Microwave-assisted Aza-Michael Addition Reaction Between Aminoheterocycle And α,β- Unsaturated Ketones

This paper implements the absence of a catalyst under microwave replaced by aminoheterocycle propylene and 1,3-diphenyl ketone aza Michael addition, Synthesized NPyridine and N-Thiazole substituted 1,3-diphenyl-3(heterocyclic-2-amino)-1-propanone compound.Using substituted benzaldehyde and substituted acetophenone synthesized twelve substituted-phenyl-1,3-propylene ketone compounds. Benzaldehyde and acetophenone as a model reaction, effects on the yield of by different condition, Determining the synthesis of 1,3-disubstituted phenyl propenone optimum reaction conditions.Under conventional heating, Use of aminoheterocycle and 1,3-disubstituted phenyl propenone Synthesized five with a strong electron withdrawing group(-Cl) and a weak electron-donating group(-CH3) substituted propenone participation 1,3-disubstituted phenyl-3-(pyridin-2-ylamino), The highest yield of 38.2%. Under conventional heating added K2CO3 catalyst, Synthesized five with a strong electron withdrawing group(-Cl) and a weak electron-donating group(-CH3) substituted propenone participation 1,3-disubstituted phenyl-3-(thiazo-2-ylamino), The highest yield of 28.7%. So there is the traditional method have long reaction time, low productivity, poor adaptability shortcomings.In microwave-assisted conditions, 2-aminopyridine and 1,3-diphenyl propenone substance as a model reaction, Investigate different reaction conditions effects on yield, Determine to synthesis of 1,3-diphenyl-3-(heterocyclic-2-amino)-1-propanone optimum reaction conditions. Under these conditions, Investigate different reaction substrate, Found both with electron withdrawing group(-Cl) and electron donating group(-CH3,-OCH3) substituted propenone and amino-heterocyclic synthesis of 1,3-disubstituted-phenyl-3-(2-amino-heterocyclic)propanone compound reaction system is universal. Therefore, in microwave assisted conditions, Aminoheterocycle with 1,3-disubstituted phenyl propenone synthesized of Twenty four 1,3- disubstituted phenyl-3-(2-amino-heterocyclic)-1-propanone compound, This method can shorten the reaction time, the yield has also been greatly improved.Then Provides a simple, mild conditions, high yield reaction pathways to achieve a new green synthetic methods aza Michael addition reaction conditions in the absence of a catalyst.