1-氨基甲基-1,2,3,4-四氢-萘-1-醇 | 50361-60-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: 1-氨基甲基-1,2,3,4-四氢-萘-1-醇
• 中文别名: 1-(氨基甲基)-1,2,3,4-四氢萘-1-酚
• 英文名称: 1-aminomethyl-1-hydroxy-1,2,3,4-tetrahydronaphthalene
• 英文别名: (+/-)-1-(aminomethyl)-1-hydroxy-1,2,3,4-tetrahydronaphthalene；1-(aminomethyl)-1,2,3,4-tetrahydro-1-naphthalenol；1-aminomethyl-1,2,3,4-tetrahydronaphthalene-1-ol；(1,2,3,4-tetrahydro-1-hydroxynaphthyl)methylamine；1-aminomethyl-1-hydroxytetralin；1-(Aminomethyl)-1,2,3,4-tetrahydronaphthalen-1-ol；1-(aminomethyl)-3,4-dihydro-2H-naphthalen-1-ol
• CAS: 50361-60-9
• 化学式: C₁₁H₁₅NO
• mdl: MFCD02179235
• 分子量: 177.246
• InChiKey: JPSHSGBMKXSDOR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.454
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  2

安全信息

• 海关编码：
  2922299090

反应信息

• 作为反应物：
  描述：

  1-氨基甲基-1,2,3,4-四氢-萘-1-醇 在 盐酸 作用下， 以 乙醇 、 水 为溶剂， 以72%的产率得到(1,2-dihydronaphthalen-4-yl)methanamine hydrochloride
  参考文献：
  名称：

  N6-Substituted adenosine receptor agonists: potential antihypertensive agents

  摘要：

  Adenosine is known to exert a wide range of pharmacological effects including hypotension. This effect of adenosine suggested that modified analogues of adenosine might provide useful antihypertensive agents. Thus, we prepared a series of novel N6-benzocycloalkyladenosines and studied their receptor binding and antihypertensive activity. The structure-activity relationship study shows that the adenosine analogues having the hydrophobic phenyl moiety one carbon away from the C6-nitrogen have modest affinity and selectivity for the A1 receptor, whereas those with the phenyl moiety two carbons away from the C6-nitrogen have excellent affinity and selectivity for the A1 receptor. Many of these analogues showed excellent antihypertensive activity with a wide range of effects on heart rate. There is no direct correlation between the receptor binding affinities and antihypertensive activity; however, it is more closely associated with A1 than A2 affinity. The bradycardic effect of these agonists seems to be due to the A1 affinity. From this set, compound 3 was further evaluated in secondary antihypertensive screens. It lowered the blood pressure dose dependently with effects lasting for over 20 h following administration of a 30 mg/kg dose. Compound 3 was also effective in lowering blood pressure in a renal hypertensive rat model. Thus, appropriately modified N6-substituted adenosines represent a novel class of antihypertensive agents.

  DOI：

  10.1021/jm00107a025
• 作为产物：
  描述：

  3,4-二氢-1(2H)-萘酮 在 lithium aluminium tetrahydride 、 三氯化铝 作用下， 以 四氢呋喃 为溶剂， 反应 21.0h， 生成 1-氨基甲基-1,2,3,4-四氢-萘-1-醇
  参考文献：
  名称：

  N6-Substituted adenosine receptor agonists: potential antihypertensive agents

  摘要：

  Adenosine is known to exert a wide range of pharmacological effects including hypotension. This effect of adenosine suggested that modified analogues of adenosine might provide useful antihypertensive agents. Thus, we prepared a series of novel N6-benzocycloalkyladenosines and studied their receptor binding and antihypertensive activity. The structure-activity relationship study shows that the adenosine analogues having the hydrophobic phenyl moiety one carbon away from the C6-nitrogen have modest affinity and selectivity for the A1 receptor, whereas those with the phenyl moiety two carbons away from the C6-nitrogen have excellent affinity and selectivity for the A1 receptor. Many of these analogues showed excellent antihypertensive activity with a wide range of effects on heart rate. There is no direct correlation between the receptor binding affinities and antihypertensive activity; however, it is more closely associated with A1 than A2 affinity. The bradycardic effect of these agonists seems to be due to the A1 affinity. From this set, compound 3 was further evaluated in secondary antihypertensive screens. It lowered the blood pressure dose dependently with effects lasting for over 20 h following administration of a 30 mg/kg dose. Compound 3 was also effective in lowering blood pressure in a renal hypertensive rat model. Thus, appropriately modified N6-substituted adenosines represent a novel class of antihypertensive agents.

  DOI：

  10.1021/jm00107a025

文献信息

• MORPHOLINE COMPOUNDS
  申请人：Casimiro-Garcia Agustin

  公开号：US20110281854A1

  公开（公告）日：2011-11-17

  Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.

