Journal of Labelled Compounds and Radiopharmaceuticals

Cover image for Vol. 54 Issue 5

15 May 2011

Volume 54, Issue 5

Pages 229–288

  1. Research Articles

    1. Top of page
    2. Research Articles
    3. Abstracts
    1. Rapid synthesis of a 13C6-benzothiazolium salt from 13C6-aniline (pages 229–232)

      Chris V. Galliford, Kimberly Voronin, David Hesk, David Koharski and Paul McNamara

      Version of Record online: 25 MAR 2011 | DOI: 10.1002/jlcr.1854

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      13C6-labeled aniline was used as a starting material for the facile synthesis of benzothiazolium salt. Copyright © 2011 John Wiley & Sons, Ltd.

    2. Radiosynthesis of 1′-[18F]fluoroethyl-β-D-lactose ([18F]-FEL) for early detection of pancreatic carcinomas with PET (pages 233–238)

      Nashaat Turkman, Ashutosh Pal, William P. Tong, Juri G. Gelovani and Mian M. Alauddin

      Version of Record online: 25 MAR 2011 | DOI: 10.1002/jlcr.1855

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      We reported Et-[18F]FDL for PET imaging of small pancreatic carcinomas in mice. Synthesis of the precursor for Et-[18F]FDL involves 11 steps, which is quite lengthy. We report now radiosynthesis of another analog of lactose for PET. Two precursors were synthesized in two and three steps, respectively. Radiofluorination of these precursors produced an intermediate product, which was purified and hydrolyzed to obtain the final product. The newly synthesized analog may be suitable for PET imaging of early pancreatic carcinomas. Copyright © 2011 John Wiley & Sons, Ltd.

    3. Synthesis of the NK3 receptor antagonist AZD2624 in C-14-, H-3- and C-13-labeled forms (pages 239–246)

      Charles S. Elmore, Peter N. Dorff, Mark E. Powell, James E. Hall and Thomas R. Simpson

      Version of Record online: 17 FEB 2011 | DOI: 10.1002/jlcr.1858

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      The synthesis of two C-14 isotopomers of the NK3 receptor antagonist AZD2624 are reported from [14C]benzoic acid and [14C]isatin. The synthesis of [13C6]AZD2624 is reported from [13C6] aniline through the intermediacy of [13C6]isatin. The synthesis of [3H]AZD2624 is reported via the Pd-catalyzed tritio-dehalogenation of AZD2624. Copyright © 2011 John Wiley & Sons, Ltd.

    4. Synthesis of deuterium-labeled analogs of the lipid hydroperoxide-derived bifunctional electrophile 4-oxo-2(E)-nonenal (pages 247–251)

      Jasbir S. Arora, Tomoyuki Oe and Ian A. Blair

      Version of Record online: 17 FEB 2011 | DOI: 10.1002/jlcr.1860

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      An efficient one-step cost-effective method has been developed for the preparation of C-9 deuterium-labeled 4-oxo-2(E)-nonenal. In addition, a method for specific deuterium labeling of ONE at C-2, C-3 or both C-2 and C-3 has been developed. Copyright © 2011 John Wiley & Sons, Ltd.

    5. Preparation of technetium-99 m human albumin nanospheres for use in the measurement of reticuloendothelial clearance capacity (pages 252–255)

      Alistair M. Millar, Martin Bodingbauer, Lesley M. O'Brien, Lynn A. Beattie, Rodger Duffin and Stephen J. Wigmore

      Version of Record online: 17 FEB 2011 | DOI: 10.1002/jlcr.1861

      Aim: To prepare human albumin nanospheres (HAN) with a diameter similar to 99 mTc-Albumin Nanocolloid (ANC) and to investigate their stability. Conclusions: HAN with a diameter of approximately 4 nm were prepared successfully. The diameter of HAN does not change over 3 months or after mixing with 99 mTc-ANC. The particle size and labelling efficiency of 99 mTc-ANC are not affected by the addition of HAN. Copyright © 2011 John Wiley & Sons, Ltd.

    6. Radiosynthesis of tritium-labeled novel nitromethylene neonicotinoids compounds with NaB3H4 (pages 256–259)

      Chao Li, Xiao-Yong Xu, Ju-Ying Li, Qing-Fu Ye and Zhong Li

      Version of Record online: 19 FEB 2011 | DOI: 10.1002/jlcr.1862

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      Radiosynthesis of [3H2]-6-Cl-PMNI and [3H2]-Paichongding (* the label site). Copyright © 2011 John Wiley & Sons, Ltd.

    7. Synthesis of a [18F]fluoroethyltriazolylthymidine radiotracer from [18F]2-fluoroethyl azide and 5-ethynyl-2′-deoxyuridine (pages 260–266)

      U. Ackermann, G. O'Keefe, S.-T. Lee, A. Rigopoulos, G. Cartwright, J. I. Sachinidis, A. M. Scott and H. J. Tochon-Danguy

      Version of Record online: 17 FEB 2011 | DOI: 10.1002/jlcr.1863

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      The radiosynthesis of a fluoroethyltriazolylthymidine analog has been increased to 32.5 ± 2.5% by employing the copper(I)-catalyzed click chemistry reaction between 5-ethynyl-2-deoxyuridine (EDU) and [19/18F] 2-fluoroethyl azide. The tracer was found to be stable in human plasma and was subsequently evaluated in an A431 tumor model in four BALB/c nude mice. Dynamic and static image acquisition using the Mosaic small animal PET scanner showed uptake in those tumors, with an average tumor to muscle ratio of 1.9. Copyright © 2011 John Wiley & Sons, Ltd.

    8. Synthesis and characterization of radiolabeled 17β-estradiol conjugates (pages 267–271)

      Suman L. Shrestha, Xuelian Bai, David J. Smith, Heldur Hakk, Francis X. M. Casey, Gerald L. Larsen and G. Padmanabhan

      Version of Record online: 17 FEB 2011 | DOI: 10.1002/jlcr.1864

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      Two efficient methods for the syntheses of [14C] labeled 17β-estradiol conjugates are described. [14C]17β-estradiol-3-glucuronide was synthesized using an enzymatic approach, while a three-step chemical synthesis method was used for [14C]17β-estradiol-17-sulphate. Copyright © 2011 John Wiley & Sons, Ltd.

    9. Heck reaction and Stille coupling as the key steps in the synthesis of carbon-14-labeled gsk-3 inhibitor alsterpaullone (pages 272–277)

      Hans F. Roth, Min Li, John Jiang, Dorothy K. Dulan and Mark B. Brendan

      Version of Record online: 17 FEB 2011 | DOI: 10.1002/jlcr.1868

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      A multi-14C-labeled approach was adopted in synthesizing glycogen synthase kinase 3 (GSK-3) inhibitor Alsterpaullone as a probe for mood disorder investigation. The synthesis of [14C]Alsterpaullone was accomplished in separate routes from methyl-[1, 2-14C]-2-bromoacetate and [1, 2-14C]-2-bromoethanol, respectively. Labeled versions were combined on the basis of molar radioactivity giving a final product with a radiochemical purity of 99.0% and a specific activity of 54.0  mCi/mmol. Copyright © 2011 John Wiley & Sons, Ltd.

  2. Abstracts

    1. Top of page
    2. Research Articles
    3. Abstracts

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