【作者】 李莉；

【导师】 李有桂； Eric A.B.Kantchev；

【作者基本信息】 合肥工业大学 ， 生物化工， 2017， 硕士

【摘要】 近年来,过渡金属催化C-H键活化直接构建C-N键偶联反应的研究发展很快,如烯基、芳基、烯丙基以及烷基的C-N键反应,其在全合成和药物合成中也有广泛的应用。C-H键活化反应中的基质和均相催化的条件对配体的要求较高。因此本文首先设计合成了 12种结构新颖的双亚砜配体,并从中筛选出了一种催化效果最好的金刚烷基双亚砜配体。使用该双亚砜配体与醋酸钯络合催化烯丙基C-H键胺化反应时,可以在较低的催化剂负载下(2 mmol%)进行反应,添加剂的使用量也在一定程度上有所减少。并且这种配体提高了 C-N键偶联的底物适用范围和产率,C-N键的偶联产物也可以在酸性或者碱性条件下脱保护。更多还原

【Abstract】 In recent years, the transition metal catalyzed coupling reactions for C-N bond formation, including alkenyl, aryl, allyl and alkyl of C-N bond reactions have been made some progress, and applications in in the total synthesis and Drug Synthesis.Challenging substrates and conditions in homogeneous catalysis usually pose a very stringent demands on the ligands used. In this paper, 12 novel disulfoxide ligands were designed and synthesized, and the best 1-adamantyl-substituted disulfoxide ligand was screened out. The catalyst permits the allylic oxidative C-N coupling reaction to proceed at lower catalyst loading (2 mmol%) while requiring smaller excess of reagents. Additionally, this ligand improves the availability and the yields of the C-N bond coupled substrate,a substrate that permits deprotection under both acidic and basic conditions, is used.更多还原