@article{52d8ab1f910c440bbc2222a0d799dc9f,
title = "A solid phase-assisted approach for the facile synthesis of a highly water-soluble zirconium-89 chelator for radiopharmaceutical development",
abstract = "Nuclear medicine has seen impressive growth in recent years. An important development in this field occurred through the application of new radionuclides, e.g., 89Zr (t1/2 = 78.4 h, β+ 0.396 MeV), the physical properties of which allow the use of antibodies as biological vectors for specific cancer targeting in combination with high resolution imaging by positron emission tomography (PET). The most commonly used chelator for 89Zr-based PET imaging is the hexadentate desferrioxamine (DFO) chelator. However, due to the instability of this complex, there has been a strong push towards the development of octadentate chelators. We report an ether derivative, oxoDFO∗, resembling the motif of DFO with four hydroxamic acid groups for the binding of the radiometal and four ether linkages to increase the water solubility. Very importantly, the synthesis of this chelator follows a solid phase-assisted approach allowing for the development of an attractive synthetic methodology and widening the scope for the access to DFO-like chelators in highly efficient synthetic sequences.",
author = "Manon Briand and Aulsebrook, {Margaret L.} and Mindt, {Thomas L.} and Gilles Gasser",
note = "Funding Information: This work was financially supported by the Swiss National Science Foundation (Professorships N° PP00P2_133568 and PP00P2_157545 to G. G. as well as Grant SNSF 205321_157216 to G. G. and T. L. M) and has received support under the program “Investissements d{\textquoteright}Avenir” launched by the French Government and implemented by the ANR with the reference ANR-10-IDEX-0001-02 PSL (G. G.). The authors thank Carla Gotzmann for the help rendered in the synthesis of one of the precursors. Funding Information: This work was financially supported by the Swiss National Science Foundation (Professorships N° PP00P2-133568 and PP00P2-157545 to G. G. as well as Grant SNSF 205321-157216 to G. G. and T. L. M) and has received support under the program {"}Investissements d'Avenir{"} launched by the French Government and implemented by the ANR with the reference ANR-10-IDEX-0001-02 PSL (G. G.). The authors thank Carla Gotzmann for the help rendered in the synthesis of one of the precursors. Publisher Copyright: {\textcopyright} 2017 The Royal Society of Chemistry.",
year = "2017",
month = dec,
day = "21",
doi = "10.1039/c7dt03639f",
language = "English",
volume = "46",
pages = "16387--16389",
journal = "Dalton Transactions",
issn = "1477-9226",
publisher = "The Royal Society of Chemistry",
number = "47",
}
