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Preparation of tritiated substituted estratrienes

✍ Scribed by A. D. Fraser; S. J. Clark; H. H. Wotiz

Publisher
John Wiley and Sons
Year
1976
Tongue
French
Weight
215 KB
Volume
12
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

2,4‐Dibromo‐1,3,5(10)‐estratriene‐3,6β,17β‐triol, 2,4‐dibromo‐1,3,5(10)‐estratriene‐3,7α,17β‐triol and 2,4‐dibromo‐1,3,5(10)‐estratriene‐3,16β,17β‐triol were prepared by bromination with N‐bromosuccinimide. 2,4‐Diiodo‐1,3,5(10)‐estratriene‐3,7α,17β‐triol, 2,4‐diiodo‐1,3,5 (10)‐estratriene‐3,11β,17β‐triol and 2,4‐diiodo‐1,3,5(10)‐estratriene‐3, 16α‐diol were formed by direct iodination with I~2~. Hydrogenolysis of the dihalo estrogen derivatives by tritium gas over 5% palladium/Al~2~O~3~ gave the 2,4‐tritiated parent compounds in good yield with high specific activity.

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