Reaction involving iodine and cupric chloride has been applied to the synthesis of iodinated dihydrotestosterones while radiolabelled estradiol-17-diphosphates and dihydrotestosterone were prepared by the same path using Na .
Radioiodination of iodinated estradiol-17-diphosphates
✍ Scribed by M. Tarle; R. Padovan; Š. Spaventi
- Book ID
- 102900892
- Publisher
- John Wiley and Sons
- Year
- 1978
- Tongue
- French
- Weight
- 597 KB
- Volume
- 15
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
✦ Synopsis
exchange labeling Estradiol and its mono and diiodo derivatives were converted to their 17-diphosphate analogs. Radioiodine labeling of monoiodinated eetradiol diphosphates with 1251 proceeds smoothly in cuprous chloride catalyzed exchange reaction utilizing acetonitrile-ethanol (1:l) as a solvent. Structural aseignmente of unlabeled compounds were made by means of mass spectral data,elemental analysis,and qualikative tests. Radiochromatographic analysis furnished information on the identity of radioiodinated products. Labeling yields up to 35-40% were achieved. Two possible mechanistic interpretations of cuprous ion catalyzed exchange labeling are proposed and their relative merits discussed. The results described in this paper seem to prefer,in harmony with argroraents put forward in some previous studies,the exchange labeling vening SNRl type reaction. a four center transition state over an inter-
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An electrochemical iodination procedure was used t o synthesize 2-iodoestradi 01 -1251 and 4-fodoestradiol -l Z 5 I . These agents were prepared i n order t o be studied as potential tunorl o c a l i z i n g radiophannaceuticals t h a t might d i f f e r e n t i a t e estrogen-responsive from non-re