Expedient multi-step synthesis of organometallic complexes of Tc and Re in high effective specific activity. A new platform for the production of molecular imaging and therapy agents

Inorganic Chemistry
Patrick W CauseyJohn F Valliant

Abstract

For over thirty years, instant labeling kits which involve no purification steps have been the only method used to prepare (99m)Tc radiopharmaceuticals for clinical studies. To address the limitations imposed by instant kits, which is hindering the development of molecularly targeted Tc- and Re-based imaging and therapy agents, a new strategy for the rapid multistep synthesis and purification of organometallic technetium-based molecular probes and corresponding rhenium-based therapeutic analogues was developed. Beginning with MO4(-) (M = (99m)Tc, (186/188)Re), the carbonyl precursor [M(CO)3(H2O)3](+) was synthesized in 3 min in quantitative yield in a microwave reactor. A dipicolyl ligand was added and the chelate complex was formed in high yield in 2 min using microwave heating at 150 degrees C. This was followed by a new purification strategy to remove unlabeled ligand which entailed using a copper resin/C18 solid phase extraction protocol giving the desired product in greater than 78% decay corrected yield (dcy). Conversion to the corresponding succinimidyl active ester was achieved following a 5 min microwave irradiation at 120 degrees C and C18 solid phase extraction purification in 60% dcy. A series of amides were prepare...Continue Reading

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Citations

Jul 12, 2011·Nuclear Medicine and Biology·Neva LazarovaJohn F Valliant
Apr 12, 2014·Chembiochem : a European Journal of Chemical Biology·Ali BarandovPeter H Seeberger
Mar 14, 2014·Chemical Communications : Chem Comm·Henrik BrabandRoger Alberto
Dec 18, 2014·Dalton Transactions : an International Journal of Inorganic Chemistry·David J HaynePaul S Donnelly
Oct 31, 2013·Dalton Transactions : an International Journal of Inorganic Chemistry·Daniela MaggioniAlessandro Lascialfari
Nov 17, 2009·Biomacromolecules·Daniela DonghiRoberta Cavalli
Mar 20, 2010·Journal of Medicinal Chemistry·Chitra SundararajanJohn F Valliant
May 7, 2019·Chemical Reviews·Audrey BeillardFrédéric Lamaty

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