14-{(methylsulfonyl)oxy}-3,6,9,12-tetraoxatetradecanol | 877239-05-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 14-{(methylsulfonyl)oxy}-3,6,9,12-tetraoxatetradecanol
• 英文别名: 14-{(Methylsulfonyl)oxy}-3,6,9,12-tetraoxatetradecanol；2-[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethoxy]ethyl methanesulfonate
• CAS: 877239-05-9
• 化学式: C₁₁H₂₄O₈S
• 分子量: 316.373
• InChiKey: JCWZPAXAWPTMFH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  20
• 可旋转键数：
  15
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  109
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  14-{(methylsulfonyl)oxy}-3,6,9,12-tetraoxatetradecanol 在 sodium azide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 2.5h， 生成 14-叠氮-3,6,9,12-四氧十四烷醇
  参考文献：
  名称：

  EP1783137

  摘要：

  公开号：
• 作为产物：
  描述：

  羟丙基淀粉磷酸酯 、 甲基磺酰氯 在 氧化银(II) silica gel 作用下， 以 二氯甲烷 为溶剂， 反应 48.0h， 以to obtain 7.8 g of the objective compound的产率得到14-{(methylsulfonyl)oxy}-3,6,9,12-tetraoxatetradecanol
  参考文献：
  名称：

  Galactose derivative, drug carrier and medicinal composition

  摘要：

  本发明涉及一种新颖且有用的半乳糖衍生物，该衍生物构成药物载体，可将药物有效地转运至肝脏，以及包括该衍生物的药物载体和载体与药物组成的制药组合物。本发明还涉及一种由半乳糖、适当的间隔物和特定脂质组成的半乳糖衍生物、包括该衍生物和阳离子脂质的药物载体，以及包括载体和药物（优选为双链RNA、双链DNA或寡核苷酸）的制药组合物。

  公开号：

  US07655768B2

文献信息

• Organocatalysis of nucleophilic substitution reactions by the combined effects of two promoters fused in a molecule: oligoethylene glycol substituted imidazolium salts
  作者：Vinod H. Jadhav、Ju-Young Kim、Dae Yoon Chi、Sungyul Lee、Dong Wook Kim

  DOI：10.1016/j.tet.2013.10.070

  日期：2014.1

  Oligoethylene glycol substituted imidazolium salts were synthesized as promoters for a range of SN2 reactions, and their efficiency was examined. These tailor-made organic promoters enhanced the nucleophilicity of alkali metal salts significantly through the combined effects of two promoters (oligoethylene glycols and imidazolium salts) in a single molecule. The effects of the oligoethylene glycol

  合成了低聚乙二醇取代的咪唑鎓盐作为一系列S N 2反应的促进剂，并检查了它们的效率。这些量身定制的有机促进剂通过两个促进剂（低聚乙二醇和咪唑鎓盐）在单个分子中的联合作用，显着增强了碱金属盐的亲核性。系统研究了低聚乙二醇侧链长度，离子液体阴离子，亲核试剂和底物的影响。[hexaEGmim] [OMs]和[dihexaEGim] [OMs]显示了使用碱金属盐进行S N 2反应的最高效率。通过检查相对S N来评估低聚乙二醇部分的末端羟基基团的作用2氯化和溴化收率。结果表明，羟基与亲核试剂的氢键强度非常重要。通过量子化学计算研究了oligoEGILs促进S N 2反应的优异机理。结果表明，低聚乙二醇部分中的氧原子和离子液体阴离子作为路易斯碱作用于抗衡阳离子K +或Na +上，从而显着提高了金属盐的反应性。
• Galactose Derivative, Drug Carrier and Medicinal Composition
  申请人：Ohgi Tadaaki

  公开号：US20070244058A1

  公开（公告）日：2007-10-18

  The present invention relates to a novel and useful galactose derivative constituting a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the carrier and a medicine. The present invention also relates to a galactose derivative made up of galactose, a suitable spacer and a certain lipid, a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, or an oligo nucleic acid).

