4,5-二氢-2-(1-萘基甲基)-1H-咪唑鎓硝酸盐 | 5144-52-5

• 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 - 萘
• 中文名称: 4,5-二氢-2-(1-萘基甲基)-1H-咪唑鎓硝酸盐
• 中文别名: 2-(1-萘基甲基)-2-咪唑啉硝酸盐；硝酸萘甲唑林；新霉素A；硝酸萘甲唑啉；2-(1-萘甲基)咪唑啉硝酸盐
• 英文名称: Naphazoline nitrate
• 英文别名: 2-(1-naphthylmethyl)-2-imidazoline nitrate；2-(1-naphthylmethyl)-2-imidazolium nitrate；2-[1]naphthylmethyl-4,5-dihydro-1H-imidazole; nitrate；2-[1]Naphthylmethyl-4,5-dihydro-1H-imidazol; Nitrat；4,5-dihydro-2-(1-naphthylmethyl)-1H-imidazolium nitrate；2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole;nitric acid
• CAS: 5144-52-5；10061-11-7
• 化学式: C₁₄H₁₄N₂*HNO₃
• 分子量: 273.291
• InChiKey: ZAHXYMFVNNUHCP-UHFFFAOYSA-N

物化性质

• 熔点：
  167-170 °C
• 溶解度：
  微溶于水，溶于乙醇（96%）。

计算性质

• 辛醇/水分配系数(LogP)：
  2.04
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  90.4
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 危险等级：
  6.1(b)
• 危险品标志：
  Xn
• 安全说明：
  S22,S36/37
• 危险类别码：
  R22
• WGK Germany：
  3
• 海关编码：
  2933290090
• RTECS号：
  NJ4376000
• 包装等级：
  III
• 危险类别：
  6.1(b)
• 危险品运输编号：
  3249

制备方法与用途

用途
该药物属于拟肾上腺素药，具有收缩血管的作用，主要用于治疗伤风、鼻炎和鼻充血等症状。

用途
本品为拟交感神经药物，主要用于相关症状的治疗。

反应信息

• 作为反应物：
  描述：

  4,5-二氢-2-(1-萘基甲基)-1H-咪唑鎓硝酸盐 、 bis-(2,4-dihydroxythiobenzoyl)sulfinyl 在 吡啶 作用下， 以 甲醇 为溶剂， 反应 10.0h， 生成 2-(1-naphthylmethyl)-1-(2,4-dihydroxythiobenzoyl)-2-imidazoline
  参考文献：
  名称：

  Synthesis of some 1-(2,4-dihydroxythiobenzoyl)imidazoles, -imidazolines and -tetrazoles and their potent activity against Candida species

  摘要：

  Various 1-(2,4-dihydroxythiobenzoyl)imidazoles, -imidazolines and -tetrazoles were synthesized and evaluated for their in vitro antifungal activity. Compounds were prepared by the reaction of sulfinyl-bis-(2,4-dihydroxythiobenzoyl) with properly substituted azoles. The MIC values against the Candida albicans ATCC 10231 strain, the azole-resistant clinical isolates of C. albicans and non-Candida species were determined. Tetrazole derivatives were the most active against C. albicans, imidazoline derivatives against non-Candida species. All compounds showed higher activity than that of comparable drugs.

  DOI：

  10.1016/s0014-827x(03)00046-6
• 作为产物：
  描述：

  1-萘乙腈 在 硝酸 、 3-巯基丙酸 作用下， 以 水 为溶剂， 反应 9.0h， 生成 4,5-二氢-2-(1-萘基甲基)-1H-咪唑鎓硝酸盐
  参考文献：
  名称：

  一种萘甲唑啉无机酸盐的合成与精制方法

  摘要：

  本发明公开了一种萘甲唑啉无机酸盐的合成与精制方法，属于药物合成领域。该方法以1‑萘乙腈和乙二胺为原料经催化缩合、与无机酸进行成盐两步反应得到萘甲唑啉无机酸盐粗品，最后经重结晶、活性炭脱色等工艺精制得到纯品萘甲唑啉无机酸盐，精制后纯品纯度高达99.5％，是一种工艺简单、操作方便、适合工业化生产的制备方法。

  公开号：

  CN113912545A

文献信息

• METHODS AND SYSTEMS FOR DESIGNING AND/OR CHARACTERIZING SOLUBLE LIPIDATED LIGAND AGENTS
  申请人：TUFTS MEDICAL CENTER

  公开号：US20160052982A1

  公开（公告）日：2016-02-25

  The present application provides methods for preparing soluble lipidated ligand agents comprising a ligand entity and a lipid entity, and in some embodiments, provides relevant parameters of each of these components, thereby enabling appropriate selection of components to assemble active agents for any given target of interest.

