Progress in the Enantioseparation of ß-Blockers by Chromatographic Methods.

ABSTRACT

ß-adrenergic antagonists (ß-blockers) with at least one chiral center are an exceedingly important class of drugs used mostly to treat cardiovascular diseases. At least 70 ß-blockers have been investigated in history. However, only a few ß-blockers, e.g., timolol, are clinically marketed as an optically pure enantiomer. Therefore, the separation of racemates of ß-blockers is essential both in the laboratory and industry. Many approaches have been explored to obtain the single enantiomeric ß-blocker, including high performance liquid chromatography, supercritical fluid chromatography and simulated moving bed chromatography. In this article, a review is presented on different chromatographic methods applied for the enantioseparation of ß-blockers, covering high performance liquid chromatography (HPLC), supercritical fluid chromatography (SFC) and simulated moving bed chromatography (SMB).