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Synthesis of 3H-labeled Tetrabenazine (TBZ)

✍ Scribed by Sung-Whi Rhee; Kenneth J. Ryan; Mary J. Tanga

Publisher: John Wiley and Sons
Year: 2011
Tongue: French
Weight: 151 KB
Volume: 54
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1881

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✦ Synopsis

Abstract

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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