设计、合成了一系列杂环类Protox抑制剂，测定其除草活性，研究其构效关系，发现了几个高活性化合物。尤其是化合物18b，在37.5 g/hm2的剂量下，对供试杂草的抑制活性也均达到了100%，略高于Fluazolate，是一个很有研究价值的新化合物。.以取代苯基1,3-丁二酮为原料，经闭环、脱水、氧化、酯化、烷基化等反应合成了一系列取代苯基异噁唑衍生物，大部分化合物具有较高除草活性，异噁唑环4位为氯取代化合物的活性与4位为氢的化合物活性相差不显著。制备了代表性化合物4a、4b的单晶，利用X-ray测定了其结构，研究表明对于这类化合物，苯环与异噁唑环的夹角大小并不是活性高低的决定因素。.设计、合成了一系列吡唑基苯并噁唑衍生物，活性测试结果表明：当吡唑环的4位无取代基时，化合物活性很低；而当吡唑环的4位为氯或溴取代时，化合物活性很高。这表明吡唑4位卤素取代对此类化合物的活性至关重要。

A several novel heterocyclic Protox inhibitors were prepared. And their herbicidal activity, structure-activity relationship were studied. Some of them exhibit high herbicidal activity to the tested gramineous weeds and latifoliate weeds. Especially, compound 18b can totally kill all tested weeds at a low dosage of 37.5 g/hm2, even a little higher than Fluazolate, is a promising new compound..The several novel 3-substituted phenyl isoxazole derivatives were prepared from substituted phenyl-butan-1,3-dione, via a serial of reactions included ring closure, dehydration, oxidation, alkylation, esterification, etc. Preliminary bioassay showed that most compounds had good activity to various weeds. And the compounds which are unsubstituted on isoxazole moiety showed similar activity with those 4-chloro-isoxazole derivatives. X-ray structure analyses of typical compounds 4a and 4b were done. The results indicated that the dihedral angles of the phenyl ring with the isoxazole ring in those compounds were not the key point of their activity..A series of new substituted pyrazolyl benzoxazole derivatives were prepared. Preliminary bioassay showed that when no substituted on pyrazole position 4, there were no herbicidal activity or low activity, but when halogen (such as chlorine or bromine) is on pyrazole, most of them showed good herbicidal efficacy.

设计、合成了一系列杂环类Protox抑制剂，测定其除草活性，研究其构效关系，发现了几个高活性化合物。尤其是化合物18b，在37.5 g/hm2的剂量下，对供试杂草的抑制活性也均达到了100%，略高于Fluazolate，是一个很有研究价值的新化合物。以取代苯基1,3-丁二酮为原料，经闭环、脱水、氧化、酯化、烷基化等反应合成了一系列取代苯基异噁唑衍生物，大部分化合物具有较高除草活性，异噁唑环4位为氯取代化合物的活性与4位为氢的化合物活性相差不显著。制备了代表性化合物4a、4b的单晶，利用X-ray测定了其结构，研究表明对于这类化合物，苯环与异噁唑环的夹角大小并不是活性高低的决定因素。设计、合成了一系列吡唑基苯并噁唑衍生物，活性测试结果表明：当吡唑环的4位无取代基时，化合物活性很低；而当吡唑环的4位为氯或溴取代时，化合物活性很高。这表明吡唑4位卤素取代对此类化合物的活性至关重要。