Direct Alkenylation and Alkylation of Pyridone Derivatives by Ni/AIMe_3 Catalysis

摘要

Pyridone derivatives constitute a core of various important biologically active compounds, and therefore, methods for rapid access to the heterocycles substituted at specific positions are of interest to synthetic and medicinal chemists.Whereas significant progress has been made in protocols for constructing the ring systems with a diverse range of substitution patterns, regioselective introduction of substituents to existing pyridone derivatives requires prefunctionalization by stoichiometric metalation or halogenation. On the other hand, an increasing number of direct C-H functionalizations of heterocycles that allow facile and regioselective direct installation of new C-C bonds are available.rnNevertheless, related transformations of pyridone derivatives remain elusive.