Radioiodinated phenoxyacetic acid derivatives as potential brain imaging agents. I. Efficient synthesis via trimethylsilyl intermediates.
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.
Ohmomo
Y
Y
Okuyama
S
S
Magata
Y
Y
Ueno
Y
Y
Tanaka
C
C
Yokoyama
A
A
D001921:Brain / Q000000981:diagnostic imaging*; D055598:Chemical Phenomena; D002621:Chemistry; D006016:Glycolates / Q000138:chemical synthesis*; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D010642:Phenoxyacetates / Q000138:chemical synthesis*; D011877:Radionuclide Imaging; D014297:Trimethylsilyl Compounds / Q000138:chemical synthesis
D006016:Glycolates; D007457:Iodine Radioisotopes; D010642:Phenoxyacetates; D014297:Trimethylsilyl Compounds