Communication

High-Yielding, Two-Step 18F Labeling Strategy for 18F-PARP1 Inhibitors

  1. Dr. Edmund J. Keliher1,†,
  2. Dr. Thomas Reiner1,†,
  3. Anna Turetsky1,
  4. Dr. Scott A. Hilderbrand1,
  5. Prof. Dr. Ralph Weissleder1,2,*

Article first published online: 4 JAN 2011

DOI: 10.1002/cmdc.201000426

Issue

ChemMedChem

ChemMedChem

Volume 6, Issue 3, pages 424–427, March 7, 2011

Additional Information

How to Cite

Keliher, E. J., Reiner, T., Turetsky, A., Hilderbrand, S. A. and Weissleder, R. (2011), High-Yielding, Two-Step 18F Labeling Strategy for 18F-PARP1 Inhibitors. ChemMedChem, 6: 424–427. doi: 10.1002/cmdc.201000426

Author Information

  1. 1

    Center for Systems Biology Department, Massachusetts General Hospital, 185 Cambridge St., Boston, MA 02114 (USA), Fax: (+1) 617-643-6133

  2. 2

    Department of Systems Biology, Harvard Medical School, 200 Longwood Ave, Boston, MA 02115 (USA)

  1. †

    These authors contributed equally to this work.

*Center for Systems Biology Department, Massachusetts General Hospital, 185 Cambridge St., Boston, MA 02114 (USA), Fax: (+1) 617-643-6133

  1. †

    These authors contributed equally to this work.

Publication History

  1. Issue published online: 1 MAR 2011
  2. Article first published online: 4 JAN 2011
  3. Manuscript Revised: 1 DEC 2010
  4. Manuscript Received: 5 OCT 2010

Funded by

  • National Institutes of Health (NIH). Grant Numbers: CA86355, EB-010011, NIGMS T32 GM008313
  • German National Academy of Sciences Leopoldina

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Keywords:

  • 18F labeling;
  • cycloadditions;
  • PARP1;
  • PET imaging;
  • tetrazines
Thumbnail image of graphical abstract

Speedy and easy! An 18F-labeled PARP1 imaging agent, based on AZD2281, was prepared via an inverse electron demand Diels–Alder cycloaddition in high radiochemical yield for positron emission tomography (PET) imaging. This strain-promoted ‘bioorthogonal’ reaction is envisioned to be a widely applicable 18F-labeling strategy for repeat and on-demand synthesis of small molecules for PET imaging.

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