7-羟基-1,2,3,4-四氢异喹啉盐酸盐 | 66393-01-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 四氢异喹啉
• 中文名称: 7-羟基-1,2,3,4-四氢异喹啉盐酸盐
• 英文名称: 7-hydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride
• 英文别名: 1,2,3,4-tetrahydroisoquinolin-7-ol hydrochloride；1,2,3,4-Tetrahydro-isochinolin-7-ol; Hydrochlorid；7-Hydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride salt；1,2,3,4-tetrahydroisoquinolin-7-ol;hydrochloride
• CAS: 66393-01-9
• 化学式: C₉H₁₁NO*ClH
• 分子量: 185.653
• InChiKey: ZVQYIOOMWIVFQP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.46
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  32.3
• 氢给体数：
  3
• 氢受体数：
  2

安全信息

• 海关编码：
  2933499090
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  7-羟基-1,2,3,4-四氢异喹啉盐酸盐 在 tris-(dibenzylideneacetone)dipalladium(0) 、 potassium carbonate 、 2-二-叔丁膦基-2',4',6'-三异丙基联苯 作用下， 以 乙二醇二甲醚 、 N,N-二甲基甲酰胺 为溶剂， 反应 5.0h， 生成 methyl [(6S)-4-{4-[7-(2-t-butoxy-2-oxoethoxy)-3,4-dihydroisoquinolin-2(1H)-yl]phenyl}-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetate
  参考文献：
  名称：

  ＢＥＴ蛋白質分解誘導作用を有するアミド化合物及びその医薬としての用途

  摘要：

  对癌细胞具有细胞损伤作用，诱导癌细胞中BET蛋白质的降解作用，以及优越的BET蛋白质与乙酰化组蛋白结合抑制作用，提供作为抗癌药物、BET蛋白质降解诱导剂和BET蛋白质抑制剂有用的化合物。该化合物或其药理学上可接受的盐由下述通用式（I）表示。{式中，各符号如在说明书中定义。}

  公开号：

  WO2020009176A1
• 作为产物：
  描述：

  7-羟基-3,4-二氢异喹啉-2(1h)-羧酸叔丁酯 在 盐酸 作用下， 以 水 、 乙酸乙酯 、 叔丁醇 为溶剂， 反应 2.0h， 以665 mg的产率得到7-羟基-1,2,3,4-四氢异喹啉盐酸盐
  参考文献：
  名称：

  ＢＥＴ蛋白質分解誘導作用を有するアミド化合物及びその医薬としての用途

  摘要：

  对癌细胞具有细胞损伤作用，诱导癌细胞中BET蛋白质的降解作用，以及优越的BET蛋白质与乙酰化组蛋白结合抑制作用，提供作为抗癌药物、BET蛋白质降解诱导剂和BET蛋白质抑制剂有用的化合物。该化合物或其药理学上可接受的盐由下述通用式（I）表示。{式中，各符号如在说明书中定义。}

  公开号：

  WO2020009176A1

文献信息

• New 1,2,3,4-tetrahydroisoquinoline derivatives as modulators of proteolytic cleavage of amyloid precursor proteins
  作者：Ming-Kuan Hu、Yung-Feng Liao、Jung-Fang Chen、Bo-Jeng Wang、Ying-Tsen Tung、Hui-Ching Lin、Kang-Po Lee

  DOI：10.1016/j.bmc.2007.10.101

  日期：2008.2.15

  processing of amyloid precursor protein (APP) by an ERK-dependent signaling pathway. Additionally, these compounds were also evaluated on the prevention of the proteolytic processing of C99 as gamma-secretase inhibitors by using a highly efficient cell-based reporter gene assay for gamma-secretase. The results suggested that certain compounds might be explored to possess both sAPPalpha-releasing stimulation

