盐酸依替福林 | 943-17-9

• 物质功能分类: 分析化学 - 标准品 - 药典标准品和杂质标准品
• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 中文名称: 盐酸依替福林
• 中文别名: 盐酸伊替福林；4-羟基-alpha-((乙基氨基)甲基)-苄醇盐酸盐；低压丁
• 英文名称: etilefrine hydrochloride
• 英文别名: Apocretin；3-[2-(ethylamino)-1-hydroxyethyl]phenol;hydron;chloride
• CAS: 943-17-9
• 化学式: C₁₀H₁₅NO₂*ClH
• mdl: MFCD00060167
• 分子量: 217.696
• InChiKey: KTNROWWHOBZQGK-UHFFFAOYSA-N

物化性质

• 熔点：
  122 °C
• 溶解度：
  易溶于水，溶于乙醇（96%），几乎不溶于二氯甲烷

计算性质

• 辛醇/水分配系数(LogP)：
  0.23
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  57.1
• 氢给体数：
  3
• 氢受体数：
  3

安全信息

• 海关编码：
  2922509090
• 储存条件：
  室温

SDS

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Section I.Chemical Product and Company Identification
Chemical Name Etilefrine Hydrochloride
Portland OR
Benzenemethanol,
Synonym
α-[(ethylamino)methyl]-3-hydroxy-hydrochloride (9CI)
HOC6H4CH(OH)CH2NHCH2CH3•HCl
Chemical Formula
CAS Number 943-17-9

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Section II. Composition and Information on Ingredients
Chemical Name CAS Number Percent (%) TLV/PEL Toxicology Data
Etilefrine Hydrochloride 943-17-9 Min. Not available. Rat LD50 (intravenous) 5 mg/kg
98.0%(Tit.) Mouse LD50 (subcutaneous) 860
mg/kg
Rat LDLO (oral) 187 mg/kg

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Section III. Hazards Identification
Harmful if ingested or inhaled. Minimize exposure to this material. Severe overexposure can result in injury or death.
Acute Health Effects
Follow safe industrial hygiene practices and always wear proper protective equipment when handling this compound.
CARCINOGENIC EFFECTS : Not available.
Chronic Health Effects
MUTAGENIC EFFECTS : Not available.
TERATOGENIC EFFECTS : Not available.
DEVELOPMENTAL TOXICITY: Not available.
Repeated or prolonged exposure to this compound is not known to aggravate existing medical conditions.

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Section IV. First Aid Measures
Eye Contact Check for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for at least 15
minutes. Get medical attention.
Skin Contact In case of contact, immediately flush skin with plenty of water. Remove contaminated clothing and shoes. Wash clothing
before reuse. Thoroughly clean shoes before reuse. Get medical attention.
If the victim is not breathing, perform mouth-to-mouth resuscitation. Loosen tight clothing such as a collar, tie, belt or
Inhalation
waistband. If breathing is difficult, oxygen can be administered. Seek medical attention if respiration problems do not
improve.
INDUCE VOMITING by sticking finger in throat. Lower the head so that the vomit will not reenter the mouth and throat.
Ingestion
Loosen tight clothing such as a collar, tie, belt or waistband. If the victim is not breathing, perform mouth-to-mouth
resuscitation. Examine the lips and mouth to ascertain whether the tissues are damaged, a possible indication that the
toxic material was ingested; the absence of such signs, however, is not conclusive.

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Section V. Fire and Explosion Data
Auto-Ignition Not available.
Flammability May be combustible at high temperature.
Flash Points Flammable Limits Not available.
Not available.
Combustion Products These products are toxic carbon oxides (CO, CO2), nitrogen oxides (NO, NO2).
WARNING: Highly toxic HCl gas is produced during combustion.
Fire Hazards
Not available.
Explosion Hazards Risks of explosion of the product in presence of mechanical impact: Not available.
Risks of explosion of the product in presence of static discharge: Not available.
Fire Fighting Media
SMALL FIRE: Use DRY chemical powder.
and Instructions LARGE FIRE: Use water spray, fog or foam. DO NOT use water jet.
Consult with local fire authorities before attempting large scale fire-fighting operations.
Continued on Next Page
Etilefrine Hydrochloride

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Section VI. Accidental Release Measures
Spill Cleanup Harmful Material.
Use a shovel to put the material into a convenient waste disposal container. Finish cleaning the spill by rinsing any
Instructions
contaminated surfaces with copious amounts of water. Consult federal, state, and/or local authorities for assistance on
disposal.

