Novel Absorbent for Efficient Enantiomer Separation

Chiral drugs, when administered in enathiomerically pure form, offer significant clinicaladvantages over their racemic counterparts. However, available methods for chiral resolution of racemiccompounds, such as diasteriomeric derivatization and chiral chromatography, have drawbacks, includinghigh cost, difficulty with scale-up and lack of applicability for many chiral compounds. This project isdirected toward demonstrating the feasibility of an economical, large-scale chromatographic process forthe chiral resolution of a broad range of racemic compounds. The main focus of this program will bethe development of a single, representative chromatographic medium suitable for use in the process.This novel medium will be packed into a highly efficient column and used to resolve three pharmacologi-cally relevant drugs on a laboratory scale. This Phase I program has three objectives: 1) to demonstratethat the process is technical feasible, 2) to demonstrate that the process can resolve three racemic drugsto enantiomeric purity suitable for pharmaceutical use, and 3) to demonstrate that the process promisesto be economical. Success in Phase I would lead to Phase II proposal focusing on expanding thetechnology to a wide range of chiral compounds, developing strategies for optimization, identifyingscale-up issues, validating the process on a larger scale, and completing a detailed economic analysis.