Skip to main content
SpringerLink
Log in

Synthesis and labeling of 5'-O-(4,4'-dimethoxytrityl)-2,3'-anhydr othymidine for [18F]FLT preparation

  • Published:
Journal of Radioanalytical and Nuclear Chemistry Aims and scope Submit manuscript

Abstract

For in vivo measurement of DNA synthesis in the patient"s tumour 3"-[18F]fluoro-3"-deoxythymidine (FLT) has been shown to be very promising. As a new labeling precursor 5"-O-(4,4"-dimethoxytrityl)-2,3"-anhydrothymidine (DMTThy) was chosen and an organic synthesis was developed including NMR and MS data for characterisation. The 18F-labeling of DMTThy can be performed within 30 minutes in radiochemical yields of almost 20% when using polar solvents such as DMF or DMSO and a temperature of 160 °C. Hydrolysis is completed with 1N HCl at 50 °C within 10 minutes without losses.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. D. CHRISTMAN, E. J. CRAWFORD, M. FRIEDKIN, A. P. WOLF, Proc. Nat. Acad. Sci. USA, 69 (1972) 988.

    Google Scholar 

  2. T. VANDER BORGHT, D. LABAR, S. PAUWELS, L. LAMBOTTE, Appl. Radiation Isotopes, 42 (1991) 103.

    Google Scholar 

  3. P. S. CONTI, J. HILTON, D. F. WONG, M. M. ALAUDDIN, R. F. DANNALS, H. T. RAVERT, A. A. WILSON, J. H. ANDERSON, Nucl. Med. Biol., 21 (1994) 1045.

    Google Scholar 

  4. J. R. GRIERSON, A. F. SHIELDS, J. Labelled Comp. Radiopharm., 42 (1999) S525.

    Google Scholar 

  5. J. R. GRIERSON, A. F. SHIELDS, J. Nucl. Med., 40 (1999) 83P.

    Google Scholar 

  6. J. R. GRIERSON, A. F. SHIELDS, J. F. EARY, J. Labelled Comp. Radiopharm., 40 (1997) 60.

    Google Scholar 

  7. X. B. KONG, Q. Y. ZHU, P. M. VIDAL, K. A. WATANABE, B. POLSKY, D. ARMSTRONG, M. OSTRANDER, S. A. LANG Jr, E. MUCHMORE, T. C. CHOU, Antimicrob. Agents Chemother., 36 (1992) 808.

    Google Scholar 

  8. A. F. SHIELDS, J. R. GRIERSON, B. M. DOHMEN, H. J. MACHULLA, J. C. STAYANOFF, J. M. LAWHORN-CREWS, J. E. OBRADOVICH, O. MUZIK, T. J. MANGNER, Nature Medicine, 4 (1998) 1334.

    Google Scholar 

  9. H. J. MACHULLA, A. BLOCHER, M. KUNTZSCH, M. PIERT, R. WEI, J. R. GRIERSON, J. Radioanal. Nucl. Chem., 243 (2000) 843.

    Google Scholar 

  10. H. SIEGMUND, W. PFLEIDERER, Helv. Chim. Acta, 79 (1996) 426.

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Sektion Radiopharmazie, PET-Zentrum, Universitätsklinikum Tübingen, Röntgenweg 15, 72076, Tübingen, Germany

    A. Blocher, M. Kuntzsch, R. Wei & H.-J. Machulla

Authors
  1. A. Blocher
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. M. Kuntzsch
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. R. Wei
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. H.-J. Machulla
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Blocher, A., Kuntzsch, M., Wei, R. et al. Synthesis and labeling of 5'-O-(4,4'-dimethoxytrityl)-2,3'-anhydr othymidine for [18F]FLT preparation. Journal of Radioanalytical and Nuclear Chemistry 251, 55–58 (2002). https://doi.org/10.1023/A:1015042227131

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1023/A:1015042227131

Keywords

Search

Navigation