cyclooct-2-ene-1,4-diol

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: cyclooct-2-ene-1,4-diol
• 英文别名: (2Z)-cyclooct-2-ene-1,4-diol
• 化学式: C₈H₁₄O₂
• 分子量: 142.198
• InChiKey: WJVTUJNZYOAXID-WAYWQWQTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  40.5
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  cyclooct-2-ene-1,4-diol 在 苯甲酸甲酯 、 silver nitrate 作用下， 以 四氢呋喃 、 乙醚 、 异丙醇 为溶剂， 反应 24.0h， 生成 C₁₆H₁₈N₄O₄
  参考文献：
  名称：

  可切割的 C2 对称反式环辛烯可实现 Molecular Probe 的快速、完全生物正交拆卸

  摘要：

  生物正交化学正在弥合静态化学连接和分子状态的动态生理调控之间的鸿沟，实现驱动多种技术的原位转化。尽管对机理的理解已经成熟，并且新的生物正交键-切割反应已经成熟，但分子 ON/OFF 控制的更广泛目标受到了现有系统无法实现快速（即几秒到几分钟，而不是几小时）和完全（即 >99%）切割的限制。为了获得高保真分子灭活所需的严格性能特征，我们设计并合成了一种新的 C2 对称反式环辛烯接头 （C2TCO），该接头表现出优异的生物稳定性，并且可以被官能化烷基、芳基和 H-四嗪快速完全裂解，而不受点击方向的影响。通过将 C2TCO 掺入荧光分子探针中，我们展示了通过全向 tetrazine 触发的切割实现高效的细胞外和细胞内生物正交分解。

  DOI：

  10.1021/jacs.0c07922

文献信息

• BIO-ORTHOGONAL DRUG ACTIVATION
  申请人：KONINKLIJKE PHILIPS N.V.

  公开号：US20160106859A1

  公开（公告）日：2016-04-21

  The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.

  该发明涉及一种用于治疗学的原药激活方法，其中使用了表现出彼此生物正交反应性的非生物活性化学基团。该发明还涉及一种包含至少一种原药和至少一种激活剂的试剂盒，其中原药包含药物和第一个生物正交反应基团（触发器），而激活剂包含第二个生物正交反应基团。该发明还涉及在上述方法和试剂盒中使用的靶向治疗剂。该发明特别适用于抗体药物偶联物和双特异性及三特异性抗体衍生物。
• PROCESS FOR PRODUCING RING-OPENING METATHESIS POLYMER
  申请人：KURARAY CO., LTD.

  公开号：EP1847558A1

  公开（公告）日：2007-10-24

  The process of producing a ring-opening metathesis polymer of the present invention is mainly characterized in that a treatment to decrease the amount of oxygen and/or peroxide in at least one kind of polymerization starting material is performed prior to the ring-opening metathesis polymerization reaction of a cyclic olefin performed in the presence of a ruthenium carbene complex (catalyst). As used herein, the "polymerization starting material" refers to various materials used for a ring-opening metathesis polymerization reaction and present in the reaction system, such as ruthenium carbene complex (catalyst) and cyclic olefin (monomer), as well as solvents, chain transfer agents and the like. In addition, the method for a treatment to decrease the amount of oxygen and/or peroxide include a method comprising applying an adsorbent to a polymerization starting material to remove oxygen and/or peroxide by adsorption, a method comprising applying an antioxidant to a polymerization starting material to decompose oxygen or peroxide and the like. According to the present invention, a ring-opening metathesis polymer can be produced at a higher reaction rate without degrading the high activity inherently possessed by a' ruthenium carbene complex (catalyst). Because of being free of a decrease in the concentration of the catalyst maintaining the high activity during reaction, the thus-obtained polymer shows a small difference between polymerization lots and becomes homogeneous, and a polymer having a comparatively sharp molecular weight distribution can be produced.

  本发明的开环偏聚聚合物生产工艺的主要特点是，在碳化钌络合物（催化剂）存在下进行环烯烃的开环偏聚聚合反应之前，先进行处理以减少至少一种聚合起始材料中的氧和/或过氧化物的含量。本文所用的 "聚合起始材料 "是指用于开环偏聚聚合反应并存在于反应体系中的各种材料，例如碳化钌络合物（催化剂）和环烯烃（单体），以及溶剂、链转移剂等。此外，减少氧气和/或过氧化物量的处理方法还包括将吸附剂应用于聚合起始材料以通过吸附去除氧气和/或过氧化物的方法、将抗氧化剂应用于聚合起始材料以分解氧气或过氧化物的方法等。 根据本发明，可以在不降低'碳化钌络合物（催化剂）固有的高活性的情况下，以更高的反应速率生产开环偏聚聚合物。由于在反应过程中保持高活性的催化剂浓度不会降低，因此得到的聚合物在聚合批次之间的差异很小，而且变得均匀，并能生产出分子量分布比较均匀的聚合物。
• PROCESS FOR PRODUCTION OF HYDROGENATED POLYMERS AND HYDROGENATED POLYMERS
  申请人：Kuraray Co., Ltd.

  公开号：EP2070964A1

  公开（公告）日：2009-06-17

  Provision of, in a process of producing a hydrogenated polymer, which comprises steps of sequentially performing, in the presence of a ruthenium carbene complex, a ring-opening metathesis polymerization reaction of a cyclic olefin and a hydrogenation reaction of a ring-opening metathesis polymer produced by the polymerization reaction to give a hydrogenated polymer, a simple and economic process of obtaining a hydrogenated polymer having an extremely small content of residual ruthenium derived from the ruthenium carbene complex. A process of producing a hydrogenated polymer, which comprises, in the presence of a ruthenium carbene complex, subjecting a cyclic monoolefin and/or a cyclic diolefin to a ring-opening metathesis polymerization, hydrogenating the resulting ring-opening metathesis polymer to give a hydrogenated polymer, and bringing the hydrogenated polymer in contact with a poor solvent of the hydrogenated polymer in the presence of dissolved hydrogen to allow precipitation. As the poor solvent of the hydrogenated polymer, alcohol having 1 to 6 carbon atoms, ketone having 3 to 6 carbon atoms and the like are preferable.

  在一种生产氢化聚合物的工艺中，包括以下步骤：在有碳化钌络合物存在的情况下，依次进行环状烯烃的开环偏聚聚合反应和由聚合反应生成的开环偏聚聚合物的氢化反应，以得到氢化聚合物。 一种氢化聚合物的生产工艺，它包括在碳化钌络合物存在的情况下，使环状单烯烃和/或环状二烯烃进行开环偏聚聚合反应，将得到的开环偏聚聚合体氢化，得到氢化聚合物，并使氢化聚合物在溶解氢存在的情况下与氢化聚合物的贫溶剂接触，使其沉淀。作为氢化聚合物的贫溶剂，最好是 1 至 6 个碳原子的醇、3 至 6 个碳原子的酮等。
• US3970673A
  申请人：——

  公开号：US3970673A

  公开（公告）日：1976-07-20
• US7700698B2
  申请人：——

  公开号：US7700698B2

  公开（公告）日：2010-04-20