益硫磷 | 116-01-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机二硫代磷酸及其衍生物
• 中文名称: 益硫磷
• 中文别名: 益果粉剂、可湿性粉剂、颗粒剂；益果；S-乙基氨基甲酰甲基-二甲基二硫代磷酸酯；OMS252；EMF25506
• 英文名称: ethoate-methyl
• 英文别名: O,O-Dimethyl-S-(N-ethyl-carbamoylmethyl)-phosphorodithioat；Di-O-methyl-S-(N-ethyl-carbamoylmethyl)-dithiophosphat；Dimethoxythiophosphorylmercapto-essigsaeure-aethylamid；2-dimethoxyphosphinothioylsulfanyl-N-ethylacetamide
• CAS: 116-01-8
• 化学式: C₆H₁₄NO₃PS₂
• 分子量: 243.288
• InChiKey: DICRHEJCQXFJBY-UHFFFAOYSA-N

物化性质

• 熔点：
  66.1°C
• 密度：
  1.1640 g/cm3(Temp: 70 °C)
• 颜色/状态：
  WHITE CRYSTALLINE SOLID
• 气味：
  SLIGHTLY AROMATIC ODOR
• 溶解度：
  In water, 8.5X10+3 mg/L at 25 °C
• 蒸汽压力：
  9.25X10-6 mm Hg at 25 °C (est)
• 稳定性/保质期：
  STABLE IN AQUEOUS SOLN BUT HYDROLYZED BY ALKALI AT ROOM TEMPERATURE
• 分解：
  When heated to decomposition it emits very toxic fumes of /nitrogen oxides, phosphorous oxides, and sulfur oxides/.
• 折光率：
  INDEX OF REFRACTION: 1.5225 @ 70 °C/D

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  13
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  105
• 氢给体数：
  1
• 氢受体数：
  5

ADMET

代谢

血浆和组织酶负责将有机磷化合物水解成相应的磷酸和磷onic酸。然而，氧化酶也参与一些有机磷化合物的代谢。抗胆碱酯酶剂

Plasma and tissue enzymes are responsible for hydrolysis /of organophosphorus compounds/ to the corresponding phosphoric and phosphonic acids. However, oxidative enzymes are also involved in the metabolism of some organophosphorus compounds. /Anticholinesterase agents/

来源:Hazardous Substances Data Bank (HSDB)

代谢

有机磷抗胆碱酯酶剂在体内被一组称为A-酯酶或对氧磷酶的酶水解。这些酶存在于血浆和肝脏中，能够水解大量的有机磷化合物...通过断裂磷酯键、酐键、P-F键或P-CN键。/抗胆碱酯酶剂/

The organophosphorus anticholinesterase agents are hydrolyzed in the body by a group of enzymes known as A-esterases or paraoxonases. These enzymes are found in the plasma and liver and hydrolyze a large number of organophosphorus compounds ... by cleaving the phosphoester, anhydride, P-F, or P-CN bonds. /Anticholinesterase agents/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 副作用

其他毒物 - 有机磷

Other Poison - Organophosphate

来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases

毒理性

• 相互作用

在长期治疗中，肾上腺皮质激素对抗抗胆碱酯酶的抗青光眼作用（增加眼压）。... 抗胆碱药对抗抗胆碱酯酶对自主神经和中枢神经系统的缩瞳（抗青光眼）和其他毒蕈碱样作用。三环类抗抑郁药（抗胆碱能效应）对抗抗胆碱酯酶在青光眼中的抗青光眼（缩瞳）作用。... 具有抗胆碱能效应的抗组胺药对抗抗胆碱酯酶的缩瞳（抗青光眼）和CNS作用。抗胆碱酯酶增强抗组胺药引起的镇静和行为改变。抗胆碱酯酶药物对自主效应细胞的作用，在一定程度上对中枢神经系统的作用，被阿托品这种首选解毒剂所拮抗。巴比妥类药物的作用被抗胆碱酯酶增强。... 二泛醇增强抗胆碱酯酶的效果。氟磷酸盐杀虫剂增强其他抗胆碱酯酶的效果。/抗胆碱酯酶/

In long term therapy, adrenocorticoids antagonize the antiglaucoma effects of anticholinesterases (incr ocular pressure). ... Anticholinergics antagonize the miotic (antiglaucoma) & other muscarinic effects of anticholinesterases on the autonomic & central nervous systems. Tricyclic antidepressants (anticholinergic effects) antagonize the antiglaucoma (miotic) effects of anticholinesterases in glaucoma. ... Antihistamines with anticholinergic effects antagonize the miotic (antiglaucoma) & CNS effects of anticholinesterases. Anticholinesterases potentiate tranquilizing & behavioral changes induced by antihistamines. The actions of anticholinesterase agents on autonomic effector cells, & to some extent those on CNS, are antagonized by atropine, an antidote of choice. Barbiturates are potentiated by anticholinesterases. ... Dexpanthenol potentiates the effects of anticholinesterases. Fluorophosphate insecticides potentiate the effects of other anticholinesterases. /Anticholinesterases/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

