Synthesis and Biological Evaluation of Novel N-Benzoxazolonyluracils as Protox-Inhibitor  

作　　者：侯仲轲 任叶果 雷满香 黄明智 宋健 陈立功 

机构地区：[1]School of Pharmaceutical and Technology, Tianjin University, Tianjin 300072, China [2]Hunan Research Institute of Chemical Industry, Changsha 410007, China

出　　处：《Transactions of Tianjin University》2005年第1期26-29,共4页天津大学学报（英文版）

基　　金：SupportedbyHunanNaturalScienceFoundation(No. 02JJY2017)andNationalNaturalScienceFoundationofChina(No. 20372021).

摘　　要：Protoporphyrinogen oxidase inhibitor has become the focus research field as herbicides.Seven novel N-benzoxazolonyluracils were obtained by cyclization of 6-aminobenzoxazolone derivatives with ethyl 3-dimethylcarbamoylamido-4,4,4-trifluorocrotonate and then methylation or amination, and the reaction yields were between 5900—8600. The chemical structures of the compounds were identified by Elemental Analysis, MS and 1H NMR. Biological results indicate that some compounds exhibit excellent control of broadleaf weeds at post-emergence by low dosage 18.75 ga.i/ha, but are not effective for grass weeds below dosage 37.5 ga.i/ha. In addition, these compounds show no damage at high-dosage 150 ga.i/ha to wheat and corn, but are unsafe to dicotyledonous plants such as cole, soybean and sorghum even at lower dosage 18.75 ga.i/ha.Protoporphyrinogen oxidase inhibitor has become the focus research field as herbicides.Seven novel N-benzoxazolonyluracils were obtained by cyclization of 6-aminobenzoxazolone derivatives with ethyl 3-dimethylcarbamoylamido-4,4,4-trifluorocrotonate and then methylation or amination, and the reaction yields were between 59~0_0—86~0_0. The chemical structures of the compounds were identified by Elemental Analysis, MS and ~1H NMR. Biological results indicate that some compounds exhibit excellent control of broadleaf weeds at post-emergence by low dosage 18.75 ga.i/ha, but are not effective for grass weeds below dosage 37.5 ga.i/ha. In addition, these compounds show no damage at high-dosage 150 ga.i/ha to wheat and corn, but are unsafe to dicotyledonous plants such as cole, soybean and sorghum even at lower dosage 18.75 ga.i/ha.

关 键 词：N-benzoxazolonyluracil protox-inhibitor SYNTHESIS biological evaluation 

分 类 号：S482.4[农业科学—农药学]