Pd-Catalyzed Synthesis Of N-substituted Pyridin-1(2H)-one Derivatives

The vast number of bioactive natural products and pharmaceutical drugs based on the pyridin-2(1H)-one ring system, such as elfamycin and ilicolicin, have become very important in the area of natural product and pharmacetical chemistry.Considering the importance of the compounds with these structural units, much attention has been paid to pyridin-1(2H)-ones as building blocks for synthesizing potassium channel activators and antitumor agents. In this paper, we introduced a variety of synthetic approaches for the synthesis of pyridin-2(1H)-ones and our research work.1. In the first chapter, we have described the representative methods to synthesis of pyridin-1(2H)-ones. These approaches including:using unimolecular compounds and polymolecular compounds to obtain the the target molecule by cyclization, inter-and intramolecular reaction, producing new compounds by way of transformation of other compounds and other ways.2. In the second chapter, we have introduced our works about sythesis of N-substitued pyridin-1(2H)-one derivatives. We developed an efficient ligand-assisted palladium-catalyzed approach for the straightforward synthesis of the pyridin-2(1H)-one framework from available2-chloropyridines and butyl acrylate. In this method, the protocol is associated with the commercially-available starting materials, mild conditions, high yields and wide range of substrate scope. All the compounds have been characterized by1H NMR,13C NMR, HRMS, FT-IR.