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Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking

Journal article
Authors C. Denk
M. Wilkovitsch
Emma Aneheim
M. M. Herth
H. Jensen
Sture Lindegren
H. Mikula
Published in ChemPlusChem
Volume 84
Issue 7
Pages 775-778
ISSN 2192-6506
Publication year 2019
Published at Institute of Clinical Sciences, Department of Radiation Physics
Pages 775-778
Language en
Keywords bioorthogonal chemistry, click chemistry, multicomponent reactions, radiochemistry, radiolabeling
Subject categories Radiology, Nuclear Medicine and Medical Imaging, Analytical Chemistry


In the past decade, several developments have expanded the chemical toolbox for astatination and the preparation of 211 At-labeled radiopharmaceuticals. However, there is still a need for advanced methods for the synthesis of astatinated (bio)molecules to address challenges such as limited in vivo stability. Herein, we report the development of multifunctional 211 At-labeled reagents that can be prepared by applying a modular and versatile click approach for rapid assembly. The introduction of tetrazines as bioorthogonal tags enables rapid radiolabeling and radio-crosslinking, which is demonstrated by steric shielding of 211 At to significantly increase label stability in human blood plasma. © 2019 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.

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