吲哚磺酰脲类化合物的合成与生物测定

Based on the QSAR results of ALS inhibitors, we synthesized a series of new sulfonylurea compounds , which of the hebicidal activities were tested through primary and binary bioassay in green house, and the IC50 results were also obtained on some special broad leaf and grass weeds. The field activities were tested in China and Europe. Thus,we selected out the best one SY4, the efficient dosage is 15g/ha. The regulation activity appeared in 40 days that SY4 was used and the weeds were killed in the rice field. The fact verified our molecular design theory that the herbicidal lead compounds can be developed from regulators. The second period toxic tests of SY4 have been finished and the third term are continued. Two formulations were developed as wet powder and suspending agent. On the other hand, we studied the synthesis methods of indole intermediate by means of Fischer rearrangment reaction, sodium bisulfite or zincum reduction, the last one is successful in industrial means. We also won the project of "10th five-year plan of National Key Technologies R&D Program " about "Pesticidal development" . During this period, we delivered four papers, one of which was accepted by SCI, applied 2 patents and were awarded "CCS-BASF Youth knowledge innovation Prize".

本课题以创制吲哚磺酰脲类超高效除草剂为目标。已发现除草活性高于杜邦产品豆磺隆的先导化合物，据现有实验结果，仍有研究潜力。本课题将深入研究吲哚中间体的合成方法，继续合成该类衍生物，测定各化合物对典型敏感性植物的抑制中浓度、杀草谱、对作物的选择性和动物毒性，确定待开发的化合物后、优化合成路线选择适应于工业化生产的反应条件。