Benzoquinoline inhibitors of vesicular monoamine transporter 2
US-2016375005-A1 · Dec 29, 2016 · US
US8993766B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-8993766-B2 |
| Application number | US-201213617357-A |
| Country | US |
| Kind code | B2 |
| Filing date | Sep 14, 2012 |
| Priority date | Jan 31, 2012 |
| Publication date | Mar 31, 2015 |
| Grant date | Mar 31, 2015 |
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The present invention relates to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ), and more specifically to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ) by using simple and short reaction processes of using 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline and 4-methyl-2-(3-(trimethylsilyl)prop-1-ene-2-yl)pentane as starting materials to sequentially perform an alkylation reaction, an Aza-Prins cyclization reaction in the presence of an oxidant and an oxidation reaction.
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What is claimed is: 1. A method for preparing tetrabenazine, comprising: a process of subjecting a compound represented by the following Formula 3 and a compound represented by the following Formula 4 to an alkylation reaction to prepare a compound represented by the following Formula 5; a process of subjecting the compound represented by the following Formula 5 to an Aza-Prins cyclization reaction in the presence of an oxidant to prepare a ring compound represented by the follo…
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