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Stoichiometric Leverage: Rapid 18F-Aryltrifluoroborate Radiosynthesis at High Specific Activity for Click Conjugation†

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  • †

    This work was supported by grants from the Canadian Cancer Society (20071), NSERC, and the CIHR. We thank Drs. Hua Yang and Qing Miao for labeling assistance.

Abstract

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Raising the 18F3-BAr: Specific activities of most 18F-labeled radiotracers fall below 2 Ci μmol−1, yet 18F-aryltrifluoroborate synthesis affords specific activities as high as 15 Ci μmol−1. This has been confirmed by using click chemistry to link an [18F]-ArBF3− to rhodamine and thereby demonstrating a rapid and generalizable one-pot method for preparing a fluorescent tracer with about 10-fold higher specific activity than usual.

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DOI

10.1002/anie.201208551

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Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim

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Keywords

  • bioconjugation;
  • click chemistry;
  • fluorine;
  • radiochemistry;
  • radiolabeling

Publication History

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  • Version of record online:
  • Manuscript Received:

Funded by

  • Canadian Cancer Society. Grant Number: 20071
  • NSERC
  • CIHR

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