Research On The Synthesis Methodology And Bioactivities Of Aza-heterocyclic Compounds

Aza-heterocyclic compounds have a wide range of applications in medicines,pesticides,organic functional materials and other fields.The development of organic chemistry is trend to high efficiency,high selectivity and green environmental.The organic combination of efficiency tandem reaction for synthesis of heterocyclic compounds is of important application value.In this dissertation,we described the new methods and new reactions for the synthesis of 1,2-dihydroquinoline derivatives,quinolone salt derivatives and indole derivatives via organic tandem reaction.The main contents are as following:1.Synthesis of polysubstituted 1,2-dihydroquinolines and indoles under mild conditions via tandem reaction of arylamines and propargylic alcohols catalyzed by FeCl3·6H2O.We provide the possible reaction mechanisms for the synthesis of polysubstituted 1,2-dihydroquinolines and indoles.The reaction conditions are economic,environmental protection,mild and easily operated,and this methodology provides a new and effective way for the synthesis of polysubstituted1,2-dihydroquinolines and indoles.2.Synthesis of quinolines and quinolinium salts from arylazide and propargylic alcohols via a cascade Friedel-Crafts-type reaction and electrophilic cyclization catalyzed by I2.An efficient,environmentally friendly and high-yielding route from inexpensive starting materials to quinolines and quinolinium salts has been developed.3.Most of the heterocyclic compounds containing nitrogen atom have broad biological activities.The antibacterial activity of the 1,2-dihydroquinolines and quinolinium salts derivatives were studied.The experiments results showed that 2-3a had significant antibacterial activities,especially on Escherichia col,Staphylococcus aureuang et al.Structure-function relationship of 2-3a had also been studied.