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  1. Article ; Online: Microfluidic Preparation of

    Earley, Daniel F / Guillou, Amaury / van der Born, Dion / Poot, Alex J / Holland, Jason P

    Molecules (Basel, Switzerland)

    2021  Volume 26, Issue 3

    Abstract: ... ...

    Abstract 89
    MeSH term(s) Humans ; Isotope Labeling ; Lab-On-A-Chip Devices ; Photochemistry ; Radiochemistry/instrumentation ; Radioisotopes/chemistry ; Serum Albumin, Human/chemistry ; Zirconium/chemistry
    Chemical Substances Radioisotopes ; Zirconium (C6V6S92N3C) ; Zirconium-89 (NTM296JU95) ; Serum Albumin, Human (ZIF514RVZR)
    Language English
    Publishing date 2021-02-02
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules26030764
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Ultrafast Photoclick Reaction for Selective ¹⁸F-Positron Emission Tomography Tracer Synthesis in Flow

    Fu, Youxin / Helbert, Hugo / Simeth, Nadja A. / Crespi, Stefano / Spoelstra, Gerbren B. / van Dijl, Jan Maarten / van Oosten, Marleen / Nazario, Luiza Reali / van der Born, Dion / Luurtsema, Gert / Szymanski, Wiktor / Elsinga, Philip H. / Feringa, Ben L.

    Journal of the American Chemical Society. 2021 June 28, v. 143, no. 27

    2021  

    Abstract: The development of very fast, clean, and selective methods for indirect labeling in PET tracer synthesis is an ongoing challenge. Here we present the development of an ultrafast photoclick method for the synthesis of short-lived ¹⁸F-PET tracers based on ... ...

    Abstract The development of very fast, clean, and selective methods for indirect labeling in PET tracer synthesis is an ongoing challenge. Here we present the development of an ultrafast photoclick method for the synthesis of short-lived ¹⁸F-PET tracers based on the photocycloaddition reaction of 9,10-phenanthrenequinones with electron-rich alkenes. The respective precursors are synthetically easily accessible and can be functionalized with various target groups. Using a flow photo-microreactor, the photoclick reaction can be performed in 60 s, and clinically relevant tracers for prostate cancer and bacterial infection imaging were prepared to demonstrate practicality of the method.
    Keywords alkenes ; bacterial infections ; prostatic neoplasms ; tomography
    Language English
    Dates of publication 2021-0628
    Size p. 10041-10047.
    Publishing place American Chemical Society
    Document type Article
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021/jacs.1c02229
    Database NAL-Catalogue (AGRICOLA)

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  3. Article ; Online: Ultrafast Photoclick Reaction for Selective

    Fu, Youxin / Helbert, Hugo / Simeth, Nadja A / Crespi, Stefano / Spoelstra, Gerbren B / van Dijl, Jan Maarten / van Oosten, Marleen / Nazario, Luiza Reali / van der Born, Dion / Luurtsema, Gert / Szymanski, Wiktor / Elsinga, Philip H / Feringa, Ben L

    Journal of the American Chemical Society

    2021  Volume 143, Issue 27, Page(s) 10041–10047

    Abstract: The development of very fast, clean, and selective methods for indirect labeling in PET tracer synthesis is an ongoing challenge. Here we present the development of an ultrafast photoclick method for the synthesis of short- ... ...

    Abstract The development of very fast, clean, and selective methods for indirect labeling in PET tracer synthesis is an ongoing challenge. Here we present the development of an ultrafast photoclick method for the synthesis of short-lived
    Language English
    Publishing date 2021-06-28
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021/jacs.1c02229
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Fluorine-18 labelled building blocks for PET tracer synthesis.

    van der Born, Dion / Pees, Anna / Poot, Alex J / Orru, Romano V A / Windhorst, Albert D / Vugts, Danielle J

    Chemical Society reviews

    2017  Volume 46, Issue 15, Page(s) 4709–4773

    Abstract: Positron emission tomography (PET) is an important driver for present day healthcare. Fluorine-18 is the most widely used radioisotope for PET imaging and a thorough overview of the available radiochemistry methodology is a prerequisite for selection of ... ...

    Abstract Positron emission tomography (PET) is an important driver for present day healthcare. Fluorine-18 is the most widely used radioisotope for PET imaging and a thorough overview of the available radiochemistry methodology is a prerequisite for selection of a synthetic approach for new fluorine-18 labelled PET tracers. These PET tracers can be synthesised either by late-stage radiofluorination, introducing fluorine-18 in the last step of the synthesis, or by a building block approach (also called modular build-up approach), introducing fluorine-18 in a fast and efficient manner in a building block, which is reacted further in one or multiple reaction steps to form the PET tracer. This review presents a comprehensive overview of the synthesis and application of fluorine-18 labelled building blocks since 2010.
    MeSH term(s) Fluorine Radioisotopes ; Molecular Structure ; Positron-Emission Tomography ; Radiopharmaceuticals/chemical synthesis ; Radiopharmaceuticals/chemistry
    Chemical Substances Fluorine Radioisotopes ; Radiopharmaceuticals ; Fluorine-18 (GZ5I74KB8G)
    Language English
    Publishing date 2017-06-13
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 1472875-8
    ISSN 1460-4744 ; 0306-0012
    ISSN (online) 1460-4744
    ISSN 0306-0012
    DOI 10.1039/c6cs00492j
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article: Design of Radioiodinated Pharmaceuticals: Structural Features Affecting Metabolic Stability towards in Vivo Deiodination.

