9.06 The Use of Preparative Chiral Chromatography for Accessing Enantiopurity in Pharmaceutical Discovery and Development

A Comparative Study of Enantioseparations of Nα-Fmoc Proteinogenic Amino Acids on Quinine-Based Zwitterionic and Anion Exchanger-Type Chiral Stationary Phases under Hydro-Organic Liquid and Subcritical Fluid Chromatographic Conditions

“…issues are also of importance for the successful chemical synthesis of different biomolecules including therapeutic peptides and proteins [3]. Especially for multistep syntheses concepts involving chiral synthons their rigorous chemical and stereochemical purity control is highly demanded and often a challenging task [4].…”

High throughput analysis enables high throughput experimentation in pharmaceutical process research

“…During this time, we developed a variety of different platforms for preparative chromatographic purification of pharmaceutical intermediates and final products. [31][32][33] Leveraging my experience at Regis enabled us to rapidly transplant successful strategies and workflows to the pharmaceutical development environment. Initially, we focused on the small-scale purifications that can powerfully enable synthetic route investigations, especially the chromatographic separation of enantiomers.…”

Cross-Pharma Collaboration on the Development and Evaluation of a New Mid-Scale Preparative Supercritical Fluid Chromatography Instrument

“…The creation of a semipreparative supercritical fluid chromatography (SFC) purification instrument addresses an important, long-standing, and somewhat unusual capability gap identified by the Analytical and Purification Working Group of the ETC. Gram-scale preparative SFC purifications have been widely used in the pharmaceutical industry for nearly 20 years and have become an important enabling technology for the rapid exploration of stereochemical complexity in drug discovery and development. − The rapid growth of the field led to a tumult in the industry supplying instrumentation to carry out this task, with startup companies entering the arena, small companies merging or being acquired by larger ones, new products entering the marketplace, and established products becoming unavailable. An upshot of this flux was the disappearance of one of the standard instruments for carrying out mid-scale SFC purifications, leaving few suitable options in the marketplace for the replacement of aging units.…”