  本申请提供了制备可溶性脂质化配体药剂的方法，包括配体实体和脂质实体，并在某些实施例中提供了这些组分的相关参数，从而使得能够适当选择组分来组装出针对任何感兴趣的靶点的活性药剂。
• Water-dispersible patch containing an active agent for dermal delivery
  申请人：McEntire Edward Enns

  公开号：US20070259029A1

  公开（公告）日：2007-11-08

  A dermal patch having comprising at least two layers wherein at least one layer is a polymer matrix system having an active agent admixed therein. At least one of the layers includes a water-dispersible or water-dissipatable polymer. The dermal patch has an elongation factor of at least 50%.

  一种皮肤贴片，包括至少两层，其中至少一层是聚合物基质系统，其中混合了活性剂。至少一层包括可水分散或可水分散的聚合物。该皮肤贴片的伸长系数至少为50％。
• Hemostatic polymer useful for RAPID blood coagulation and hemostasis
  申请人：Cochrum C. Kent

  公开号：US20050226916A1

  公开（公告）日：2005-10-13

  Provided herein is a novel hemostatic polymer composition comprising a substance containing uncharged organic hydroxyl groups and a substance containing at least one of a halogen atom and an epoxy group, which is characterized as inducing rapid blood coagulation and hemostasis at a wound or bleeding site. Methods of use of the novel polymer composition are also provided.

  本文提供了一种新型止血聚合物组合物，包括含有未带电的有机羟基的物质和含有至少一个卤素原子和环氧基的物质。该组合物的特点是在伤口或出血部位引起快速的血液凝固和止血。本文还提供了使用该新型聚合物组合物的方法。
• Phenylacetic Acid Compound
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：US20140357630A1

  公开（公告）日：2014-12-04

  A compound represented by formula (I), wherein R 1 represents a hydrogen atom, etc., R 2 and R 3 each independently represents a hydrogen atom, optionally oxidized C1-4 alkyl group or optionally protected hydroxyl group, or R 2 and R 3 taken together represent optionally oxidized C2-5 alkylene group, R 4 represents an optionally oxidized C1-6 alkyl group, etc., R 5 represents an optionally oxidized C1-6 alkyl group, etc., R 6 represents an optionally oxidized C1-6 alkyl group, etc., m represents 0 or an integer from 1 to 3, n represents 0 or an integer from 1 to 4, and i represents 0 or an integer from 1 to 7.

  化合物的化学式为（I），其中R1代表氢原子等，R2和R3各自独立地代表氢原子，可选的氧化C1-4烷基或可选择保护的羟基，或者R2和R3一起代表可选的氧化C2-5亚烷基，R4代表可选的氧化C1-6烷基等，R5代表可选的氧化C1-6烷基等，R6代表可选的氧化C1-6烷基等，m代表0或1至3的整数，n代表0或1至4的整数，i代表0或1至7的整数。
• Powdery pharmaceutical composition and powdery preparation for application to the nasal mucosa, and method for administration thereof
  申请人：TEIJIN LIMITED

  公开号：EP0023359A2

  公开（公告）日：1981-02-04

  A powdery pharmaceutical composition and a powdery preparation in unit dosage form for application to the mucosa of the nasal cavity, at least about 90% of which consists of particles having an effective particle diameter of about 20 to about250 microns, said composition comprising a lower alkyl ether or cellulose having a viscosity, determined at about 376C for a 2% aqueous solution thereof, of at least about 5 centipoises and a pharmaceutically effective amount of a drug; and a method for treating or preventing a human nasal disease, which comprises administering a powdery preparation in unit dosage form to the nasal cavity of a human being requiring treatment or prevention of a nasal disease through his nostrils.

  一种用于鼻腔粘膜的粉状药物组合物和单位剂型的粉状制剂，其中至少约90％由有效颗粒直径约20至约250微米的颗粒组成，所述组合物包括低级烷基醚或纤维素，其2％水溶液在约376℃下测定的粘度至少约为5厘泊，以及药学上有效量的药物；以及一种治疗或预防人类鼻病的方法，该方法包括将单位剂型的粉状制剂通过鼻孔施用到需要治疗或预防鼻病的人的鼻腔中。