Asymmetric Synthesis and Absolute Configuration of (+)- and (-)-Perhexiline

被引：3

作者：

Tseng, Chih-Chung ^{[1
]}

Greig, Iain R. ^{[1
]}

Harrison, William T. A. ^{[2
]}

Zanda, Matteo ^{[1
,3
]}

机构：

[1] Univ Aberdeen, Inst Med Sci, Kosterlitz Ctr Therapeut, Aberdeen AB25 2ZD, Scotland

[2] Univ Aberdeen, Dept Chem, Aberdeen AB24 3UE, Scotland

[3] CNR, ICRM, I-20131 Milan, Italy

来源：

SYNTHESIS-STUTTGART | 2016年 / 48卷 / 01期

关键词：

perhexiline; asymmetric synthesis; stereochemistry; medicinal chemistry; crystal structure; PERHEXILINE; HEART; HYDROGENATION; INHIBITION; TARGETS; ACID;

D O I：

10.1055/s-0035-1560708

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Racemic perhexiline has been used (or is currently undergoing clinical trials) for the treatment of a variety of cardiovascular disorders. Increasing evidence suggests that the (-)-enantiomer should be used, as opposed to the racemic mixture. Here, we report the first asymmetric synthesis of both enantiomers of perhexiline in high enantiomeric excess and the assignment of their (-)-S/(+)-R absolute stereochemistry by X-ray crystallography.

引用

页码：73 / 78

页数：6