| Due to its unique structural advantages,multi-functionalized indole compounds have been widely used in the fields of food,pesticides,spices,and dyes.Therefore,how to efficiently construct multi-functionalized indole compounds has attracted much attention in the field of organic synthesis.This article introduced the classification and synthesis of indole compounds.In recent years,great progress has been made in the efficient synthesis of multi-functionalized indole compounds through transition-metal-catalyzed C-H direct functionalization strategies.On the basis of previous work,we have developed a more advantageous method of constructing indoles using C(sp~2)-H bond direct functionalization strategy.For the first time,the 1,1-difunctionalization of the terminal vinyl on 2-vinylanilines has been achieved to construct indole skeleton.The innovation of this strategy is the first realization of the selective continuous arylation/amination of vinyl groups on 2-alkenylanilines with arylboronic acids.This article mainly contains two parts:In the first chapter,in recent years,great progress has been made in the synthesis of indole compounds,which provides a more effective new route for the synthesis of natural products and biologically active molecules containing indole skeleton.This chapter briefly introduced the recent progress in the synthesis of indole compounds.In the second chapter,for the first time,a palladium-catalyzed selective and successive vinylic C-H arylation/amination of 2-vinylanilines with arylboronic acids to generate indoles has been developed.The method can rapidly and efficiently synthesize2-arylindoles derivatives,which provides a simple,direct and economical new choice for the synthesis of multifunctional 2-arylindoles compounds.In addition,we have also studied the mechanism of this reaction,and initially determined the course of the reaction... |
