Design, Synthesis And Activity Studies Of A New Benzenedicarboxamide Derivative And New Herbicides Safeners

Agriculture is an important foundation for good and harmonious development of society and economy. But crops are suffering more and more serious diseases under the influence of weather or various anthropic factors. Using agrochemicals is a main method to control plant diseases, protect crops and maintain sustainable agricultural development. The agrochemicals used widely include pesticides, fungicides and herbicides. According to the actual needs of the development of agriculture, we made some studies on two parts of pesticides and herbicides.1. The design and synthesis of benzenedicarboxamide derivative as new potential pesticides. After pesticides were discovered, they have developed rapidly. But low activity, selectivity and safety have still limited their development, and the resistance would have occured after misuse, which eliminate some old types of pestcides and make it important to develop new agrochemicals with new chemical structures or new mode of action. Fubendiamide was a novel benzenedicarboxamide pesticide. It is used widely nowadays and has good activity. A new benzenedicarboxamide compound with similar structure was designed and synthesized. Its structure was conformed by1H-NMR. The bioactivity to larvae of Diamondback moth(Phutella xylostella L.). Beet Armyworm(Spodoplera exigua) and Chilo suppressalis was tested using Chlorantraniliprole as the positive control. The new compound showed more significant activity to Beet Armyworm(Spodoplera exigua) than to Diamondback moth(Plutella xylostella L.) and Chilo suppressalis,which indicated that it may be a new pesticide candidate to Beet Armyworm(Spodopterae exigud).2. The design, synthesis and activity assay of new compounds as potential herbicides safeners. Herbicides safener was also took as herbicides antidote, corn safener or corn protective agent and so on. It can protect the corn from the damage of herbicides without affecting the activity of herbicides to target weeds significantly. Many studies have been conducting in the countries of USA, Germany, Japan, Switzerland and Canada, as well as Russia and Hungary. The study on the mechanism of safeners is important to explain the targets and mode of action of herbicides, and it gives new ideas to develop new herbicides. Herbicides safeners will have broader prospects as a branch of the field of herbicides, however, it have not caused concern in China until80th last century. The study in China was at an elementary step. Recently, with the development of modern agriculture, more and more new herbicides appeared on the market. But herbicides safeners could not keep up with the needs of herbicedes market. Be inspired by the activity of newly developed safener Cyprosulfamide (CSA). we designed and synthesized18CSA derivatives based on the principle of similarity. The structures of the18new compounds was determined by IR,1H-NMR,13C-NMR and HR-MS.The activity as safener of the new compounds was also tested using our own synthesized CSA as the positive control and conclude four parallel groups. The preliminary results indicated that five compounds had the inhibition activity lower than TCM. which could be potential safeners. Although all of these compounds had less protection activity than CSA. the given structure-activity relationship of them was useful for design of more novel potential molecules.