phenyl(1-trityl-1H-imidazol-4-yl)methanol | 135773-27-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: phenyl(1-trityl-1H-imidazol-4-yl)methanol
• 英文别名: 1-triphenylmethyl-4-[(1-hydroxy-1-phenyl)methyl]-1H-imidazole；phenyl-(1-tritylimidazol-4-yl)methanol
• CAS: 135773-27-2
• 化学式: C₂₉H₂₄N₂O
• 分子量: 416.522
• InChiKey: LMVLGPNXQKDJHR-UHFFFAOYSA-N

物化性质

• 沸点：
  590.7±45.0 °C(Predicted)
• 密度：
  1.11±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.6
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  38
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  phenyl(1-trityl-1H-imidazol-4-yl)methanol 在 三氟乙酸 作用下， 反应 1.0h， 以84%的产率得到(1H-Imidazol-4-yl)-phenyl-methanol; compound with trifluoro-acetic acid
  参考文献：
  名称：

  A facile route to imidazol-4-yl anions and their reaction with carbonyl compounds

  摘要：

  Treatment of N-protected 4-iodoimidazoles 1-3 in CH2Cl2 solution with an ethereal solution of ethyl-magnesium bromide generates the corresponding imidazol-4-yl anions, which react with carbonyl compounds to give carbinols 4-14 in 60-83% yield.

  DOI：

  10.1021/jo00020a002
• 作为产物：
  描述：

  1-三苯甲基咪唑-4-甲醛 在 苯基锂 作用下， 以 四氢呋喃 、 正己烷 、 水 为溶剂， 以76%的产率得到phenyl(1-trityl-1H-imidazol-4-yl)methanol
  参考文献：
  名称：

  Benzopyranone and quinolone inhibitors of ras farnesyl transferase

  摘要：

  本发明提供了化学式I的Ras法尼西基转移酶抑制化合物。本发明还提供了一种治疗癌症、治疗或预防再狭窄或动脉粥样硬化的方法。本发明还提供了一种含有化学式I化合物的药用可接受组合物。

  公开号：

  US06143766A1

文献信息

• [EN] IMIDAZOLE DERIVATIVES AS IDO INHIBITORS<br/>[FR] DÉRIVÉS IMIDAZOLE COMME INHIBITEURS DE L'IDO
  申请人：NEWLINK GENETICS

  公开号：WO2011056652A1

  公开（公告）日：2011-05-12

  Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.

  目前提供的是通用结构式（VII）、（VIII）所示的IDO抑制剂及其药物组合物，用于调节色胺酸2,3-二氧化酶的活性；治疗色胺酸2,3-二氧化酶（IDO）介导的免疫抑制；治疗受益于色胺酸-2,3-二氧化酶酶活性抑制的医疗状况；增强包括给予抗癌药物在内的抗癌治疗的有效性；治疗与癌症相关的肿瘤特异性免疫抑制；以及治疗与传染性疾病相关的免疫抑制。
• Indolinones having kinase-inhibiting activity
  申请人：Boehringer Ingelheim Pharma KG

  公开号：US06043254A1

  公开（公告）日：2000-03-28

  The present invention relates to indolinones of general formula ##STR1## wherein R.sub.1 to R.sub.3 are defined in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

  本发明涉及一般式##STR1##中R.sub.1至R.sub.3的定义如权利要求1所述，其异构体和盐，特别是具有有价值的药理特性的生理上可接受的盐，特别是对各种激酶和cycline/CDK复合物以及各种肿瘤细胞增殖具有抑制作用的盐，含有这些化合物的药物组合物，它们的用途和制备它们的方法。
• Simultaneous Deprotection and Purification Based on Ionic Resin Capture: Application to Amide Formations and Grignard and Mitsunobu Reactions
  作者：Peter Meier、Sascha Müller

  DOI：10.1055/s-2007-983758

  日期：——

  Tr-protected amines were caught directly out of reaction mixtures by simultaneous cleavage of the protecting group. By releasing the products with ammonia the corresponding free amines were obtained in high yields and purities. The broadly applicable method of simultaneous deprotection and purification based on ionic resin capture was applied for Grignard and Mitsunobu reactions as well as amide formations

  通过同时裂解保护基团，将含有 Boc-或 Tr-保护胺的产物直接从反应混合物中捕获。通过用氨释放产物，以高产率和纯度获得相应的游离胺。基于离子树脂捕获的广泛适用的同时脱保护和纯化方法被应用于格氏反应和光信反应以及酰胺形成，并显示出多平行合成的高潜力。
• [EN] ALPHA-KETOAMIDE DERIVATIVES AS CATHEPSIN K INHIBITORS<br/>[FR] DERIVES D'ALPHA-CETOAMIDE UTILISES EN TANT QU'INHIBITEURS DE LA CATHEPSINE K
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2003013518A1

  公开（公告）日：2003-02-20

  Biaryl ketoamide derivatives (I), which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such biaryl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.

  本文描述了有用于作为蛋白酶K抑制剂的双芳基酮酰胺衍生物(I)。所述的发明还包括制备这种双芳基酮酰胺衍生物的方法，以及在治疗与增强骨转换相关的疾病，包括骨质疏松症，最终可能导致骨折的方法。
• Alpha-ketoamide derivatives as cathepsin k inhibitors
  申请人：Barrett David Gene

  公开号：US20050107616A1

  公开（公告）日：2005-05-19

  Biaryl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such biaryl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.

  本文介绍了用作猫hepsin K抑制剂的联苯基酮酰胺衍生物。所述发明还包括制备这种联苯基酮酰胺衍生物的方法，以及将其用于治疗与增强骨转换有关的疾病，包括骨质疏松症，该疾病最终可能导致骨折的方法。