Arsenic pentoxide | 1303-28-2

• 分子结构分类: 无机化合物 - 混合金属/非金属化合物 - 类金属有机物
• 英文名称: Arsenic pentoxide
• CAS: 1303-28-2
• 化学式: As₂O₅
• 分子量: 229.84
• InChiKey: COHDHYZHOPQOFD-UHFFFAOYSA-N

物化性质

• 密度：
  4.32
• 物理描述：
  Arsenic pentoxide appears as a white crystalline solid. Noncombustible. Corrosive to metals in the presence of moisture. Toxic by ingestion.
• 颜色/状态：
  White amorphous powder
• 熔点：
  315 °C
• 闪点：
  Not flammable (EPA, 1998)
• 溶解度：
  In water, 65.8 g/100 g at 20 °C
• 稳定性/保质期：
  1. 如果按照规定使用和储存，不会分解，未发现有已知危险反应。避免接触酸、碱、卤素及卤素化合物。具有潮解性，在315℃以上时会分解为氧气和三氧化二砷。在水中溶解后形成砷酸；将其加热至130℃蒸发冷却时，则变成蜂蜜状黏性的液体。放置于硫酸干燥器中，可得到美观且透明的H3AsO4·1/2H2O结晶；而在-30℃下放置几天之后，则会生成H3AsO4·2H2O结晶。另外，将H3AsO4水溶液加热至175℃浓缩时，会产生As2O5·5/3H2O。 2. 稳定性：稳定。 3. 禁配物：酸类、卤素、水及水蒸气。 4. 避免接触的条件：潮湿空气。 5. 聚合危害：不聚合。 6. 分解产物：氧化砷。
• 分解：
  Arsenic pentoxide is thermally unstable & begins to decompose near the melting point, about 300 °C. The vapor obtained is /completely/ dissociated into oxygen & arsenic trioxide.
• 腐蚀性：
  Corrosive to metals in the presence of moisture.

计算性质

• 辛醇/水分配系数(LogP)：
  -1.31
• 重原子数：
  7
• 可旋转键数：
  0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  77.5
• 氢给体数：
  0
• 氢受体数：
  5

ADMET

代谢

砷主要通过吸入或摄入进入人体，其次是皮肤接触。进入人体后，砷会在全身分布，根据需要被还原成亚砷酸盐，然后通过亚砷酸盐甲基转移酶被甲基化成单甲基砷（MMA）和二甲基硅酸（DMA）。砷及其代谢物主要通过尿液排出体外。已知砷能诱导金属结合蛋白金属硫蛋白，通过绑定砷和其他金属并使其生物活性失效，以及作为抗氧化剂的作用，从而减少砷和其他金属的毒性效应。

Arsenic is absorbed mainly by inhalation or ingestion, as to a lesser extent, dermal exposure. It is then distributed throughout the body, where it is reduced into arsenite if necessary, then methylated into monomethylarsenic (MMA) and dimethylarsenic acid (DMA) by arsenite methyltransferase. Arsenic and its metabolites are primarily excreted in the urine. Arsenic is known to induce the metal-binding protein metallothionein, which decreases the toxic effects of arsenic and other metals by binding them and making them biologically inactive, as well as acting as an antioxidant. (L20)

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 毒性总结

砷及其代谢物通过多种机制干扰ATP的产生。在柠檬酸循环层面，砷抑制了丙酮酸脱氢酶，并通过与磷酸竞争，解偶联氧化磷酸化，从而抑制了与能量相关的NAD+的还原、线粒体呼吸和ATP的合成。过氧化氢的产生也增加了，这可能会形成活性氧物种和氧化应激。砷的致癌性受到砷与微管蛋白结合的影响，这会导致非整倍体、多倍体和有丝分裂的停滞。其他砷蛋白靶点的结合也可能导致DNA修复酶活性的改变、DNA甲基化模式的改变和细胞增殖的增加。(T1, A17)

