Design,Synthesis And Biological Activity Of Quinazoline Derivatives

In recent years,nitrogenous heterocyclic compounds have received wide concern due to their unique physicochemical property and biological activity,thus making it possible for them to gain the leading role in such fields as chemical synthesis,medicine,pesticide and new materials.Quinazoline derivative,an important branch of the nitrogenous heterocyclic compounds,also greatly shows its pharmacological property and biological activity through performing its role in fields including medicine anticancer and sterilization.As a series of high effective pesticidal chemicals including acaricide like fenazaquin,bactericide like benzene oxygen quinoline and herbicide like metribuzin is successfully commercialized,more and more chemicals with quinazoline heterocyclic structure are employed in the development and production of new types of pesticides,leading it to become one of the hottest heterocycle structures.In the study,16 quinazoline derivatives are synthesized by means of active substructure splicing and isostere with quinazoline derivative as the leading role,and through exploring the synthetic techniques,the optimized synthetic technique is finally confirmed.A test in door is carried out on the target compounds,and biological activity is also conducted on quinazoline derivatives in terms of sterilization,insecticide and acaricide.Compound ?3c,?4a,?5a,?5b and ?6d can completely inhibit acarid eggs when the mass concentration is 100 mg/L,among which ?3c can100 percent inhibit acarid eggs although the mass concentration is 50 mg/L and the inhibition rate of the others ?4a,?5a,?5b,?6d are over 90% when the massconcentration the same,showing great inhibition activity on tetranychus cinnabarinus eggs.In addition,the chemicals also show great sterilization activity,among which the inhibition rate of ?4a??6b??7b on the tested germs reaches 90%.