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Radiobromination of the 1-position of estradiol using no-carrier-added bromine-77

✍ Scribed by Mark D. Hylrides; Patricia L. Buksa; Fred A. Mettler; D. Scott Wilbur

Publisher
John Wiley and Sons
Year
1985
Tongue
French
Weight
215 KB
Volume
22
Category
Article
ISSN
0022-2135

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✦ Synopsis

The t a r g e t compound, 1-([ Br1bromo)estradlol (la), was prepared i n t h r e e steps from 4-amlnoestradlol 3-methyl ether (2). E l e c t r o p h l l l c bromlnatlon o f 2 w l t h I n s l t u generated 7 7 B r C l f o l l o w e d by deamlnatlon I n t h e same r e a c t i o n m i x t u r e gave 1-([ Br]bromo)estradlol 3-methyl ether (4a) I n 59% radlochemlcal e f f l c l e n c y . Subsequent demethylatlon of fi gave I n 92% radlochemlcal e f f l c l e n c y w l t h an estimated s p e c i f i c a c t l v l t y o f 300-600 Cl/mnol. An o v e r a l l radlochemlcal y i e l d o f approximately 20% was obtalned. S t a b l l l t y studles o f 3 showed no decomposltlon over a three-day perlod.

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