Tag: 317.4226

Preparation and evaluation of tetrabenazine enantiomers and all eight stereoisomers of dihydrotetrabenazine as VMAT2 inhibitors was written by Yao, Zhangyu;Wei, Xueying;Wu, Xiaoming;Katz, Jonathan L.;Kopajtic, Theresa;Greig, Nigel H.;Sun, Hongbin. And the article was included in European Journal of Medicinal Chemistry in 2011.Recommanded Product: 1026016-83-0 This article mentions the following:

Tetrabenazine (TBZ) ((±)-1) and dihydrotetrabenazines (DHTBZ) are potent inhibitors of vascular monoamine transporter 2 (VMAT2). A practical chem. resolution of (±)-tetrabenazine and enantioselective synthesis of all eight DHTBZ stereoisomers were described. The result of VMAT2 binding assay revealed that (+)-tetrabenazine I (R^2aR^2b = O) (K_i = 4.47 nM) was 8000-fold more potent than (-)-tetrabenazine (II) (K_i = 36,400 nM). Among all eight DHTBZ stereoisomers, (+)-(2R,3R,11bR)-DHTBZ I (R^2a = OH, R^2b = H) (K_i = 3.96 nM) showed the greatest affinity for VMAT2. The (3R,11bR)-configuration appeared to play a key role for VMAT2 binding. In summary, (+)-tetrabenazine, (+)-(2R,3R,11bR)-DHTBZ and their derivatives warrant further studies in order to develop more potent and safer drugs for the treatment of chorea associated with Huntington’s disease and other hyperkinetic disorders. In the experiment, the researchers used many compounds, for example, Tetrabenazine (+)- (cas: 1026016-83-0Recommanded Product: 1026016-83-0).

Tetrabenazine (+)- (cas: 1026016-83-0) belongs to isoquinoline derivatives. Although isoquinoline derivatives can be synthesized by several methods, relatively few direct methods deliver the unsubstituted isoquinoline. Lewis acid activation and nucleophilic attack can produce multiple regioisomers in quinolines and pyridines; isoquinolines generally only undergo attack at the 1-position.Recommanded Product: 1026016-83-0

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Real-Time Monitoring of Solid-Liquid Slurries: Optimized Synthesis of Tetrabenazine was written by Sato, Yusuke;Liu, Junliang;Kukor, Andrew J.;Culhane, Jeffrey C.;Tucker, John L.;Kucera, David J.;Cochran, Brian M.;Hein, Jason E.. And the article was included in Journal of Organic Chemistry in 2021.Computed Properties of C19H27NO3 This article mentions the following:

Solid-liquid slurries are vital and increasingly prevalent in the pharmaceutical and chem. industries. Despite the importance of these heterogeneous systems, process control and optimization are fundamentally hindered by a lack of compatible real-time anal. techniques. We present herein an online HPLC monitoring platform enabling access to real-time compositional information on slurries. We demonstrate the system by investigating the heterogeneous synthesis reaction of tetrabenazine. Furthermore, we integrated our online HPLC platform with the orthogonal monitoring techniques of a pH probe and a microscopic imaging probe to provide addnl. mechanistic insight. These combined insights enable the optimization of tetrabenazine synthesis in terms of reaction time, byproduct formation, and diastereomeric purity of the final product. In the experiment, the researchers used many compounds, for example, Tetrabenazine (+)- (cas: 1026016-83-0Computed Properties of C19H27NO3).

Tetrabenazine (+)- (cas: 1026016-83-0) belongs to isoquinoline derivatives. Quinoline and isoquinoline skeletons are among the most attractive frameworks with a wide range of biological and pharmacological activities. Other industrial applications include their use as corrosion inhibitors, preservatives, and as solvents for resins and terpenes.Computed Properties of C19H27NO3

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem