Successful therapeutic intervention often requires chiral medicines due to the chirality of many molecules in biological systems.  Potency, efficacy and safety can be highly dependent on the stereochemical geometry of the molecules.  Determining the biological profile of enantiomers in the early stages of drug discovery is important for successful optimization towards clinical candidates.  New methods for stereo-selective synthesis are emerging at a rapid rate.  Early stages of lead discovery and optimization reactions often yield racemic mixtures that lead to questions about the relative activity of the individual isomers.  Fortunately, chiral stationary phases can be used with HPLC and/or SFC to purify the individual isomers, enabling establishment of structure activity relationships for the individual enantiomers. <br/><br/>This work demonstrates screening of several privileged scaffolds and cores including thiazoles, indoles, triazines, benzothiazoles, biphenyls, leucolines, and pyranoquinolones, to identify the best chiral stationary phases and methods for optimal separations.<br/>

Enantiomeric separation of chiral scaffolds and cores used in drug discovery

254th National Meeting (2017)

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