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）：无论是单独还是在库中，合理且可预测地制备功能化有机分子的能力对于有机合成、药物化学和制药工业来说至关重要。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，并将这种化学应用于制备各种具有药用价值的化合物。这项工作包括开发制备杂环化合物的新策略和技术，杂环化合物是药物化学和制药工业的基石。此外，从这项工作中获得的信息将有助于理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。有机合成新方法的开发是整个有机化学领域发展的关键。本文所述的碳-氮和碳-氧键形成方法通常被制药工业中的技术人员用来制备具有增加的效力和减少的副作用的类似物。此外，该方法可用于制备大量用于临床前和临床测试的新物质以及用于药剂的实际制造。正在开发的技术允许以比以前更快、更有效的方式执行这些重要功能。此外，它们还可以制备以前无法获得的新物质。这些新化合物有可能具有在药物化学和制药工业中非常重要的生理特性。