Supercritical Fluid Chromatography (SFC) has been successfully applied for chiral separations and achiral purifications in Drug Discovery to provide large quantity of compounds for various in-vivo studies.  This technology advance attributes mainly to its faster method development cycle, readiness in scale-up, higher throughput, and reduced solvent consumption. While traditional Cellulose- and Amylose-derivatized phases have been used successfully in SFC, applications of these phases are limited to chiral resolution of certain molecules and restricted to compounds only soluble in alcohols and acetonitrile due to solvent compatibility. Many discovery compounds are not well resolved in the traditional CSPs, and often have poor solubility in alcohols, requiring non-alcoholic solvents for sample dissolution and as co-solvents in carbon dioxide.  Chiral phases having different recognition mechanisms and ensuring compatibility with non-alcohols such as chlorinated solvents are hence needed to expand SFC applications. This presentation will discuss SFC applications on new chlorinated chiral phases in delivering high quality drug candidates in Discovery Chemistry and its challenges.

Large-scale SFC using chlorinated chiral stationary phases in drug discovery

246th National Meeting (2013)

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