Synthesis And Herbicidal Activity Of Novel Triazolinone Derivatives

Heterocyclic compounds widely exist in the nature with widespread biological activities, which attract scientists's interests significantly. Triazolinone derivativeas are one of the important families in heterocyclic compounds. Triazolinone derivatives have been found to have widespread biological activities, especially as herbicides, which show characteristics of high bioactivities, low poison, and environmental friendship. In the contemporary herbicides research area, they become one of the most popular topics. The application of triazolinones in pesticide has brought various pesticide companies attention especially in recent two decades.This paper optimizes the well-performed activity compound Y5060 in previous research in combined with our seminar's basic work. In the meanwhile, in order to seek high activity compounds, we take the Y5060 as lead-structure according to the method of the active structural stitching and the bioisosterism to transform and synthesis a series of novel compounds, and make a study on their bioactivity as well. The specific research contents include the following:1. This paper has summarized the research progress of triazolinone derivatives in pesticide, chemical and some other fields, supporting the theory basis of compounding novel triazolinone derivatives.2. Conclude the previous research work; optimize the synthetic route of well-performed compound Y5060, and make an in-depth study of it.3. Based on the method of the active structural stitching and the bioisosterism, take the compound Y5060 as lead structure to transform and synthesis a series of novel compounds which are all characterized by 1H NMR,MS,elemental analysis.4. Bioactivities of all compounds in postemergence treatments were performed at the concentration of 150 gai/ha using Echinochloa crusgalli, Digiatra sanguinalis, Annual bluegrass, Brassica juncea, Amaranthus retroflexus and Eclipta prostrate as inhibition target. For example, the compound Ik, II and Im showed 70% herbicides activity against Eclipta prostrate, the compound Ip and Iq showed 60% inhibition toward Annual bluegrass and 50% inhibition toward Digiatra sanguinalis.