    Cavina, Lorenzo / van der Born, Dion / Klaren, Peter H M / Feiters, Martin C / Boerman, Otto C / Rutjes, Floris P J T

    European journal of organic chemistry

    2017  Volume 2017, Issue 24, Page(s) 3387–3414

    Abstract: Radioiodinated pharmaceuticals are convenient tracers for clinical and research investigations because of the relatively long half-lives of radioactive iodine isotopes (i.e., ...

    Abstract Radioiodinated pharmaceuticals are convenient tracers for clinical and research investigations because of the relatively long half-lives of radioactive iodine isotopes (i.e.,
    Language English
    Publishing date 2017-04-26
    Publishing country Germany
    Document type Journal Article ; Review
    ZDB-ID 1475010-7
    ISSN 1099-0690 ; 1434-193X
    ISSN (online) 1099-0690
    ISSN 1434-193X
    DOI 10.1002/ejoc.201601638
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Efficient synthesis of [18F]trifluoromethane and its application in the synthesis of PET tracers.

    van der Born, Dion / Herscheid, J Koos D M / Orru, Romano V A / Vugts, Danielle J

    Chemical communications (Cambridge, England)

    2013  Volume 49, Issue 38, Page(s) 4018–4020

    Abstract: A new strategy towards [(18)F]trifluoromethyl-containing compounds is developed. [(18)F]trifluoromethane is synthesised in a fast and efficient manner and subsequently used in the reaction with aldehydes and ketones forming [(18)F]trifluoromethyl ... ...

    Abstract A new strategy towards [(18)F]trifluoromethyl-containing compounds is developed. [(18)F]trifluoromethane is synthesised in a fast and efficient manner and subsequently used in the reaction with aldehydes and ketones forming [(18)F]trifluoromethyl carbinols in good yields.
    MeSH term(s) Aldehydes/chemistry ; Chlorofluorocarbons, Methane/chemical synthesis ; Chlorofluorocarbons, Methane/chemistry ; Fluorine Radioisotopes/chemistry ; Ketones/chemistry ; Positron-Emission Tomography
    Chemical Substances Aldehydes ; Chlorofluorocarbons, Methane ; Fluorine Radioisotopes ; Ketones ; fluoroform (ZJ51L9A260)
    Language English
    Publishing date 2013-05-11
    Publishing country England
    Document type Journal Article
    ZDB-ID 1472881-3
    ISSN 1364-548X ; 1359-7345 ; 0009-241X
    ISSN (online) 1364-548X
    ISSN 1359-7345 ; 0009-241X
    DOI 10.1039/c3cc37833k
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article ; Online: Corrigendum: Modular Medical Imaging Agents Based on Azide-Alkyne Huisgen Cycloadditions: Synthesis and Pre-Clinical Evaluation of 18F-Labeled PSMA-Tracers for Prostate Cancer Imaging.

    Böhmer, Verena I / Szymanski, Wiktor / van den Berg, Keimpe-Oeds / Mulder, Chantal / Kobauri, Piermichele / Helbert, Hugo / van der Born, Dion / Reeβing, Friederike / Huizing, Anja / Klopstra, Marten / Samplonius, Douwe F / Antunes, Ines F / Sijbesma, Jürgen W A / Luurtsema, Gert / Helfrich, Wijnand / Visser, Ton J / Feringa, Ben L / Elsinga, Philip H

    Chemistry (Weinheim an der Bergstrasse, Germany)

    2021  Volume 27, Issue 23, Page(s) 6993

    Language English
    Publishing date 2021-03-24
    Publishing country Germany
    Document type Published Erratum
    ZDB-ID 1478547-X
    ISSN 1521-3765 ; 0947-6539
    ISSN (online) 1521-3765
    ISSN 0947-6539
    DOI 10.1002/chem.202100648
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article: Efficient synthesis of [18F]trifluoromethane and its application in the synthesis of PET tracers

    van der Born, Dion / Herscheid, J. (Koos) D. M / Orru, Romano V. A / Vugts, Danielle J

    Chemical communications. 2013 Apr. 16, v. 49, no. 38

    2013  

    Abstract: A new strategy towards [18F]trifluoromethyl-containing compounds is developed. [18F]trifluoromethane is synthesised in a fast and efficient manner and subsequently used in the reaction with aldehydes and ketones forming [18F]trifluoromethyl carbinols in ... ...

