Late Transition Metal Catalysts for Organic Synthesis

有机合成用后过渡金属催化剂

• 批准号: 7138861
• 负责人: STEPHEN L BUCHWALD
• 金额: $ 59.38万
• 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: 1998-09-01 至 2010-05-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7138861
• 关键词: amidation /deamidation; analog; catalyst; chemical bond; chemical kinetics; chemical synthesis; combinatorial chemistry; drug discovery /isolation; heterocyclic compounds; method development

DESCRIPTION (provided by applicant): The ability to prepare functionalized organic molecules rationally and predictably, whether individually or in libraries is central to organic synthesis, medicinal chemistry and the pharmaceutical industry. The aims of this work are to develop new and/or improved methods for the formation of carbon-nitrogen and carbon-oxygen bonds and to apply this chemistry for the preparation of a variety of medicinally interesting compounds. Included in this work is the development of new strategies and techniques for the preparation of heterocyclic compounds, which are the building blocks of medicinal chemistry and the pharmaceutical industry. Further, information gained from this work will help to understand the mechanism of the processes that are being developed in order to increase the rate of improvement of the techniques that we are studying. The development of new methods for organic synthesis is key to the development of the field of organic chemistry as a whole. The methods for carbon-nitrogen and carbon-oxygen bond formation, described herein, are regularly used by those in the pharmaceutical industry for the preparation of analogues with increased potency and reduced side effects. Moreover, the methods can be employed for the preparation of quantities of new substances for preclinical and clinical testing and for the actual manufacture of a pharmaceutical agent. The techniques that are being developed allow for these important functions to be carried out in a more rapid and efficient fashion than previously possible. Moreover, they allow for the preparation of new substances, which have previously been inaccessible. These new compounds have the possibility of having physiological properties of great importance in medicinal chemistry and the pharmaceutical industry.

描述（由申请人提供）：可以理性地和可预测地准备功能化有机分子的能力，无论是单独还是在库中，无论是有机合成，药物化学和制药行业的核心。这项工作的目的是开发新的和/或改进的方法来形成碳氮和碳氧键，并将这种化学作用用于制备各种具有药物有趣的化合物。这项工作中包括的是制定杂环化合物的新策略和技术，这是药物化学和制药行业的基础。此外，从这项工作中获得的信息将有助于了解正在开发的过程的机制，以提高我们正在研究的技术的改进速度。有机合成的新方法的发展是整个有机化学领域发展的关键。本文描述的碳氮和碳氧键形成的方法经常被制药行业中的人使用，以制备具有增加效力和副作用降低的类似物。此外，这些方法可用于制备临床前和临床测试的新物质以及药物的实际生产。所开发的技术允许这些重要功能以比以前可能更快，更有效的方式执行。此外，它们允许制备以前无法访问的新物质。这些新化合物具有在药物化学和制药行业中具有重要意义的生理特性。