  通过简洁的方法，从市售的四氢异喹啉合成了一种新的1,2,3,4-四氢异喹啉衍生物。这些衍生物经过精心设计，具有与单胺氧化酶抑制剂雷沙吉兰模拟的炔丙基相关的药效团。我们研究了这些合成的四氢异喹啉衍生物对ERK依赖性信号传导途径对淀粉样蛋白前体蛋白（APP）的蛋白水解过程的调节作用。另外，还通过使用高效的基于细胞的γ-分泌酶报告基因检测方法，评估了这些化合物是否可预防C99作为γ-分泌酶抑制剂的蛋白水解过程。结果表明，可以探索某些化合物同时具有sAPPalpha释放刺激和γ分泌酶抑制能力，
• 1,2,3,4-Tetrahydroisoquinoline Derivatives, Preparation Process therefor and Pharmaceutical Composition Containing the Same
  申请人：Hu Ming-Kuan

  公开号：US20100016309A1

  公开（公告）日：2010-01-21

  The invention provides a type of novel 1,2,3,4-tetrahydroisoquinoline derivatives with a structure of formula (I): wherein R1 represents propargyl or cyclopropylmethyl; wherein R2 represents N-ethyl-N-methylamino, 1-Pyrrolidyl, 1-Piperidinyl, or 1-Morpholinyl. The invention provides further a process for preparing said derivatives and a pharmaceutical composition containing the same. Said derivatives can be used to modulate the proteolytic process of amyloid precursor proteins (APP), and provides further novel compounds useful for treating Alzheimer's disease (AD).

  该发明提供了一种具有式(I)结构的新型1,2,3,4-四氢异喹啉衍生物，其中R1代表丙炔基或环丙基甲基；其中R2代表N-乙基-N-甲基氨基，1-吡咯基，1-哌啶基或1-吗啉基。该发明进一步提供了制备上述衍生物的方法和含有它们的药物组合物。这些衍生物可用于调节淀粉样前体蛋白（APP）的蛋白酶过程，并进一步提供了用于治疗阿尔茨海默病（AD）的新型化合物。
• AMIDE COMPOUND HAVING BET PROTEOLYSIS-INDUCING ACTION AND MEDICINAL APPLICATION THEREOF
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP3819305A1

  公开（公告）日：2021-05-12

  Provided are a compound superior in a cytotoxic action on cancer cells, an action inducing degradation of BET protein in cancer cells, and an inhibitory action on the binding of BET protein and acetylated histone, and useful as an anticancer agent, a BET protein degradation inducer or a BET protein inhibitor. A compound represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof

  本发明提供了一种化合物，该化合物对癌细胞具有卓越的细胞毒性作用、诱导癌细胞中 BET 蛋白降解的作用以及抑制 BET 蛋白与乙酰化组蛋白结合的作用，可用作抗癌剂、BET 蛋白降解诱导剂或 BET 蛋白抑制剂。下式（I）代表的化合物 其中各符号如说明书中所定义，或其药理上可接受的盐
• Patterns of Religious Practice and Belief in the Last Year of Life
  作者：E. L. Idler、S. V. Kasl、J. C. Hays

  DOI：10.1093/geronb/56.6.s326

  日期：2001.11.1

  Objectives. Although it is frequently assumed that issues of religious faith become more salient at the end of life. there is little or no population-based empirical evidence testing this assumption.Methods. Using data from the New Haven site of the Established Populations for Epidemiologic Studies of the Elderly (N = 2.812). the authors examined self-reports of attendance at services. self-ratings of religiousness, and strength and comfort felt from religion for respondents who did and did not die within 12 months following an interview. Religiousness was assessed at baseline (1982) and in follow-up interviews in 1985, 1988, and 1994. Cross-sectional comparisons of levels of religiousness were made among persons in their last 6 months of life, persons in their last 12 months of life, and persons who survived 12 months, and longitudinal comparisons were made with religiousness at the previous wave.Results. After adjusting for age, sex, education. marital status, religious affiliation, and a set of health status measures. the authors found that although attendance at religious services declined among the near-deceased, this group showed either stability or a small increase in feelings of religiousness and strength/comfort received from religion. Overall levels of attendance and religious feelings were high for this religiously diverse sample.Discussion. Community studies of respondents in their last year of life are rare. In this sample, religious involvement appears to continue throughout the last months of life.
• US8173648B2
  申请人：——

  公开号：US8173648B2

  公开（公告）日：2012-05-08

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