| Autor: |
Duncan William P, Rotert Gary A, Jay A. Spicer, Richard J. Baranczuk |
| Rok vydání: |
1988 |
| Předmět: |
|
| Zdroj: |
International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology. 15:ii |
| ISSN: |
0883-2897 |
| DOI: |
10.1016/0883-2897(88)90170-5 |
| Popis: |
A method of preparation of halogen labeled organic compounds is described. In particular, estradiol derivatives labeled by halogen substitution at C-16 are synthesized according to the present invention. A triflate intermediate is prepared from which either 16-alpha-halo-substituted-17- beta-estradiols or 16-beta-halo-substituted-17-beta-estradiols can be rapidly formed as desired. ln particular, the preparation of 16-alpha- 123 I-17-beta-estradiol and 16-beta- 123 I-17-beta-estradiol are shown and are synthesized from a 17-beta-estradiol-16-beta-triflate. Both 16-alpha- 123 I-and 16- beta- 123 I-17-beta-estradiol made according to the present invention are shown to have a high specific activity. The method of synthesis is sufficiently rapid so that the relatively short half-life of 123 I is readily accommodated. The high stereospecificity of each step of the reaction sequence in preparing the labeled estradiols provides for highly efficient syntheses and little waste of radio-label. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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