Studies On Synthesis And Properties Of Indene Derivatives

Modern pesticide must have the characteristics of safety, high effect, low cost and environmentally-friend. The inden-fused heterocyclic derivatives have a structure similar to natural substances and specific biological activity characteristics; Enamine is the important intermediate of agricultural chemicals and medicine which is also the common pharmacophore.The indanone -fused heterocyclic compounds and compounds with emine increasingly attracted people’s attention and were in-depth research. Specific studies are as follows:1.The recent research and development of the indanone fused heterocyclic compounds and enamine compound were reviewed in this thesis,the methods for the synthesis of the enamine ketones are also described.2.The novels were designed and prepared by using the indanone fused heterocycle and enamine as lead compounds based on pesticide molecular design technologies, such as Similar synthesis,Oisosterisms and Prodrug theory, these compounds can be divided into three series as followings: (1) 2,3-dihydro-1-amine -2-methyl indene compounds 1(Ⅰa～Ⅰ1):(2) 2,3-dihydro-l-indanone-2-carboxylic acid amide (ester) compounds Ⅱ (Ⅱa-Ⅱc):(3) 2,3-dihydro-1-amine-2-carboxylic acid allyl indene compounds Ⅲ(Ⅲa-Ⅲ1):3. Synthesis methods for intermediates, target compounds and the reaction mechanism were studied, and structures of the prepared compounds were confirmed by IR, 1H NMR and MS.4. The bioassays of insecticidal activity were carried out according to the operation procedure of pesticide bioassay. The results showed that compounds exhibited different extent of insecticidal activity against acaricidal activity against Mite (e.g. Tetranychus urticae). Lepidoptera pest (e.g. Mythimna separata) and Sheath blight fungus, Sclerotinia sclerotiorum, Powdery mildew fungus, but had no significant herbicidal activity.5. The structure-activity relationship based on insecticidal activity for the novel compounds was discussed, It provide some theoretical guidance for the future to design a higher biological activity of compounds and prediction of biological activity of unknown compounds.