Selective Transition Metal-Catalyzed Alkene and Alkyne Functionalization Reactions

项目摘要 在碳和氢之后，碳、氧、氮和硫是最常见的四种元素 在药物和候选药物中发现。销售线索识别和优化通常是最长的部分 在药物发现过程中，将一种药物推向市场平均需要15年中的5年。这 部分原因是需要通过以下途径合成和测试大量潜在的候选药物 结构活性关系(SAR)研究。因此，开发新的有机方法来解决 有机分子的快速合成对合成化学家来说至关重要。这项研究描述了 这里着重于开发合成C-N、C-S、C-O和C-C键的新方法， 以选择性和权宜之计的方式。此外，它寻求允许不同的合成；从单一的 潜在药物的通用中间体文库可以在一种合成方法中合成 只需改变试剂即可转化。更具体地说，该提案侧重于 过渡金属催化剂对碳-碳双键的氢化和氧化功能化。

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.