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Molecules 2017, 22(1), 158; doi:10.3390/molecules22010158

Preparative Scale Resolution of Enantiomers Enables Accelerated Drug Discovery and Development

1
Respiratory, Inflammation and Autoimmunity, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Pepparedsleden 1, 431 83 Molndal, Sweden
2
Cardiovascular and Metabolic Diseases, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Pepparedsleden 1, 431 83 Molndal, Sweden
*
Author to whom correspondence should be addressed.
Academic Editor: Yoshio Okamoto
Received: 22 November 2016 / Revised: 12 January 2017 / Accepted: 13 January 2017 / Published: 18 January 2017
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Abstract

The provision of pure enantiomers is of increasing importance not only for the pharmaceutical industry but also for agro-chemistry and biotechnology. In drug discovery and development, the enantiomers of a chiral drug depict unique chemical and pharmacological behaviors in a chiral environment, such as the human body, in which the stereochemistry of the chiral drugs determines their pharmacokinetic, pharmacodynamic and toxicological properties. We present a number of challenging case studies of up-to-kilogram separations of racemic or enriched isomer mixtures using preparative liquid chromatography and super critical fluid chromatography to generate individual enantiomers that have enabled the development of new candidate drugs within AstraZeneca. The combination of chromatography and racemization as well as strategies on when to apply preparative chiral chromatography of enantiomers in a multi-step synthesis of a drug compound can further facilitate accelerated drug discovery and the early clinical evaluation of the drug candidates. View Full-Text
Keywords: chiral resolution; chiral stationary phases; preparative chromatography; supercritical fluidchromatography; racemization; active pharmaceutical ingredient; drug discovery; drug development chiral resolution; chiral stationary phases; preparative chromatography; supercritical fluidchromatography; racemization; active pharmaceutical ingredient; drug discovery; drug development
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Leek, H.; Andersson, S. Preparative Scale Resolution of Enantiomers Enables Accelerated Drug Discovery and Development. Molecules 2017, 22, 158.

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