Arsenic and its metabolites disrupt ATP production through several mechanisms. At the level of the citric acid cycle, arsenic inhibits pyruvate dehydrogenase and by competing with phosphate it uncouples oxidative phosphorylation, thus inhibiting energy-linked reduction of NAD+, mitochondrial respiration, and ATP synthesis. Hydrogen peroxide production is also increased, which might form reactive oxygen species and oxidative stress. Arsenic's carginogenicity is influenced by the arsenical binding of tubulin, which results in aneuploidy, polyploidy and mitotic arrests. The binding of other arsenic protein targets may also cause altered DNA repair enzyme activity, altered DNA methylation patterns and cell proliferation. (T1, A17)

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 致癌性证据

致癌性分类：1）人类证据：充分；2）动物证据：有限。对人类致癌风险的总体评估为第1组：对人类致癌。注意：此评估适用于整个化学物质组，而不一定适用于组内所有单个化学物质。/砷和砷化合物/

Classification of carcinogenicity: 1) evidence in humans: sufficient; 2) evidence in animals: limited. Overall summary evaluation of carcinogenic risk to humans is Group 1: Carcinogenic to humans. NOTE: This evaluation applies to the group of chemicals as a whole and not necessarily to all individual chemicals within the group. /Arsenic and arsenic compounds/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 致癌性证据

癌症分类：A组人类致癌物

Cancer Classification: Group A Human Carcinogen

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 致癌性证据

分类：A；人类致癌物。分类依据：基于充足的人类数据证据。在主要通过吸入暴露的多个人类群体中观察到了肺癌死亡率的增加。此外，在饮用富含无机砷的水的人群中，观察到了多个内部器官癌症（肝脏、肾脏、肺和膀胱）死亡率的增加以及皮肤癌发病率的增加。人类致癌性数据：充足。动物致癌性数据：不足。/无机砷/ /基于先前的分类系统/

CLASSIFICATION: A; human carcinogen. BASIS FOR CLASSIFICATION: Based on sufficient evidence from human data. An increased lung cancer mortality was observed in multiple human populations exposed primarily through inhalation. Also, increased mortality from multiple internal organ cancers (liver, kidney, lung, and bladder) and an increased incidence of skin cancer were observed in populations consuming drinking water high in inorganic arsenic. HUMAN CARCINOGENICITY DATA: Sufficient. ANIMAL CARCINOGENICITY DATA: Inadequate. /Inorganic Arsenic/ /based on former classification system/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 致癌性证据

A1：已确认的人类致癌物。/砷和无机砷化合物，如As/

A1: Confirmed human carcinogen. /Arsenic and inorganic compounds, as As/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

实验中，将放牧的奶牛和室内饲养的奶牛进行对比，研究饲料中的有毒元素如何转移到牛奶和可食用组织中。第一次实验是在奶牛上进行的。有毒元素通过含有镉、铅、乙酸汞和五氧化二砷的浓缩物片剂给予。投药期为三个月，每头牛每天摄入的镉、铅、汞和砷的量分别为152、200、1.7和33毫克。对照组牛每天摄入的这些元素分别为2、50、0.2和3.4毫克。第二次实验是在室内饲养并喂食浓缩物和粗饲料的奶牛上进行的。一组牛接受了镉、铅、乙酸汞和三氧化二砷。投药期持续了28个月或3个连续的完整泌乳期。肝脏尤其是肾脏是元素积累的主要部位。只有镉在肝脏和肾脏中的建议耐受水平被超过了。增加饮食中元素的含量并没有导致牛奶、血液和肌肉组织中显著更高的浓度。只有可溶性砷导致肌肉组织中这种元素的更高水平。关于病理变化的性质，对照组和实验组之间没有观察到本质的差异。

