Synthesis of 3H-Labeled Tetrabenazine (TBZ)


Rhee, S. W., Ryan, K. J., & Tanga, M. J. (2011). Synthesis of 3H‐labeled Tetrabenazine (TBZ). Journal of Labelled Compounds and Radiopharmaceuticals, 54(7), 367-370.


Tetrabenazine (TBZ) (1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolin-2-one), a vesicular monamine transporter 2 inhibitor, was prepared as a tritium-labeled compound with high specific activity and radiochemical purity. Catalytic hydrogenation of a precursor with the terminal double bond was used to introduce the tritium. This method provides tritium-labeled TBZ with high specific activity and radiochemical purity, which allow the further investigation of a TBZ in the neurological field. Copyright © 2011 John Wiley & Sons, Ltd.

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