2-amino-5-(benzyloxy)phenol | 54026-40-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 2-amino-5-(benzyloxy)phenol
• 英文别名: 2-Amino-5-benzyloxy-phenol；2-amino-5-benzyloxyphenol；2-amino-5-phenylmethoxyphenol
• CAS: 54026-40-3
• 化学式: C₁₃H₁₃NO₂
• 分子量: 215.252
• InChiKey: XOJGECMCKLYLDB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  55.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-amino-5-(benzyloxy)phenol 在 palladium 10% on activated carbon 、 氢气 、 potassium carbonate 作用下， 以 四氢呋喃 、 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 20.0 ℃ 、101.33 kPa 条件下， 反应 6.5h， 生成 tert-butyl 3-(6-hydroxy-2-oxobenzo[d]oxazol-3(2H)-yl)-2,6-dioxopiperidine-1-carboxylate
  参考文献：
  名称：

  [EN] AMINE-LINKED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN DEGRADATION
  [FR] DÉGRONIMÈRES DE C3-GLUTARIMIDE LIÉS À UNE AMINE POUR LA DÉGRADATION DE PROTÉINES CIBLES

  摘要：

  这项发明提供了胺连接的C3-戊二酰亚胺Degronimers和Degrons，用于治疗应用，如本文进一步描述的，以及它们的使用方法、组合物以及它们的制备方法。

  公开号：

  WO2017197051A1
• 作为产物：
  描述：

  3-苄氧基苯酚 在 sodium dithionite 、 硝酸 、 溶剂黄146 作用下， 以 水 为溶剂， 反应 4.5h， 生成 2-amino-5-(benzyloxy)phenol
  参考文献：
  名称：

  Structure-activity relationships of benzoxazolinones with respect to auxin-induced growth and auxin-binding protein

  摘要：

  The structure-activity relationships of the naturally occurring auxin-inhibiting substance, 6-methoxy-2-benzoxazolinone, isolated from maize shoots, and its artificial analogues with respect to auxin activity and membrane-bound auxin-binding protein, were studied. 6-Isobutoxy-2-benzoxazolinone strongly inhibited auxin (1-naphthylacetic acid, NAA)-induced growth of etiolated maize coleoptile segments. 6-Isopropoxy-2-benzoxazolinone, 6-ethoxy-2-benzoxazolinone and 6-methoxy-2-benzoxazolinone showed significant inhibitory activity. However, 2-benzoxazolinone and 6-benzyloxy-2-benzoxazolinone did not inhibit auxin-induced growth. On the basis of these data, it seemed reasonable to assume that the auxin-inhibitory activity was enhanced by increasing the side chain length at position C-6 on the 2-benzoxazolinone, although the attachment of a ring at C-6 destroyed activity. Competition by benzoxazolinones with an alkoxy group at C-6 with H-3-NAA at auxin-binding protein(s) isolated from endoplasmic reticulum (ER) membrane of maize shoots showed a positive correlation with their physiological effects. However, since the inhibitory activity of the benzoxazolinones for auxin-receptor(s) binding was small compared with their physiological activity, the benzoxazolinones may contribute to inhibition of auxin-induced growth through interference with other auxin-receptors.

  DOI：

  10.1016/0031-9422(94)85050-x

文献信息

• Compound
  申请人：——

  公开号：US20040019016A1

  公开（公告）日：2004-01-29

  There is provided a compound of Formula I 1 wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH 2 and C═O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.

  提供了一个式I1的化合物，其中每个T分别选自H、烃基、—F—R和与D、E、P或Q中的一个之一形成键，或者与P和Q中的一个一起形成环；Z是一个适当的原子，其价数为m；D、E和F分别独立于彼此，是可选的连接基团，其中当Z是氮时，E不是CH2和C═O；P、Q和R独立于彼此，是一个环系统；至少Q包含一个磺酰胺基团。
• [EN] HETEROCYCLE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CNS DISORDERS<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES ET LEUR UTILISATION POUR LE TRAITEMENT DE TROUBLES DU SNC
  申请人：TRILLIUM THERAPEUTICS INC

  公开号：WO2017070796A1

  公开（公告）日：2017-05-04

  The present application relates to novel heterocycle derivatives of Formula (I), to processes for preparing them, pharmaceutical compositions containing them, and their use thereof in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognitive disorders and/or memory deficits, as well as chronic and acute pain and other related CNS disorders.

