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A rapid synthesis of A-ring bromine-77-labelled estrogens with high specific activity

✍ Scribed by D. S. Wilbur; G. E. Bentley; H. A. O'Brien Jr.

Publisher
John Wiley and Sons
Year
1981
Tongue
French
Weight
375 KB
Volume
18
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A rapid method of no‐carrier‐added radiobrominations of A‐ring estrogens has been demonstrated. The method employs N‐chlorosuccinimide and high specific activity sodium bromide‐77 to generate an electrophilic brominating agent, which when reacted with phenolic steroids, yields three primary products. Two of the radiobrominated products have been shown to be the phenolic ortho brominated regioisomers, and the third product is believed to be a reaction intermediate. The use of HPLC afforded a method of separation and isolation of radiobrominated products. The 2‐bromo‐^77^Br‐ and 4‐bromo‐^77^Br‐ isomers were found to be quite stable in vitro, where‐as the suspected intermediates were not. A specific activity range of 600‐1200 Ci/mmole and radiochemical yields of 25‐30% were obtained for the 4‐bromo‐^77^Br regioisomers.

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