Experiments with grazing cows and cows kept indoors were performed to study the transfer of toxic elements from their ration into milk and edible tissues. First experiment was carried out with dairy cows. The toxic elements were administered, via wafers of concentrates which contained a mixture of cadmium, lead and mercury acetate and arsenic pentoxide. The dosing period was three months in which the daily intake for each cow was 152, 200, 1.7, and 33 mg for cadmium, lead, mercury, and arsenic, respectively. The daily intake of these elements for the control cows was 2, 50, 0.2, and 3.4 mg, respectively. The second experiment was carried out with dairy cows which were kept indoors and fed on concentrates and roughage. One group received cadmium, lead and mercury acetate, and arsenic trioxide. The dosing period lasted 28 months or 3 consecutive complete lactations. Liver and in particular kidney were the primary sites of element accumulation. Only for cadmium the proposed tolerance levels in liver and kidney were exceeded. Increased dietary concentrations of elements did not result in significantly higher concentrations in milk, blood and muscle tissue. Only soluble arsenic resulted in higher levels of this element in muscle tissue. Regarding the character of the pathological changes, no essential differences were observed between the control and experimental groups.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险等级：
  6.1
• 危险品标志：
  T,N
• 安全说明：
  S45,S53,S60,S61
• 危险类别码：
  R50/53,R45,R23/25
• 海关编码：
  2811290010
• 包装等级：
  II
• 危险类别：
  6.1

SDS

Name:	Arsenic(V) oxide 99.9+% Material Safety Data Sheet
Synonym:	Arsenic pentoxid
CAS:	1303-28-2

Section 1 - Chemical Product MSDS Name:Arsenic(V) oxide 99.9+% Material Safety Data Sheet
Synonym:Arsenic pentoxid

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Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS

CAS#	Chemical Name	content	EINECS#
1303-28-2	Arsenic(V) oxide	99.9+%	215-116-9

Hazard Symbols: T N
Risk Phrases: 23/25 45 50/53

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Section 3 - HAZARDS IDENTIFICATION
EMERGENCY OVERVIEW
Toxic by inhalation and if swallowed. May cause cancer. Very toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment.Moisture sensitive.
Potential Health Effects
Eye:
May cause conjunctivitis. May cause eye irritation and possible burns.
Skin:
May cause irritation with burning pain, itching and redness. May cause dermatitis.
Ingestion:
May be fatal if swallowed. May cause liver damage. May cause cardiac disturbances. May cause severe digestive tract irritation with abdominal pain, nausea, vomiting and diarrhea. May cause central nervous system effects.
Inhalation:
May cause ulceration and perforation of the nasal septum if inhaled in excessive quantities. May cause chemical bronchitis with coughing and difficulty in breathing. Toxic if inhaled.
Chronic:
Prolonged or repeated inhalation may cause kidney and lung damage.
Chronic ingestion may cause liver damage. Prolonged or repeated skin contact may cause dermatitis. May cause bone marrow abnormalities with damage to blood forming tissues. Chronic inhalation may cause nasal septum ulceration and perforation. Repeated exposure may cause kidney damage and digestive tract abnormalities. Repeated exposure may cause central nervous system damage.

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Section 4 - FIRST AID MEASURES
Eyes: Immediately flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid immediately.
Skin:
Get medical aid immediately. Immediately flush skin with plenty of water for at least 15 minutes while removing contaminated clothing and shoes.
Ingestion:
Induce vomiting. If victim is conscious and alert, give 2-4 cupfuls of milk or water. Never give anything by mouth to an unconscious person. Get medical aid immediately.
Inhalation:
Get medical aid immediately. Remove from exposure and move to fresh air immediately. If not breathing, give artificial respiration. If breathing is difficult, give oxygen.
Notes to Physician:

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Section 5 - FIRE FIGHTING MEASURES
General Information:
As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. Substance is noncombustible.
Extinguishing Media:
Use extinguishing media most appropriate for the surrounding fire.

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Section 6 - ACCIDENTAL RELEASE MEASURES
General Information: Use proper personal protective equipment as indicated in Section 8.
Spills/Leaks:
Vacuum or sweep up material and place into a suitable disposal container. Avoid generating dusty conditions.

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Section 7 - HANDLING and STORAGE
Handling:
Use only in a well-ventilated area. Do not breathe dust, vapor, mist, or gas. Do not get in eyes, on skin, or on clothing. Use only in a chemical fume hood.
Storage:
Store in a cool, dry place. Store in a tightly closed container.
Poison room locked.

