16α-[77Br]-Bromoestradiol-17β (3a) has been synthesized from estrone enol diacetate (1) by bromination with Na 77Br and hydrogen peroxide-acetic acid, followed by reduction with lithium aluminum hydride to give a mixture of 16α-[77Br]-bromoestradiol-17β (3a) and 16α-[77Br]-bromoestradiol-17α (3a) from which the desired epimer (3a) can be obtained in 50% overall radiochemical yield (from Na77Br) by HPLC. Analogous procedures can be used in the preparation of 16α-[77Br]-bromo-11β-methoxyestradiol-17β. (4a) The effective specific activities of these radiopharmaceuticals, determined by binding to the uterine estrogen receptor, are 900-1500 Ci/mmol. Both have high affinity and good binding selectivity for the estrogen receptor and are useful as imaging agents for mammary tumors.
|Original language||English (US)|
|Number of pages||7|
|Journal||The International Journal Of Applied Radiation And Isotopes|
|State||Published - Jul 1982|
ASJC Scopus subject areas
- Nuclear Energy and Engineering
- Radiology Nuclear Medicine and imaging