I+/--(Aminomethyl)-4-hydroxy-3,5-dimethylbenzenemethanol | 325151-59-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 英文名称: I+/--(Aminomethyl)-4-hydroxy-3,5-dimethylbenzenemethanol
• 英文别名: 4-(2-amino-1-hydroxyethyl)-2,6-dimethylphenol
• CAS: 325151-59-5
• 化学式: C₁₀H₁₅NO₂
• 分子量: 181.235
• InChiKey: IWYUHYMMFSTZRE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  66.5
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  聚合甲醛 、 I+/--(Aminomethyl)-4-hydroxy-3,5-dimethylbenzenemethanol 在 palladium on activated charcoal 氢气 作用下， 以 甲醇 为溶剂， 反应 14.0h， 以70%的产率得到4-[2-(dimethylamino)-1-hydroxyethyl]-2,6-dimethylphenol
  参考文献：
  名称：

  Turbotoxins A and B, Novel Diiodotyramine Derivatives from the Japanese Gastropod Turbo marmorata

  摘要：

  Bioassay-guided separation of the aqueous ethanol extract of the viscera of the Japanese gastropod Turbo marmorata resulted in the isolation of two toxins, turbotoxins A and B. Their structures were determined by spectral analysis and confirmed by organic synthesis to be diiodotyramine derivatives. Turbotoxins A and B exhibited acute toxicity against ddY mice, with LD99 values of 1.0 and 4.0 mg/kg, respectively. The structure-toxicity relationships of turbotoxins were examined, and it was proved that the iodine atoms and trimethyl ammonium groups are important for its acute toxicity. Turbotoxin A inhibits acetylcholinesterase with an IC50 of 28 muM. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0040-4020(00)00759-6
• 作为产物：
  描述：

  3,5-二甲基-4-羟基苯甲醛 在 lithium aluminium tetrahydride 、 zinc(II) iodide 作用下， 以 四氢呋喃 为溶剂， 反应 61.5h， 生成 I+/--(Aminomethyl)-4-hydroxy-3,5-dimethylbenzenemethanol
  参考文献：
  名称：

  Turbotoxins A and B, Novel Diiodotyramine Derivatives from the Japanese Gastropod Turbo marmorata

  摘要：

  Bioassay-guided separation of the aqueous ethanol extract of the viscera of the Japanese gastropod Turbo marmorata resulted in the isolation of two toxins, turbotoxins A and B. Their structures were determined by spectral analysis and confirmed by organic synthesis to be diiodotyramine derivatives. Turbotoxins A and B exhibited acute toxicity against ddY mice, with LD99 values of 1.0 and 4.0 mg/kg, respectively. The structure-toxicity relationships of turbotoxins were examined, and it was proved that the iodine atoms and trimethyl ammonium groups are important for its acute toxicity. Turbotoxin A inhibits acetylcholinesterase with an IC50 of 28 muM. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0040-4020(00)00759-6

文献信息

• Oxazolidine derivatives having anti-diabetic and anti-obesity properties, their preparation and their therapeutic uses
  申请人：SANKYO COMPANY LIMITED

  公开号：EP0590793A1

  公开（公告）日：1994-04-06

  Compounds of formula (I): wherein: R is an alkyl group; X is oxygen or sulphur; Y is hydrogen atom or -A-COOH, in which A is an alkylene group; Ar is aryl or substituted aryl group; and pharmaceutically acceptable salts and esters thereof, have use in the treatment or prophylaxis of diabetes, obesity, hyperlipaemia, hyperglycaemia, complications of diabetes, obesity-related hypertension and osteoporosis.

  式(I)化合物： 其中R为烷基；X为氧或硫；Y为氢原子或-A-COOH，其中A为亚烷基；Ar为芳基或取代芳基；及其药学上可接受的盐和酯，可用于治疗或预防糖尿病、肥胖症、高脂血症、高血糖、糖尿病并发症、肥胖相关性高血压和骨质疏松症。
• Polymeric prodrugs
  申请人：Complex Biosystems GmbH

  公开号：EP2087910A2

  公开（公告）日：2009-08-12

  The present invention relates to a polymeric cascade prodrug comprising: an amine containing biologically active moiety, a polymeric carrier, a masking group having at least one nucleophile and being distinct from the carrier, wherein the prodrug is predominantly non-enzymatically cleavable.

  本发明涉及一种聚合级联原药，包括：含生物活性分子的胺、聚合载体、至少有一个亲核且与载体不同的掩蔽基团，其中原药主要是非酶可裂解的。
• POLYMERIC PRODRUG WITH A SELF-IMMOLATIVE LINKER
  申请人：Ascendis Pharma GmbH

  公开号：EP1732607B1

  公开（公告）日：2019-05-15
• Polymeric Prodrug with a Self-Immolative Linker
  申请人：Hersel Ulrich

  公开号：US20080241102A1

  公开（公告）日：2008-10-02

  A cascade carrier linked prodrug is described which comprises a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier.
• POLYMERIC PRODRUG WITH SELF-IMMOLATIVE LINKER
  申请人：Ascendis Pharma GmbH

  公开号：US20130150281A1

  公开（公告）日：2013-06-13

  A cascade carrier linked prodrug is described comprising a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier.