双亚砜—钯催化烯丙基C-H键胺化反应的研究

发布时间：2018-04-26 23:36

本文选题：C-H键活化 + 双亚砜　；参考：《合肥工业大学》2017年硕士论文

【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。
[Abstract]:In recent years, the transition metal catalyzed C-H bond activation has been developed rapidly, such as the C-N bond reactions of allyl, aryl, allyl and alkyl. It is also widely used in the synthesis of total and pharmaceutical compounds. The conditions of matrix and homogeneous catalysis in the activation of .C-H bond require higher ligands. In this paper, 12 novel bissulfoxide ligands were designed and synthesized, and one of the best catalytic ligands was selected. The reaction of allyl C-H bond amination with palladium acetate was catalyzed by the ligand of disulfoxide, and the amount of additive was reduced to a certain extent. Moreover, the ligand enhanced the suitable range of substrate and yield of C-N bond and the coupling product of C-N bond could also be deprotected under acidic or alkaline conditions.
【学位授予单位】：合肥工业大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：O621.251

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