Redioiodinated Phenoxyacetic Acid Derivatives as Potential Brain Imaging Agents. I. : Effcient Synthesis via Trimethylsilyl Intermediates

Abstract

The usefulness of radioiodination via demetallation of aryltrimethylsilanes was demonstrated. The radioiodination reaction was found to be very rapid and the regiospecific incorporation of radioiodine could be carried out with high radiochemical yields and high radiospecific activity. ¹²⁵I-Labeled dimethylaminoethyl iodophenoxyacetate derivatives (5a-e), dimethylaminoethyl iodophenoxyacetamide derivatives (7a-c), iodophenoxyethyl ethylenediamine derivatives (9, 14) and an iodophenoxyethylpiperazine derivative (18) were efficiently synthesized from the corresponding aryltrimethylsilyl intermediates (4a-e, 6a-c, 8, 13, 17) by this method.