Chromatographic resolution of the enantiomers of a pharmaceutical intermediate from the milligram to the kilogram scale.

The preparative chromatographic resolution of racemic mixtures is rapidly becoming a standard approach for the generation of enantiomers in pharmaceutical R&D. This paper will discuss the optical resolution of a pharmaceutical intermediate as the separation is scaled up from the milligram to the kilogram scale. Difficulties encountered and their solutions at each scale will be discussed. In addition, the exploration of Simulated Moving Bed (SMB) for the separation will also be discussed. Finally, a comparison of the productivities and solvent consumption for each method and scale will be presented.

Preparative chromatographic resolution of enantiomers using polar organic solvents with polysaccharide chiral stationary phases.

The preparative chromatographic resolution of racemic mixtures is rapidly becoming a standard approach for the generation of enantiomers in pharmaceutical research and development. This paper will discuss the optical resolution of numerous pharmaceutical intermediates and final products using polar organic solvents with polysaccharide chiral stationary phases. The advantages of this approach compared to more traditional mobile phases for preparative separations will be presented. In addition the ability to reverse elution order using polar organic solvents will be presented.