Chiral resolution methods for racemic pharmaceuticals based on cocrystal formation

文献信息

发布日期 2023-10-16

DOI 10.1039/D3CE00853C

影响因子 3.545

作者

摘要

Currently, more than half of available drugs on the market are chiral, and approximately 90% of these drugs are marketed as racemates. When these racemic medications are exposed to the chiral environment of the human body, differences in their activity appear. The enantiomers of a chiral drug may potentially have distinct pharmacokinetic, metabolic, and toxicological features. As a result, regulatory requirements promote the production of enantiopure drugs to reduce the complexity of pharmacodynamics and the administration dose or to eliminate unwanted side effects, while also providing some economic savings by enabling a totally effective pharmaceutical formulation. There are a variety of procedures employed in the pharmaceutical industry for chiral separation of racemic drugs, such as developing de novo enantiomerically pure pharmaceuticals by asymmetric synthesis or chiral resolution of currently available racemic compounds via different approaches like chiral chromatography methods, diastereoisomeric salt formation, and cocrystallization-based methods. This review will focus on cocrystallization techniques such as the generation of host–guest inclusion compounds, diastereomeric cocrystal pairs, enantiospecific cocrystals, conglomerates, ionic cocrystals, and preferential enrichment of cocrystals. Overall, this review outlined the crucial importance of pharmaceutical cocrystals in chiral resolution techniques of racemic compounds.

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来源期刊

CrystEngComm

CiteScore: 5.5

自引率: 7.7%

年发文量: 643

CrystEngComm is the forum for the design and understanding of crystalline materials. We welcome studies on the investigation of molecular behaviour within crystals, control of nucleation and crystal growth, engineering of crystal structures, and construction of crystalline materials with tuneable properties and functions. We publish hypothesis-driven research into… how crystal design affects thermodynamics, phase transitional behaviours, polymorphism, morphology control, solid state reactivity (crystal-crystal solution-crystal, and gas-crystal reactions), optoelectronics, ferroelectric materials, non-linear optics, molecular and bulk magnetism, conductivity and quantum computing, catalysis, absorption and desorption, and mechanical properties. Using Techniques and methods including… Single crystal and powder X-ray, electron, and neutron diffraction, solid-state spectroscopy, spectrometry, and microscopy, modelling and data mining, and empirical, semi-empirical and ab-initio theoretical evaluations. On crystalline and solid-state materials. We particularly welcome work on MOFs, coordination polymers, nanocrystals, host-guest and multi-component molecular materials. We also accept work on peptides and liquid crystals. All papers should involve the use or development of a design or optimisation strategy. Routine structural reports or crystal morphology descriptions, even when combined with an analysis of properties or potential applications, are generally considered to be outside the scope of the journal and are unlikely to be accepted.