Synthesis And Biological Activity Of Novel Spiro Quinone Acids And Quinazoline Derivatives

Spiro quaternary acid compounds are the main force in current acaricides.Compounds such as spirodiclofen and spiromesifen have attracted widespread attention in the field of pesticides due to their unique mechanism of action.In addition,the current lack of insecticide market varieties,and gradually appeared to varying degrees of resistance,so the characteristics of the spirocyclic ketoacid acaricide and other acaricides without cross-resistance are precious.It is very practical to modify and modify the spirocyclic ketoacids;In addition,quinazoline compounds have been favored by the medical community for their various pharmacological characteristics.With the advent of a series of quinazoline acaricide fungicides,quinazoline structures have been increasingly used in pesticide creation.In this paper,using the active substructure splicing,electronic isosteric principle and other means,using spironolactone as the precursor,we have developed 10 unseen spiro quaternary acid derivatives.And six quinazoline derivatives were synthesized with quinazoline as the precursor.And The optimum process conditions were determined through process research.The bioactivity of target compounds was tested in laboratory.Among them,the insecticidal and acaricidal activities were tested on spiro quaternary acid derivatives,and four compounds II7 b,II7c,II7 d and II7 e with good insecticidal activity and scorpion egg inhibitory activity were screened.Among them,II7 c and compound II7 d had a mortality rate of more than 80% for Plutella xylostella and Spodoptera exigua at concentration of 5 mg/L.At a mass concentration of 0.1 mg/L,the inhibition rate of the eggs was also above 80%.The quinazoline derivatives were tested for bactericidal and acaricidal activity,in which both compound III3 a and compound III4 showed good inhibitory activity against eggs and mites of T.cinnabarinus,and eggs at 1 mg/L.The inhibition rate is over 90%.