6-氯-2-氨基萘 | 23417-61-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 中文名称: 6-氯-2-氨基萘
• 英文名称: 6-chloro-2-naphthylamine
• 英文别名: 6-Chloronaphthalen-2-amine
• CAS: 23417-61-0
• 化学式: C₁₀H₈ClN
• 分子量: 177.633
• InChiKey: NKYFZBWHIXNTKV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

安全信息

• 海关编码：
  2921450090

反应信息

• 作为反应物：
  描述：

  6-氯-2-氨基萘 在 镍 氢气 作用下， 28.0 ℃ 、344.73 kPa 条件下， 反应 24.0h， 生成 N-(6-chloronaphthalen-2-yl)-N-[(2,4-diaminoquinazolin-6-yl)methyl]formamide
  参考文献：
  名称：

  Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines

  摘要：

  A series of 6-[(arylamino)methyl]-2,4-quinazolinediamines have been prepared by catalytic hydrogenation of the requisite 2,4-diamino-6-quinazolinecarbonitriles in the presence of the appropriate benzenamine. Formylation, acetylation, and nitrosation provided N omega derivatives of these compounds. A variety of the compounds exhibited potent antimalarial, antibacterial, and antitumor activity. In particular, 5-methyl-6-[[(3,4,5-trimethoxyphenyl)-amino]methyl]-2, 4-quinazolinediamine (trimetrexate, 15) has shown a broad spectrum of antitumor effects and is undergoing preclinical toxicology evaluation prior to trial in man.

  DOI：

  10.1021/jm00366a018
• 作为产物：
  描述：

  6-氯萘-2-羧酸 在 二苯基磷酸 、 三乙胺 、 水 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 4.0h， 生成 6-氯-2-氨基萘
  参考文献：
  名称：

  1-(2-Naphthyl)-1 H -pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors

  摘要：

  Using N,N-dialkylated benzamidines as the novel P4 motifs, we have designed and synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent and selective fXa inhibitors with significantly improved hydrophilicity and in vitro anticoagulant activity. These benzamidine-P4 fXa inhibitors have displayed excellent oral bioavailability and long half-life. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2003.12.054

文献信息

• [EN] GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE<br/>[FR] INHIBITEURS DE GLYCOLATE OXYDASE POUR LE TRAITEMENT D'UNE MALADIE
  申请人：BIOMARIN PHARM INC

  公开号：WO2020257487A1

  公开（公告）日：2020-12-24

  Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.

  本文描述了化合物、制备这种化合物的方法、含有这种化合物的药物组合物和药物，以及使用这种化合物治疗或预防与甘氧酸代谢缺陷相关的疾病或紊乱的方法，例如与甘氧酸氧化酶（GO）或草酸代谢变化相关的疾病或紊乱。这些疾病或紊乱包括与产生过多草酸相关的甘氧酸代谢紊乱，例如原发性高草酸尿症。
• Inhibitors of factor Xa
  申请人：——

  公开号：US20020091116A1

  公开（公告）日：2002-07-11

  Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

  揭示了针对哺乳动物因子Xa具有活性的新化合物、它们的盐和相关组合物。这些化合物在体外或体内用于预防或治疗凝血障碍。
• Synthesis of some heteronuclear mono- and di-chloro-2-naphthylamines
  作者：Andre Rosowsky、Josephine Battaglia、Katherine K. N. Chen、Nickolas Papathanasopoulos、Edward J. Modest

  DOI：10.1039/j39690001376

  日期：——

  Improved methods of preparation of 6- and 7-chloro-2-naphthylamine from sodium 2-naphthol-6-sulphonate and disodium naphthalene-2,7-disulphonate, respectively, are described. Syntheses of 5,6-, 5,7-, and 6,7-dichloro-2-naphthylamines are also reported.

  描述了分别由2-萘酚-6-磺酸钠和萘-2,7-二磺酸二钠制备6-氯和7-氯-2-萘胺的改进方法。还报道了5，6-，5，7-和6，7-二氯-2-萘胺的合成。
• Neurocognitive Symptoms and Impairment in an HIV Community Clinic
  作者：D.H. Kim、C. Power、M.J. Gill、D.L. Jewison、G.R. Milner、S.B. Rourke

  DOI：10.1017/s0317167100001372

  日期：2001.8

  Neurocognitive impairment is a frequent complication of HIV infection and heralds a poor survival prognosis. With the availability of highly active antiretroviral therapy (HAART), survival times for HIV-infected patients have markedly increased although the effects of HAART on the prevalence of neurocognitive impairment remain uncertain.

  To determine the relationship between self-reported neurocognitive symptoms and neuropsychological (NP) performance together with the impact of HAART among HIV-infected patients.

  A cross-sectional study was performed in which patients without previously documented neurocognitive impairment attending an HIV community clinic were questioned about neurocognitive symptoms and a NP test battery was administered.

  Of the eighty-three patients examined, neurocognitive symptoms were reported by 34% of patients and were associated with a shorter duration of HAART and higher viral loads. Patients reporting neurocognitive symptoms were also more likely to exhibit impaired NP performance (p<0.005) with NP impairment being detected in 46% of all patients examined (12% with HIV-associated dementia). Neuropsychological impairment was directly correlated with age (p<0.001), plasma viral load (p<0.005) and inversely correlated with the number of prescribed antiretroviral drugs (p<0.01).

  These results suggest that neurocognitive symptoms are predictive of impaired NP performance and that NP impairment remains a frequent finding among older patients with higher viral loads. An increased number of antiretroviral drugs may be neuroprotective.

  背景：神经认知障碍是艾滋病病毒感染的常见并发症，预示着不良的生存预后。随着高效抗逆转录病毒疗法（HAART）的出现，艾滋病病毒感染者的生存时间明显延长，但HAART对神经认知障碍发生率的影响仍不确定。目的：确定艾滋病病毒感染者自我报告的神经认知症状与神经心理学（NP）表现之间的关系以及HAART的影响。结果：在接受检查的 83 名患者中，有 34% 的患者报告了神经认知症状，这些症状与较短的 HAART 持续时间和较高的病毒载量有关。报告有神经认知症状的患者也更有可能表现出NP功能受损（p<0.005），在所有受检患者中，46%的患者（12%患有HIV相关性痴呆）发现了NP功能受损。神经心理障碍与年龄（p<0.001）、血浆病毒载量（p<0.005）直接相关，与处方抗逆转录病毒药物的数量成反比（p<0.01）。更多的抗逆转录病毒药物可能具有神经保护作用。
• HETEROCYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE COMPRISING SAME
  申请人：LG CHEM, LTD.

  公开号：US20200048226A1

  公开（公告）日：2020-02-13

  The present specification relates to a heterocyclic compound of Chemical Formula 1, and an organic light emitting device comprising the same. The heterocyclic compound as a material of an organic material layer of the organic light emitting device provides enhanced efficiency, low driving voltage and increased lifetime.

  本规范涉及化学式1的杂环化合物，以及包含该化合物的有机发光器件。作为有机发光器件有机材料层的材料，这种杂环化合物提供了增强效率、低驱动电压和延长寿命的特性。