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Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION
Engineering Controls:
Use adequate ventilation to keep airborne concentrations low.
Exposure Limits CAS# 1303-28-2: United Kingdom, MEL - TWA: (listed as arsenic compounds, n.o.s.): mg/m3 TWA (as As, except arsine) United States OSHA: 5 g/m3 Action Level (as As); 10 g/m3 PEL (a As. Cancer hazard - see 29 CFR 1 910.1018. Arsine excepted) (listed under Arsenic, inorganic compounds).
Belgium - TWA: (listed as arsenic, inorganic compounds): 0.01 mg/ VLE (as As) Germany: 0.1 mg/m3 TWA (inhalable fraction) Japan: (listed as arsenic compounds, n.o.s.): 3 g/m3 OEL (refere value, as As) Malaysia: (listed as arsenic, inorganic compounds): 0.01 mg/m3 TW (as As, except arsine) Netherlands: (listed as arsenic, inorganic compounds): 0.1 mg/m3 (as As) Netherlands: (listed as arsenic, inorganic compounds): 0.050 mg/m MAC (as As) Russia: (listed as arsenic, inorganic compounds): 0.04 mg/m3 TWA As) Russia: (listed as arsenic, inorganic compounds): 0.01 mg/m3 STEL As) Spain: (listed as arsenic, inorganic compounds): 0.1 mg/m3 VLA-ED As) Personal Protective Equipment Eyes: Not available.
Skin:
Wear appropriate protective gloves to prevent skin exposure.
Clothing:
Wear appropriate protective clothing to prevent skin exposure.
Respirators:
Follow the OSHA respirator regulations found in 29 CFR 1910.134 or European Standard EN 149. Always use a NIOSH or European Standard EN 149 approved respirator when necessary.

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Section 9 - PHYSICAL AND CHEMICAL PROPERTIES

Physical State: Solid
Color: Not available.
Odor: Not available.
pH: Not available.
Vapor Pressure: Not available.
Viscosity: Not available.
Boiling Point: Not available.
Freezing/Melting Point: 315 deg C(decom)
Autoignition Temperature: Not available.
Flash Point: Not available.
Explosion Limits, lower: Not available.
Explosion Limits, upper: Not available.
Decomposition Temperature:
Solubility in water: 150 g/100ml water (19C)
Specific Gravity/Density:
Molecular Formula: As2O5
Molecular Weight: 229.84

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Section 10 - STABILITY AND REACTIVITY
Chemical Stability:
Stable under normal temperatures and pressures.
Conditions to Avoid:
High temperatures, incompatible materials, exposure to moist air or water.
Incompatibilities with Other Materials:
Strong oxidizing agents, strong acids, strong bases, active metals, halogens.
Hazardous Decomposition Products:
Oxides of arsenic, arsine.
Hazardous Polymerization: Will not occur.

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Section 11 - TOXICOLOGICAL INFORMATION
RTECS#:
CAS# 1303-28-2: CG2275000 LD50/LC50:
CAS# 1303-28-2: Oral, mouse: LD50 = 55 mg/kg; Oral, rat: LD50 = 8 mg/kg.
Carcinogenicity:
Arsenic(V) oxide - California: carcinogen, initial date 2/27/87 (listed as Arsenic, inorg NTP: Known carcinogen (listed as Arsenic, inorganic compounds).
IARC: Group 1 carcinogen (listed as Arsenic compounds, n.o.s.).
Other:
See actual entry in RTECS for complete information.

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Section 12 - ECOLOGICAL INFORMATION

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Section 13 - DISPOSAL CONSIDERATIONS
Dispose of in a manner consistent with federal, state, and local regulations.