巴比妥类药物可被抗胆碱酯酶增强。尽管巴比妥类药物可以谨慎用于治疗癫痫，但在处理由于抗胆碱酯酶导致的毒物中毒时，必须极度小心，特别是对于有机磷农药。毒扁豆碱是一种用作缩瞳剂胆碱酯酶抑制剂，它增强其他此类抑制剂的效果...用于其他目的（附加效果）或可能的协同作用。接触有机磷杀虫剂的人必须采取严格预防措施。...有机磷杀虫剂：附加的抗胆碱酯酶效果。危险。使用抗胆碱酯酶的患者（甚至是局部使用的，如眼药水）应避免去最近使用过有机磷杀虫剂的地方。/抗胆碱酯酶/

Barbiturates are potentiated by anticholinesterases. Although barbiturates may be used cautiously in treating convulsions, extreme care is essential in handling poisonings due to anticholinesterases, particularly organophosphorus pesticides. Echothiophate, a cholinesterase inhibitor used as miotic, potentiates other such inhibitors ... Used for other purposes (additive effects) or possibly synergistic. Those exposed to organophosphate insecticides must take strict precautions. ... Organophosphorus insecticides: additive anticholinesterase effects. Hazardous. Patients on anticholinesterases (even topical, such as eye drops) should avoid areas where organophosphorus insecticides ...recently ...used. /Anticholinesterase/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

抗胆碱酯酶（有机磷）杀虫剂会对抗极化肌肉松弛剂。吩噻嗪类/和硫杂蒽类/：... 可能增强有机磷杀虫剂的有毒效果。/杀虫剂，有机磷/

Anticholinesterase (organophosphorus) insecticides antagonize polarizing muscle relaxants. Phenothiazines /and thioxanthenes/: ... May enhance toxic effects of organophosphorus insecticides. /Insecticides, organophosphorus/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

一个昏迷的病人，全身出汗，瞳孔缩小，衣物或呼吸中有杀虫剂的气味，并且肌肉出现颤动，这是有机磷中毒的典型表现。... 管理的具体步骤包括以下内容。1. 去污。... 2. 气道。如有必要，建立气道。... 3. 呼吸状态。事实上，这些病人由于多种原因经常出现呼吸窘迫。... 4. 心脏监测。... 5. 胆碱酯酶水平。... 6. 普瑞洛昔姆。普瑞洛昔姆是有机磷中毒的首选治疗方法，应几乎用于所有临床上有显著有机磷中毒的病人，特别是那些肌肉颤动和虚弱的病人。... 7. 阿托品。阿托品是有机磷中毒的生理性拮抗剂。当怀疑有机磷中毒时，应基于临床情况给予试验剂量的阿托品。/有机磷中毒/

A comatose patient who is diaphoretic, has pinpoint pupils and the odor of an insecticide on clothing or breath, and is noted to have muscle fasciculations represents the classic presentation of organophosphate poisoning. ... Specific steps in management include the following. 1. Decontamination. ... 2 Airway. Establish an airway if necessary. ... 3. Respiratory Status. Respiratory distress, in fact, is commonly found in these patients from multiple causes. ... 4. Cardiac Monitoring. ... 5. Cholinesterase Level. ... 6. Pralidoxime. Pralidoxime is the treatment of choice for organophosphate poisoning and should be used for nearly all patients with clinically significant orgnophosphate poisoning, particularly whose patients with muscular fasciculations and weakness. ... 7. Atropine. Atropine is the physiologic antidote for organophosphate poisoning. A trial dose of atropine should be instituted on clinical ground when one suspects organophosphate intoxication. /Organophosphate poisoning/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

大多数有机磷化合物能够通过皮肤、结膜、胃肠道和肺部被吸收。/有机磷化合物/

Most organophosphate compounds are ... absorbed from skin, conjunctiva, gastrointestinal tract, & lung. /Organophosphate compounds/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

有机磷杀虫剂的皮肤吸收率可能会受到所使用溶剂的影响。

The rate of dermal absorption /of organophosphorus pesticides/ may be ... influenced by the solvent used. /Organophosphorus insecticides/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

