Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 60 Issue 1

Early View (Online Version of Record published before inclusion in an issue)

Editors-in-Chief: R F Dannals and K M W Lawrie

Impact Factor: 1.532

ISI Journal Citation Reports © Ranking: 2015: 42/59 (Chemistry Medicinal); 47/75 (Chemistry Analytical); 62/77 (BIOCHEMICAL RESEARCH METHODS)

Online ISSN: 1099-1344

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  1. 1 - 5
  1. REVIEWS

    1. Tritium-labelled alkaloids: Synthesis and applications

      Crist N. Filer

      Version of Record online: 10 JAN 2017 | DOI: 10.1002/jlcr.3480

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      This review discusses the synthetic methods used to tritiate nonmorphinan alkaloids as well as their applications.

  2. RESEARCH ARTICLES

    1. The synthesis of a tritium, carbon-14, and stable isotope-labeled cathepsin C inhibitors

      Paul Allen, Ryan A. Bragg, Moya Caffrey, Cecilia Ericsson, Michael J. Hickey, Lee P. Kingston and Charles S. Elmore

      Version of Record online: 21 DEC 2016 | DOI: 10.1002/jlcr.3483

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      As part of a medicinal chemistry program aimed at developing a highly potent and selective cathepsin C inhibitor, tritium, carbon-14, and stable isotope-labeled materials were required. The synthesis of tritium-labeled methanesulfonate 5 was achieved via catalytic tritiolysis of a chloro precursor, albeit at a low radiochemical purity of 67%. Tritium-labeled AZD5248 was prepared via a 3-stage synthesis, utilizing amide-directed hydrogen isotope exchange. Carbon-14 and stable isotope-labeled AZD5248 were successfully prepared through modifications of the medicinal chemistry synthetic route, enabling the use of available labeled intermediates.

  3. SHORT NOTES

    1. Synthesis of carbon-13 labeled oxalates exhibiting extended nuclear singlet state lifetimes

      Lynda J. Brown, Giuseppe Pileio, Malcolm H. Levitt and Richard C.D. Brown

      Version of Record online: 19 DEC 2016 | DOI: 10.1002/jlcr.3479

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      Unsymmetrical perdeuterated doubly 13C-labeled oxalates exhibit extended lifetimes in the nuclear singlet state. Synthesis of 1,2 13C2 oxalates from commercially available precursors is described, facilitating the preparation of unsymmetrical oxalates in a controlled manner.

  4. RESEARCH ARTICLES

    1. Synthesis and preliminary biological evaluation of a 99mTc-chlorambucil derivative as a potential tumor imaging agent

      Jianguo Lin, Ling Qiu, Gaochao Lv, Ke Li, Wei Wang, Guiqing Liu, Xueyu Zhao and Shanshan Wang

      Version of Record online: 7 DEC 2016 | DOI: 10.1002/jlcr.3481

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      A new analog of the anticancer drug chlorambucil was synthesized after covalent bonding with the dipicolylamine chelating group. The resulting ligand DPA-CLB was successfully radiolabeled with 99mTc(CO)3(H2O)3 in high yield, and it is very stable in vitro and in vivo. The radiotracer has the property of favorable tumor uptake and retention, fast clearance from background and good T/NT ratios, suggesting it has potential as a tumor imaging agent for breast cancer.

    2. Synthesis of C-14 radiolabeled glucagon receptor antagonist and its use in a human mass balance study

      Boris A. Czeskis and Darlene K. Satonin

      Version of Record online: 1 DEC 2016 | DOI: 10.1002/jlcr.3477

      Thumbnail image of graphical abstract

      The synthesis of the radiolabeled glucagon receptor antagonist 1-[14C] was accomplished based on decarboxylative iodination of acid 2 followed by “reattachment” of 14C carboxylic function to form 2-[14C]. Coupling with β-alanine fragment completed the synthesis of the target molecule. The resulting compound was utilized in a mass balance and metabolism study.

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