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Section 14 - TRANSPORT INFORMATION

IATA
Shipping Name: ARSENIC COMPOUND, SOLID, N.O.S.
Hazard Class: 6.1
UN Number: 1557
Packing Group: II
IMO
Shipping Name: ARSENIC COMPOUND, SOLID, N.O.S.
Hazard Class: 6.1
UN Number: 1557
Packing Group: II
RID/ADR
Shipping Name: ARSENIC COMPOUND, SOLID, N.O.S.
Hazard Class: 6.1
UN Number: 1557
Packing group: II
USA RQ: CAS# 1303-28-2: 1 lb final RQ; 0.454 kg final RQ

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Section 15 - REGULATORY INFORMATION

European/International Regulations
European Labeling in Accordance with EC Directives
Hazard Symbols: T N
Risk Phrases:
R 45 May cause cancer.
R 23/25 Toxic by inhalation and if swallowed.
R 50/53 Very toxic to aquatic organisms, may cause
long-term adverse effects in the aquatic environment.
Safety Phrases:
S 53 Avoid exposure - obtain special instructions
before use.
S 45 In case of accident or if you feel unwell, seek
medical advice immediately (show the label where
possible).
S 60 This material and its container must be
disposed of as hazardous waste.
S 61 Avoid release to the environment. Refer to
special instructions/safety data sheets.
WGK (Water Danger/Protection)
CAS# 1303-28-2: 3
Canada
CAS# 1303-28-2 is listed on Canada's DSL List.
CAS# 1303-28-2 is listed on Canada's Ingredient Disclosure List.
US FEDERAL
TSCA
CAS# 1303-28-2 is listed on the TSCA inventory.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

制备方法

将100克三氧化二砷放入圆底烧瓶中，加入100毫升浓硝酸，然后加热。当不再产生棕色的氧化氮气体时，将溶液通过倾析法转移到另一个烧瓶中，再加入50毫升浓硝酸并继续加热，在300℃以下蒸干。蒸发剩余物后，用少量水浸湿并溶解。使用玻璃过滤器过滤，然后在250～300℃之间逐渐脱水：如果温度过高，则会放出氧气而分解，变成三氧化二砷，因此必须注意。随着脱水的进行，将出现白色粉末状的剩余物，并且完全固化之后，应将其存放在装有五氧化二磷或浓硫酸的干燥器中。

合成制备方法

步骤与前述相同：将100克三氧化二砷放入圆底烧瓶中，加入100毫升浓硝酸，加热直至不再产生棕色的氧化氮气体。之后通过倾析法转移溶液至另一烧瓶，并再加50毫升浓硝酸后继续加热，在300℃以下蒸干。蒸发剩余物后用少量水浸湿并溶解，然后使用玻璃过滤器过滤。在250～300℃之间逐渐脱水：如果温度过高，则会放出氧气而分解，变成三氧化二砷，因此必须注意。随着脱水的进行，将出现白色粉末状的剩余物，并且完全固化之后，应将其存放在装有五氧化二磷或浓硫酸的干燥器中。

用途简介

1. 制备砷酸盐。
2. 制造有色玻璃。
3. 金属粘合剂。
4. 木材防腐。
5. 杀真菌剂。

用途

1. 制备砷酸盐。
2. 制造有色玻璃。
3. 金属粘合剂。
4. 木材防腐。
5. 杀真菌剂。
6. 用于制药物、杀虫剂、金属粘接剂和有色玻璃等。 [16]

反应信息

• 作为反应物：
  描述：

  Arsenic pentoxide 生成 oxoarsinite
  参考文献：
  名称：

  GOROXOVA, L. G.;MAXMETOV, M. ZH.;EMELINA, A. V., IZV. VUZOV. XIMIYA I XIM. TEXNOL., 32,(1989) N, S. 124-125

  摘要：

  DOI：
• 作为产物：
  描述：

  砷化氢 生成 Arsenic pentoxide
  参考文献：
  名称：

  SIOSAKI, TADASI, KOGE DZAJRE, 36,(1988) N0, S. 22-27

  摘要：

  DOI：

文献信息

• Herbicidal cyclohexane-1,3-dione-5-isoquinoline derivatives
  申请人：ICI Australia Limited

