The determination and separation of enantiomers is an interesting and important topic of research in various fields, e.g., biochemistry, food science, pharmaceutical industry, environment, etc. Although these compounds possess identical physicochemical properties, a pair of enantiomers often has different pharmacological, toxicological, and metabolic activities. For this reason, chiral discrimination by using chromatographic and electromigration techniques has become an urgent need in the pharmaceutical field. This review intends to offer the “state of the art” about the separation of chiral antifungal drugs and several related precursors by both liquid and gas chromatography, as well as electromigration methods. This overview is organized into two sections. The first one describes general considerations on chiral antifungal drugs. The second part deals with the main analytical methods for the enantiomeric discrimination of these drugs, including a brief description of chiral selectors and stationary phases. Moreover, many recent applications attesting the great interest of analytical chemists in the field of enantiomeric separation are presented.
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