抗阿尔茨海默病候选药物Blarcamesine对映体绝对构型的分配

IF 16.4 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY

Accounts of Chemical Research Pub Date : 2022-08-30 DOI:10.3311/ppch.20662

Zsuzsanna Szokol, Károly Lozsi, A. Virág, A. Dancsó, L. Szlávik, G. Simig, Balázs Volk

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引用次数: 2

摘要

Blarcamesine是一种很有前途的治疗阿尔茨海默病的研究药物。国际非专利名称blarcamesine指的是一种外消旋化合物，尽管它很可能以对映不纯的形式上市。在文献中描述了一种分解过程，但尚未公开对映体的绝对构型。本研究制备了适于单晶x射线衍射测量的(R)-(-)-和(S)-(+)-黑狼胺的(R)-(+)-黑狼胺的(R)-(+)-黑狼胺本身的(R)-(+)-黑狼胺的绝对构型，并确定了(+)-和(-)-黑狼胺的绝对构型。

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Assignment of Absolute Configuration to Enantiomers of Anti-Alzheimer Drug Candidate Blarcamesine

Blarcamesine is a promising investigational drug for the treatment of Alzheimer's disease. The international nonproprietary name blarcamesine refers to a racemic compound, although it seems likely that it will be marketed in an enantiopure form. A resolution process has been described in the literature, but the absolute configurations of the enantiomers have not yet been disclosed. In the present study, crystals of (R)-(-)- and (S)-(+)-mandelate salts of (+)- and (-)-blarcamesine and also that of (R)-(+)-blarcamesine itself, suitable for single-crystal X-ray diffraction measurement were prepared and the absolute configurations of (+)- and (-)-blarcamesine have been determined.

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来源期刊

Accounts of Chemical Research 化学-化学综合

CiteScore

31.40

自引率

1.10%

发文量

312

审稿时长

2 months

期刊介绍： Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.