LATE TRANSITION METAL CATALYSTS FOR ORGANIC SYNTHESIS

这项提案中描述的工作旨在开发新的 有机合成中的通用方法。具体来说， 影响碳氮、碳氧和碳硫的技术 债券形成将得到发展或改善。此外，这些 技术将被应用于合成一些不同的 有趣而重要的杂环物种。这种类型的化学 在学术和医药(以及其他)方面都很重要 设置。例如，大量具有重要药学意义的药物 化合物的结构成分是芳基胺或芳基醚。这个 能够以高效的方式获得这些化合物中最广泛的种类 以这种方式，从现成的前体中提取是非常有意义的。这个 新化合物的产生是开发新铅的关键 化合物，药物发现不可或缺的一部分。一种强大的手段 发现新的线索是组合化学。的成功之处 组合化学依赖于新的、通用的和 高效的合成方法。一旦确定了一种先导化合物， 准备衍生品通常很重要，以便克服 原铅化合物存在的问题，如毒性、溶解性或 生物利用度。做到这一点的能力取决于哪些技术 可用。一旦一种化合物被确定为继续前进，它就是 需要制造越来越大的数量以进行测试和 临床试验。快速准备这种材料的能力和 效率越来越重要，原因有很多，包括 将药物评估所涉及的成本降至最低。如果药物真的 商业化，其合成技术必须很高 令人满意且可靠。我们提出的化学反应可以影响所有人 上述问题中的一部分。我们的目标是创造高产、 用于有机合成的通用和可靠的方法。我们在寻找 访问最广泛数量的结构变化的方法和 这既可以在非常小的规模上进行，也可以在非常大的规模上进行。

The work described in this proposal is aimed at the development of new methods of general utility in organic synthesis. Specifically, techniques to effect carbon-nitrogen, carbon-oxygen and carbon-sulfur bond formation will be developed or improved. In addition, these techniques will be applied to the synthesis of a number of different interesting and important heterocyclic species. Chemistry of this type is of importance in both academic and pharmaceutical (and other) settings. For example, a great number of pharmaceutically important compounds have aryl amines or aryl ethers as structural components. The ability to access the widest variety of these compounds, in an efficient manner, from readily available precursors is of great interest. The generation of new compounds is key to the development of new lead compounds, an integral part of drug discovery. One powerful means of discovering new leads is combinatorial chemistry. The success of combinatorial chemistry depends on the availability of new, general and efficient synthetic methods. Once a lead compound has been identified, it is often important to prepare derivatives in order to overcome problems in the original lead compound such as toxicity, solubility or bioavailability. The ability to do this is based on what techniques are available. Once a compound has been identified to go forward, it is necessary to make increasingly large quantities for testing and for clinical trial. The ability to prepare this material rapidly and efficiently is increasingly important for many reasons, including minimizing the cost involved in drug evaluation. If the drug actually becomes commercial, the techniques for its synthesis must be high yielding and reliable. The chemistry which we propose can impact all of the issues mentioned above. Our goals are to create high yielding, general and reliable methods for use in organic synthesis. We seek methods which access the widest number of structural variations and which can be carried out on both very small and very large scale.