Selective Transition Metal-Catalyzed Alkene and Alkyne Functionalization Reactions

选择性过渡金属催化的烯烃和炔烃官能化反应

• 批准号: 9382741
• 负责人: Kami Lee Hull
• 金额: $ 34.54万
• 依托单位: UNIVERSITY OF ILLINOIS AT URBANA-CHAMPAIGN
• 依托单位国家: 美国
• 财政年份: 2017
• 资助国家: 美国
• 起止时间: 2017-08-01 至 2018-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/9382741
• 关键词: Alkenes; Alkynes; Carbon; Development; Elements; Hydrogen; Investigation; Lead; Libraries; Methodology; Nitrogen; Organic Synthesis; Oxygen; Pharmaceutical Preparations; Pharmacologic Substance; Process; Reaction; Reagent; Research; Structure-Activity Relationship; Sulfur; Testing; Transition Elements; catalyst; drug candidate; drug discovery; novel; novel strategies; pi bond

Project Summary After carbon and hydrogen; carbon, oxygen, nitrogen, and sulfur are the four of the most common elements found in pharmaceuticals and drug candidates. Lead identification and optimization is typically the longest part of the drug discovery process, taking about five out of the average fifteen years, to bring a drug to market. This is partially due to the requirement to synthesize and test of a large number of potential drug candidates through structure activity relationship (SAR) studies. As such, the development of new organic methodologies for the rapid synthesis of organic molecules is of utmost importance to synthetic chemists. The research described herein focuses on the development of novel approaches for the synthesis of C–N, C–S, C–O, and C–C bonds, in a selective and expedient manner. Moreover, it seeks to allow for divergent synthesis; where from a single common intermediate libraries of potential pharmaceuticals could be synthesized in a single synthetic transformation simply by varying the reagents. More specifically, the proposal focuses on the development of hydro- and oxidative functionalization of carbon-carbon double bonds using transition metal catalysts.

项目摘要 碳、氧、氮和硫是仅次于碳和氢的四种最常见的元素 在药物和候选药物中发现的。铅识别和优化通常是最长的部分 在药物发现过程中，平均十五年中有五年的时间，将药物推向市场。这 部分原因是需要合成和测试大量潜在的候选药物， 构效关系（SAR）研究。因此，开发新的有机方法， 有机分子的快速合成对于合成化学家来说是极其重要的。描述的研究 本文重点关注合成C-N、C-S、C-O和C-C键的新方法的开发， 以选择性和权宜的方式。此外，它试图允许发散的综合;从一个单一的 潜在药物的通用中间体库可以在单一合成方法中合成， 通过改变试剂就能转化。更具体地说，该提案侧重于发展 使用过渡金属催化剂的碳-碳双键的氢化和氧化官能化。