sebacimide | 6719-04-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: sebacimide
• 英文别名: 1-Azacycloundecane-2,11-dione；azacycloundecane-2,11-dione
• CAS: 6719-04-6
• 化学式: C₁₀H₁₇NO₂
• 分子量: 183.25
• InChiKey: VRQBDNAOTUKKIG-UHFFFAOYSA-N

物化性质

• 沸点：
  347.2±11.0 °C(Predicted)
• 密度：
  0.994±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  46.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2-氮杂环壬酮 在 甲基(三氟甲基)-1,3-二环氧丙烷 、 三氟乙酸 作用下， 以 丙酮 为溶剂， 反应 3.0h， 以55%的产率得到sebacimide
  参考文献：
  名称：

  杂解（2 e）与均解（1 e）氧化反应性：二环氧乙烷对内酰胺的氧化中的NH与CH转换

  摘要：

  二恶英是强大的氧化剂，可通过两种不同的机制起作用：1）均溶（H提取和氧回弹）和2）杂溶（亲电子氧化）。迄今为止，已经报道了底物的性质决定了反应模式，而与所使用的二环氧乙烷无关。在此，我们报道了前所未有的情况，其中二环氧乙烷的性质决定了氧化化学选择性。特别是，在内酰胺从二甲基二环氧乙烷（DDO）转移到甲基（三氟甲基）二环氧乙烷（TFDO）的内酰胺氧化中观察到了从CH到NH的转换。一项物理有机化学研究，将氧化与其他两种二氧杂环戊烷甲基（氟甲基）二环氧乙烷，MFDO和甲基（二氟甲基）二环氧乙烷相结合，通过计算研究，DFDO指出二恶英类化合物具有稳定同源或杂合途径的多种能力。

  DOI：

  10.1002/chem.201604507

文献信息

• A Process for Preparing Olodaterol and Intermediates Thereof
  申请人：REDDY G. Pratap

  公开号：US20170260149A1

  公开（公告）日：2017-09-14

  The present invention relates to a process for preparing olodaterol and intermediates thereof. The process comprises of forming compound of Formula 1 by reacting compound of Formula 2 or its acid salt with compound of Formula 3 in the presence of an organic solvent to obtain compound of Formula 4. Protecting groups are removed from compound of Formula 4 in the presence of a suitable solvent to form compound of Formula 1.

  本发明涉及一种制备奥洛达特罗及其中间体的方法。该方法包括通过在有机溶剂存在下，将化合物Formula 2或其酸盐与化合物Formula 3反应形成化合物Formula 1，从而获得化合物Formula 4。在适当溶剂的存在下，从化合物Formula 4中去除保护基，形成化合物Formula 1。
• SCAFFOLD-FREE SELF-ORGANIZING THREE-DIMENSIONAL ARTIFICIAL TISSUE AND ARTIFICIAL BONE COMPOSITE FOR OSTEOCHONDRAL REGENERATION
  申请人：Yoshikawa, Hideki

  公开号：EP2799093A1

  公开（公告）日：2014-11-05

  An improved method of treating an osteochondral defect is provided, which is a composite tissue for treating or preventing a disease, disorder, or condition associated with an osteochondral defect, comprising a three-dimensional synthetic tissue and an artificial bone, wherein the three-dimensional synthetic tissue is substantially made of a cell and an extracellular matrix derived from the cell, the extracellular matrix contains fibronectin, collagen I, collagen III, and vitronectin, and the extracellular matrix is diffusedly distributed in the tissue.

