naphthalen-1-yl(thiophen-3-yl)methanone

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: naphthalen-1-yl(thiophen-3-yl)methanone
• 英文别名: (4-Thiophenyl)-naphth-1-yl-ketone
• 化学式: C₁₅H₁₀OS
• 分子量: 238.31
• InChiKey: VVJUGVBWEPGJSY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  45.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  噻吩 、 diethyl hydroxy(naphthalen-1-yl)methylphosphonate 在 iron(III) chloride 、 potassium tert-butylate 、 氧气 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 8.0h， 生成 naphthalen-1-yl(thiophen-2-yl)methanone 、 naphthalen-1-yl(thiophen-3-yl)methanone
  参考文献：
  名称：

  1-萘基（芳基）甲基膦酸酯的Oxy-Wittig反应：萘基芳基酮的新方法

  摘要：

  有价值的化合物，萘基芳基酮是通过在室温下通过产生水溶性副产物的各种1-萘基（芳基）甲基膦酸酯的氧-维蒂希（膦酸碳负离子的氧化）型反应合成的。使用这种无过渡金属，操作简单的策略，可以轻松合成商业上已知但合成未曝光且价格昂贵的萘基芳基酮。作为前体，可以通过涉及FeCl 3的直接且清洁的合成方案以优异的收率和区域选择性获得一系列新的萘基（芳基）甲基膦酸酯。 或三氟甲磺酸（TfOH）介导的易于在室温下接近的（羟基）-1-萘甲基膦酸酯与活化和未活化的芳烃（包括卤化的茴香醚，联苯，萘和pyr（扩展π系统））的芳基化反应。

  DOI：

  10.1016/j.tet.2016.02.053

文献信息

• [EN] MERCAPTO-PHENYL-NAPHTHYL-METHANE DERIVATIVES AND PREPARATION THEREOF<br/>[FR] DERIVES DE MERCAPTO-PHENYLE-NAPHTHYLE-METHANE ET LEUR PREPARATION
  申请人：COUNCIL SCIENT IND RES

  公开号：WO2004087644A1

  公开（公告）日：2004-10-14

  The present invention relates to the field of pharmaceuticals and organic chemistry and provides novel mercapto phenyl naphthyl methane derivatives, their pharmaceutically acceptable salts and compositions and preparation thereof, that are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.

  本发明涉及制药和有机化学领域，提供了新颖的巯基苯基萘甲烷衍生物，其药用可接受的盐和组合物以及其制备，可用于预防或治疗与雌激素依赖性疾病或与骨质疏松、骨质流失、骨形成、心血管疾病、神经退行性疾病、绝经障碍、生理障碍、糖尿病障碍、前列腺癌、乳腺癌、子宫癌、宫颈癌和结肠癌相关的各种医学指征。包括威胁性或习惯性流产、肥胖、卵巢发育或功能、产后哺乳和抑郁症。
• 2-amino-3-aroyl-4,5 alkylthiophenes: agonist allosteric enhancers at human A1 adenosine receptors
  申请人：——

  公开号：US20030078248A1

  公开（公告）日：2003-04-24

  The present invention relates to a compound of formula (I): 1 wherein: R 3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl; and R 4 and R 5 taken together form a ring having from 5 to 10 carbon atoms. Additionally, the invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal subject, such as a human, wherein increased angiogenesis is desired, comprising administering to a mammal in need of such therapy an effective amount of the aforementioned thiophene selective adenosine A 1 allosteric enhancer.

  本发明涉及以下式（I）的化合物：其中：R3选择自1-萘基、2-萘基和环烷基苯基所组成的群；以及R4和R5一起形成含有5到10个碳原子的环。此外，本发明提供了一种治疗方法，用于预防或治疗哺乳动物主体（如人类）中的病理状况或症状，其中需要增加血管生成，包括向需要此类治疗的哺乳动物中施用上述噻吩选择性腺苷A1受体变构增强剂的有效量。
• Novel mercaptophenyl naphthyl methane compounds and synthesis thereof
  申请人：COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH

  公开号：US20040229869A1

  公开（公告）日：2004-11-18

  Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.

  新型巯基苯基萘甲烷化合物及其药学上可接受的盐和组成物，可用于预防或治疗与雌激素依赖性疾病或与骨质疏松、骨质流失、骨形成、心血管疾病、神经退行性疾病、更年期疾病、生理疾病、糖尿病疾病、前列腺癌、乳腺癌、子宫癌、宫颈癌和结肠癌、威胁性流产或习惯性流产、肥胖、卵巢发育或功能、产后泌乳和抑郁症相关的各种医学症状。
• 2-Amino-3-aroyl-4,5 alkylthiophenes: agonist allosteric enhancers at human A1 adenosine receptors
  申请人：——

  公开号：US20040180948A1

  公开（公告）日：2004-09-16

  The present invention relates to a compound of formula (I): 1 wherein: R 3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl; and R 4 and R 5 taken together form a ring having from 5 to 10 carbon atoms. Additionally, the invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal subject, such as a human, wherein increased angiogenesis is desired, comprising administering to a mammal in need of such therapy an effective amount of the aforementioned thiophene selective adenosine A 1 allosteric enhancer.

  本发明涉及一种式（I）的化合物：1其中：R3选自1-萘基，2-萘基和环烷基苯基的群组；以及R4和R5一起形成一个具有5至10个碳原子的环。此外，本发明提供了一种治疗方法，用于预防或治疗哺乳动物受体中的病理状况或症状，例如人类，其中需要增加血管生成，包括向需要此种治疗的哺乳动物中注射上述噻吩选择性腺苷A1异构增强剂的有效剂量。
• Mercaptophenyl naphthyl methane compounds and synthesis thereof
  申请人：Council of Scientific and Industrial Research

  公开号：US07250446B2

  公开（公告）日：2007-07-31

  Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.

  新型巯基苯基萘甲烷化合物及其药用可接受盐和组合物可用于预防或治疗与雌激素依赖性疾病或与骨质疏松症、骨质流失、骨形成、心血管疾病、神经退行性疾病、更年期疾病、生理疾病、糖尿病、前列腺癌、乳腺癌、子宫癌、宫颈癌和结肠癌相关的综合症，威胁性或习惯性流产、肥胖、卵巢发育或功能、产后泌乳和抑郁症。