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

S. Poty; R. Membreno; J. M. Glaser; A. Ragupathi; W. W. Scholz; B. M. Zeglis; J. S. Lewis

doi:10.1039/C7CC09129J

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

S. Poty,

^a R. Membreno,^bc J. M. Glaser,^a A. Ragupathi,^a W. W. Scholz,^d B. M. Zeglis

*^abce and J. S. Lewis

*^aefg

Author affiliations

* Corresponding authors

^a Department of Radiology, Memorial Sloan Kettering Cancer Center, USA
E-mail: lewisj1@mskcc.org

^b Department of Chemistry, Hunter College of the City University of New York, USA
E-mail: bz102@hunter.cuny.edu

^c Ph.D. Program in Chemistry, Graduate Center of the City University of New York, USA

^d MabVax Therapeutics, USA

^e Weill Cornell Medical College, USA

^f Molecular Pharmacology Program, Memorial Sloan Kettering Cancer Center, USA

^g Radiochemistry and Molecular Imaging Probes Core, Memorial Sloan Kettering Cancer Center, USA

Abstract

The inverse electron-demand Diels–Alder reaction between tetrazine (Tz) and trans-cyclooctene (TCO) facilitates the efficient radiosynthesis of ²²⁵Ac-labelled radioimmunoconjugates in a two-step method, outperforming conventional approaches based on isothiocyanate couplings.

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Article information

DOI: https://doi.org/10.1039/C7CC09129J
Article type: Communication
Submitted: 27 Nov 2017
Accepted: 26 Jan 2018
First published: 26 Jan 2018

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Chem. Commun., 2018,54, 2599-2602

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

S. Poty, R. Membreno, J. M. Glaser, A. Ragupathi, W. W. Scholz, B. M. Zeglis and J. S. Lewis, Chem. Commun., 2018, 54, 2599 DOI: 10.1039/C7CC09129J

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