Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 59 Issue 6

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

Impact Factor: 1.273

ISI Journal Citation Reports © Ranking: 2014: 45/59 (Chemistry Medicinal); 54/74 (Chemistry Analytical); 67/79 (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. Synthesis of the derivatives of 6-amino-uracil labelled with 14C

    Tomáš Elbert, Petr Hezký and Petr Jansa

    Version of Record online: 19 MAY 2016 | DOI: 10.1002/jlcr.3405

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    The 6-amino-5-nitroso-[6-14C]uracil (1) and 5-acetyl-6-amino-1,3-dimethyl-[6-14C]uracil (2) were prepared from common precursor – [cyano-14C]cyanoacetic acid. Several ACS reagents had to be repurified to achieve successful synthesis of 14C-labelled compounds on tenth of milligrams scale. It is shown that specific activity assay can be made from standard 13C NMR spectra avoiding the need to perform lengthier inverse gated 13C NMR experiments.

  2. Synthesis of enantiomerically pure [14C]-labelled morpholine derivatives for a class of trace amine-associate receptor 1 agonists

    Martin R. Edelmann, Thomas Hartung, René Trussardi, Hans Iding, Guido Galley, Philippe Pflieger and Roger D. Norcross

    Version of Record online: 15 MAY 2016 | DOI: 10.1002/jlcr.3403

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    An efficient synthesis for a class of carbon-14 labelled trace amine-associate receptor 1 agonists is described starting from [14C]-potassium cyanide. The 14-step asymmetric synthesis includes an enzymatic reduction using an alcohol dehydrogenase (ADH).

  3. [14C]-AZD1152 drug substance manufacture: challenges of an IV-infusion dosed human mass balance study in patients (pages 250–254)

    Nick Bushby, Julie Bergin and John Harding

    Version of Record online: 12 MAY 2016 | DOI: 10.1002/jlcr.3376

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    [14C]AZD1152 (barasertib) drug substance was prepared in order to support a hADME study that was to be dosed as an intravenous (IV) infusion to acute myeloid leukemia (AML) patients. A method was developed to purify the [14C]AZD1152 to a GMP-like standard at high specific activity to provide several batches of the [14C]AZD1152 drug substance.

  4. The syntheses of [14C]BMS-823778 for use in a human ADME clinical study and of [13CD313CD2]BMT-094817, a stable-isotope labeled standard of a newly detected human metabolite (pages 255–259)

    Brad D. Maxwell, Scott B. Tran, Michael Lago, Jun Li and Samuel J. Bonacorsi Jr.

    Version of Record online: 12 MAY 2016 | DOI: 10.1002/jlcr.3383

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    To support the development of BMS-823778 as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 for type 2 diabetes, the synthesis of [14C]BMS-823778 for use in a human adsorption, distribution, metabolism, and excretion (ADME) study was required. One result of the ADME study was the detection of a new human metabolite, BMT-094817. [13CD313CD2]BMT-094817 was then prepared for use as a liquid chromatography/mass spectrometry standard.

  5. The synthesis of [14C]AZD5122. Incorporation of an IV 14C-microtracer dose into a first in human study to determine the absolute oral bioavailability of AZD5122 (pages 245–249)

    Michael J. Hickey, Paul H. Allen, Lee P. Kingston and David J. Wilkinson

    Version of Record online: 12 MAY 2016 | DOI: 10.1002/jlcr.3385

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    In support of a medicinal chemistry programme aimed at developing antagonists of the CXCR2 receptor, the synthesis carbon-14 labelled AZD5122 from [14C]thiourea is described. [14C]AZD5122 was used in an IV microtracer study to gain a better understanding of the human pharmacokinetic profile.