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Synthesis and Biological Evaluation of Novel N-Benzoxazolonyluracils as Protox-Inhibitor
作者姓名:侯仲轲  任叶果  雷满香  黄明智  宋健  陈立功
作者单位:[1]SchoolofPharmaceuticalandTechnology,TianjinUniversity,Tianjin300072,China//HunanResearchInstituteofChemicalIndustry,Changsha410007,China [2]HunanResearchInstituteofChemicalIndustry,Changsha410007,China [3]SchoolofPharmaceuticalandTechnology,TianjinUniversity,Tianjin300072,China
基金项目: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 59%-86%. 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:合成  生物学评价  N-苯并噁唑酮基尿嘧啶  原卟啉原氧化酶抑制剂  植物生长调节剂

Synthesis and Biological Evaluation of Novel N-Benzoxazolonyluracils as Protox-Inhibitor
HOU Zhongke,Ren Yeguo,LEI Manxiang,Huang Mingzhi,SONG Jian,Chen Ligong.Synthesis and Biological Evaluation of Novel N-Benzoxazolonyluracils as Protox-Inhibitor[J].Transactions of Tianjin University,2005,11(1):26-29.
Authors:HOU Zhongke  Ren Yeguo  LEI Manxiang  Huang Mingzhi  SONG Jian  Chen Ligong
Institution:1. School of Pharmaceutical and Technology, Tianjin University, Tianjin 300072, China;Hunan Research Institute of Chemical Industry, Changsha 410007, China
2. Hunan Research Institute of Chemical Industry, Changsha 410007, China
3. School of Pharmaceutical and Technology, Tianjin University, Tianjin 300072, China
Abstract: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 590%-860%. 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.
Keywords:N-benzoxazolonyluracil  protox-inhibitor  synthesis  biological evaluation
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