Studies For The Synthesis Of N-heterocycles Via Pd-catalyzed C(sp~2)-H Bond Activation Strategies

N-heterocycles are the core structure units in many natural products, drug molecules and biologically active molecules. In addition, N-heterocycles widely exist in organic catalysts and auxiliary ligands in transition-metal-catalysts. Therefore, how to construct N-heterocyclic compounds is of great importance in modern synthetic chemistry. Compared with the traditional methods, the synthesis of N-heterocycles via C-H activation shows more advantages. Thus, it has draw considerable attention in the field of synthetic methodologies.This thesis consists of two chapters. In the first chapter, the synthesis of N-heterocyclic compounds via Pd-catalyzed C(sp2)-H bond activation has made a great development in recent years, which provides efficient and selective access to many natural products and biologically active molecules. This part summarizes recent progress in the construction of five, six and seven-membered N-heterocycles by Pd-catalyzed C(sp2)-H activation strategy.In the second chapter, a new method to efficiently synthesize 2-aminoquinolines was developed based on Pd-catalyzed direct coupling of 2-vinylanilines and isocyanides, which is the first example of oxidative coupling of anilines and alkenes involving isocyanides. A variety of 2-vinylanilines and isocyanides were smoothly converted to 2-aminoquinolines with the oxidant Ag2CO3 in the presence of Pd(OAc)2. In addtion, the mechanism was primarily studied.