  公开号：US04680400A1

  公开（公告）日：1987-07-14

  The invention concerns novel compounds of the formula I ##STR1## wherein: A, B, D and E are selected from CH, N and N-Z wherein Z is selected from oxygen and the group YAn wherein Y is selected from alkyl and benzyl and An is an anion, and provided that no more than three of A, B, D and E are selected from N and N-Z and no more than one of A, B, D and E is selected from N-Z; W is a saturated or unsaturated C.sub.2 to C.sub.5 hydrocarbon chain; X and X.sup.1 are independently selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, amino, substituted amino and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof, or two of X.sup.1 on the same carbon atom may form an oxo group; R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation; R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl; R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl; R.sup.4 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl; n is 0 or an integer chosen from 1 to 3; and n.sup.1 is 0 or an integer chosen from 1 to 5. The compounds of the invention show herbicidal properties and plant growth regulating properties and in further embodiments the invention provides processes for the preparation of compounds of formula I, intermediates useful in the preparation of the compounds of formula I, compositions containing as active ingredient a compound of formula I, and herbicidal and plant growth regulating processes utilizing compounds of formula I.

  本发明涉及化合物I的新型化合物，其化学式为：##STR1##其中：A、B、D和E选择自CH、N和N-Z，其中Z选择自氧和YAn基团，其中Y选择自烷基和苯甲基，An是阴离子，并且保证A、B、D和E中最多只有三个选择自N和N-Z，最多只有一个选择自N-Z；W是饱和或不饱和的C.sub.2至C.sub.5烃基链；X和X.sup.1独立选择自卤素、硝基、氰基、烷基、取代烷基、羟基、烷氧基、取代烷氧基、烯基、烯氧基、炔基、炔氧基、酰氧基、烷氧羰基、烷基硫基、烷基亚磺酰基、烷基磺酰基、磺酰胺基、取代磺酰胺基、烷酰氧基、苄氧基、取代苄氧基、氨基、取代氨基和甲酰基和烷酰基及其氧肟、亚胺和席夫碱衍生物，或X.sup.1中的两个在同一碳原子上可以形成氧代基；R.sup.1选择自氢、烷基、烯基、炔基、取代烷基、烷基磺酰基、芳基磺酰基、酰基和无机或有机阳离子；R.sup.2选择自烷基、取代烷基、烯基、卤代烯基、炔基和卤代炔基；R.sup.3选择自烷基、氟烷基、烯基、炔基和苯基；R.sup.4选择自氢、卤素、烷基、氰基和烷氧羰基；n为0或从1到3选择的整数；n.sup.1为0或从1到5选择的整数。本发明的化合物具有除草和植物生长调节性能，在进一步实施中，本发明提供了制备化合物I的工艺、制备化合物I的中间体、含有化合物I作为活性成分的组合物以及利用化合物I进行除草和植物生长调节的过程。
• PHARMACEUTICAL COMPOUNDS
  申请人：——

  公开号：US20010053783A1

  公开（公告）日：2001-12-20

  A pharmaceutical compound of the formula 1 in which R 1 is hydrogen, C 1-4 alkyl, C 1-4 alkoxy or halo, and R 2 is hydrogen, C 1-4 alkyl or C 1-4 alkoxy; or a salt thereof.

  一种药物化合物，其化学式为1，其中R1为氢，C1-4烷基，C1-4烷氧基或卤素，R2为氢，C1-4烷基或C1-4烷氧基；或其盐。
• 4-Methyl-5-(unsubstituted and substituted
  申请人：The United States of America as represented by the Secretary of the Army

  公开号：US04431807A1

  公开（公告）日：1984-02-14

  Compounds of the class including 4-methyl-5-(unsubstituted and substituted henoxy)-6-methoxy-8-(aminoalkylamino)quinolines as the free bases and pharmaceutically acceptable acid amine salts are described. The compounds are highly effective antimalarial agents which possess, surprisingly, both tissue schizonticidal (radical curative) and blood schizonticidal (suppressive) activity. In addition, these drugs have significantly better therapeutics indices than primaquine which is the current tissue schizonticidal drug of choice. Primaquine possesses no useful blood schizonticidal activity at tolerated dose levels.

