The Studies On Synthesis Of Silyl/Alkylindolo[2,1-a]Isoquinoline-6(5H)-one

Polysubstituted silyl heterocyclic compounds have gain wide application in drug design development,functional materials and agrochemicals due to their special properties,which are important synthetic intermediates in the construction of various natural product molecules and bioactive molecules.Therefore,the development of new economical and easy to implement methods for the synthesis of sily heterocyclic compounds is still a subject of extensive research by researchers.Recently,the radical alkene difunctionalization reactions were considered as one of the most effective methods for the preparation of silicon-containing multifunctional products.Compared with other synthesis methods,the radical alkene difunctionalization reactions have the advantages of mild reaction condition,high efficiency and avoiding the use of precious metals as catalysts.This paper primarily studies the strategies for construction of silylindolo[2,1-a]isoquinoline-6（5H）-one derivatives through the radical cyclization reaction of N-methylacryyl-2-phenyl indoles compounds and silanes.The text mainly contains the following three parts:Part Ⅰ:Organosilicon compounds,a kind of new chemical materials are used more and more widely,have the advantages of environmental protection,low toxicity and follow-up easy-handing.This part mainly describes the development and application of organosilicon,summarizes the current experimental methods for the construction of C-Si bond,and concludes the mechanism research,advantages and disadvantages and research significance of this kind of reaction.Part Ⅱ:Isoquinolines are an important class of N-heterocyclic compounds,the key structural skeleton of numerous drugs,functional materials and active natural products,and a significant synthetic intermediate in the field of organic chemistry.In this part,the current research on the synthesis of isoquinoline and gucocyclic isoquinoline compounds is summarized,and the synthesis methods of silicone-substituted indoleisoquinoline derivatives are introduced.Part Ⅲ:The application of N-propenyl-2-phenylindole compounds in the synthesis of polysubstituted nitrogen heterocyclic compounds was summarized.On this basis,we developed the one-pot strategy to prepare5-silylindolo[2,1-a]isoquinoline derivatives via N-methylacryyl-2-phenyl indoles compounds and silanes with TBPB（tert-butyl peroxide benzoate）as oxidation,tert-butanol as solvent and Cu（acac）₂ as catalyst through the silicon radical pathway.The maximum yield of the obtained target product by this method is 83%,and the substrate is widely applicable and has excellent functional group tolerance.The series cyclization method has also been extended to synthesize methyl substituted indolo[2,1-a]isoquinolines.