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Synthesis of [2-d]estradiol, [4-d]estradiol, [2-t]estradiol and [4-t]estradiol with high specificity

✍ Scribed by David J. Porubek; Moses J. Namkung; Mont R. Juchau; Sidney D. Nelson

Publisher
John Wiley and Sons
Year
1984
Tongue
French
Weight
345 KB
Volume
21
Category
Article
ISSN
0022-2135

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✦ Synopsis

17-P-Estradiol has been labeled in the 2 or 4 position with tritium Both 2-and 4-iodoestradiol. were prepared by treatment of or deuterium. estradiol with N-iodosuccinimide in ethanol followed by chromatographic separation. Reductive dehalogenation of 2-and 4-iodoestradiol with tritium gas gave [2-tlestradiol and [4-t]estradiol, respectively, with specific activities of approximately 2 Cilmmole. radiolabel was incorporated into the target positions as determined by rehalogenation of the radiolabeled compounds. Analysis of the deuterium labeled compounds, [2-d]estradiol and [4-d]estradiol, similarlv prepared by reduction with deuterium gas, revealed that isotope incorporation was high and specific.

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