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Expeditious synthesis of ‘P’-protected macrocycles en route to lanthanide chelate metal complexes |
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| Authors: | H Charles Manning Mingfeng Bai Rafal Lisiak Darryl J Bornhop |
| Institution: | a Vanderbilt University Institute of Imaging Science, Nashville, TN 37235, USA b Department of Chemistry, Vanderbilt University, 7300 Stevenson Center, Nashville, TN 37235, USA c Department of Chemistry, Wroclaw University of Technology, Poland d Vanderbilt Institute for Chemical Biology, Nashville, TN 37235, USA |
| Abstract: | Phosphonic acid appended tetraazacyclododecane (cyclen)-based macrocycles are attractive metal-ion chelators for diagnostic imaging and therapeutic delivery. Here, we report a novel P-protected methodology that facilitates the rapid synthesis and purification of targeted phosphonic acid bearing macrocycles. Purification of these intermediates is facile, and deprotection using neat TFA is rapid, yet mild enough to preserve the integrity of delicate peptides and/or targeting moieties. |
| Keywords: | Lanthanide chelate MRI Phosphonate |
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