  本类化合物包括4-甲基-5-(未取代和取代的苯氧基)-6-甲氧基-8-(氨基烷基)喹啉作为自由碱和药学上可接受的酸胺盐。这些化合物是高效的抗疟疾药物，出人意料地具有组织无性红体杀灭（根治性）和血液无性红体杀灭（抑制性）活性。此外，这些药物的治疗指数显著优于目前组织无性红体杀灭药物首选的前奎宁。在可耐受的剂量水平下，前奎宁没有有用的血液无性红体杀灭活性。
• Optionally substituted 6,8-quinolines
  申请人：Syntex (U.S.A.) Inc.

  公开号：US05455252A1

  公开（公告）日：1995-10-03

  A compound of the formula ##STR1## wherein: R.sup.1 is independently selected from hydrogen, lower-alkyl, cycloalkyl, cycloalkyl lower-alkyl, lower-alkoxy, formyl, (lower-alkyl)-hydroxylmethyl, aryl, benzyl, arylmethyl, pyridylmethyl, where aryl, benzyl, arylmethyl and pyridylmethyl are unsubstituted or independently mono, di or tri substituted with hydrogen, hydroxy, thiol, amino, halo, nitro, lower-alkylthio, lower-alkoxy, mono-lower-alkylamino, di-lower-alkylamino, hydroxycarbonyl, lower-alkoxycarbonyl, hydroxysulfonyl, lower-alkoxysulfonyl, lower-alkylsulfonyl, lower-alkylsulfinyl, trifluoromethyl, cyano, tetrazoyl, carbamoyl, lower-alkylcarbamoyl, and di-lower-alkylcarbamoyl; and R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth in the specification.

  化合物的式子为##STR1##其中：R.sup.1是独立选择的氢，较低的烷基，环烷基，环烷基较低的烷基，较低的烷氧基，甲酰基，(较低的烷基)-羟甲基，芳基，苄基，芳基甲基，吡啶基甲基，其中芳基，苄基，芳基甲基和吡啶基甲基未取代或独立单取代，双取代或三取代为氢，羟基，硫醇基，氨基，卤素，硝基，较低的烷基硫醇基，较低的烷氧基，单较低的烷基氨基，双较低的烷基氨基，羟基甲酰基，较低的烷氧羰基，羟基磺酰基，较低的烷氧基磺酰基，较低的烷基磺酰基，较低的烷基亚磺酰基，三氟甲基，氰基，四氮杂环酰基，氨基甲酰基，较低的烷基氨基甲酰基和双较低的烷基氨基甲酰基；以及R.sup.2，R.sup.3，R.sup.4，R.sup.5和R.sup.6如规范所述。
• Herbicidal cyclohexane-1,3-dione derivatives
  申请人：ICI Australia Limited

  公开号：US04640708A1

  公开（公告）日：1987-02-03

  Compounds of the formula ##STR1## wherein: R.sup.5 is a bicyclic aryl or nitrogen-containing heteroaryl ring system such as naphthyl, quinolyl, isoquinolyl or tetrahydroisoquinolyl, optionally substituted by a wide variety of groups; R.sup.4 and R.sup.1 are preferably hydrogen but may be other groups and R.sup.2 and R.sup.3 are selected from alkyl, haloalkyl, alkenyl, haloalkenyl and alkynyl, show high general grass-killing activity with good selectivity to many broad-leaf crops and in some instances selectivity to small-grain cereals. Processes for the preparation of compounds of formula I, intermediates in the preparation of compounds I and the herbicidal properties of compounds I are described.

  化合物的公式为##STR1##其中：R.sup.5是一个双环芳基或含氮杂环环系统，例如萘基，喹啉基，异喹啉基或四氢异喹啉基，可选择地被各种基团取代；R.sup.4和R.sup.1优选是氢，但也可以是其他基团，R.sup.2和R.sup.3选择自烷基，卤代烷基，烯基，卤代烯基和炔基，具有良好的选择性对许多广叶作物表现出高的杀草活性，并在某些情况下对小粒谷物表现出选择性。描述了制备公式I化合物的过程，制备公式I化合物的中间体以及公式I化合物的除草性能。