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.

本提案中描述的工作旨在开发新的 有机合成中通用的方法。具体来说， 影响碳-氮、碳-氧和碳-硫的技术 债券的形成将得到发展或改善。此外，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。 此类化学 在学术和制药（及其他）方面都很重要 设置。 例如，大量具有重要药学意义的物质 化合物具有芳基胺或芳基醚作为结构成分。 这 能够以有效的方式获取最广泛的这些化合物 从容易获得的前体中提取的方法引起了人们极大的兴趣。这 新化合物的产生是开发新先导化合物的关键 化合物，药物发现的一个组成部分。 一种强有力的手段 发现新的线索是组合化学。 的成功 组合化学取决于新的、通用的和 高效的合成方法。 一旦确定了先导化合物， 为了克服这些问题，制备衍生物通常很重要 原始先导化合物存在问题，例如毒性、溶解度或 生物利用度。 做到这一点的能力取决于所采用的技术 可用的。一旦确定了一种化合物可以继续使用， 需要生产越来越多的数量来进行测试和 临床试验。 快速制备该材料的能力 由于多种原因，高效变得越来越重要，包括 最大限度地减少药物评价的成本。 如果药物确实 商业化，其合成技术必须很高 产量高且可靠。 我们提出的化学反应可以影响所有 的上述问题。我们的目标是创造高产、 有机合成中使用的通用且可靠的方法。 我们寻求 获得最广泛的结构变化的方法和 可以在非常小和非常大的规模上进行。