title: Synthesis of the first radiolabeled 188Re N-heterocyclic carbene complex and initial studies on its potential use in radiopharmaceutical applications.
abstract: A novel approach towards the synthesis of radiolabeled organometallic rhenium complexes is presented. We successfully synthesized and analyzed the first (188)Re-labeled N-heterocyclic biscarbene complex, trans-dioxobis(1,1'-methylene-bis(3,3'-diisopropylimidazolium-2-ylidene))(188)rhenium(V) hexafluorophosphate ((188)Re-4) via transmetalation using an air-stable and moisture-stable silver(I) biscarbene complex. In order to assess the viability of this complex as a potential lead structure for in vivo applications, the stability of the (188)Re-NHC complex was tested in physiologically relevant media. Ultimately, our studies illustrate that the complex we synthesized dissociates rapidly and is therefore unsuitable for use in radiopharmaceuticals. However, it is clear that the transmetalation approach we have developed is a rapid, robust, and mild method for the synthesis of new (188)Re-labeled carbene complexes.
authors.affiliation: Chair of Inorganic Chemistry/Molecular Catalysis, Department of Chemistry and Catalysis Research Center, Technische Universität München, Garching b. München, Germany.
authors.forename: Thomas
authors.initials: T
authors.lastname: Wagner
authors.forename: Brian M
authors.initials: BM
authors.lastname: Zeglis
authors.forename: Sam
authors.initials: S
authors.lastname: Groveman
authors.forename: Claudia
authors.initials: C
authors.lastname: Hille
authors.forename: Alexander
authors.initials: A
authors.lastname: Pöthig
authors.forename: Lynn C
authors.initials: LC
authors.lastname: Francesconi
authors.forename: Wolfgang A
authors.initials: WA
authors.lastname: Herrmann
authors.forename: Fritz E
authors.initials: FE
authors.lastname: Kühn
authors.forename: Thomas
authors.initials: T
authors.lastname: Reiner
mesh_terms: D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry; D008697:Methane / Q000031:analogs & derivatives* / Q000737:chemistry; D011868:Radioisotopes / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D012211:Rhenium / Q000737:chemistry*
chemical_list: D056831:Coordination Complexes; D007093:Imidazoles; D011868:Radioisotopes; D019275:Radiopharmaceuticals; C030011:carbene; D012211:Rhenium; D008697:Methane
keywords: 188Re carbene complex; N-heterocyclic carbene; radiopharmaceutical application; transmetalation