N-乙基-1-萘胺盐酸盐 | 36101-15-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 中文名称: N-乙基-1-萘胺盐酸盐
• 中文别名: N-1-萘乙胺盐酸盐
• 英文名称: N-ethyl-α-naphthylamine hydrochloride
• 英文别名: ethyl-[1]naphthyl-amine; hydrochloride；Aethyl-[1]naphthyl-amin; Hydrochlorid；N-ethyl-1-naphthylamine hydrochloride；N-ethylnaphthalen-1-amine;hydrochloride
• CAS: 36101-15-2
• 化学式: C₁₂H₁₃N*ClH
• 分子量: 207.703
• InChiKey: CZPDZIFRRRQSHM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.79
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.166
• 拓扑面积：
  12
• 氢给体数：
  2
• 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：

  N-乙基-1-萘胺盐酸盐 、 环氧氯丙烷 生成 1-(ethyl-[1]naphthyl-amino)-3-chloro-propan-2-ol
  参考文献：
  名称：

  Woroshzow; Kutkewitschus, Zhurnal Obshchei Khimii, 1957, vol. 27, p. 2152,2159, engl. Ausg. S. 2210, 2215, 2216

  摘要：

  DOI：

文献信息

• [EN] PROCESS FOR PREPARING CINACALCET<br/>[FR] PROCEDE DE PREPARATION DE CINACALCET
  申请人：ZACH SYSTEM SPA

  公开号：WO2011029833A1

  公开（公告）日：2011-03-17

  A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine of formula hydrochloride salt of formula (I); i.e. Cinacalcet.HC1 and its intermediate of formula (IX).

  一种制备化学式为盐酸盐(I)的N-[(1R)-1-(1-萘基)乙基]-3-[3-(三氟甲基)苯基]丙基胺（即Cinacalcet.HCl）及其中间体化学式为(IX)的方法。
• PROCESS FOR PREPARING CINACALCET HYDROCHLORIDE
  申请人：Shanghai Jingxin Biomedical Co., Ltd.

  公开号：US20150080608A1

  公开（公告）日：2015-03-19

  Method for preparing cinacalcet hydrochloride having the steps of heating (R)-1-naphthyl ethylamine (Formula I) and 3-(trifluoromethyl)benzene (Formula II) wherein L is a halogen atom, methanesulfonate group (OMs), p-Toluenesulfonate (OTs), or triflate (OTf), in an organic solvent in presence of an inorganic base, refluxing until 3-(trifluoromethyl)benzene is completely consumed, obtaining a reaction mixture containing cinacalcet, and after treatment, obtaining cinacalcet hydrochloride having a formula of The post treatment separates (R)-1-naphthyl ethylamine hydrochloride and cinacalcet hydrochloride by adjusting pH value, extraction, and other simple operations, and the (R)-1-naphthyl ethylamine obtained is recycled for preparing the next batch of cinacalcet hydrochloride.

  制备盐酸西那卡塞的方法包括以下步骤：在有机溶剂中，加入无机碱的存在下，加热(R)-1-萘乙胺（式I）和3-(三氟甲基)苯（式II），其中L为卤素原子，甲磺酸基团（OMs），对甲苯磺酸基团（OTs）或三氟甲烷磺酸基团（OTf）；回流至3-(三氟甲基)苯完全消耗，得到含有西那卡塞的反应混合物；经处理后，得到公式为的盐酸西那卡塞；后处理通过调节pH值、萃取和其他简单操作来分离(R)-1-萘乙胺盐酸盐和西那卡塞盐酸盐，所得的(R)-1-萘乙胺可回收用于制备下一批盐酸西那卡塞。
• [EN] NEW NPY ANTAGONISTS<br/>[FR] NOUVEAUX ANTAGONISTES DE NPY
  申请人：ASTRAZENECA AB

  公开号：WO1999015498A1

  公开（公告）日：1999-04-01

  (EN) There is provided pharmaceutically useful compounds of formula (I), wherein Ar1, R1, R2, R3, R4, R5 and R6 have meanings given in the description, which are useful as antagonists of neuropeptide Y and in particular in the treatment of cardiovascular diseases, for example vasoconstriction.(FR) L'invention se rapporte à de nouveaux composés pharmaceutiquement utiles et représentés par la formule (I), dans laquelle Ar1, R1, R2, R3, R4, R5 et R6 possèdent les significations données dans le descriptif de l'invention. Ces composés s'avèrent utiles en tant qu'antagonistes du neuropeptide Y et servent notamment à traiter les maladies cardio-vasculaires, telles que la vasoconstriction.

  提供了公式（I）的药用化合物，其中Ar1，R1，R2，R3，R4，R5和R6具有描述中给出的含义，这些化合物可用作神经肽Y的拮抗剂，特别是用于治疗心血管疾病，例如血管收缩。
• Tri- and tetra-substituted guanidines and their use as excitatory amino
  申请人：State of Oregon, acting by and through the Oregon State Board of Higher

  公开号：US05637622A1

  公开（公告）日：1997-06-10

  Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

  三取代和四取代的胍基化合物具有高结合亲和力，可与苯环环庚啡（PCP）受体结合，更好的是，它们对大脑σ受体的亲和力较低。这些胍基衍生物作为非竞争性抑制剂，通过作为NMDA受体离子通道复合物的通道阻滞剂，阻止谷氨酸诱导的NMDA受体反应。这些化合物因此具有神经保护活性，并可用于治疗低氧、低血糖、脑或脊髓缺血、脑或脊髓创伤引起的神经元丧失，并且对于治疗癫痫、阿尔茨海默病、肌萎缩性侧索硬化、帕金森病、亨廷顿病、唐氏综合症、科萨科夫病和其他神经退行性疾病也有用。
• Tri-and tetra-substituted guanidines and their use as excitatory amino
  申请人：State of Oregon, acting by and through the Oregon State Board of Higher

  公开号：US05767162A1

  公开（公告）日：1998-06-16

  Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

  三取代和四取代的胍基化合物具有高结合亲和力，可与苯环哌啶（PCP）受体结合，并更倾向于低亲和力与大脑西格玛受体结合。这些胍基衍生物作为非竞争性抑制剂，通过阻断NMDA受体离子通道复合物的离子通道作用，从而抑制谷氨酸诱导的NMDA受体反应。这些化合物因此具有神经保护作用，并可用于治疗缺氧、低血糖、脑或脊髓缺血、脑或脊髓创伤以及癫痫、阿尔茨海默病、肌萎缩性侧索硬化、帕金森病、亨廷顿病、唐氏综合症、科萨科夫病和其他神经退行性疾病的治疗。

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