Rigid H4OCTAPA derivatives as model chelators for the development of Bi(iii)-based radiopharmaceuticals†,10.1039/D2CC06876A

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Rigid H4OCTAPA derivatives as model chelators for the development of Bi(iii)-based radiopharmaceuticals†

Fátima Lucio-Martínez,David Esteban-Gómez,Laura Valencia,Anikó Fekete,Dezső Szikra,Gyula Tircsó,Carlos Platas-Iglesias

Chemical Communications Pub Date : 02/21/2023 00:00:00 , DOI:10.1039/D2CC06876A

Abstract

Octadentate ligands containing ethyl (H₄OCTAPA), cyclohexyl (H₄CHXOCTAPA) or cyclopentyl (H₄CpOCTAPA) spacers were assessed as chelators for Bi(III)-based radiopharmaceuticals. The H₄CHXOCTAPA chelator displays excellent properties, including ^205/206Bi-nuclide radiolabelling under mild conditions, excellent stability in serum and in the presence of competing cations or H₅DTPA. The poor performance of H₄CpOCTAPA appears to be related to the stereochemical activity of the Bi(III) lone pair.