Radiosynthesis and in vitro stability evaluation of various radioiodine-labelled beta-iodoalkylether prosthetic groups linked to model compounds.
A systematic comparative investigation into the in vitro radiochemical stabilities of model compounds containing radioiodinated beta-iodoethoxyl units and derivatives thereof, as well as those of similar compounds lacking a beta-oxygen to serve as control references, was undertaken. The radioiodinations were carried out in fair to modest yields by means of substitution of a tosyl group by iodide. Stability evaluations were carried out by incubating the labeled compounds in human blood serum at 37 degrees C and measuring free radioiodide by means of radio-HPLC and radio-TLC. The compounds containing beta-iodoethoxyl units displayed much superior stabilities than those without, while the presence of small alkyl or aryl groups in such a unit rendered an additional degree of stability to the carbon-iodine bond, especially over a long period.
Rossouw
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Institut für Nuklearchemie, Forschungszentrum Jülich GmbH, 52425 Jülich, Germany. niel@tlabs.ac.za
Coenen
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D002851:Chromatography, High Pressure Liquid; D004355:Drug Stability; D006847:Hydrocarbons, Iodinated / Q000138:chemical synthesis* / Q000737:chemistry; D007457:Iodine Radioisotopes / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry
D006847:Hydrocarbons, Iodinated; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals