Radiosynthesis and in vitro stability evaluation of various radioiodine-labelled beta-iodoalkylether prosthetic groups linked to model compounds

Nuclear Medicine and Biology
D D Rossouw, H H Coenen

Abstract

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.

Citations

Dec 20, 2005·Bioorganic & Medicinal Chemistry Letters·Martine FayolleAsha Parbhu Patel

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