2-hydroxy-7-methyl-1,2,3,4-tetrahydronaphthalene | 87751-15-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 2-hydroxy-7-methyl-1,2,3,4-tetrahydronaphthalene
• 英文别名: 7-Methyl-1,2,3,4-tetrahydronaphthalen-2-ol
• CAS: 87751-15-3
• 化学式: C₁₁H₁₄O
• 分子量: 162.232
• InChiKey: NJBBPZLNKGAUAG-UHFFFAOYSA-N

物化性质

• 熔点：
  84-85 °C
• 沸点：
  286.9±29.0 °C(Predicted)
• 密度：
  1.084±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  20.2
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2-hydroxy-7-methyl-1,2,3,4-tetrahydronaphthalene 在 硫酸 、 碘 作用下， 以 苯 为溶剂， 反应 4.0h， 生成 3-Methoxy-8-methyl-1,3,4,5-tetrahydro-benzo[c]oxepine
  参考文献：
  名称：

  A Novel Route for the Synthesis of 3,4-Dihydro-1H-2-benzopyrans and 1,3,4,5-Tetrahydro-2-benzoxepins

  摘要：

  DOI：

  10.1055/s-1983-30443
• 作为产物：
  描述：

  1,2-epoxy-7-methyl-1,2,3,4-tetrahydronaphthalene 在 lithium aluminium tetrahydride 作用下， 以 乙醚 为溶剂， 反应 2.0h， 以74%的产率得到2-hydroxy-7-methyl-1,2,3,4-tetrahydronaphthalene
  参考文献：
  名称：

  A Novel Route for the Synthesis of 3,4-Dihydro-1H-2-benzopyrans and 1,3,4,5-Tetrahydro-2-benzoxepins

  摘要：

  DOI：

  10.1055/s-1983-30443

文献信息

• Bicyclic Amide, Carbamate or Urea Derivatives as Vanilloid Receptor Modulators
  申请人：Mogi Muneto

  公开号：US20080058377A1

  公开（公告）日：2008-03-06

  This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

  本发明涉及用作药物制剂活性成分的双环酰胺、氨基甲酸酯或脲衍生物及其盐。本发明的双环酰胺、氨基甲酸酯或脲衍生物具有vanilloid受体（VR1）拮抗活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗泌尿系统疾病或障碍，如膀胱过度活动（过度活跃的膀胱）、尿失禁、神经源性膀胱过度活动（膀胱过度活跃）、特发性膀胱过度活动（膀胱不稳定）、良性前列腺增生和下尿路症状；慢性疼痛、神经痛、术后疼痛、风湿性关节炎疼痛、神经痛、神经病、疼痛、神经损伤、缺血、神经变性、中风以及哮喘和慢性阻塞性肺（或气道）疾病（COPD）等炎症性疾病。
• 2-AMINOBENZAMIDE DERIVATIVE
  申请人：Kuramochi Takahiro

  公开号：US20090233900A1

  公开（公告）日：2009-09-17

  To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.

  本发明提供了一种基于对辣椒素受体VR1激活的抑制作用的新型优良药剂，用于治疗或预防伤害性疼痛、神经病理性疼痛、癌症疼痛、头痛、膀胱功能障碍等疾病。本发明通过确认一种苯甲酰胺衍生物，其特征在于其苯环上的单环在酰胺基氮原子上被紧缩，其低烷基氨基或邻位于酰胺基的环基取代的氨基具有对VR1激活的强抑制作用和优良的药理作用，从而发现它可以成为治疗或预防伤害性疼痛、神经病理性疼痛、癌症疼痛、头痛、膀胱功能障碍等VR1相关疾病的优良药剂。
• FUSED HETEROCYCLIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
  申请人：Kuduk Scott D.

  公开号：US20110201607A1

  公开（公告）日：2011-08-18

  The present invention is directed to fused heterocyclic compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

  本发明涉及公式(I)的融合杂环化合物，其为M1受体正向变构调节剂，可用于治疗M1受体参与的疾病，如阿尔茨海默病、精神分裂症、疼痛或睡眠障碍。本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗M1受体介导的疾病中的使用。
• 2-AMINOBENZAMIDE DERIVATIVES AS VANILLOID RECEPTOR 1 (VR1) INHIBITORS USEFUL FOR THE TREATMENT OF PAIN OR BLADDER FUNCTION DISORDER
  申请人：Astellas Pharma Inc.

  公开号：EP1955697B1

  公开（公告）日：2012-05-02
• TALEKAR, D. G.;RAO, A. S., SYNTHESIS, BRD, 1983, N 7, 595-597
  作者：TALEKAR, D. G.、RAO, A. S.

  DOI：——

  日期：——