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Labeling of steroids by activated tritium

Labeling of steroids by activated tritium

Journal of Labelled Compounds & Radiopharmaceuticals 25(6): 585-602

Steroid hormones and derivatives are labeled to high specific activities with activated tritium generated by microwave discharge of tritium gas. The steroid nucleus is not degraded by reactions with tritium; the hydroxyl and oxo groups at 3, 11, 17, and 20 positions of the steroid nucleus are not displaced by tritium but are oxidized or reduced to form the labeled by-products. Saturation of A ring occurs readily, but tritium addition to the isolated C = C double bond occurs in the order of .DELTA.1 > .DELTA.4 > .DELTA.5. Steroids with the 21-hydroxyl group are not tritiated. Despite the addition reaction, the final products from the unsaturated steroids may still contain significant amounts of the labeled. Specific activities of the labeled by-products steroids can approach 29 Ci/mM.

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Accession: 005787065

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DOI: 10.1002/jlcr.2580250603

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