Studies On The Construction Of Nitrogen-Containing Heterocycles Using Multicomponent Reactions

Multicomponent reactions(MCRs) can be used to synthesis of a large amount of structural diversity and complex compounds with its advantages of high yield, high atom economy, convergence, and easy operation. Simultaneously, nitrogen heterocyclic compounds abound in natural products. They are widely used in medical and pesticide fields with its high pharmacological and physiological activities; and also, they can be widely used in chemical dyes and organic light-emitting devices with its unique photophysical properties(OLED). In this paper three series of nitrogen-containing heterocyclic compounds have been synthesized by multicomponent reactions.In part one, the research progress of multicomponent reactions for the synthysis of nitrogen-containing heterocyclic compounds in recent years have been reviewed.In part two, an synthetic procedure for pyrrolo[1,2-a]pyrimidinederivatives was successfully developed by a three-component reaction of malononitrile, aminopyrazole, and acetylenedicarboxylate in acetonitrile. This method has the advantages of short reaction time, environment friendly and simple operation.In part three, an synthetic procedure for indole derivatives was successfully developed by a three-component reaction of 4-hydroxy-6-methyl-2H-pyran-2-one, 2, 2-dihydroxy-1-phenylethanone, and aniline in the presence of a catalytic amount of trifluoroacetic acid in the mixture of ethanol and water(ethanol: water =1:1). This method has the advantages of short reaction time, simple operation, and high atom utilization.