LATE TRANSITION METAL CATALYSTS FOR ORGANIC SYNTHESIS

用于有机合成的后过渡金属催化剂

• 批准号: 6386994
• 负责人: STEPHEN L BUCHWALD
• 金额: $ 32.38万
• 依托单位: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-07-01 至 2002-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6386994
• 关键词: catalyst; chemical synthesis; combinatorial chemistry; drug discovery /isolation; heavy metals

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.

本提案所述工作旨在开发新的 有机合成中的通用方法。具体地说， 影响碳氮、碳氧和碳硫的技术 将发展或改进键合形成。另外这些 技术将被应用于合成许多不同的 有趣且重要的杂环物种。 这类化学 在学术和制药（和其他）方面都很重要 设置. 例如，大量的药学上重要的 化合物具有芳基胺或芳基醚作为结构组分。 的 能够以高效的方式获得各种各样的这些化合物， 的方式，从现成的前体是极大的兴趣。的 新化合物的产生是开发新铅的关键 化合物，药物发现的一个组成部分。 一个强大的手段， 发现新线索是组合化学。 的成功 组合化学取决于新的、通用的和 有效的合成方法。 一旦确定了先导化合物， 制备衍生物以克服 原始先导化合物的问题，如毒性、溶解性或 生物利用度 做到这一点的能力是基于什么技术是 available.一旦一种化合物被确定可以继续使用， 需要越来越多的大量用于测试和 临床试验 快速制备这种材料的能力， 由于许多原因，效率越来越重要，包括 最大限度地降低药物评价的成本。 如果药物实际上 要想商业化，其合成技术必须很高， 屈服和可靠。 我们提出的化学反应可以影响所有 上述问题。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。 我们寻求 访问最广泛数量的结构变化的方法， 其可以在非常小和非常大的规模上进行。