INTERMEDIATES FOR ORGANIC SYNTHESIS

有机合成中间体

• 批准号: 2711236
• 负责人: Paul G. Williard
• 金额: $ 7.29万
• 依托单位: BROWN UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1986
• 资助国家: 美国
• 起止时间: 1986-01-01 至 1998-05-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2711236
• 关键词: INTERMEDIATES; ORGANIC; SYNTHESIS

The principal aim of the research program set forth in this application is to obtain structural information about reactive intermediates in organic chemical reactions. These structural results are invaluable for the development of new synthetic methodology. I particular, the stereoselectivity of common organic reactions is of utmost concern and importance in the design of chemical syntheses of every small organic molecule that is listed in publications such as the NCI publication Chemical Structures of Interest to the Division of Cancer Treatment. The structural information obtained in this research program will permit the rational design of new synthetic reactions and will also yield improved efficiency in organic synthesis. Since a stated goal of the NIH is to obtain chemical compounds for screening as well as for utilization in clinical trails, and since a large number of compounds on the current list of compounds used in clinical trials and in earlier stages of development by the NIH are prepared by organic chemical synthesis, it is extremely important that efficient and useful processes exist for the preparation of such compounds. The research proposed herein will greatly assist with the ongoing development of synthetic organic chemistry leading to the synthesis of physiologically active, small organic molecules. the efficiency of total syntheses of both naturally occurring and non-naturally occurring analogs of such compounds will be improved thorough understanding of the intimate structural details of the reactive intermediates involved in the synthesis of such compounds. Synthetic methodology will be proposed and developed as a consequence of the structural results. The structural results will be obtained by utilizing the techniques of NMR spectroscopy, x-ray diffraction analysis and computional chemistry. The structural results generally are presented as three dimensional representations of aggregated species formed as reactive intermediates is almost all synthetic reactions involving carbanions. This structural information will be utilized to design models to explain and to predict the stereospecificity of organic chemical reactions. Additionally, the structural information will be utilized to develop and to improve new synthetic reagents for the asymmetric synthesis of physiologically active organic molecules. Hence, the structural work will be accompanied by experimental work on the development of new asymmetric reactions for use in the total synthesis of physiologically active compounds.

该应用程序中规定的研究计划的主要目的 是获取有关反应性中间体的结构信息 有机化学反应。 这些结构性结果对于 新合成方法的发展。 我特别， 常见有机反应的立体选择性是最关注的问题， 在每个小有机物的化学合成设计中的重要性 在NCI出版物等出版物中列出的分子 分裂癌症治疗的化学结构。 这 在本研究计划中获得的结构信息将允许 新合成反应的合理设计，也将产生改善 有机合成的效率。 由于NIH的明确目标是 获得用于筛选的化学化合物以及用于利用 临床足迹，并且由于电流上有大量化合物 临床试验中使用的化合物列表以及在早期的阶段 NIH的开发是通过有机化学合成制备的 非常重要的是，存在高效且有用的过程 制备此类化合物。 本文提出的研究将大大 协助持续开发合成有机化学 导致生理活性的小有机物的合成 分子。 两者自然存在的总合成的效率 这种化合物的非天然类似物将得到改善 对反应性的亲密结构细节的透彻理解 参与此类化合物的合成的中间体。 合成方法将被提出和开发 结构结果。 结构性结果将通过 利用NMR光谱的技术，X射线衍射分析 和构成化学。 结构结果通常是 作为聚集物种的三维表示 形成为反应性中间体几乎是所有合成反应 涉及Carbanions。 这些结构信息将用于 设计模型来解释和预测有机的立体特异性 化学反应。 此外，结构信息将是 用于开发并改善新的合成试剂 生理活性有机分子的不对称合成。 因此， 结构性工作将伴随于 开发用于总合成的新不对称反应 生理活性化合物的。