  本申请涉及式(I)的新异环衍生物，以及制备它们的方法，含有它们的药物组合物，以及它们在治疗或预防急性和/或慢性神经系统疾病，如精神病、癫痫、精神分裂症、阿尔茨海默病、认知障碍和/或记忆力缺陷，以及慢性和急性疼痛和其他相关中枢神经系统疾病中的应用。
• [EN] 1,2,4-TRIAZOLE DERIVATIVES CONTAINING A SULPHAMATE GROUP AS AROMATASE INHIBITORS<br/>[FR] DERIVES 1,2,4-TRIAZOLE CONTENANT UN GROUPE SULFAMATE EN TANT QU'INHIBITEURS D'AROMATASE
  申请人：STERIX LTD

  公开号：WO2003045925A1

  公开（公告）日：2003-06-05

  There is provided a compound of Formula (I), wherein each T is independently selected from H, hydrocarbyl, -F-R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and C=O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.

  提供了一个化合物的式子（I），其中每个T独立地选自H，烃基，-F-R和与D，E，P或Q中的一个之一形成键，或与P和Q中的一个形成环；Z是适当的原子，其价数为m；D，E和F分别独立于彼此的可选连接基团，其中当Z为氮时，E不是CH2和C=O；P，Q和R独立于彼此的环系统；并且至少Q包含一个磺酰胺基团。
• HETEROARYLAMIDE LOWER CARBOXYLIC ACID DERIVATIVE
  申请人：Machinaga Nobuo

  公开号：US20090324581A1

  公开（公告）日：2009-12-31

  To provide a novel compound which has S1P receptor agonistic activity, exhibits excellent immunosuppressing effect, gives less adverse side effects, and can be orally administered. The invention provides a compound represented by general formula (I) (wherein A is a single bond, —O—, or —CH 2 —; R 1 represents a hydrogen atom or a C 1 -C 6 alkyl group, and V represents any one group selected from among the following groups (1) to (3): (1) -G 1 -, (2) -G 2 -N(R 2 )-G 3 -, and (3) a group represented by formula 2, wherein each of Z 1 and Z 2 represents a hydrogen atom or a C 1 -C 6 alkyl group, Z 3 represents a hydrogen or the like, Q represents —CH 2 —O— or the like, and Y represents a group represented by formula 3, a salt thereof, or a solvate thereof.

  提供一种新型化合物，具有S1P受体激动活性，表现出优异的免疫抑制效果，产生较少的不良副作用，并可口服。本发明提供一种由通式（I）表示的化合物（其中A是单键，-O-或-CH2-；R1表示氢原子或C1-C6烷基基团，V表示从以下组（1）至（3）中选择的任一组：（1）-G1-，（2）-G2-N（R2）-G3-，以及（3）由式2表示的组，其中Z1和Z2分别表示氢原子或C1-C6烷基基团，Z3表示氢或类似物，Q表示-CH2-O-或类似物，Y表示由式3表示的基团，其盐或溶剂化物。
• Cyclic sulfones useful as mitochondrial sodium-calcium exchangers
  申请人：Bold Guido

  公开号：US20100029626A1

  公开（公告）日：2010-02-04

  The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.

  本发明涉及公式（I）的新化合物及其在动物或人体治疗中的应用，包括含有公式（I）化合物的制药组合物，以及使用公式（I）化合物制备用于治疗蛋白激酶依赖性疾病的制药组合物，特别是增殖性疾病，如特定的肿瘤疾病。