Advances and applications of chiral resolution in pharmaceutical field

The attention to chiral drugs has been raised to an unprecedented level as drug discovery and development strategies grow rapidly. However, separation of enantiomers is still a huge task, which leads to an increasing significance to equip a wider range of expertise in chiral separation science to meet the current and future challenges. In the last few decades, remarkable progress of chiral resolution has been achieved. This review summarizes and classifies chiral resolution methods in analytical scale and preparative scale systematically and comprehensively, including crystallization‐based method, inclusion complexation, chromatographic separation, capillary electrophoresis, kinetic resolution, liquid–liquid extraction, membrane‐based separation, and especially one bold new progress based on chiral‐induced spin selectivity theory. The advances and recent applications will be presented in detail, in which the contents may bring more thinking to wide‐ranging readers in various professional fields, from analytical chemistry, pharmaceutical chemistry, natural medicinal chemistry, to manufacturing of drug production. Chiral resolution plays a critical role in pharmaceutical field for different enantiomers may have different bioavailability, distribution, metabolism, and excretion, as well as different pharmacological or toxic properties. And as an active and vibrant research area with continuous new discoveries in recent year, especially one novel progress based on chiral‐induced spin selectivity (CISS), it is necessary to constantly update and summarize the chiral resolution in pharmaceutical field. Hence, we intended to make a systematic and complete overview about chiral resolution. In this paper, the chiral resolution methods, included crystallization resolution, inclusion complexation, chromatographic separation, kinetic resolution, enantioselective liquid–liquid extraction, membrane‐based separation, and chiral‐induced spin selectivity (CISS) were summarized. We hope that this review has the extensive applicability and practical significance which can bring readers a comprehensive understanding of chiral resolution.