Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 55 Issue 3

March 2012

Volume 55, Issue 3

Pages i–iv, 97–134

  1. Cover and Masthead

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

      Version of Record online: 9 MAR 2012 | DOI: 10.1002/jlcr.2912

  2. Research Articles

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Notes
    5. Abstracts
    1. Degradation of acetonitrile in eluent solutions for [18F]fluoride PET chemistry: impact on radiosynthesis of [18F]FACBC and [18F]FDG (pages 97–102)

      Anders Svadberg, Torild Wickstrøm and Ole Kristian Hjelstuen

      Version of Record online: 5 JAN 2012 | DOI: 10.1002/jlcr.1956

      Thumbnail image of graphical abstract

      We discovered that typical eluent solutions containing K222 and K2CO3 in aqueous acetonitrile, degraded relatively quickly upon storage. Acetonitrile hydrolyse into acetamide and ammonium acetate. Acetamide is a known carcinogen and acetate can serve as a competing nucleophile. These implications were investigated in the synthesis of [18F]FDG and [18F]FACBC. An alternative eluent with methanol instead of acetonitrile was developed.

    2. Development of 170Tm-DOTA-cetuximab for radioimmunotherapy (pages 103–107)

      Simindokht Shirvani-Arani, Ali Bahrami-Samani, Amir Reza Jalilian, Amirsaleh Shirvani-Arani and Mohammad Ghannadi-Maragheh

      Version of Record online: 28 FEB 2012 | DOI: 10.1002/jlcr.1957

      Thumbnail image of graphical abstract

      170Tm was produced by thermal neutron bombardment of natural Tm(NO3)3. Conjugated cetuximab was obtained by the addition of cetuximab pharmaceutical solution to a glass tube pre-coated with in situ prepared 1,4,7,10-tetraazacyclododecane-N,N,N,N-tetraacetic acid mono-(N-hydroxysuccinimidyl) ester. Conjugated cetuximab was labeled with 170Tm (radiochemical purity >99%, specific activity = 77–385 TBq/mmol). Biodistribution studies in wild-type rats for free Tm-170 and the radioimmunoconjugate were performed up to 72 h. The major organs of accumulation were shown to be the lung, liver, and spleen, respectively.

    3. Synthesis of [14C]boceprevir, [13C3]boceprevir, and [D9]boceprevir, a hepatitis C virus protease inhibitor (pages 108–114)

      Sumei Ren, Pernilla Royster, Carolee Lavey, David Hesk, Paul McNamara, David Koharski, Van Truong and Scott Borges

      Version of Record online: 18 JAN 2012 | DOI: 10.1002/jlcr.1960

      Thumbnail image of graphical abstract

      Boceprevir is an HCV NS3 protease inhibitor for HCV treatment. [14C]Boceprevir (SCH 503034, trade name Victrelis) was synthesized from K14CN in 11 steps with an overall yield of 16.4%. [13C3] Boceprevir was synthesized in 16 steps with a 2.5% overall yield. The carbon-13 in the molecule was distributed along the peptide chain. [D9]Boceprevir was synthesized from [D9]-t-butylamine in 4 steps with an overall yield of 69%.

    4. Recoil and conversion electron implications to be taken into account in the design of therapeutic radiopharmaceuticals utilising in vivo generators (pages 115–119)

      Jan Rijn Zeevaart, Zoltan Szucs, Sandor Takacs, Johann van Rooyen and David Jansen

      Version of Record online: 16 FEB 2012 | DOI: 10.1002/jlcr.2906

      Thumbnail image of graphical abstract

      The use of radionuclides as potential therapeutic radiopharmaceuticals is increasingly investigated. An important aspect is the delivery of the radionuclide to the target whereby the radionuclide is not lost from the chelating agent. For in vivo generators, it is important whether the daughter radionuclide stays inside the chelator after decay of the parent radionuclide. In our previous work, we showed that the classical recoil effect for β-decay only applies to decays with a Q value higher than 0.6 MeV. The loss of the daughter nuclide by a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) chelator was measured for the 166Dy/166Ho generator (Q = 0.486 MeV) and the 90Sr/90Y generator (Q = 0.546 MeV)—transition via the Auger process is absent. It was found that 72% of the daughter (166Ho) was liberated from the DOTA chelator, in contrast to our recoil calculations but corresponding to the ratio of transition of holmium atoms via the Auger process. For the β 90Sr/90Y generator, a 1% release from the DOTA chelator was recorded as compared with the estimated 10.2% from the β-continuum spectrum of 90Sr. The discrepancy between the experimental and theoretically calculated release can be explained by a correction of the chemical bond energy to 4.4 eV.

  3. Notes

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Notes
    5. Abstracts
    1. Fully automated synthesis and purification of 4-(2′-methoxyphenyl)-1-[2′-(N-2″-pyridinyl)-p-[18F]fluorobenzamido]ethylpiperazine (pages 120–124)

      Kazutaka Hayashi, Kenji Furutsuka, Takehito Ito, Masatoshi Muto, Hatsumi Aki, Toshimitsu Fukumura and Kazutoshi Suzuki

      Version of Record online: 5 JAN 2012 | DOI: 10.1002/jlcr.1958

      Thumbnail image of graphical abstract

      The nucleophilic [18F]fluorination was performed with 3 mg of the nitro-precursor in DMSO (0.4 mL) at 190 °C for 20 min, followed by preparative HPLC purification (column: COSMOSIL Cholester, Nacalai Tesque, Kyoto, Japan; mobile phase: MeCN/25 mm AcONH4/AcOH = 200/300/0.15; flow rate: 6.0 mL/min) to afford p-[18F]MPPF (retention time = 9.5 min). p-[18F]MPPF was obtained automatically, with a radiochemical yield of 38.6 ± 5.0%, a specific activity of 214.3 ± 21.1 GBq/µmol, and a radiochemical purity of >99% within a total synthesis time of about 55 min.

  4. Abstracts

    1. Top of page
    2. Cover and Masthead
    3. Research Articles
    4. Notes
    5. Abstracts
    1. Abstracts of the 20th International Isotope Society (UK group) Symposium: Synthesis & Applications of Labelled Compounds 2011 (pages 125–134)

      F. Aigbirhio, M. V. C. L. Appleyard, R. L. Arrowsmith, S. A. Baldwin, M. Bayrakdarian, N. P. Botting, L. D. Cantin, D. R. Carbery, M. A. Carroll, L. I. Dixon, P. N. Dorff, G. Ellames, C. S. Elmore, C. W. G. Fishwick, O. Foot, N. J. Geach, J. Gowdy, R. S. Grainger, T. Gregson, W. R. R. Harker, P. J. F. Henderson, J. R. Heys, S. W. Homans, Z. Hu, S. Jackson, J. Johnston, P. Johnson, A. Kalverda, C. Kay, S. L. Kitson, B. Lanoue, M. H. Levitt, Y. Li, W. J. S. Lockley, X Luo, P. Ma, D. A. Middleton, J. Newsome, B. Pandya, S. I. Pascu, S. G. Patching, M. K. Phillips-Jones, M. E. Powell, P. Riss, J. Simmons, T. M. Simpson, A. D. Smith, A. M. Thompson, L. Trembleau, R. Turtle, K. W. Watters and Q. Zhang

      Version of Record online: 6 MAR 2012 | DOI: 10.1002/jlcr.2907

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