  本发明涉及一种新颖且有用的半乳糖衍生物，该衍生物构成了一种药物载体，可以有效地将药物转运到肝脏，包括该衍生物的药物载体以及包含该载体和药物的制药组合物。本发明还涉及由半乳糖、适当的间隔物和某种脂质组成的半乳糖衍生物，该衍生物构成了一种药物载体，包括该衍生物和阳离子脂质的药物载体，以及包含该载体和药物（优选为双链RNA、双链DNA或寡核苷酸）的制药组合物。
• GALACTOSE DERIVATIVE, DRUG CARRIER AND MEDICINAL COMPOSITION
  申请人：Nippon Shinyaku Co., Ltd.

  公开号：EP1783137A1

  公开（公告）日：2007-05-09

  The object of the invention is to provide a novel and useful galactose derivative constituting a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the carrier and a medicine. The present invention relates to a galactose derivative made up of galactose, a suitable spacer and a certain lipid, a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double strand RNA, a double strand DNA, an oligo nucleic acid) .

  本发明的目的是提供一种新颖而有用的半乳糖衍生物，它构成一种药物载体，通过它可以将药物有效地转移到肝脏中；提供一种由该衍生物组成的药物载体；提供一种由该载体和药物组成的药物组合物。 本发明涉及一种由半乳糖、适当的间隔物和某种脂质组成的半乳糖衍生物，一种由该衍生物和阳离子脂质组成的药物载体，以及一种由该载体和药物（最好是双链 RNA、双链 DNA、寡核酸）组成的药物组合物。
• Conjugate of dezocine and polyethylene glycol
  申请人：JenKem Technology Co., Ltd. (Beijing)

  公开号：US10596268B2

  公开（公告）日：2020-03-24

  The present invention relates to the technical field of medicine, in particular to a conjugate of dezocine and polyethylene glycol and a pharmaceutical composition thereof. The conjugate of dezocine and water-soluble oligomer provided by the present invention has better pharmacokinetic properties and a high drug absorption degree, may reduce the side effects of the drug, and achieve a smaller administration dosage and a more diverse mode of administration, such as oral administration, in clinic. Compared with dezocine, the conjugate of the present invention has a stronger analgesic effect and a longer analgesic duration, may reduce the frequency of drug administration, improve patient compliance, and has advantages in effectiveness and safety of the drug, as well as drug tolerance, etc.

  本发明涉及医药技术领域，尤其涉及一种地佐辛与聚乙二醇的共轭物及其药物组合物。本发明提供的地佐辛与水溶性低聚物的共轭物具有较好的药代动力学特性和较高的药物吸收度，可减少药物的副作用，在临床上可实现更小的给药剂量和更多样化的给药方式，如口服给药。与地佐辛相比，本发明的共轭物镇痛效果更强，镇痛持续时间更长，可减少给药次数，提高患者的依从性，在药物的有效性、安全性以及药物耐受性等方面具有优势。
• CONJUGATE OF DEZOCINE AND POLYETHYLENE GLYCOL
  申请人：JenKem Technology Co., Ltd. (Beijing)

  公开号：US20190298845A1

  公开（公告）日：2019-10-03

  The present invention relates to the technical field of medicine, in particular to a conjugate of dezocine and polyethylene glycol and a pharmaceutical composition thereof. The conjugate of dezocine and water-soluble oligomer provided by the present invention has better pharmacokinetic properties and a high drug absorption degree, may reduce the side effects of the drug, and achieve a smaller administration dosage and a more diverse mode of administration, such as oral administration, in clinic. Compared with dezocine, the conjugate of the present invention has a stronger analgesic effect and a longer analgesic duration, may reduce the frequency of drug administration, improve patient compliance, and has advantages in effectiveness and safety of the drug, as well as drug tolerance, etc.