    Abstract A new strategy towards [18F]trifluoromethyl-containing compounds is developed. [18F]trifluoromethane is synthesised in a fast and efficient manner and subsequently used in the reaction with aldehydes and ketones forming [18F]trifluoromethyl carbinols in good yields.
    Keywords aldehydes ; chemical communication ; chemical reactions ; ketones ; tracer techniques
    Language English
    Dates of publication 2013-0416
    Size p. 4018-4020.
    Publishing place The Royal Society of Chemistry
    Document type Article
    ZDB-ID 1472881-3
    ISSN 1364-548X ; 1359-7345 ; 0009-241X
    ISSN (online) 1364-548X
    ISSN 1359-7345 ; 0009-241X
    DOI 10.1039/c3cc37833k
    Database NAL-Catalogue (AGRICOLA)

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  9. Article ; Online: Modular Medical Imaging Agents Based on Azide-Alkyne Huisgen Cycloadditions: Synthesis and Pre-Clinical Evaluation of

    Böhmer, Verena I / Szymanski, Wiktor / van den Berg, Keimpe-Oeds / Mulder, Chantal / Kobauri, Piermichele / Helbert, Hugo / van der Born, Dion / Reeβing, Friederike / Huizing, Anja / Klopstra, Marten / Samplonius, Douwe F / Antunes, Ines F / Sijbesma, Jürgen W A / Luurtsema, Gert / Helfrich, Wijnand / Visser, Ton J / Feringa, Ben L / Elsinga, Philip H

    Chemistry (Weinheim an der Bergstrasse, Germany)

    2020  Volume 26, Issue 47, Page(s) 10871–10881

    Abstract: Since the seminal contribution of Rolf Huisgen to develop the [3+2] cycloaddition of 1,3-dipolar compounds, its azide-alkyne variant has established itself as the key step in numerous organic syntheses and bioorthogonal processes in materials science and ...

    Abstract Since the seminal contribution of Rolf Huisgen to develop the [3+2] cycloaddition of 1,3-dipolar compounds, its azide-alkyne variant has established itself as the key step in numerous organic syntheses and bioorthogonal processes in materials science and chemical biology. In the present study, the copper(I)-catalyzed azide-alkyne cycloaddition was applied for the development of a modular molecular platform for medical imaging of the prostate-specific membrane antigen (PSMA), using positron emission tomography. This process is shown from molecular design, through synthesis automation and in vitro studies, all the way to pre-clinical in vivo evaluation of fluorine-18- labeled PSMA-targeting 'F-PSMA-MIC' radiotracers (t
    MeSH term(s) Alkynes/chemistry ; Azides/chemistry ; Cycloaddition Reaction ; Fluorine Radioisotopes/chemistry ; Humans ; Male ; Positron-Emission Tomography/methods ; Prostatic Neoplasms/diagnostic imaging ; Radioactive Tracers
    Chemical Substances Alkynes ; Azides ; Fluorine Radioisotopes ; Radioactive Tracers ; Fluorine-18 (GZ5I74KB8G)
    Language English
    Publishing date 2020-07-21
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 1478547-X
    ISSN 1521-3765 ; 0947-6539
    ISSN (online) 1521-3765
    ISSN 0947-6539
    DOI 10.1002/chem.202001795
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: A universal procedure for the [¹⁸F]trifluoromethylation of aryl iodides and aryl boronic acids with highly improved specific activity.

    van der Born, Dion / Sewing, Claudia / Herscheid, J Koos D M / Windhorst, Albert D / Orru, Romano V A / Vugts, Danielle J

    Angewandte Chemie (International ed. in English)

    2014  Volume 53, Issue 41, Page(s) 11046–11050

    Abstract: Herein, we describe a valuable method for the introduction of the [(18)F]CF3 group into arenes with highly improved specific activity by the reaction of [(18)F]trifluoromethane with aryl iodides or aryl boronic acids. This [(18)F]trifluoromethylation ... ...

    Abstract Herein, we describe a valuable method for the introduction of the [(18)F]CF3 group into arenes with highly improved specific activity by the reaction of [(18)F]trifluoromethane with aryl iodides or aryl boronic acids. This [(18)F]trifluoromethylation reaction is the first to be described in which the [(18)F]CF3 products are generated in actual trace amounts and can therefore effectively be used as PET tracers. The method shows broad scope with respect to possible aryl iodide and aryl boronic acid substrates, as well as good to excellent conversion. In particular, the [(18)F]trifluoromethylation of boronic acids was found to outperform [(18)F]trifluoromethylation reactions of halogenated aryl precursors with regard to conversion, reaction conditions, and kinetics.
    MeSH term(s) Boronic Acids/chemistry ; Chlorofluorocarbons, Methane/chemistry ; Fluorine Radioisotopes/chemistry ; Humans ; Iodides/chemistry ; Isotope Labeling ; Neoplasms/diagnosis ; Positron-Emission Tomography ; Radiopharmaceuticals/chemistry
    Chemical Substances Boronic Acids ; Chlorofluorocarbons, Methane ; Fluorine Radioisotopes ; Iodides ; Radiopharmaceuticals ; fluoroform (ZJ51L9A260)
    Language English
    Publishing date 2014-10-06
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.201406221
    Database MEDical Literature Analysis and Retrieval System OnLINE

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