  矿物皮质激素受体拮抗剂（MRa），含有这类抑制剂的药物组合物以及利用这类抑制剂治疗哺乳动物，包括人类，例如糖尿病肾病和高血压。
• Aminoalkyl dihydronaphthalenes
  申请人：Abbott Laboratories

  公开号：US04473586A1

  公开（公告）日：1984-09-25

  Disclosed herein are 1-aminoalkyl-3,4-dihydronaphthalenes represented by the formula ##STR1## wherein n is 1 or 2; R, R.sub.1, and R.sub.2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, thiomethyl, halo, or ##STR2## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula ##STR3## wherein R.sub.7 is loweralkyl of 1 to 4 carbon atoms; or R and R.sub.1, or R.sub.1 and R.sub.2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R.sub.1 or R.sub.2 must be other than hydrogen; and R.sub.3 and R.sub.4 are independently selected from hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula ##STR4## wherein m is 0, 1 or 2, p is 0 or 1, R.sub.8 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R.sub.9 and R.sub.10 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1 to 4 carbon atoms, or halo, or R.sub.9 and R.sub.10 can be taken together to form a methylenedioxy or ethylenedioxy bridge; or 1,4-benzodioxan of the formula ##STR5## wherein q is 1, 2 or 3, and R.sub.11 is hydrogen, methoxy, or halo; or R.sub.3 and R.sub.4 can be taken together to form a piperazino, piperidino or morpholino moiety; and the pharmaceutically acceptable salts thereof. Also disclosed are novel intermediates useful in the preparation of these compounds.

  本公开涉及由下式表示的1-氨基烷基-3,4-二氢萘烯衍生物，其中n为1或2；R、R.sub.1和R.sub.2分别选自氢、羟基、1至3个碳原子的低烷氧基、1至3个碳原子的低烯氧基、硫甲基、卤素，或下式中的其中一种：其中R.sub.5和R.sub.6分别选自氢、1至4个碳原子的低酰基或下式的磺酰基：其中R.sub.7为1至4个碳原子的低烷基；或R和R.sub.1，或R.sub.1和R.sub.2可结合形成亚甲二氧桥或乙烯二氧桥；但R、R.sub.1或R.sub.2中至少有一个必须为氢以外的其他基团；R.sub.3和R.sub.4分别选自氢、1至4个碳原子的低烷基、1至4个碳原子的卤素取代的低烷基、下式的芳基烷基：其中m为0、1或2，p为0或1，R.sub.8为氢或1至4个碳原子的低烷基，R.sub.9和R.sub.10分别选自氢、羟基、甲氧基、1至4个碳原子的低烷基或卤素，或R.sub.9和R.sub.10可结合形成亚甲二氧桥或乙烯二氧桥；或下式的1,4-苯二氧杂环己烷：其中q为1、2或3，R.sub.11为氢、甲氧基或卤素；或R.sub.3和R.sub.4可结合形成哌嗪基、哌啶基或吗啉基；以及其药用盐。还公开了用于制备这些化合物的新型中间体。
• Propanolamine derivatives
  申请人：Fujisawa Pharmaceutical Co. Ltd.

  公开号：US20020120148A1

  公开（公告）日：2002-08-29

  This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: 1 Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

  这项发明涉及新的丙醇胺衍生物或其盐，其化学式如下所示：1其中每个符号如规范中定义，或具有选择性肠道交感神经兴奋作用、抗溃疡、抗胰腺炎、脂解作用、抗尿失禁和抗尿频活性的盐，以及其制备方法、包含相同的药物组合物以及用于预防和/或治疗规范中指示的疾病的方法，适用于人类或动物。
• Tetracyclic spirobenzazepine dopamine antagonists
  申请人：Abbott Laboratories

  公开号：US05158948A1

  公开（公告）日：1992-10-27

  Novel tetracyclic spirobenzazepine compounds of the formula ##STR1## or a pharmaceutically-acceptable salt, amide or ester thereof, which are dopamine D-1 receptor antagonists useful for treating dopamine-related neurological and psychological disorders, cognitive impairment, attention deficit disorders and addictive behavior disorders.

  新型四环螺合苯并哌啶类化合物的化学式为##STR1##或其药用盐、酰胺或酯，这些化合物是多巴胺D-1受体拮抗剂，用于治疗与多巴胺相关的神经和心理障碍、认知障碍、注意力缺陷障碍和成瘾行为障碍。
• Fused imidazole derivative
  申请人：——

  公开号：US20040198791A1

  公开（公告）日：2004-10-07

  According to the present invention, fused imidazole derivatives of the general formula: 1 wherein R 1 is a hydrogen atom, a halogen atom, hydroxy group, a lower alkyl group or a lower alkoxy group, R 2 is an aryl group, benzodioxanyl group, or 5-6 membered, monocyclic, unsaturated, heterocyclic group containing nitrogen atom(s) which may be substituted with lower alkyl, trityl or oxo, R 3 is a hydrogen atom or hydroxy group, A is a group represented by the formula: —(CH 2 ) m — or —O—(CH 2 ) m — [wherein m is an integer of 1-3] and their salts are provided.

  根据本发明，提供了一般式为：1的熔融咪唑衍生物，其中R1为氢原子、卤素原子、羟基、低碳基或低氧基；R2为芳基、苯二氧基基团或含有氮原子的5-6成员单环不饱和杂环基团，可被低碳基、三苯基或氧代取代；R3为氢原子或羟基；A为以下式子所代表的基团：—(CH2)m—或—O—(CH2)m—[其中，m为1-3的整数]及其盐。