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          | 編輯推薦: |   
          | 1.原创性专著,我国新农药创制的阶段性成果。 |  
         
          | 內容簡介: |   
          | 本专著系统总结了我国新农药创制性的成果——烷基膦酸酯类除草剂的研发总结。从化合物的合成、毒性研究、作用机制,从中试到生产整个程序,为今后我国农药新创制提供一条有效途径。
來源:香港大書城megBookStore,http://www.megbook.com.hk 本书可供广大新农药研发、生产等人员阅读,也可供高等学校农药、植保等相关专业师生阅读。
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          | 關於作者: |   
          | 贺红武,华中师范大学,教授、所长,毕业于华中师范大学化学专业。在日本九州大学获农学博士学位。1989~1990年日本九州大学农学部农药化学研究室访问研究员,1996年晋升教授,1998~1999年德国美因兹大学药物化学研究所访问教授,1999年获博士生导师资格,2001年赴日本九州大学农学研究院农药化学研究室和日本神户大学农学部生物功能研究室进行为期3个月的学术访问。2007,8月-11月:日本九州大学农学研究院农药化学研究室,访问教授。 兼任社会职务:第六届国务院学位委员会植物保护学科评议组成员,中国化工学会农药专业委员会委员 ; 中国植物保护学会农药学分会委员;湖北省化学化工学会理事;湖北省化学化工学会农药专业委员会主任委员《世界农药》、《农药》、《现代农药》、《农药学学报》、《化学与生物工程》、《农药研究与应用》杂志编委。
 长期从事有机化学、农药化学、有机磷化学以及新农药创制研究工作。先后承担国家及省部级的科研项目40余项,连续承担国家七.五,八.五,九.五十.五、十一.五国家新农药创制科技攻关项目。先后承担了六个农药新品种及一个农药增效剂的应用基础研究与工业化开发,其技术和成果在农药工业中得到创新性的应用和发展。为具有我国发明专利权的新型除草剂氯酰草膦(己获农药三证。)的第一发明人。
 在新农药品种的创制研究、技术开发、产业化等工作中获得11项授权中国发明专利, 获得湖北省自然科学奖一等奖, 教育部科技进步一等奖,教育部科技进步二等奖;湖北省科技进步二等奖二项;八?五”国家技术创新优秀项目奖等9项省部级科技奖励。2001年评为湖北省科技精英和全国优秀科技工作者。2009获得建国60周年中国农药工业突出贡献奖。
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          | 目錄: |   
          | 1.Overview. 1.1.Introduction.
 1.1.1.Mode.of.Action.of.Herbicide.
 1.1.2.Herbicide.Resistance.
 1.1.3.New.Opportunity.for.Novel.Herbicides.
 1.1.4.Basic.Methodology.for.Discovery.of.HitLeadCompounds.
 1.2.Pyruvate.Dehydrogenase.Complex.PDHc.
 1.2.1.Function.of.PDHc.
 1.2.2.Distribution.of.PDHc
 1.2.3.Plant.PDHc.E1.as.Site.of.Action.of.Herbicide.
 1.3.Progress.in.the.Research.of.PDHc.Inhibitors.
 1.3.1.OP.Compounds.as.Inhibitors.of.E.coli.PDHc.
 1.3.2.OP.Compounds.as.Inhibitors.of.Plant.PDHc.
 1.3.3.Enzyme-Selective.Inhibition.of.OP.Compounds.
 1.4.Design.of.Novel.PDHc.E1.Inhibitors.as.Herbicides.
 1.4.1.Selecting.Plant.PDHc.E1.as.Target.of.NewHerbicide.
 1.4.2.PDHc.E1.Inhibitor.Acylphosphonate.as.HitCompound.
 1.4.3.Finding.Lead.Structure.IA.
 1.4.4.Optimization.Strategy
 1.5.Book.Chapter.Organization.
 References
 
 2.Alkylphosphonates.
 2.1.Alkyl.or.Substituted.PhenylMethylphosphonates.IA-IF.
 2.1.1.Introduction.
 2.1.2.Synthesis.of.O,O-Dialkyl1-Hydroxyalkylphosphonates.M2.
 2.1.3.Synthesis.of.Substituted.Phenoxyacetic.Acids.Mand.Substituted.Phenoxyacetyl.Chlorides.M5.
 2.1.4.Synthesis.of.IA-IF.
 2.1.5.Spectroscopic.Analysis.of.IA-IF.
 2.1.6.Crystal.Structure.Analysis.of.IC-7.
 2.1.7.Herbicidal.Activity.of.IA-IF.
 2.1.8.Structure-Herbicidal.Activity.Relationships.
 2.1.9.Herbicidal.Activity.of.IC-22.
 2.1.10.Summary.
 2.2.Heterocyclylmethylphosphonates.IG-IJ.
 2.2.1.Introduction.
 2.2.2.Synthesis.of.IG-IJ.
 2.2.3.Spectroscopic.Analysis.of.IG-IJ.
 2.2.4.Crystal.Structure.Analysis.of.IH-18.and.IG-21.
 2.2.5.Herbicidal.Activity.of.IG-IJ.
 2.2.6.Structure-Herbicidal.Activity.Relationships.
 2.2.7.Herbicidal.Activity.of.IG-21.
 2.2.8.Summary.
 2.3.1-Phenyl-1,2,4-Triazol-3-yloxyacetoxyAlkylphosphonates.IK.
 2.3.1.Introduction.
 2.3.2.Synthesis.of.IK.
 2.3.3.Spectroscopic.Analysis.of.IK.
 2.3.4.Herbicidal.Activity.of.IK.
 2.3.5.Summary.
 References
 
 3.Salts.of.Alkylphosphonates.
 3.1.Alkali.Metal.Salts.of.O-Alkyl.Alkylphosphonic
 Acids.IIA-IIE.
 3.1.1.Introduction.
 3.1.2.Synthesis.of.IIA-IIE.
 3.1.3.Spectroscopic.Analysis.of.IIA-IIE.
 3.1.4.Crystal.Structure.Analysis.of.IIB-20.
 3.1.5.Herbicidal.Activity.of.IIA-IIE.
 3.1.6.Summary.
 3.2.Alkali.Metal.Salts.of.Alkylphosphonic.Acids.IIF,IIGandIIH.
 3.2.1.Introduction.
 3.2.2.Synthesis.of.IIF,.IIG.and.IIH.
 3.2.3.Spectroscopic.Analysis.of.IIF,.IIG.and.IIH.
 3.2.4.Herbicidal.Activity.of.IIF,.IIG.and.IIH.
 3.2.5.Summary.
 3.3.t-Butylaminium.Salts.of.Alkylphosphonates.IIJ.
 3.3.1.Introduction.
 3.3.2.Synthesis.of.IIJ
 3.3.3.Spectroscopic.Analysis.of.IIJ.
 3.3.4.Crystal.Structure.Analysis.of.IIJ-
 3.3.5.Herbicidal.Activity.of.IIJ.
 3.3.6.Summary.
 References
 
 4.Alkylphosphinates.
 4.1.Alkylphosphinates.IIIA-IIIG.
 4.1.1.Introduction.
 4.1.2.Synthesis.of.DichloroMethylPhosphine.M10.
 4.1.3.Synthesis.of.O-Methyl.1-Hydroxyalkyl-Methylphosphinates.M12.
 4.1.4.Synthesis.of.IIIA-IIIG.
 4.1.5.Spectroscopic.Analysis.of.IIIA-IIIG.
 4.1.6.Crystal.Structure.Analysis.of.IIIE-
 4.1.7.Herbicidal.Activity.of.IIIA-IIIG.
 4.1.8.Summary.
 4.2.Sodium.Salts.of.Alkylphosphinic.Acids.IIIH.
 4.2.1.Introduction.
 4.2.2.Synthesis.of.IIIH
 4.2.3.Spectroscopic.Analysis.of.IIIH.
 4.2.4.Herbicidal.Activity.of.IIIH.
 4.2.5.Summary.
 4.3.[5-Methylisoxazol-3-yloxyacetoxyAlkyl]-Methylphosphinates.IIIJ.
 4.3.1.Introduction.
 4.3.2.Synthesis.of.IIIJ.
 4.3.3.Spectroscopic.Analysis.of.IIIJ.
 4.3.4.Herbicidal.Activity.of.IIIJ.
 4.3.5.Summary.
 References
 
 5.Cyclic.Phosphonates.and.Caged.Bicyclic.Phosphates.
 5.1.Cyclic.1-Hydroxyalkylphosphonates.IVA.and.IVB
 5.1.1.Introduction.
 5.1.2.Synthesis.of.IVA.and.IVB.
 5.1.3.Spectroscopic.Analysis.of.IVA.and.IVB.
 5.1.4.Crystal.Structure.Analysis.of.IVA-3.
 5.1.5.Herbicidal.Activity.of.IVA.and.IVB.
 5.1.6.Summary.
 5.2.Cyclic.Alkylphosphonates.IVC-IVF.
 5.2.1.Introduction.
 5.2.2.Synthesis.of.IVC-IVF.
 5.2.3.Spectroscopic.Analysis.of.IVC-IVF.
 5.2.4.Crystal.Structure.Analysis.of.IVC-
 5.2.5.Herbicidal.Activity.of.IVC-IVF.
 5.2.6.Summary.
 5.3.Caged.Bicyclic.Phosphates.IVG.and.IVH.
 5.3.1.Introduction.
 5.3.2.Synthesis.of.IVG.and.IVH.
 5.3.3.Spectroscopic.Analysis.of.IVG.and.IVH.
 5.3.4.Crystal.Structure.Analysis.of.IVG-
 5.3.5.Herbicidal.Activity.of.IVG.and.IVH.
 5.3.6.Summary.
 References
 
 6.Optically.Active.Alkylphosphonates.
 6.1.Optically.Active.1-Hydroxyalkylphosphonates.IVB.and.M2.
 6.1.1.Introduction.
 6.1.2.Asymmetric.Synthesis.of.1-Hydroxyalkylphosphonates
 IVB.and.M2.via.Hydrophosphonylation.
 6.1.3.Asymmetric.Synthesis.of.1-HydroxyalkylphosphonatesM2.via.Hydroxylation
 6.1.4.Summary.
 6.2.Optically.Active.Substituted.Phenylmethylphosphonates.IA,IEandIF.
 6.2.1.Introduction.
 6.2.2.Synthesis.of.Optically.Active.IA,.IE.and.IF.
 6.2.3.Herbicidal.Activity.of.Optically.Active.IA,IEandIF.
 6.2.4.Summary.
 6.3.Optically.Active.Substituted.Ethylphosphonates.IA.and.IC.
 6.3.1.Introduction.
 6.3.2.Synthesis.of.Optically.Active.IA.and.IC.
 6.3.3.Herbicidal.Activity.of.Optically.Active.IA.and.IC.
 6.3.4.Aquatic.Toxicity.of.Optically.Active.IA.and.IC.
 6.3.5.Summary.
 References
 
 7.Biochemical.Mechanism.of.Alkylphosphonates.
 7.1.Molecular.Docking.and.3D-QSAR.Studies.
 7.1.1.Introduction.
 7.1.2.Binding.Conformational.Analysis.
 7.1.3.CoMFA.and.CoMSIA.Analysis.
 7.1.4.Validation.of.the.3D-QSAR.Models.
 7.1.5.Molecular.Docking.
 7.1.6.Molecular.Alignment.and.3D-QSAR.Modeling.
 7.1.7.CoMFA.Analysis.and.CoMSIA.Analysis.Modeling.
 7.1.8.PLS.Calculations.and.Validations.
 7.1.9.Summary.
 7.2.Enzyme.Inhibition.
 7.2.1.Introduction.
 7.2.2.Inhibitory.Potency.Against.Plant.PDHc.
 7.2.3.Kinetic.Experiment.of.PDHc.
 7.2.4.Selective.Enzyme.Inhibition.
 7.2.5.Structure-Activity.Relationships.
 7.2.6.Assay.of.PDHc.from.Plant.
 7.2.7.Assay.of.PDHc.from.E.coli.and.Pig.Heart.
 7.2.8.Assay.of.Other.Enzymes.
 7.2.9.Summary.
 References.
 
