Synthesis And Biological Activity Of Acyl Acetonitrile Derivatives

Cyanide has been widely used in the synthesis of medicines and pesticides due to the biological activities.Because of the unique mechanism and excellent biological activity,acyl acetonitrile compounds attracted a lot of attention.In this paper,a series of acyl acetonitrile compounds were designed and synthesized in order to discover high active pesticide lead structure.Cyanide C were synthesized using chloromethyl-substituted aromatic compounds A as the raw materials by cyanation reaction.Then compounds C were reacted with phenylacetyl chloride D and diethyl carbonate E respectively to generate intermediate F 3-oxo-4-phenyl-2-substituted butanenitrile and G 2-cayno-2-substituted ethyl acetate.Finally,101 novel title compounds were synthesized by acylation reactions of intermediate F and G with substituted carboxylic acid chloride.The structure of the compounds were confirmed by ~1H NMR and MS.The preliminary bioassay showed that some of the target compounds exhibited good herbicidal activities at the concentration of 200 mg/L.And compound Kd10 still showed good biological in the concentration of 150 g ai/ha,therefore it could be the potential lead compound for further research.