4.7 Article

The inverse electron-demand Diels-Alder reaction as a new methodology for the synthesis of 225Ac-labelled radioimmunoconjugates

Journal

CHEMICAL COMMUNICATIONS
Volume 54, Issue 21, Pages 2599-2602

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c7cc09129j

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Funding

  1. NIH [P30 CA08748]
  2. National Institutes of Health [R00 CA1440138]
  3. Thompson grant
  4. Francois Wallace Monahan Fellowship from the JLM Benevolent Fund

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The inverse electron-demand Diels-Alder reaction between tetra-zine (Tz) and trans-cyclooctene (TCO) facilitates the efficient radio-synthesis of Ac-225-labelled radioimmunoconjugates in a two-step method, outperforming conventional approaches based on isothio-cyanate couplings.

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