 8.Evaluation.and.Application.of.Clacyfos.and.HWS.
 8.1.Evaluation.of.Clacyfos.
 8.1.1.Introduction.
 8.1.2.Physiochemical.Properties.
 8.1.3.Stability.of.Clacyfos.
 8.1.4.Herbicidal.Activity.in.Greenhouse.
 8.1.5.Systemic.Property.of.Clacyfos.
 8.1.6.Rainfast.Characteristics.of.Clacyfos.
 8.1.7.Field.Trials.of.Clacyfos.
 8.1.8.Toxicity.Evaluation.
 8.1.9.Environmental.Fate.
 8.1.10.Residues.
 8.1.11.Adsorption.of.Clacyfos.on.Soils.
 8.1.12.Ecological.Effects.
 8.1.13.Summary.
 8.2.Evaluation.of.HWS.
 8.2.1.Introduction.
 8.2.2.Physiochemical.Properties.
 8.2.3.Herbicidal.Activity.in.Greenhouse.
 8.2.4.Systemic.Property.of.HWS.
 8.2.5.Rainfast.Characteristics.of.HWS.
 8.2.6.Field.Trials.of.HWS.
 8.2.7.Toxicity.Evaluation.
 8.2.8.Ecological.Effects.
 8.2.9.Summary.
 
 References.
 9.General.Methodology.
 9.1.General.Synthetic.Procedure.
 9.1.1.Chemicals,.Reagents,.and.Solvents.
 9.1.2.O,O-Dialkyl.Phosphonates.M1.
 9.1.3.O,O-Dialkyl.1-Hydroxyalkylphosphonates.M2.
 9.1.4.O,O-Dialkyl.1-Chloroacetoxy-Alkylphosphonates.M3.
 9.1.5.Substituted.Phenoxyacetic.Acids.M4.
 9.1.6.Substituted.Phenoxyacetyl.Chlorides.M5.
 9.1.7.O,O-Dialkyl.1-Substituted.Phenoxyacetoxy-Alkylphosphonates.IA-IJ.
 9.1.8.Phenylhydrazinecarboxamide.M6.and.SodiumTriazol-3-olate.M7.
 9.1.9.1-Phenyl-1,2,4-Triazol-3-yloxyacetoxy-Alkylphosphonates.IK.
 9.1.10.Alkali.Metal.Salts.of.O-Alkyl.AlkylphosphonicAcids.IIA-IIE.
 9.1.11.O,O-BisTrimethylsilyl.AlkylphosphonatesM8.and.Alkylphosphonic.Acids.M9.
 9.1.12.Alkali.Metal.Salts.of.AlkylphosphonicAcids.IIF-IIH.
 9.1.13.t-Butylaminium.Salts.of.Alkylphosphonates.IIJ.
 9.1.14.DichloroMethylPhosphine.M10.
 9.1.15.O-Methyl.Methylphosphinate.M11.
 9.1.16.O-Methyl.1-HydroxyalkylMethylphosphinatesM12.
 9.1.17.Alkylphosphinates.IIIA-IIIG.
 9.1.18.Sodium.Salts.of.Alkylphosphinic.Acids.IIIH.
 9.1.19.3-Hydroxy-5-Methylisoxazole.DerivativesM13-M16.
 9.1.20.O-Methyl.[1-5-Methylisoxazol-3-yloxyacetoxy-Alkyl]Methylphosphinates.IIIJ.
 9.1.21.1-Phenyl-2,2-Dimethyl-1,3-Propanediol.M17.
 9.1.22.Cyclic.Phosphonates.M18.
 9.1.23.Cyclic.1-Hydroxyalkylphosphonates.IVA.and.IVB.
 9.1.24.Substituted.Phenoxypropionic.Acids.M19.
 9.1.25.Substituted.Phenoxypropionyl.Chlorides.M20.
 9.1.26.Cyclic.Alkylphosphonates.IVC-IVF.
 9.1.27.4-Hydroxymethyl-2,6,7-Trioxa-1-Phosphabicyclo-[2.2.2]Octane-1-OneThione.M21M22.
 9.1.28.Caged.Bicyclic.Phosphates.IVG.and.IVH.
 9.1.29.Optically.Active.Cyclic.1-HydroxyalkylphosphonatesIVB.
 9.1.30.O,O-Diethyl.Substituted.BenzylPhosphonatesM23.
 9.1.31.Optically.Active.1-Hydroxyalkylphosphonates.M2.
 9.1.32.Optically.Active.Substituted.Phenyl-Methylphosphonates.IA,.IE,.and.IF.
 9.1.33.1-Keto.Phosphonates.M24.and.VinylphosphonatesM25.
 9.1.34.Optically.Active.1-Substituted.EthylphosphonatesIAandIC.
 9.2.General.Information.of.Structural.Characterization.
 9.3.Herbicidal.Activity.Assay.
 9.3.1.Test.in.Petri.Dishes.
 9.3.2.Test.in.Greenhouse.
 References.
 Index.
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