Reduction of no-carrier added [188Re04]-(ng range) in thf-[NBu4]C1 with BH3.thf under an atmosphere of CO yields [ 188ReC13(CO)3]2-and [ 188Re3(p-H)3(CO)12]; under similar conditions as with [188Re04]-, the first p-hydrido-bridged 99Tc hydrido carbonyl complex is prepared and structurally characterised.We have recently reported a simple one-pot synthesis of the useful MI precursor complexes [NEt4]2[MC13(C0)3] (M = Tc la, Re lb) starting directly from [NBu4][MO4] under ambient conditions. 1 Dissolution of 1 in water yields the corresponding air-stable 'aqua ion' [M(OH2)3(CO)3]+ (M = 99Tc 2a, Re 2b, 188Re 2c).2 Technetium-99m carbonyl complexes of appropriately derivatized ligands may find applications in nuclear medicine, as recently demonstrated by the imaging of brain receptors using a technetium(v) complex.3 2c can be used as a direct radiolabelling agent for proteins and applied in radioimmunotherapy.4 The synthetic conditions for the preparation of l a or lb, as depicted in Scheme 1, are almost identical. We found that the main product is [M2(p-C1)3(CO)& which can, by addition of [NEt4]C1, be quantitatively converted into l a and lb. However, adaptation of the synthetic conditions to trace amounts of [188Re04]-(37 MBq = 1 ng) revealed at least two products, as evidenced by TLC [Rf = 0.39 corresponds to 2a with one unknown species at R f = 0.69). The amount of the unknown species increased with the amount of BH3.thf. Consequently, the reduction of [Tc04]-was performed exclusively in the presence of BH3.thf, 1 atm of CO in thf and at room temperature. TLC experiments confirmed the compound
This study indicates a promising method for the treatment of superficial bladder cancer. Although the mean initial tumor uptake was high, effective therapy of bladder tumors will require an increased retention of the cytotoxic radionuclide in tumor tissue.
Tumor uptake and tumor to blood ratio, as well as serum clearance of the triconstruct are similar to those observed with intact iodinated anti-CEA antibodies. In the patient studied for 7 days the tumor residence time was favorable. Further improvements, however, need to be obtained before considering this approach for radioimmunotherapy.
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