MAPPICINE LIBRARIES BY FLUOROUS MIXTURE SYNTHESIS

描述：（申请人的描述）开发一种基本的新的 提出了一种合成含氟混合物的工艺。一系列新型氟 将制造标签并测试其介导氟混合物的能力 代表性有机小分子的合成。标签的使用和 新的混合物方法将通过合成100种化合物来验证 天然产物马匹辛的类似物库。混合图书馆 合成将需要13个步骤，而现有的氟平行合成 方法需要130个步骤。 这种新的氟混合物技术将大大加快合成 用于药物发现和药物治疗的小分子组合文库 优化研究该技术不是“疾病特异性”， 适用于任何疾病领域的广泛生物靶点。的 技术也不是“化学特定的”，可以应用于几乎任何 一种有机反应序列。该技术利用了 混合物合成（更少的步骤，更少的费用，更少的努力，更多的化合物 制得），但仍然提供易于鉴定的纯化合物。 拟定商业应用： 商业应用沿着两条线设想。 首先，公司将 与制药和生物技术公司合作， to make libraries图书馆of new新drug药物candidates候选. 其次，该技术将商业化 为那些不愿意将申请表外发的公司提供内部申请的选择- 他们的发现努力。

DESCRIPTION: (Applicant's description) Development of a fundamental new technology for fluorous mixture synthesis is proposed. A series of new fluorous tags will be made and tested for their ability to mediate fluorous mixture synthesis of representative small organic molecules. The use of the tags and the new mixture method will be validated with the synthesis of a 100 compound library of analogs of the natural product mappicine. The mixture library synthesis will require 13 steps whereas existing fluorous parallel synthesis methods would require 130 steps. This new fluorous mixture technology will dramatically expedite the synthesis of small molecule combinatorial libraries for use in drug discovery and drug optimization research. The technology is not "disease specific" and can be applied to a broad range of biological targets in any disease area. The technology is also not "chemistry specific" and can be applied to virtually any kind of organic reaction sequence. The technology captures the advantages of mixture synthesis (fewer steps, less expense, less effort, more compounds made), but still provides pure compounds that are readily identified. PROPOSED COMMERCIAL APPLICATION: Commercial applications along two lines are envisioned. First, the company will contract with pharmaceutical and biotechnological companies to use its proprietary technologies to make libraries of new drug candidates. Second, the technology will be commercialized to provide the option of in house application for those companies who perfer not to out- source their discovery efforts.