DEVELOPMENT OF STILLE CROSS COUPLINGS THAT ARE CATALYTIC IN TIN

锡催化静止交叉联轴器的开发

• 批准号: 6258834
• 负责人: ROBERT E MALECZKA
• 金额: $ 0.02万
• 依托单位: MICHIGAN STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1997
• 资助国家: 美国
• 起止时间: 1997-06-01 至 1999-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6258834
• 关键词: animal tissue; biological products; biomedical resource; growth factor; male; proteins; reproductive system

We recognize that refinements in biological screening protocols will allow scientists to discover pharmacologically significant natural products that are available in only minute quantities. In such cases, the power of organic synthesis will undoubtedly be called upon to provide sufficient material for full biological evaluation. Given natures propensity for structurally complicated molecules, this is sure to be quite a challenge for synthetic chemists. To address this challenge we look to invent unique catalytic reactions and strategies that are of high efficiency and general utility. The use of stoichiometric amounts of organotin compounds in palladium-mediated divinyl cross-couplings, aminations, and related reactions is a primary disadvantage of the Stille coupling protocol. The invention and development of new methods allowing for the catalytic employment of organostannanes in such reactions would significantly reduce the amount of tin waste and thereby be of great value with respect to both environmental and practical concerns. The specific aim of this research program is the development of reaction procedures which will allow for the in situ generation of organotins and their subsequent coupling or amination under conditions that are catalytic in tin as well as palladium. In support of this research it is essential that advanced mass spectral facilities be available to provide high resolution spectra of our synthetic compounds.

我们认识到生物筛选方案的改进 将使科学家们能够发现 只有微量的天然产品。 在 在这种情况下，有机合成的力量无疑将被称为 为全面生物学评价提供足够的材料。 鉴于性质结构复杂的分子的倾向，这 对合成化学家来说肯定是一个挑战。 解决 这个挑战，我们期待发明独特的催化反应， 具有高效率和通用性的策略。 使用 化学计量量的有机锡化合物在钯介导的 二乙烯基交叉偶联，胺化和相关反应是一种 Stille偶联方案的主要缺点。 本发明 和开发新的方法，使催化就业 在这种反应中的有机锡烷将显着减少 大量的锡废料，从而具有很大的价值， 环境和实际问题。 其具体目的是 研究计划是开发反应程序，该程序将 允许原位生成有机锡及其随后的 在锡催化的条件下进行偶联或胺化， 以及钯。 为了支持这项研究， 先进的质谱设备可提供高质量的 我们合成的化合物的分辨率光谱。