Progress in the Enantioseparation of β-Blockers by Chromatographic Methods

Molecules. 2021 Jan 17;26(2):468. doi: 10.3390/molecules26020468.

Abstract

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

Keywords: HPLC; SFC; SMB; chromatography; enantioseparation; β-blockers.

Publication types

  • Review

MeSH terms

  • Adrenergic beta-Antagonists / chemistry
  • Adrenergic beta-Antagonists / isolation & purification*
  • Chromatography, High Pressure Liquid
  • Chromatography, Supercritical Fluid*
  • Stereoisomerism

Substances

  • Adrenergic beta-Antagonists