Direct n.c.a. electrophilic radioiodination of tyrosine analogues; their in vivo stability and brain-uptake in mice
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2013, Bioorganic and Medicinal ChemistryCitation Excerpt :After extensive experimental trials with different radioiodination methods, we successfully radiolabeled rotenone with 125I and 123I using the direct non-carrier-added electrophilic radioiodination approach with iodogen in trifluoroacetic acid (TFA) solvent. The method was developed for radioiodination of less activated anisole (methoxy benzene) and O-methyl-tyrosine derivatives.31,32 The use of a homogeneous iodogen/TFA/water system allows the direct electrophilic radioiodination of anisole derivatives, which is almost impossible by the classical chloramine-T or iodogen method in aqueous solution.
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