NOVEL ABSORBENT FOR EFFICIENT ENANTIOMER SEPARATION

手性药物，当以对映体纯形式给药时，提供 与外消旋体相比具有显著的临床优势。 然而，手性拆分外消旋化合物的现有方法， 如非对映异构体衍生化和手性层析 缺点，包括成本高、扩容困难、缺乏 适用于多种手性化合物。这个项目的目标是 论证了经济的、大规模的 大范围手性拆分的色谱学方法 外消旋化合物。 该计划的主要重点将是开发一种单一的、 适合在该过程中使用的代表性色谱介质。 这种新的介质将被包装成高效的柱并使用 在实验室规模上拆分三种药理上相关的药物。 此第一阶段计划有三个目标：1)证明 工艺在技术上是可行的，2)证明工艺可以 拆分三种外消旋药物的对映体纯度适用于 医药用途，以及3)证明这一过程承诺 要节约。 第一阶段的成功将导致第二阶段的提案，重点是扩展 将该技术应用于多种手性化合物，发展策略 对于优化，确定纵向扩展问题，验证流程 规模更大，并完成详细的经济分析。

Chiral drugs, when administered in enathiomerically pure form, offer significant clinical advantages over their racemic counterparts. However, available methods for chiral resolution of racemic compounds, such as diasteriomeric derivatization and chiral chromatography, have drawbacks, including high cost, difficulty with scale-up and lack of applicability for many chiral compounds. This project is directed toward demonstrating the feasibility of an economical, large-scale chromatographic process for the chiral resolution of a broad range of racemic compounds. The main focus of this program will be the 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 pharmacologically relevant drugs on a laboratory scale. This Phase I program has three objectives: 1) to demonstrate that the process is technical feasible, 2) to demonstrate that the process can resolve three racemic drugs to enantiomeric purity suitable for pharmaceutical use, and 3) to demonstrate that the process promises to be economical. Success in Phase I would lead to Phase II proposal focusing on expanding the technology to a wide range of chiral compounds, developing strategies for optimization, identifying scale-up issues, validating the process on a larger scale, and completing a detailed economic analysis.