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

Authors

  • Dr. Edmund J. Keliher,

    1. Center for Systems Biology Department, Massachusetts General Hospital, 185 Cambridge St., Boston, MA 02114 (USA), Fax: (+1) 617-643-6133
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    • These authors contributed equally to this work.

  • Dr. Thomas Reiner,

    1. Center for Systems Biology Department, Massachusetts General Hospital, 185 Cambridge St., Boston, MA 02114 (USA), Fax: (+1) 617-643-6133
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    • These authors contributed equally to this work.

  • Anna Turetsky,

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

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

    Corresponding author
    1. Center for Systems Biology Department, Massachusetts General Hospital, 185 Cambridge St., Boston, MA 02114 (USA), Fax: (+1) 617-643-6133
    2. Department of Systems Biology, Harvard Medical School, 200 Longwood Ave, Boston, MA 02115 (USA)
    • Center for Systems Biology Department, Massachusetts General Hospital, 185 Cambridge St., Boston, MA 02114 (USA), Fax: (+1) 617-643-6133

    Search for more papers by this author

Abstract

original image

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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