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).

Highlights

  • Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations

  • We focus the chromatographic methods employed to the enantioseparation of β-blockers in the 21 century, covering liquid chromatography and supercritical fluid chromatography

  • An enantioselective environment must be created by applying a chiral stationary phase (CSP) or one kind of chiral mobile phase additives (CMPAs) to achieve the separation of enantiomers, which is thereby called the direct chiral separation method [19]

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Summary

Enantioseparation of β-Blockers by HPLC

In the last 30 years, HPLC has obtained a great reputation in the field of enantioseparation, owing to its rapidness, reproducibility, sensitivity, mild operating temperature and availability of a tremendous number of chiral selectors [16,17,18]. Each has its advantages and disadvantages, which we will discuss later

Direct Chiral Separations
Polysaccharide Derivatives
Cyclodextrin-Based CSPs
Macrocyclic Antibiotics
Crown Ethers
Protein-Based CSPs
Indirect Separation Methods
Enantioseparation of β-Blockers by SMB
Enantioseparation of Propranolol
Methods
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