." Chemical Communications 57, no. 37 (2021): 4544–47. http://dx.doi.org/10.1039/d1cc01047f.

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Neumann, Constanze N., and Tobias Ritter. "Late-Stage Fluorination: Fancy Novelty or Useful Tool?" Angewandte Chemie International Edition 54, no. 11 (February 4, 2015): 3216–21. http://dx.doi.org/10.1002/anie.201410288.

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Campbell, Michael G., and Tobias Ritter. "ChemInform Abstract: Late-Stage Fluorination: From Fundamentals to Application." ChemInform 45, no. 25 (June 5, 2014): no. http://dx.doi.org/10.1002/chin.201425239.

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Yerien, Damian E., Sergio Bonesi, and Al Postigo. "Fluorination methods in drug discovery." Organic & Biomolecular Chemistry 14, no. 36 (2016): 8398–427. http://dx.doi.org/10.1039/c6ob00764c.

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Late stage fluorination methods applied to biologically-active drugs have provided the pharmaceutical industry with new leads that show improved properties such as modulation of lipophilicity, electronegativity, basicity, bioavailability, and deceleration of metabolic degradation.
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Neumann, Constanze N., and Tobias Ritter. "ChemInform Abstract: Late-Stage Fluorination: Fancy Novelty or Useful Tool?" ChemInform 46, no. 19 (April 23, 2015): no. http://dx.doi.org/10.1002/chin.201519317.

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S. Clemente, Gonçalo, Tryfon Zarganes-Tzitzikas, Alexander Dömling, and Philip H. Elsinga. "Late-Stage Copper-Catalyzed Radiofluorination of an Arylboronic Ester Derivative of Atorvastatin." Molecules 24, no. 23 (November 20, 2019): 4210. http://dx.doi.org/10.3390/molecules24234210.

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There is an unmet need for late-stage 18F-fluorination strategies to label molecules with a wide range of relevant functionalities to medicinal chemistry, in particular (hetero)arenes, aiming to obtain unique in vivo information on the pharmacokinetics/pharmacodynamics (PK/PD) using positron emission tomography (PET). In the last few years, Cu-mediated oxidative radiofluorination of arylboronic esters/acids arose and has been successful in small molecules containing relatively simple (hetero)aromatic groups. However, this technique is sparsely used in the radiosynthesis of clinically significant molecules containing more complex backbones with several aromatic motifs. In this work, we add a new entry to this very limited database by presenting our recent results on the 18F-fluorination of an arylboronic ester derivative of atorvastatin. The moderate average conversion of [18F]F− (12%), in line with what has been reported for similarly complex molecules, stressed an overview through the literature to understand the radiolabeling variables and limitations preventing consistently higher yields. Nevertheless, the current disparity of procedures reported still hampers a consensual and conclusive output.
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Dissertations / Theses on the topic "Late stage fluorination"

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Ó, Dúill Miriam Leslie. "Late-stage fluorination and perfluoroalkylation." Thesis, University of Oxford, 2015. https://ora.ox.ac.uk/objects/uuid:25373cc9-ae25-45c4-aafc-a1706e289ea3.

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In this thesis new synthetic routes towards perfluorinated compounds are described, as well as their radiolabelling with fluorine-18, with the aim of application in pharmaceutically interesting targets. Part A investigates late-stage fluorination, i.e. retrosynthetic C–F bond disconnections. A silver catalysed electrophilic fluorodecarboxylation of fluorinated carboxylic acids for the formation of difluoromethyl-, trifluoromethyl-, and pentafluoroethylarenes is developed and transferred to a radiochemistry setting using [18F]Selectfluor bis(triflate). Part B explores late-stage perfluoroalkylation via cross-coupling strategies. The use of visible light-mediated ruthenium catalysis is investigated for the radical trifluoromethylation and pentafluoroethylation of vinyl- and alkynylsilanes and alkynes. Finally, the first generally applicable copper-mediated cross-coupling of Ruppert-Prakash-like aryl(tetrafluoroethyl)trimethylsilanes (ArCF2CF2SiMe3) is presented.
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Kamlet, Adam Seth. "Late-Stage Fluorination with \(^{18}F\)." Thesis, Harvard University, 2012. http://dissertations.umi.com/gsas.harvard:10530.

