Research Project
3502343
Chiral drugs when administered in enantiomerically pure form offer significant clinical advantages over their racemic counterparts. However, available methods to prepare enantiomerically pure compounds have drawbacks, including high cost, limits on chemical and enantiomeric purity, and difficulty with scale-up. This project is directed at demonstrating the feasibility of a reliable and economical process to prepare enantiomerically pure (R)-cyanohydrins. Chiral cyanohydrins are important substances leading to synthons (e.g., alpha-hydroxyacids, beta-amino alcohols, beta-amino ketones, and alpha- amino acids), intermediates used to prepare enantiomerically pure drugs. This Phase I program will focus on preparing an enantiomerically pure chiral cyanohydrin that can be used to prepare (R)-albuterol, and important bronchial asthma drug. This Phase I program has three objectives: 1) demonstration that the process is technically feasible, 2) demonstration that the process can produce a target (R)-cyanohydrin of enantiomeric purity suitable for use in the production of pharmaceuticals, and 3) demonstration that the process promises to be scalable and economical. Success in Phase I would lead to a Phase II proposal focused on characterizing of the technology, expanding the technology to a wider range of chiral cyanohydrins, developing strategies for optimization, identifying scale-up issues, validating the methods at the 1-kg scale, and completing a detailed economic analysis.
