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A condition variation study for radioiodination via triazene intermediates
Authors:N I Foster  R Dannals  H D Burns  N D Heindel
Institution:(1) Center for Health Sciences, Lehigh University, 18015 Bethlehem, Pa, (USA);(2) Division of Nuclear Medicine, John Hopkins University, 21205 Baltimore, MD, (USA);(3) Center for Health Sciences, Lehigh University, 18015 Bethlehem, Pa
Abstract:Pyrrolidyl triazenes prepared by interception of the diazonium transient in the Sandmeyer reaction of amines can serve as useful intermediates in the iodination and radioiodination of aryl rings. Decomposition of such triazenes in the presence of iodide is acid-catalyzed and is sensitive to choice of solvent, acid, and triazene structure. A condition variation study by HPLC of four different solvent systems and two non-nucleophilic acids was carried out on the123I iodination of the triazenes of p-nitroaniline, p-anisidine and p-toluidine. This method has proven useful in radiolabeling of two pharmaceutical analogs which were not amenable to labeling through the classic Sandmeyer method.
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