SBIR Phase II: Chiral Polymers for Pharmaceutical Purification

这个小型企业创新研究(SBIR)第二阶段项目开发用于药物纯化的新型手性固定相。药物制造商寻求具有高通量、扩展的手性选择性、高负载能力、能够容忍广泛的流动相的新型手性固定相。为了满足这一需要，人工糖将被合成并聚合成100%立体特异的手性固定相，用于对映体的高效液相色谱。这些聚合物具有显著的性质，如立体专一性、五个不对称中心、可定制的相/配体识别功能、广泛的交联性和醚键。这一化学已在第一阶段得到证明，在第二阶段将产生一系列新的手性聚合物，以加快药物发现并降低药物制造成本。这项研究的更广泛影响将是提供人工多糖，以提供与目前销售的天然产品相比的新活性。多糖具有多个手性中心，无与伦比的光学完整性，以及所有已知分子中最高密度的官能团。人工多糖最容易功能化和定制，以形成所需的手性选择剂。该项目将从分子上设计手性选择剂。这项研究的影响从药物纯化扩展到糖分离、高性能纤维、组织支架和纳米机械。

This Small Business Innovation Research (SBIR) Phase II project develops new chiral stationary phases for pharmaceutical purification. Drug manufacturers seek new chiral stationary phases with high throughput, extended chiral selectivity, high loading capacity, with the ability to tolerate a wide range of mobile phases. To meet this need, artificial saccharides will be synthesized and polymerized into a 100% stereo specific chiral stationary phase for liquid chromatography of enantiomers. These polymers have remarkable propertie such as stereo specificity, five asymmetric centers, functionality for tailoring phase/ligand recognition, extensive crosslinking capability, and ether bonding. This chemistry was demonstrated in Phase I and in Phase II will lead to a new family of chiral polymers to speed drug discovery and reduce the cost of drug manufacture.The broader impact of this research will be to provide artificial polysaccharides to provide novel activities versus the natural products currently sold. Polysaccharides have multiple, chiral centers, unparalleled optical integrity; and the highest density of functional groups of all known molecules. Artificial polysaccharides are most readily functionalized and tailored to form desired chiral selectors. This project will molecularly design chiral selectors. The impact of this research extends beyond drug purification to sugar separations, high performance fibers, tissue scaffolds, and nano machinery.