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Positron emission tomography (PET) is a powerful, non-invasive in vivo imaging technique used for diagnostics and drug development. The synthesis of \(^{18}F\)-PET tracers is challenging due to the short half-life of the unnatural isotope that necessitates late-stage fluorination, and the limited reactivity of nucleophilic fluoride, the preferred and widely accessible form of \(^{18}F\). This thesis describes the development of an electrophilic fluorination reagent derived from fluoride. The reagent can be employed in a late-stage fluorination reaction of palladium aryl complexes to give access to small molecule aryl fluorides. The reagent can be made from \([^{18}F]\)fluoride and used to synthesize radiolabeled small molecules for PET imaging experiments. Two small molecules known to interact with the serotonergic system were synthesized, radiolabeled, and imaged in rats and non-human primates and evaluated for use as PET tracers.
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Craig, Austin [Verfasser], and Bernd [Gutachter] Neumaier. "Preparation of Labeled Aromatic Amino Acids via Late-Stage 18F-Fluorination of Chiral Nickel and Copper Complexes / Austin Craig ; Gutachter: Bernd Neumaier." Köln : Universitäts- und Stadtbibliothek Köln, 2020. http://d-nb.info/1232404470/34.

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Sang, Ruocheng Verfasser], Tobias [Akademischer Betreuer] Ritter, and Carsten [Akademischer Betreuer] [Bolm. "Late-stage functionalization of arenes: site-selective C-H oxygenation and fluorination via aryl sulfonium salts / Ruocheng Sang ; Tobias Ritter, Carsten Bolm." Aachen : Universitätsbibliothek der RWTH Aachen, 2020. http://d-nb.info/1221697455/34.

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Books on the topic "Late stage fluorination"

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Postigo, Al. Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates. Elsevier, 2018.

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Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates. Elsevier, 2019. http://dx.doi.org/10.1016/c2016-0-03574-x.

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Postigo, Al. Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates. Elsevier, 2018.

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Book chapters on the topic "Late stage fluorination"

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Shibatomi, Kazutaka. "Enantioselective Fluorination." In Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates, 137–58. Elsevier, 2019. http://dx.doi.org/10.1016/b978-0-12-812958-6.00004-5.

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Raviola, Carlotta, Stefano Protti, and Davide Ravelli. "Photocatalytic Fluorination Reactions." In Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates, 183–221. Elsevier, 2019. http://dx.doi.org/10.1016/b978-0-12-812958-6.00006-9.

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Zaikin, Pavel A., and Gennady I. Borodkin. "Electrophilic and Oxidative Fluorination of Aromatic Compounds." In Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates, 105–35. Elsevier, 2019. http://dx.doi.org/10.1016/b978-0-12-812958-6.00003-3.

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Postigo, Al. "Fluorination of Bioactive Compounds by Electron Transfer Reactions." In Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates, 287–320. Elsevier, 2019. http://dx.doi.org/10.1016/b978-0-12-812958-6.00009-4.

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Barata-Vallejo, Sebastian. "Fluorination of Allylic Positions Toward the Synthesis of Fluorinated Bioactive Compounds." In Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates, 223–41. Elsevier, 2019. http://dx.doi.org/10.1016/b978-0-12-812958-6.00007-0.

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Postigo, Al. "Introduction and Outline." In Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates, 1–27. Elsevier, 2019. http://dx.doi.org/10.1016/b978-0-12-812958-6.00001-x.

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Edem, Patricia E., E. Johanna L. Steen, Andreas Kjær, and Matthias M. Herth. "Fluorine-18 Radiolabeling Strategies—Advantages and Disadvantages of Currently Applied Labeling Methods." In Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates, 29–103. Elsevier, 2019. http://dx.doi.org/10.1016/b978-0-12-812958-6.00002-1.

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Zhou, Lei, and Devireddy Anand. "Visible Light–Mediated C–F Bond Activation." In Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates, 159–81. Elsevier, 2019. http://dx.doi.org/10.1016/b978-0-12-812958-6.00005-7.

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Postigo, Al. "Difluoromethylation of Bioactive Compounds." In Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates, 243–85. Elsevier, 2019. http://dx.doi.org/10.1016/b978-0-12-812958-6.00008-2.

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Han, Jianlin, Alicja Wzorek, Karel D. Klika, and Vadim A. Soloshonok. "Fluorine-Containing Pharmaceuticals and the Phenomenon of the Self-Disproportionation of Enantiomers." In Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates, 321–55. Elsevier, 2019. http://dx.doi.org/10.1016/b978-0-12-812958-6.00010-0.

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Conference papers on the topic "Late stage fluorination"

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Ritter, Tobias. "Late-Stage Fluorination." In 15th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-15bmos-speech9.

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