Study On The Synthesis Of Novel Heterocycle-fused Pyrazoles And Indoles

Pyrazoles and indoles are important fused heterocyclic compounds,with a variety of physiological effects,can be used as certain pharmaceuticals,pesticide intermediates.Therefore,it is very important to study the synthesis of novel heterocycle-fused pyrazoles and indoles.This paper is divided into four parts:In the first part,by referring to a large number of relevant literatures,the synthesis methods of heterocyclic compounds,the related applications,the basis and significance of the research are introduced.In the second part,with 2-phenyl-3-methyl-4-acetyl pyrazole as starting material,intermediate 2-phenyl-3-methylbromide-4-acetyl pyrazole by bromination reaction,and its synthetic pyrazole compound on with bifunctional nucleophile(salicylonitriles,2-mercaptobenzonitrile and 3-cyanopyridin-2(1H)-thiones))(Thorpe-Ziegler reaction),it's a new way to realize the synthesis of heterocycle-fused pyrazoles.In the third part,an efficient tandem process for the synthesis of pyridoimidazo-fused ?-carbolines: pyrido[2”,1”:2',3']imidazo[4',5':2,3]pyrido[4,5-b]indole,is described.The construction of these compounds was achieved by one-pot three component reaction of 1-benzylindole-3-carbaldehyde,2-aminopyridine and trimethylsilyl cyanide GroebkeBlackburn-Bienaymé reaction,followed by cyclization through the Pictet-Spengler reaction of the resulting imidazo[1,2-a]pyridine which allowed access to the title heterocycles.In the fourth part,through the cyclization reaction of indole-3-carbaldehyde and 2-aminopyrazine and trimethylsilyl cyanide(Groebke-Blackburn-Bienaym reaction),and further through cyclization reaction of aldehydes(Picter-Spengler reaction),the synthesis strategy of pyrazinoimidazo-fused ?-carbolines.The structures of all the synthesized compounds were characterized by IR spectra and NMR spectra.