环境友好型烃基膦酸酯类除草剂

定　价：¥280.00

作　者：	贺红武，彭浩，谭效松著
出版社：	化学工业出版社
丛编项：
标　签：	农业/林业植物保护

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ISBN：	9787122213815	出版时间：	2015-03-01	包装：	精装
开本：	16开	页数：	455	字数：

内容简介

《环境友好型烃基膦酸酯类除草剂》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。
　　《环境友好型烃基膦酸酯类除草剂》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。

作者简介

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。

图书目录

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 Hit/Lead Compounds
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 New Herbicide
1.4.2 PDHc E1 Inhibitor Acylphosphonate as Hit Compound
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 Phenyl）Methylphosphonates IA-IF
2.1.1 Introduction
2.1.2 Synthesis of O，O-Dialkyl
1-Hydroxyalkylphosphonates M2
2.1.3 Synthesis of Substituted Phenoxyacetic Acids M and 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-yloxyacetoxy） Alkylphosphonates 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 Dichloro（Methyl）Phosphine 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-yloxyacetoxy）Alkyl]-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-Hydroxyalkylphosphonates M2.via Hydroxylation
6.1.4 Summary
6.2 Optically Active （Substituted Phenyl）methylphosphonates 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 Sodium Triazol-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 Alkylphosphonic Acids IIA-IIE
9.1.11 O，O-Bis（Trimethylsilyl） Alkylphosphonates M8.and Alkylphosphonic Acids M9
9.1.12 Alkali Metal Salts of Alkylphosphonic Acids IIF-IIH
9.1.13.t-Butylaminium Salts of Alkylphosphonates IIJ
9.1.14 Dichloro（Methyl）Phosphine M10
9.1.15 O-Methyl Methylphosphinate M11
9.1.16 O-Methyl （1-Hydroxyalkyl）Methylphosphinates M12
9.1.17 Alkylphosphinates IIIA-IIIG
9.1.18 Sodium Salts of Alkylphosphinic Acids IIIH
9.1.19.3-Hydroxy-5-Methylisoxazole Derivatives M13-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-One/Thione M21/M22
9.1.28 Caged Bicyclic Phosphates IVG and IVH
9.1.29 Optically Active Cyclic 1-Hydroxyalkylphosphonates IVB
9.1.30 O，O-Diethyl （Substituted Benzyl）Phosphonates M23
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 Ethylphosphonates IAandIC
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