Enaminones-Based Multicomponent Reation For The Synthesis Of Indole And Its Derivatives

The discourse includes four parts.The first part displayed the Enaminones-Based Multicomponent for the synthesis ofheterocyclic compounds home and abroad, the significance and base of the selection of thesubject, the original points and the research techniques.The second part involves the challenging annulation of enamines with arylglyoxalmonohydrate and the subsequent allylic sp~3C-H activation with aliphatic carboxylic acidsas nucleophile reagents yielding multifunctionalized indoles. The novelty of the presentdomino reaction is shown by the fact that the formation of indole skeleton and itsfunctionalization were simultaneously achieved via metal-free allylic sp~3-C-H bondsactivation in an intermolecular manner and in a one-pot operation.The third part involves an efficient multicomponent dimino reaction is shown by thefact that the construction of pyrrole skeleton and the direct a C(sp~3)–S bond formationwere readily achieved via Bronsted acid catalyzed divergent reaction involving allylicsubstitution in which the allylic component was generated in site through metal-free [3+2]cycloaddition in a one-pot operation.The forth part described the construction of indole-3,4-dionederivatives from5,5-dimethyl-3-(4-chlorophenylamino)cyclohex-2-enone andphenyl-2,2-dihydroxyethanone under microwave irradiation catalyzed with formicacid. The syntheses were finished within short periods with good to excellentchemical yields and regioselectivity that avoided tedious work-up isolations. Furtherinvestigations are in progress in our laboratory to evaluate the process with a broaderrange of substrates, and to synthesize more complex products and test their biologicalactivity.The structures of the products were determined by IR,1H NMR, Furthermore, thestructures of some products were confirmed X-ray analysis. The microwave-assistedreactions mentioned above have advantages of shorter reaction time, higher yields andeasier work-up as well as environmentally friendly. Therefore, a new and environmentallyfriendly method for the synthesis of these important compounds is provided.