Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 59 Issue 11

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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Young Scientists Award

Congratulations to the 2015 Young Scientists JLCR Awardees


From left to right
Renyuan Yu (Princeton University)
Iron catalysed hydrogen isotope exchange in drug molecules

Dr Marc Reid (University of Edinburgh)
Design and application of Iridium catalysts for C-H activation towards hydrogen Isotope exchange processes

Ken Lawrie

Miss Philippa Owens (University of Strathclyde)
Iridium catalysed hydrogen isotope exchange for the regioselective deuteration of N-heterocycles

Thomas Andersen (Aarhus University)
Efficient 11C-carbonylation of isolated aryl palladium complexes for PET:application to challenging radiopharmaceutical synthesis

Recently Published Articles

  1. Carbon-14 radiolabeling and tissue distribution evaluation of MMV390048

    Molahlehi S. Sonopo, Adushan Pillay, Kelly Chibale, Biljana Marjanovic-Painter, Cristina Donini and Jan R. Zeevaart

    Version of Record online: 20 SEP 2016 | DOI: 10.1002/jlcr.3445

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    The antimalarial compound MMV390048 ([14C]-11) was labeled with carbon-14 isotope via a 3-step synthesis. It was obtained in a 15.5% radiochemical overall yield from carbon-14 labeled methyl iodide with a radiochemical purity of >99%. After single oral administration of [14C]-11 to albino and pigmented rats its tissue distribution profile was studied. Tissue distribution results showed high local exposure in the GI tract and excretory organs but low exposure of all other tissues.

  2. You have full text access to this OnlineOpen article
    NMR analysis of t-butyl-catalyzed deuterium exchange at unactivated arene localities

    Douglas E. Stack and Rachel Eastman

    Version of Record online: 19 SEP 2016 | DOI: 10.1002/jlcr.3440

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    The exchange of the unactivated proton at C1 in estrone occurs in the presence of t-butyl alcohol and a 50:50 mixture of CF3CO2D : D2O; no exchange at C1 occurs in the absence of t-butyl alcohol. Nuclear magnetic resonance analysis of the reaction using 2-t-butylestrone, or a reaction mixture of estrone and t-butyl alcohol, displays a mechanism that involves reversible addition/elimination of the t-butyl group. Selective back exchange of the activated protons at C2 and C4 can produced estrone-1-d regioselectively.

  3. Synthesis of ceramides NS and NP with perdeuterated and specifically ω deuterated N-acyl residues

    Stefan Sonnenberger, Stefan Lange, Andreas Langner, Reinhard H.H. Neubert and Bodo Dobner

    Version of Record online: 16 SEP 2016 | DOI: 10.1002/jlcr.3443

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    Six ceramides [NS] and six ceramides [NP] with perdeuterated and specifically deuterated fatty acids in the ω position were synthesized. For the synthesis of the perdeuterated fatty acid literature method was used, while the specifically deuterated acids were prepared for the first time by a copper-catalyzed Grignard coupling of two suitably functionalized bromides. For the coupling of the acids with the sphingoid bases, PyBOP® was successfully used as activator and the corresponding ceramides could be isolated in high yields.

  4. Radioiodination and biological evaluation of candesartan as a tracer for cardiovascular disorder detection

    M.H. Sanad, Kh.M. Sallam, F.A. Marzook and S.M. Abd-Elhaliem

    Version of Record online: 16 SEP 2016 | DOI: 10.1002/jlcr.3435

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    Candesartan is angiotensin II receptor blocker (ARB) was labeled with iodine (125) in the presence of 75 μg of candesartan, 50 μg of Ch-T, at pH 8, at room temperature and 15 minutes reaction time. With high radiochemical yield, high purity and in vivo / in vitro stability. That accumulated in heart with high ratio, make it a tracer for cardiovascular disorder detection.

  5. The syntheses of isotopically labelled CB-1 antagonists for the treatment of obesity

    Scott B. Tran, Brad D. Maxwell, Richard Burrell and Samuel J. Bonacorsi Jr.

    Version of Record online: 14 SEP 2016 | DOI: 10.1002/jlcr.3433

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    BMS-725519, BMS-811064 and BMS-812204 are potent and selective central cannabinoid receptor antagonists that have been investigated for the treatment of human obesity. To further understand their biotransformation profiles, radiolabelled and stable-labelled products were required. This paper describes the utility of [14C]1,1-carbonyldiimidazole as a radiolabelling reagent for the syntheses of carbonyl-labelled [14C]BMS-725519, [14C]BMS-811064 and [14C]BMS-812204. The syntheses of stable-labelled [13C6]BMS-725519 and [13CD313CD2]BMS-812204 synthesized from of [13C6]4-chloroacetophenone and [13CD313CD2]iodoethane, respectively, are also described.