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Section VII. Handling and Storage
Handling and Storage HARMFUL. Keep away from heat. Mechanical exhaust required. When not in use, tightly seal the container and store in
a dry, cool place. Avoid excessive heat and light. Do not breathe dust.
Information
Always store away from incompatible compounds such as oxidizing agents.

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Section VIII. Exposure Controls/Personal Protection
Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below
recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to
airborne contaminants below the exposure limit.
Personal Protection Splash goggles. Lab coat. Dust respirator. Boots. Gloves. Suggested protective clothing might not be sufficient; consult
a specialist BEFORE handling this product. Be sure to use a MSHA/NIOSH approved respirator or equivalent.
Exposure Limits Not available.

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Section IX. Physical and Chemical Properties
Physical state @ 20°C Solid. (White Crystalline powder.) Solubility Not available.
Not available.
Specific Gravity
Molecular Weight 217.69 Partition Coefficient Not available.
Boiling Point Not available. Vapor Pressure Not applicable.
Melting Point 122°C (251.6°F) Vapor Density Not available.
Not available. Volatility Not available.
Refractive Index
Not available.
Critical Temperature Not available. Odor
Not available. Not available.
Viscosity Taste

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Section X. Stability and Reactivity Data

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This material is stable if stored under proper conditions. (See Section VII for instructions)
Stability
Conditions of Instability
Avoid excessive heat and light.
Incompatibilities
Reactive with oxidizing agents.

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Section XI. Toxicological Information
RTECS Number DO5618000
Routes of Exposure Eye Contact. Ingestion. Inhalation.
Rat LD50 (intravenous) 5 mg/kg
Toxicity Data
Mouse LD50 (subcutaneous) 860 mg/kg
Rat LDLO (oral) 187 mg/kg
CARCINOGENIC EFFECTS : Not available.
Chronic Toxic Effects
MUTAGENIC EFFECTS : Not available.
TERATOGENIC EFFECTS : Not available.
DEVELOPMENTAL TOXICITY: Not available.
Repeated or prolonged exposure to this compound is not known to aggravate existing medical conditions.
Acute Toxic Effects Harmful if ingested or inhaled. Minimize exposure to this material. Severe overexposure can result in injury or death.
Follow safe industrial hygiene practices and always wear proper protective equipment when handling this compound.
Continued on Next Page
Etilefrine Hydrochloride

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Section XII. Ecological Information
Ecotoxicity Not available.
Not available.
Environmental Fate

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Section XIII. Disposal Considerations
Recycle to process, if possible. Consult your local regional authorities. You may be able to dissolve or mix material with a
Waste Disposal
combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber system. Observe all
federal, state and local regulations when disposing of the substance.

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Section XIV. Transport Information
DOT Classification Not a DOT controlled material (United States).
Not applicable.
PIN Number
Proper Shipping Name
Not applicable.
Packing Group (PG) Not applicable.
DOT Pictograms

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Section XV. Other Regulatory Information and Pictograms
TSCA Chemical Inventory This product is NOT on the EPA Toxic Substances Control Act (TSCA) inventory. The following notices are required by 40
CFR 720.36 (C) for those products not on the inventory list:
(EPA)
(i) These products are supplied solely for use in research and development by or under the supervision of a technically
qualified individual as defined in 40 CFR 720.0 et sec.
(ii) The health risks of these products have not been fully determined. Any information that is or becomes available will be
supplied on an MSDS sheet.
WHMIS Classification Not available.
(Canada)
EINECS Number (EEC) Not available.
EEC Risk Statements R20/21/22- Harmful by inhalation, in contact with skin and if swallowed.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

盐酸依替福林，化学名称为2-乙胺基1-(3-羟基苯基)乙醇盐酸盐，是一种广泛应用的医药原料中间体。其主要作用是增强心肌收缩力、收缩血管和升高血压，主要用于低血压的医疗急救。

反应信息

• 作为反应物：
  描述：

  盐酸依替福林 在 氯化亚砜 作用下， 以 苯 为溶剂， 反应 1.0h， 以46%的产率得到N-乙基-2-氯-2-(3-羟基苯基)乙胺盐酸盐
  参考文献：
  名称：

  Synthesis and radioprotective activity of 2-phenylethylamine derivatives

  摘要：

  DOI：

  10.1007/bf00773617

文献信息

• METHODS AND COMPOSITIONS FOR TREATING INFECTION
  申请人：UNIVERSITY OF ROCHESTER

  公开号：US20150238473A1

  公开（公告）日：2015-08-27

  Provided herein are compositions and methods for treating or preventing infection.