许多有机磷杀虫剂会通过牛奶排出体外...有机磷杀虫剂

Many of /the organophosphorus insecticides/ are excreted in the milk ... /Organophosphorus insecticides/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

有毒物质可以通过吸入、摄入和皮肤渗透被吸收。在肝脏和其他组织中，它们通常在吸收后的几小时内经历水解降解。降解产物毒性较低，并通过尿液和粪便排出体外。/有机磷胆碱酯酶抑制剂类农药/

Toxicants can be absorbed by inhalation, ingestion, and skin penetration. ... All undergo hydrolytic degradation in liver and other tissues, usually within hr of absorption. Degradation products are of low toxicity, and are excreted in urine and feces. /Organophosphate cholinesterase-inhibiting pesticides/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

它们...通过消化系统、呼吸系统和皮肤的粘膜迅速吸收，并通过血液输送到各种身体组织。......主要的排泄途径...是肾脏。/有机磷农药/

/They/ ...are rapidly absorbed through mucous membrane of digestive system, respiratory system and the skin, and conveyed by the blood to various body tissues. ...The main route of elimination ... /is/ the kidneys. /Organophosphorus pesticides/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险等级：
  6.1(b)
• 危险品标志：
  Xn
• 海关编码：
  2930909063
• 危险类别：
  6.1(b)
• 安全说明：
  S36/37
• 危险类别码：
  R21/22
• 包装等级：
  III
• 危险品运输编号：
  UN 2783

制备方法与用途

类别：农药

• 毒性分级：高毒
• 急性毒性：
  • 口服-大鼠 LD50: 125毫克/公斤
  • 口服-小鼠 LD50: 350毫克/公斤

可燃性危险特性：受热分解产生有毒氧化磷、氧化硫及氧化氮气体。

储运特性：

• 库房通风、低温干燥保存
• 与食品原料分开储存和运输

灭火剂：砂土、干粉或泡沫

反应信息

• 作为产物：
  描述：

  2-氯-N-乙基乙酰胺 、 O,O-二甲基二硫代磷酸盐,钾盐 以 水 、 甲苯 为溶剂， 生成 益硫磷
  参考文献：
  名称：

  O,O-Dialkyl S-(carbamoylalkyl) phosphorodithioates

  摘要：

  DOI：

  10.1021/jo01351a033

文献信息

• [EN] MICROBIOCIDAL OXADIAZOLE DERIVATIVES<br/>[FR] DÉRIVÉS D'OXADIAZOLE MICROBIOCIDES
  申请人：SYNGENTA PARTICIPATIONS AG

  公开号：WO2017157962A1

  公开（公告）日：2017-09-21

  Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially fungicides.

  式(I)的化合物，其中取代基如权利要求1所定义，作为杀虫剂特别是杀菌剂有用。
• Thieno-pyrimidine compounds having fungicidal activity
  申请人：Brewster Kirkland William

  公开号：US20070093498A1

  公开（公告）日：2007-04-26

  The present invention relates to thieno[2,3-d]-pyrimidine compounds having fungicidal activity.

  本发明涉及具有杀真菌活性的噻吩[2,3-d]-嘧啶化合物。
• [EN] INSECTICIDAL TRIAZINONE DERIVATIVES<br/>[FR] DÉRIVÉS DE TRIAZINONE INSECTICIDES
  申请人：SYNGENTA PARTICIPATIONS AG

  公开号：WO2013079350A1

  公开（公告）日：2013-06-06

  Compounds of the formula (I) or (I'), wherein the substituents are as defined in claim 1, are useful as pesticides.

  式(I)或(I')的化合物，其中取代基如权利要求1所定义的那样，可用作杀虫剂。
• Novel insecticides
  申请人：Syngenta Participations AG

  公开号：EP2540718A1

  公开（公告）日：2013-01-02

  Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.

  式I的化合物 其中取代基如权利要求1所定义，并且式I化合物的农药可接受盐以及所有立体异构体和互变异构形式可用作杀虫剂，并且可以按照已知的方法制备。
• Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
  申请人：Dow AgroSciences LLC

  公开号：US20180279612A1

  公开（公告）日：2018-10-04

  This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).

  这份披露涉及具有对节肢动物门、软体动物门和线虫门害虫具有杀虫效用的分子领域，用于生产此类分子的过程，用于此类过程的中间体，含有此类分子的杀虫组合物，以及使用此类杀虫组合物对抗此类害虫的过程。这些杀虫组合物可以用作螨虫剂、杀虫剂、螨虫剂、软体动物杀虫剂和线虫杀虫剂。本文件披露了具有以下式（“式一”）的分子。