Synthesis of testosteron-1, 2-T

Elemental tritium is obtained during the decontamination process of the moderator from Cernavoda Nuclear Power Plant. It might be stored for use in controlled fusion in a relatively far future, or it might be immediately used as raw material in the synthesis of labelled compounds with important economic value. Labelling of testosteron with tritium was necessary for carrying out radiometric and molecular biological studies concerning androgen dependent diseases. Testosteron was labelled by selective hydrogenation of 1,2 dihydrotestosterone acetate. The forerunner was synthesized in two steps: 1) esterification of testosteron using acetic anhydride and 2) selective dehydrogenation with 2,6-dichloro-3,5-dicyan-1,4 quinone (DDQ) of the esther formed in the first step. Testosteron acetate was synthesized and purified with yields of 73%, and 80%, respectively. The dehydrogenation process was characterized by yields of 82% for synthesis and 33% for purification. The tritium labelled hormone was obtained in two steps: 1) selective hydrogenation of Δ1 - testosteron acetate in the presence of T2 gas, at low pressure, and 2) hydrolysis of the esther at basic pH. The raw product obtained was purified by preparative thin layer chromatography. The physical and chemical characterization of labelled testosteron reveals a radiochemical purity higher than 98% and a specific activity of 53.4 Ci/mmol. (authors)