  本文提供了用于治疗或预防感染的组合物和方法。
• PRIMARY AMINE COMPOUND OR SECONDARY AMINE COMPOUND-ACIDIC POLYSACCHARIDE CONJUGATE AND PRODUCTION METHOD THEREFOR
  申请人：Seikagaku Corporation

  公开号：US20220040318A1

  公开（公告）日：2022-02-10

  Provided is a novel conjugate of a primary or secondary amine compound with an acidic polysaccharide, which is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof, where in Formula (I), D, R 1 , R 2 , A, and Poly are as defined in the specification.

  提供的是一种主要或次要胺化合物与酸性多糖结合的新型共轭物，该化合物由式（I）表示或其药用盐，其中在式（I）中，D、R1、R2、A 和 Poly 如规范中定义。
• Ceramic structures for controlled release of biologically active substances
  申请人：Moerck E. Rudi

  公开号：US20060210634A1

  公开（公告）日：2006-09-21

  The present invention provides compositions for controlled drug delivery, dosage forms, and processes for producing dosage forms. In a composition aspect of the present invention, a composition including a drug and a ceramic structure is provided. The ceramic structure has either a hollow portion wherein the drug is included in the hollow portion or is a collection of smaller particles bound together.

  本发明提供了用于控制药物释放的组成物、剂型和制造剂型的过程。在本发明的组成方面，提供了一种包括药物和陶瓷结构的组合物。陶瓷结构具有空心部分，药物包含在空心部分中，或者是由许多小颗粒组成的结合体。
• Sweetener compositions and uses thereof
  申请人：AJINOMOTO CO. INC

  公开号：US20040105928A1

  公开（公告）日：2004-06-03

  The present invention provides compositions containing one or more aspartyl dipeptide derivatives represented by formulas (1) and/or (2) mixed with another high intensity sweetner, such Aspartame, sugar, sugar alcohol, and oligosaccharide; food, beverages, and/or medicinal products containing these compositions, methods of using the compositions to impart sweetness in food, beverages, and/or medicinal products to impart sweetness or suppress a bitter taste; and methods of making the compositions and products.

  本发明提供了一种含有一个或多个由式(1)和/或式(2)表示的天冬氨酰二肽衍生物与另一种高强度甜味剂混合的组合物；含有这些组合物的食品、饮料和/或药品；使用这些组合物在食品、饮料和/或药品中赋予甜味或抑制苦味的方法；以及制备这些组合物和产品的方法。其中，另一种高强度甜味剂可以是阿斯巴甜、糖、糖醇和寡糖。
• Coated fine particles containing drug for intrabuccally fast disintegrating tablet
  申请人：Kurimoto Ippei

  公开号：US20050175689A1

  公开（公告）日：2005-08-11

  The present invention makes it possible to provide drug-containing coated microparticles for quick-disintegrating oral tablets wherein microparticles containing a drug with an unpleasant taste are coated with a film composed of (1) a pH-independent water-insoluble polymer accounting for 60% or more but less than 80% of the film and (2) a pH-independent water-soluble substance accounting for more than 20% to 40% or less of the film, these microparticles being characterized in that the rate of dissolution of the drug from the drug-containing microparticles is 0% to 10% in one minute and 80% to 100% in 30 minutes, and the average particle diameter is 350 μm or less, in order to realize sufficient control of oral drug dissolution and fast gastrointestinal drug dissolution.

  本发明使得能够提供含有药物的涂层微粒，用于快速分解口服片，其中含有不愉快口感的药物的微粒被涂上由(1)占膜层60%或以上但少于80%的pH独立水不溶性聚合物和(2)占膜层20%至40%以上的pH独立水溶性物质组成的薄膜。这些微粒的特征在于，药物从含药微粒中的溶解速率在一分钟内为0%至10%，在30分钟内为80%至100%，平均粒径为350微米或更小，以实现口服药物溶解的充分控制和快速肠道药物溶解。

表征谱图