Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Journal of Labelled Compounds and Radiopharmaceuticals

January 2010

Volume 53, Issue 1

Pages 1–52

  1. Review Articles

    1. Top of page
    2. Review Articles
    3. Research Articles
    4. Notes
    1. Preparation and biodistribution of [125I]Melphalan: a potential radioligand for diagnostic and therapeutic applications (pages 1–5)

      A. M. Amin, S. E. Soliman and H. A. El-Aziz

      Version of Record online: 25 NOV 2009 | DOI: 10.1002/jlcr.1698

      Thumbnail image of graphical abstract

      This paper addresses the development of a new radiopharmaceutical for cancer imaging and therapy. The optimization of the labeling conditions of thymidine analogue, melphalan, with 125I is described. High radiochemical yield 96.8 % was obtained by reacting 0.2 mg melphalan with 125I in the presence of choloramin-T as oxidizing agent in 0.5M phosphate buffer, pH 7, at 70°C for 15 minutes. Preliminary in-vivo study was done in non-tumor bearing mice. The results revealed that this new tracer, 125I-melphalan, has a high affinity to be localized in the tumor site for a long period which indicates the specificity of this tracer to the tumor cells. Copyright © 2009 John Wiley & Sons, Ltd.

  2. Research Articles

    1. Top of page
    2. Review Articles
    3. Research Articles
    4. Notes
    1. Cigarettes labeled with [11C]nicotine: formulation and administration for PET inhalation (pages 6–10)

      S. M. Apana and M. S. Berridge

      Version of Record online: 30 OCT 2009 | DOI: 10.1002/jlcr.1692

      Thumbnail image of graphical abstract

      Nicotine was used to radiolabel cigarettes, formulated for use in PET studies. Copyright © 2009 John Wiley & Sons, Ltd.

    2. An evaluation of paper chromatography for measuring the levels of radiochemical impurities in 99mTc Medronate Injection (pages 11–14)

      Alistair M. Millar, Lesley M. O'Brien, Lynn A. Beattie and Fiona Craig

      Version of Record online: 11 NOV 2009 | DOI: 10.1002/jlcr.1693

      Thumbnail image of graphical abstract

      The European Pharmacopoeia specifies Instant Thin-Layer Chromatography Silica Gel (ITLC-SG) as the stationary phase for measuring radiochemical impurities in 99mTc Medronate. The Pall Corporation has stopped manufacturing ITLC-SG. Five Whatman papers (1CHR, 31ET, 3MM, 4CHR and 54SFC) were evaluated as possible alternatives. The 54SFC is a suitable alternative to ITLC-SG for measuring radiochemical impurities in 99mTc Medronate. The sample spot should be wet when the paper strip is placed in the chromatography tank. Copyright © 2009 John Wiley & Sons, Ltd.

    3. Synthesis of labeled ambroxol and its major metabolites (pages 15–23)

      Bachir Latli, Matt Hrapchak, Heinz-Karl Switek, Daniel M. Retz, Dhileepkumar Krishnamurthy and Chris H. Senanayake

      Version of Record online: 9 NOV 2009 | DOI: 10.1002/jlcr.1694

      Thumbnail image of graphical abstract

      Carbon-14 labeled ambroxol with the radioactive atom(s) either on the benzylic carbon or uniformly in the cyclohexyl ring was synthesized. We also describe the preparation of deuterium labeled ambroxol, its deuterium labeled tetrahydroquinazoline metabolite (DHTQ), carbon-13 labeled 3,5-dibromoanthranilic acid metabolite (DBAA), as well as an unlabeled O-glucuronide conjugate. Copyright © 2009 John Wiley & Sons, Ltd.

    4. Use of perfluoro groups in nucleophilic 18F-fluorination (pages 24–30)

      Elisabeth Blom, Farhad Karimi and Bengt Långström

      Version of Record online: 25 NOV 2009 | DOI: 10.1002/jlcr.1695

      Thumbnail image of graphical abstract

      Perfluorous structures were applied as a part of a leaving group in labelling chemistry. [18F](Fluoromethyl)benzene was used as the model target compound. Several precursors containing perfluoroalkyl and perfluoroaryl sulfonate moieties were subjected to nucleophilic 18F-fluorination and the impact on the reactivity of the substitution reaction and its use in the purification by fluorous solid phase extraction (F-SPE) was explored. Copyright © 2009 John Wiley & Sons, Ltd.

