3-(tetrahydrofuran-3-yl)propan-1-ol | 1050496-53-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氧唑烯
• 英文名称: 3-(tetrahydrofuran-3-yl)propan-1-ol
• 英文别名: 3-(Tetrahydro-3-furanyl)-1-propanol；3-(oxolan-3-yl)propan-1-ol
• CAS: 1050496-53-1
• 化学式: C₇H₁₄O₂
• 分子量: 130.187
• InChiKey: VGNSJJUNWUMZMR-UHFFFAOYSA-N

物化性质

• 沸点：
  227.9±8.0 °C(Predicted)
• 密度：
  0.991±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  9
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  29.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-(tetrahydrofuran-3-yl)propan-1-ol 在 [1,3-双(二苯基膦基)丙烷]二氯化钯(II) 、 四溴化碳 、 potassium tert-butylate 、 二异丁基氢化铝 、 三乙基硼氢化锂 、 三苯基膦 、 pyridinium chlorochromate 作用下， 以 四氢呋喃 、 正己烷 、 二氯甲烷 、 甲苯 为溶剂， 反应 13.33h， 生成 3-[(3E,7E,11E)-4,8,12,16-tetramethylheptadeca-3,7,11,15-tetraenyl]tetrahydrofuran
  参考文献：
  名称：

  Concise synthesis and structure–activity relationship of furospinosulin-1, a hypoxia-selective growth inhibitor from marine sponge

  摘要：

  Structure activity relationship of furospinosulin-1 (1), a hypoxia-selective growth inhibitor isolated from marine sponge, was investigated. Concise synthetic method of 1 was developed, and some structurally modified analogues were prepared. Biological evaluation of them revealed that the whole chemical structure was important for the hypoxia-selective growth inhibitory activity of 1. Among prepared, the desmethyl analogue 30 showed excellent hypoxia-selective inhibitory activity similar to that of 1 and also exhibited in vivo anti-tumor activity with oral administration. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2011.05.009
• 作为产物：
  描述：

  四氢呋喃-3-甲醛 在 palladium on activated charcoal 、 氢气 、 二异丁基氢化铝 、 sodium hydroxide 作用下， 以 正己烷 、 二氯甲烷 、 水 、 乙酸乙酯 为溶剂， 反应 24.0h， 生成 3-(tetrahydrofuran-3-yl)propan-1-ol
  参考文献：
  名称：

  Concise synthesis and structure–activity relationship of furospinosulin-1, a hypoxia-selective growth inhibitor from marine sponge

  摘要：

  Structure activity relationship of furospinosulin-1 (1), a hypoxia-selective growth inhibitor isolated from marine sponge, was investigated. Concise synthetic method of 1 was developed, and some structurally modified analogues were prepared. Biological evaluation of them revealed that the whole chemical structure was important for the hypoxia-selective growth inhibitory activity of 1. Among prepared, the desmethyl analogue 30 showed excellent hypoxia-selective inhibitory activity similar to that of 1 and also exhibited in vivo anti-tumor activity with oral administration. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2011.05.009

文献信息

• [EN] QUINAZOLINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER<br/>[FR] DERIVES QUINAZOLINE, UTILISATIONS DE CES DERNIERS DANS LE TRAITEMENT DU CANCER
  申请人：ASTRAZENECA AB

  公开号：WO2004096226A1

  公开（公告）日：2004-11-11

  The invention concerns quinazoline derivatives of the formula: (I); wherein X1, Q1, Z, R1, R2, Y, a and m are as defined in the description, which are erbB tyrosine kinase inhibitors, particularly EGFR tyrosine kinase inhibitors. Also claimed are processes for their preparation; pharmaceutical compositions containing them; and their use as therapeutic agents in the treatment of erbB tyrosine kinase mediated diseases such as cancer.

  该发明涉及喹唑啉衍生物的公式(I)；其中X1、Q1、Z、R1、R2、Y、a和m如描述中定义，它们是erbB酪氨酸激酶抑制剂，特别是EGFR酪氨酸激酶抑制剂。还要求保护它们的制备方法；含有它们的药物组合物；以及它们作为治疗剂在治疗erbB酪氨酸激酶介导的疾病如癌症中的应用。
• [EN] QUINAZOLINE DERIVATIVES<br/>[FR] DERIVES DE QUINAZOLINE
  申请人：ASTRAZENECA AB

  公开号：WO2005026156A1

  公开（公告）日：2005-03-24

  The invention concerns quinazoline derivatives of Formula (I) wherein each of R1, R3, R20, X1, X2, Z, W, (a) and (q) have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of turnours which are sensitive to inhibition of erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.

  这项发明涉及式(I)的喹唑啉衍生物，其中R1、R3、R20、X1、X2、Z、W、(a)和(q)中的每一个具有描述中定义的任何含义；它们的制备方法，含有它们的药物组合物以及它们在制造用作抗增殖剂的药物时的用途，用于预防或治疗对erbB受体酪氨酸激酶抑制敏感的肿瘤，特别是EGFR酪氨酸激酶。
• [EN] QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS<br/>[FR] DERIVES DE QUINAZOLINE UTILISES COMME INHIBITEURS DE LA TYROSINE KINASE
  申请人：ASTRAZENECA AB

  公开号：WO2005026150A1

  公开（公告）日：2005-03-24

  The invention concerns quinazoline derivatives of the Formula (I); wherein each of R1, R2, W, X1, X2, Z, a and b are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula (I) are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.

  该发明涉及配方（I）的喹唑啉衍生物；其中R1、R2、W、X1、X2、Z、a和b在描述中有定义；它们的制备方法；含有它们的药物组合物以及它们在制造用于提供抗增殖效果的药物的用途。配方（I）的喹唑啉衍生物预计在治疗某些由erbB受体酪氨酸激酶介导的癌症等疾病中具有用处，特别是EGFR酪氨酸激酶。
• [EN] 2-PYRAZINYLBENZIMIDAZOLE DERIVATIVES AS RECEPTOR TYROSINE KINASE INHIBITORS<br/>[FR] DÉRIVÉS DE 2-PYRAZINYLBENZIMIDAZOLE EN TANT QU'INHIBITEURS DES RÉCEPTEURS TYROSINE KINASE
  申请人：ASTRAZENECA AB

  公开号：WO2009024825A1

  公开（公告）日：2009-02-26

  The invention concerns pyrazine derivatives of Formula (I) or a pharmaceutically-acceptable salt thereof, wherein each of G1, G2, Ring A, R1, m, R2, R3, n and R4 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositionscontaining them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.

  本发明涉及式（I）的吡嗪衍生物或其药用可接受的盐，其中G1、G2、环A、R1、m、R2、R3、n和R4中的每一个具有在描述中之前定义的任何含义；其制备方法，含有它们的药物组合物以及它们在制造用于治疗细胞增殖性疾病的药物中的用途。
• Quinazoline derivatives as antitumor agents
  申请人：Hennequin Francois Andre Laurent

  公开号：US20050043336A1

  公开（公告）日：2005-02-24

  The invention concerns quinazoline derivatives of Formula (I); wherein each of Q 1 , Q 2 , Z, R 1 , R 2 , R 3 , and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosin kinases.

  该发明涉及公式（I）的喹唑啉衍生物；其中Q1，Q2，Z，R1，R2，R3和m的每个定义在说明中具有任何意义；它们的制备过程，包含它们的制药组合物以及它们在制造对erbB受体酪氨酸激酶抑制敏感的肿瘤的预防或治疗药物中的使用。