2002
DOI: 10.1021/bc015568r
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Steps toward High Specific Activity Labeling of Biomolecules for Therapeutic Application:  Preparation of Precursor [188Re(H2O)3(CO)3]+ and Synthesis of Tailor-Made Bifunctional Ligand Systems

Abstract: Two kit preparations of the organometallic precursor [ 188 Re(H 2 O) 3 (CO) 3 ] + in aqueous media are presented. Method A uses gaseous carbon monoxide and amine borane (BH 3 ‚NH 3 ) as the reducing agent. In method B CO(g) is replaced by K 2 [H 3 BCO 2 ] that releases carbon monoxide during hydrolysis. Both procedures afford the desired precursor in yields >85% after 10 min at 60 °C. HPLC and TLC analyses revealed 7 ( 3% of unreacted 188 ReO 4and <5% of colloidal 188 ReO 2 . Solutions of up to 14 GBq/mL Re-18… Show more

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Cited by 184 publications
(157 citation statements)
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“…[19][20][21][22][23] The corresponding technetium and rhenium precursors [M(CO) 3 (H 2 O) 3 ] + 1 can be conveniently accessed by synthetic procedures, are water soluble, and the three aqua ligands are labile and can readily undergo ligand exchange. [24][25][26] The [M(CO) 3 ] + 1 core is chemically robust, and complexes are chemically inert because of the d 6 low-spin electronic configuration, thus maintaining their integrity under the most forcing conditions. Whereas 99m…”
Section: Introductionmentioning
confidence: 99%
“…[19][20][21][22][23] The corresponding technetium and rhenium precursors [M(CO) 3 (H 2 O) 3 ] + 1 can be conveniently accessed by synthetic procedures, are water soluble, and the three aqua ligands are labile and can readily undergo ligand exchange. [24][25][26] The [M(CO) 3 ] + 1 core is chemically robust, and complexes are chemically inert because of the d 6 low-spin electronic configuration, thus maintaining their integrity under the most forcing conditions. Whereas 99m…”
Section: Introductionmentioning
confidence: 99%
“…[30][31][32] This is interesting for therapeutic as well as diagnostic purposes as rhenium has two isotopes with favourable β-emitting properties ( 188 Re, t ½ = 16.9 h, E β = 2.1 MeV; 186 Re, t ½ = 3.78 d, E β = 1.07 MeV, E γ = 137 keV) and additionally, the Re(CO) 3 core resembles the diagnostically important 99m Tc(CO) 3 core. [18,[33][34][35][36][37][38] For the attachment of the ligands to e.g. a polymeric backbone, an additional functional group has to be present in the molecule.…”
Section: Introductionmentioning
confidence: 99%
“…Re-(CO) 3 -A7 [20]. In CAE analyses, intact A7 migrated to the 2-2.5 cm anode from the origin, which was determined by Ponceau S dye, and 186/188 Re-(CO) 3 -A7 also migrated to the 2-2.5 cm anode (Figure 1) showed a radiochemical purity of over 95%.…”
Section: Preparation Of 186/188mentioning
confidence: 99%