    5. Influence of [2H]-labelled acetic acid as solvent in the synthesis of [2H]-labelled perhexiline (pages 31–35)

      Søren Christian Schou

      Version of Record online: 25 NOV 2009 | DOI: 10.1002/jlcr.1696

      Thumbnail image of graphical abstract

      A pyridine analogue of perhexiline was synthesized and used as the precursor for deuterium-labelled perhexiline via reduction using deuterium gas. Using PtO2 in acetic acid, a solvent effect was observed. High incorporation was observed using deuterium-labelled acetic acid e.g. acetic acid-OD or acetic acid-d4, but changing the solvent to acetic-d3 acid or acetic acid, lower incorporation was observed. High levels of deuterium incorporation was also seen when hydrogen gas was used in acetic acid-OD or acetic acid-d4. Copyright © 2009 John Wiley & Sons, Ltd.

    6. Chemical, radiochemical and biological studies of Sm and Ho complexes of H4dota analogues containing one methylphosphonic/phosphinic acid pendant arm (pages 36–43)

      Sara Lacerda, Fernanda Marques, Paula Campello, Lurdes Gano, Vojtěch Kubíček, Petr Hermann and Isabel Santos

      Version of Record online: 8 DEC 2009 | DOI: 10.1002/jlcr.1697

      Thumbnail image of graphical abstract

      Sm(III)/Ho(III) complexes of monomethylphosphonic/monomethylphosphinic acid analogs of H4dota were studied. The effect of phosphorus acid pendant arm functionalization on the complexation efficiency, labeling properties and on the biological profile of 153Sm/166Ho complexes was evaluated. To get a better insight on the radiochemical results, stability constants of the complexes with the lanthanide(III) ions were determined and speciation in solution under the labeling conditions was identified. Copyright © 2009 John Wiley & Sons, Ltd.

    7. A route to the γ-secretase inhibitor [2,3,4-3H]BMS299897 via an α-phenylselenide derivative (pages 44–46)

      Jonas Malmquist, Alexandra Bernlind and Peter Ström

      Version of Record online: 10 DEC 2009 | DOI: 10.1002/jlcr.1719

      Thumbnail image of graphical abstract

      A method for the preparation of [2,3,4-3H]-BMS299897 obtaining a specific activity of 1.6 TBq/mmol, has been developed. Copyright © 2009 John Wiley & Sons, Ltd.

  3. Notes

    1. Top of page
    2. Review Articles
    3. Research Articles
    4. Notes
    1. A facile and efficient synthesis of d6-labeled PU-H71, a purine-scaffold Hsp90 inhibitor (pages 47–49)

      Tony Taldone, Danuta Zatorska, Yanlong Kang and Gabriela Chiosis

      Version of Record online: 3 DEC 2009 | DOI: 10.1002/jlcr.1689

      Thumbnail image of graphical abstract

      PU-H71 is a purine-scaffold Hsp90 inhibitor currently undergoing late stage preclinical evaluation for the treatment of cancer. In this investigation, we present a simple method for the synthesis of d6-labeled PU-H71 for use as an internal standard to accurately quantitate the drug in biological matrices based on an LC-MS-MS method. PU-H71-d6 was synthesized in five steps using readily available 1,3-dibromopropane-d6 and is an important compound for the advancement of our clinical program. Copyright © 2009 John Wiley & Sons, Ltd.

    2. Lindlar catalyst mediated tritiation of a triazole substituted isoxazoline insecticide (pages 51–52)

      James J. Rauh, George P. Lahm, Thomas F. Pahutski, Giliyar V. Ullas and Crist N. Filer

      Version of Record online: 25 NOV 2009 | DOI: 10.1002/jlcr.1700

      Thumbnail image of graphical abstract

      Lindlar catalyst mediated reductive tritium dehalogenation of an aromatic bromo compound with other potentially reducible groups is reported. Copyright © 2009 John Wiley & Sons, Ltd.

SEARCH

SEARCH BY CITATION