7-methoxy-1-aminomethyl-1-hydroxytetraline | 57314-43-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 7-methoxy-1-aminomethyl-1-hydroxytetraline
• 英文别名: 7-Methoxy-1-aminomethyl-1,2,3,4-tetrahydro-1-naphthol；1-aminomethyl-7-methoxy-1,2,3,4-tetrahydro-1-naphthalenol；1-aminomethyl-1-hydroxy-7-methoxytetralin；1-(Aminomethyl)-7-methoxy-1,2,3,4-tetrahydronaphthalen-1-ol；1-(aminomethyl)-7-methoxy-3,4-dihydro-2H-naphthalen-1-ol
• CAS: 57314-43-9
• 化学式: C₁₂H₁₇NO₂
• mdl: MFCD11590981
• 分子量: 207.272
• InChiKey: LNGNAFBJTXOICZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  55.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  7-methoxy-1-aminomethyl-1-hydroxytetraline 在 sodium nitrite 作用下， 以 水 、 溶剂黄146 、 乙酸乙酯 为溶剂， 生成 3-methoxy-6,7,8,9-tetrahydro-5H-benzo[a]cyclohepten-6-one
  参考文献：
  名称：

  Ethanolamine derivatives having sympathomimetic and anti-pollakiuria

  摘要：

  这项发明涉及具有肠道选择性交感兴奋作用和抗多尿活性的新乙醇胺衍生物，其通式为[I]：其中R.sup.1是芳基或杂环基，每个都可以用卤素等取代，R.sup.2是氢、卤素、硝基、羟基、可选择用酰基取代的较低烷基、可选择用酰基取代的较低烯基、可选择用酰基取代的较低烷氧基、或者可选择用酰基（较低）烷基取代的氨基，R.sup.3是氢、N-保护基，或者可选择用较低烷基硫代取代的较低烷基，n是0到3的整数，重实线表示单键或双键，但当n为1时，则1）R.sup.1是缩合芳香烃基或杂环基，每个都可以用卤素等取代，等等，以及其药学上可接受的盐，以及制备它们的方法和包含相同的药物组合。

  公开号：

  US05387710A1
• 作为产物：
  描述：

  7-methoxy-1-(trimethylsilyloxy)-1,2,3,4-tetrahydronaphthalene-1-carbonitrile 在 lithium aluminium tetrahydride 作用下， 生成 7-methoxy-1-aminomethyl-1-hydroxytetraline
  参考文献：
  名称：

  Novel Potent Antagonists of Human Neuropeptide Y Y5 Receptors. Part 3: 7-Methoxy-1-hydroxy-1-substituted Tetraline Derivatives

  摘要：

  As a part of our continuing research on NPY-Y5 receptor antagonists in the series of novel 6-methoxybenzo[a]cycloheptene derivatives, we discovered a novel skeleton, 7-methoxy-1-hydroxytetraline 7 which had been used as an intermediate, to be more suitable for increasing potencies leading to compound 3 (FR230481). Additionally. we discovered that the naphthalenesulfonamide moiety which was thought to be an essential pharmacophore could be replaced by the 5-chlorobenzothiazolin-3-acetic acid moiety to lead to potent compound 4 (FR233118). The structure-activity relationships on compounds 3, 4 and their related derivatives are described. Unfortunately. although compounds 3 and 4 had very high affinities for Y5 receptors, their poor permeabilities to brain were shown by exo-vivo binding assays when orally administered. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00018-5

文献信息

• Ethanolamine derivatives having sympathomimetic and anti-pollakiuria
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US05387710A1

  公开（公告）日：1995-02-07

  This invention relates to new ethanolamine derivatives having gut selective sympathomimetic and anti-pollakiuria activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is aryl or a heterocyclic group, each of which may be substituted with halogen, etc., R.sup.2 is hydrogen, halogen, nitro, hydroxy, lower alkyl optionally substituted with acyl, lower alkenyl optionally substituted with acyl, lower alkoxy optionally substituted with acyl, or amino optionally substituted with acyl(lower)alkyl, R.sup.3 is hydrogen, an N-protective group, or lower alkyl optionally substituted with lower alkylthio, n is an integer of 0 to 3, and a heavy solid line means a single bond or a double bond, provided that when n is 1, then 1) R.sup.1 is a condensed aromatic hydrocarbon group or a heterocyclic group, each of which may be substituted with halogen, etc., and the like, and pharmaceutically acceptable salts thereof to processes for the preparation thereof and to a pharmaceutical composition comprising the same.

  这项发明涉及具有肠道选择性交感兴奋作用和抗多尿活性的新乙醇胺衍生物，其通式为[I]：其中R.sup.1是芳基或杂环基，每个都可以用卤素等取代，R.sup.2是氢、卤素、硝基、羟基、可选择用酰基取代的较低烷基、可选择用酰基取代的较低烯基、可选择用酰基取代的较低烷氧基、或者可选择用酰基（较低）烷基取代的氨基，R.sup.3是氢、N-保护基，或者可选择用较低烷基硫代取代的较低烷基，n是0到3的整数，重实线表示单键或双键，但当n为1时，则1）R.sup.1是缩合芳香烃基或杂环基，每个都可以用卤素等取代，等等，以及其药学上可接受的盐，以及制备它们的方法和包含相同的药物组合。
• 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。
• 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.

  本文披露了由以下式子表示的1-氨基烷基-3,4-二氢萘烯：##STR1## 其中n为1或2；R、R.sub.1和R.sub.2分别选择自氢、羟基、1至3个碳原子的低烷氧基、1至3个碳原子的低烷基氧基、硫甲基、卤素或##STR2## 其中R.sub.5和R.sub.6分别选择自氢、1至4个碳原子的低酰基或公式##STR3## 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可以结合形成亚甲二氧基或乙亚甲二氧基桥；但必须至少有一个R、R.sub.1或R.sub.2不是氢；而R.sub.3和R.sub.4分别选择自氢；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；公式##STR4## 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，而R.sub.9和R.sub.10分别选择自氢、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可以结合形成亚甲二氧基或乙亚甲二氧基桥；或公式##STR5## 其中q为1、2或3，而R.sub.11为氢、甲氧基或卤素；或R.sub.3和R.sub.4可以结合形成哌嗪基、哌啶基或吗啉基；以及其药学上可接受的盐。本文还披露了制备这些化合物有用的新型中间体。
• FUSED IMIDAZOLE DERIVATIVE
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP1403256A1

  公开（公告）日：2004-03-31

  According to the present invention, fused imidazole derivatives of the general formula: wherein R1 is a hydrogen atom, a halogen atom, hydroxy group, a lower alkyl group or a lower alkoxy group, R2 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, R3 is a hydrogen atom or hydroxy group, A is a group represented by the formula : -(CH2)m - or -O-(CH2)m- [wherein m is an integer of 1-3] and their salts are provided.

  根据本发明，通式如下的融合咪唑衍生物 其中 R1 是氢原子、卤素原子、羟基、低级烷基或低级烷氧基、 R2 是芳基、苯并二恶烷基或含有氮原子的 5-6 位单环、不饱和杂环基团，可被低级烷基、三烷基或氧代取代、 R3 是氢原子或羟基，A 是由式：-(CH2)m-或-O-(CH2)m-[其中 m 为 1-3 的整数]。 以及它们的盐。
• EP1403256
  申请人：——

  公开号：——

  公开（公告）日：——