Preparation and characterization of tetrabenazine enantiomers against vesicular monoamine transporter 2

Q Yu, W Luo, J Deschamps, HW Holloway…

Index: Yu, Qian-Sheng; Luo, Weiming; Deschamps, Jeffery; Holloway, Harold W.; Kopajtic, Theresa; Katz, Jonathan L.; Brossi, Arnold; Greig, Nigel H. ACS Medicinal Chemistry Letters, 2010 , vol. 1, # 3 p. 105 - 109

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Citation Number: 12

Abstract

As a clinical medication for the treatment of hyperkinetic movement disorders, in conditions such as Huntington's disease, tetrabenazine (TBZ) has always been used in its racemic form. To establish whether or not its beneficial therapeutic actions are enantiospecific, a practical total synthetic route was developed to yield each enantiomeric form to allow their chemical and pharmacological characterization. We briefly summarize the total synthesis ...