6-Methoxy-2-(3-methoxy-phenyl)-1,2,3,4-tetrahydro-quinoline | 476159-13-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 6-Methoxy-2-(3-methoxy-phenyl)-1,2,3,4-tetrahydro-quinoline
• 英文别名: 6-methoxy-2-(3-methoxyphenyl)-1,2,3,4-tetrahydroquinoline
• CAS: 476159-13-4
• 化学式: C₁₇H₁₉NO₂
• 分子量: 269.343
• InChiKey: SPHOKLLEWNCLKV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  30.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-Methoxy-2-(3-methoxy-phenyl)-1,2,3,4-tetrahydro-quinoline 在 lithium aluminium tetrahydride 、 三溴化硼 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 生成 2-(3-Hydroxy-phenyl)-1-[4-(2-piperidin-1-yl-ethoxy)-benzyl]-1,2,3,4-tetrahydro-quinolin-6-ol
  参考文献：
  名称：

  Tetrahydroquinoline-Based selective estrogen receptor modulators (SERMs)

  摘要：

  A new series of estrogen receptor ligands based on a 6-hydroxy-tetrahydroquinoline scaffold is described, in addition to their binding affinity and functional activity in MCF-7 cells. Several 1,2-disubstituted tetrahydroquinolines bearing a basic side chain were shown to be high affinity ligands and antagonists in the MCF-7 proliferation assay. Compounds lacking the basic side chain were agonists in the MCF-7 assay. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00306-8
• 作为产物：
  描述：

  6-methoxy-2-(3-methoxyphenyl)quinoline 在 乙醇 、 sodium 作用下， 生成 6-Methoxy-2-(3-methoxy-phenyl)-1,2,3,4-tetrahydro-quinoline
  参考文献：
  名称：

  Tetrahydroquinoline-Based selective estrogen receptor modulators (SERMs)

  摘要：

  A new series of estrogen receptor ligands based on a 6-hydroxy-tetrahydroquinoline scaffold is described, in addition to their binding affinity and functional activity in MCF-7 cells. Several 1,2-disubstituted tetrahydroquinolines bearing a basic side chain were shown to be high affinity ligands and antagonists in the MCF-7 proliferation assay. Compounds lacking the basic side chain were agonists in the MCF-7 assay. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00306-8

文献信息

• 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods
  申请人：——

  公开号：US20040215018A1

  公开（公告）日：2004-10-28

  The current invention provides novel 2-substituted 1,2,3,4-tetrahydroquinolin-6-ols and derivatives thereof of the formula (I) (A); pharmaceutical compositions thereof, optionally in combination with estrogen or progestin; methods for inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen. 1

  当前发明提供了新型的2-取代的1,2,3,4-四氢喹啉-6-醇及其衍生物，其化学式为(I) (A)；其中包括与雌激素或孕激素可选地结合的制药组合物；用于抑制与雌激素缺乏有关的疾病的方法；以及用于抑制与内源性雌激素异常生理反应有关的疾病的方法。
• Tetrahydroquinolin derivatives for the inhibition of diseases associated with estrogen deprivation or with an aberrant physiological response to endogenous estrogen
  申请人：——

  公开号：US20040132770A1

  公开（公告）日：2004-07-08

  The current invention provides methods for inhibiting a disease associated with estrogen deprivation and for inhibiting disease associated with an aberrant physiological response to endogenous estrogen comprising administering 2-substituted 1,2,3,4-tetrahydroquinolin-6-ols and derivatives thereof.

  本发明提供了一种抑制与雌激素缺乏相关疾病和抑制与内源性雌激素异常生理反应相关疾病的方法，包括给予2-取代的1,2,3,4-四氢喹啉-6-醇及其衍生物。
• Tetrahydroquinoline derivatives for the inhibition of osteoporosis, estrogen dependent breast cancer, endometriosis and uterine fibrosis
  申请人：Wallace Owen Brendan

  公开号：US06962928B2

  公开（公告）日：2005-11-08

  The current invention provides methods for inhibiting osteoporosis, estrogen dependent breast cancer, endometriosis and uterine fibrosis comprising administering to a patient in need thereof a compound of the formula:

  当前发明提供了一种抑制骨质疏松症、雌激素依赖性乳腺癌、子宫内膜异位症和子宫纤维化的方法，包括向需要该方法的患者施用式中的化合物：
• 2-SUBSTITUTED 1,2,3,4-TETRAHYDROQUINOLINES AND DERIVATIVES THEREOF, COMPOSITIONS AND METHODS
  申请人：ELI LILLY AND COMPANY

  公开号：EP1395563A1

  公开（公告）日：2004-03-10
• TETRAHYDROQUINOLIN DERIVATIVES FOR THE INHIBITION OF DISEASES ASSOCIATED WITH ESTROGEN DEPRIVATION OR WITH AN ABERRANT PHYSIOLOGICAL RESPONSE TO ENDOGENOUS ESTROGEN
  申请人：ELI LILLY AND COMPANY

  公开号：EP1401446B1

  公开（公告）日：2005-02-09