Novel Approaches to Heterocyclic Synthons

杂环合成子的新方法

• 批准号: 1120184
• 负责人: Jon Njardarson
• 金额: $ 14.44万
• 依托单位: University of Arizona
• 依托单位国家: 美国
• 项目类别: Continuing Grant
• 财政年份: 2010
• 资助国家: 美国
• 起止时间: 2010-11-04 至 2012-02-29
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=1120184&HistoricalAwards=false
• 关键词: Novel; Approaches; Heterocyclic; Synthons

This project is focused on developing useful new catalytic ring forming reactions. A detailed plan is put forth to utilize mechanistic insights to design new catalysts for the ring expansion of strained heterocyclic synthons. The information gained from these catalyst design and development studies will be used to build chiral variants of the optimal ligand frameworks. The resulting new chiral catalysts will be used for asymmetric desymmetrizations and kinetic resolutions. Concurrently, new and efficient synthetic routes for assembling these heterocyclic synthons will be developed. This will be accomplished in one pot by adding carbon nucleophiles to uniquely activated carbonyl electrophiles. With this award, the Organic and Macromolecular Chemistry Program is supporting the research of Professor Jon T. Njardarson of the Department of Chemistry and Chemical Biology at Cornell University. Professor Njardarson's research efforts revolve around the development of new and useful methods for building valuable heterocyclic frameworks. Successful advancement of these new synthetic methods will provide access to a wide range of important heterocyclic products, which will benefit researchers both in academia and the pharmaceutical industry.

本项目致力于开发有用的新型催化成环反应。提出了一个详细的计划，利用力学的洞察力来设计新的催化剂，用于应变杂环合成子的扩环。从这些催化剂设计和开发研究中获得的信息将被用于构建最佳配体框架的手性变体。由此得到的新型手性催化剂将用于不对称脱对称化和动力学拆分。同时，还将开发组装这些杂环合成子的新的有效的合成路线。这将在一锅中完成，方法是将碳亲核试剂添加到独特活化的羰基亲电试剂中。通过这一奖项，有机和高分子化学项目支持康奈尔大学化学和化学生物学系的乔恩·T·纳尔达森教授的研究。Njardarson教授的研究工作围绕着开发新的、有用的方法来构建有价值的杂环框架。这些新的合成方法的成功发展将提供获得广泛的重要杂环产品的途径，这将使学术界和制药行业的研究人员受益。