Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 55 Issue 14

December 2012

Volume 55, Issue 14

Pages i–iv, 477–506

  1. Cover and Masthead

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Short Notes
    5. Compound Index
    1. Editorial Board (pages i–iv)

      Article first published online: 21 DEC 2012 | DOI: 10.1002/jlcr.3014

  2. Research Articles

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Short Notes
    5. Compound Index
    1. Combinatorial synthesis of labelled drugs and PET tracers: synthesis of a focused library of 11C-carbonyl-labelled acrylamides as potential biomarkers of EGFR expression (pages 477–483)

      Ola Åberg and Bengt Långström

      Article first published online: 14 NOV 2012 | DOI: 10.1002/jlcr.2981

      Thumbnail image of graphical abstract

      We are presenting a combinatorial chemistry approach for radiosynthesis of 11C-labelled compounds for positron emission tomography. Specifically, we have utilised the three-component aminocarbonylation reaction, [11C]carbon monoxide, vinyl iodides and anilines in a palladium-mediated reaction, to form labelled acrylamides. In this work, the labelled compounds were designed to target the epidermal growth factor, a well-known target for cancer therapy and imaging.

    2. Pharmacological characterization of 18F-labeled vorozole analogs (pages 484–490)

      Håkan Hall, Kayo Takahashi, Maria Erlandsson, Sergio Estrada, Pasha Razifar, Elisabeth Bergström and Bengt Långström

      Article first published online: 20 NOV 2012 | DOI: 10.1002/jlcr.2982

      Thumbnail image of graphical abstract

      Two 18F-labeled analogs of vorozole ([18F]FVOZ and [18F]FVOO) have been evaluated using in vitro binding and in vivo distribution studies in the rat and primate. Ex vivo and in vitro autoradiography of the rat brain showed specific binding of both ligands mainly in the amygdala, and positron emission tomography (PET) studies with [18F]FVOZ in the Rhesus monkey showed specific binding in the amygdala. This suggests that [18F]FVOZ might be a suitable tracer for the study of aromatase in vivo in human PET studies.

    3. Rapid, one-step, high yielding 18F-labeling of an aryltrifluoroborate bioconjugate by isotope exchange at very high specific activity (pages 491–496)

      Zhibo Liu, Ying Li, Jerome Lozada, Jinhe Pan, Kuo-Shyan Lin, Paul Schaffer and David M. Perrin

      Article first published online: 21 DEC 2012 | DOI: 10.1002/jlcr.2990

      Thumbnail image of graphical abstract

      The specific activity of most 18F-radiotracers is limited to ~6 Ci/μmol while labeling is often cumbersome due fluoride's lack of reactivity in water. With 800 mCi, an aryltrifluoroborate is 18F-labeled by isotope exchange at 30-40° C, buffered pH 2-3 in yields of 50% at specific activities of ~15 Ci/μmol in 10-15 minutes. To measure such high specific activity we took advantage of a pendant Rhodamine which now provides for 18F-labeled fluorophores at extraordinarily high specific activity in one step.

  3. Short Notes

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Short Notes
    5. Compound Index
    1. The synthesis of [carboxamido-14C]SAR240550, [carboxamido-14C]Iniparib, via monocarboxylation of 1,4-diiodobenzene (pages 497–498)

      Thomas J. Gregson, Andrew D. Kohler and Daniel W. Spurr

      Article first published online: 27 NOV 2012 | DOI: 10.1002/jlcr.2983

      Thumbnail image of graphical abstract

      The simple, yet previously not reported, monocarboxylation of 1,4-diodobenzene via lithiation was demonstrated to be an efficient method for the synthesis of [carboxyl-14C]-4-iodobenzoic acid. This preparation was then used in the synthesis of [carboxamido-14C]Iniparib for ADME (absorption, distribution, metabolism and elimination) studies.

    2. Carbon-14 labeling of hydrochlorothiazide via [14C]formaldehyde production from [14C]carbon dioxide at ambient temperature (pages 499–500)

      Johan Sandell

      Article first published online: 4 DEC 2012 | DOI: 10.1002/jlcr.2984

      Thumbnail image of graphical abstract

      A synthesis of [14C]formaldehyde by reducing 14CO2 at ambient temperature with Schwartz's reagent is described. The [14C]formaldehyde has been applied in the radiosynthesis of high specific activity (2.1 GBq/mmol) [14C]hydrochlorothiazide via cyclization of 4-amino-5-chloro-1,3-benzenedisulfonamide.

  4. Compound Index

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Short Notes
    5. Compound Index

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