  提供了一种治疗骨软骨缺损的改进方法，它是一种用于治疗或预防与骨软骨缺损相关的疾病、失调或病症的复合组织，包括三维合成组织和人工骨，其中三维合成组织基本上由细胞和源自细胞的细胞外基质构成，细胞外基质包含纤维连接蛋白、胶原蛋白 I、胶原蛋白 III 和玻璃连蛋白，细胞外基质弥散分布在组织中。
• CREATION OF THREE-DIMENSIONAL ARTIFICIAL TISSUE FROM PLURIPOTENT STEM CELL-DERIVED CELLS, AND OSTEOCHONDRAL REGENERATION TREATMENT USING SAID ARTIFICIAL TISSUE
  申请人：Osaka University

  公开号：EP2949747A1

  公开（公告）日：2015-12-02

  Provided are an improved three-dimensional synthetic tissue, a composite tissue thereof, and a production method of the same. The present invention provides : an implantable synthetic tissue substantially made of a mesenchymal stem cell induced from a pluripotent stem cell or an equivalent cell thereof, and an extracellular matrix derived from the cell; a composite tissue for treating or preventing a disease, disorder, or condition associated with an osteochondral defect, comprising a synthetic tissue and an artificial bone, wherein the artificial bone is smaller in size than a depth of a defect of a bone section in the osteochondral defect; and a production method of the same.

  本发明提供了一种改进的三维合成组织、其复合组织及其生产方法。本发明提供了：一种可植入的合成组织，主要由从多能干细胞或其等效细胞诱导的间充质干细胞和从该细胞衍生的细胞外基质制成；一种复合组织，用于治疗或预防与骨软骨缺损有关的疾病、失调或病症，包括合成组织和人工骨，其中人工骨的尺寸小于骨软骨缺损中骨部分缺损的深度；以及其生产方法。
• Eight-arm polyethylene glycol derivative, production method therefor, and modified bio-related substance thereof
  申请人：Xiamen Sinopeg Biotech Co., Ltd.

  公开号：US10660969B2

  公开（公告）日：2020-05-26

  Disclosed are an 8-arm polyethylene glycol (PEG) derivative (formula 1), manufacturing method and modified bio-related substance thereby, wherein a tetravalent group U and four trivalent groups Ec form a highly symmetric octavalent central structure CORE0 together, Lc connects the octavalent center to eight PEG arms having polydiversity or monodiversity and having n1-n8 as the degrees of polymerization thereof. The terminal of one PEG chain is connected to at least one functional group F (k≥1), and said PEG chain and F can be directly connected (g=0) or connected with a divalent linking group L0 connected with a terminal branched group G (g=1) therebetween. The latter provides more reacting sites to combine more pharmaceutical molecules, thereby increasing the drug loading capacity. The near-center symmetric structure of the derivative allows more precise control over the molecular weight during large-scale production, thereby facilitating acquisition of a product having a narrower molecular weight distribution. A bio-related substance modified thereby has a more uniform and controllable performance.

  本发明公开了一种 8 臂聚乙二醇（PEG）衍生物（式 1）、其制造方法和改性生物相关物质，其中一个四价基团 U 和四个三价基团 Ec 共同形成一个高度对称的八价中心结构 CORE0，Lc 将八价中心连接到八个 PEG 臂上，这些 PEG 臂具有多元性或单元性，其聚合度为 n1-n8。一条 PEG 链的末端与至少一个官能团 F（k≥1）相连，所述 PEG 链和 F 可以直接相连（g=0），也可以通过二价连接基 L0 与末端支化基 G（g=1）相连。后者提供了更多的反应位点，可结合更多的药物分子，从而提高药物负载能力。衍生物的近中心对称结构可以在大规模生产过程中更精确地控制分子量，从而有利于获得分子量分布更窄的产品。由此改性的生物相关物质具有更均匀、更可控的性能。
• Multifunctionalized polyethylene glycol derivative and preparation method therefor
  申请人：XIAMEN SINOPEG BIOTECH CO., LTD.

  公开号：US11324827B2

  公开（公告）日：2022-05-10

  Disclosed are a multifunctionalized polyethylene glycol derivative and a preparation method therefor. The derivative has an H-shaped structure as represented by formula (1) and comprises one linear core LPEG and four PEG branch chains, where n1, n2, n3, and n4 respectively are the degrees of polymerization of the branch chains, U1 and U2 are trivalent branching groups connecting the core LPEG to two of the PEG branch chains, F1 and F2 contain a functional group or a protected form R01 thereof and may or may not contain a branched group G, correspondingly, the number of R01 is one or more, F1 and F2 are either identical or different, any one linking group in the molecule or any linking group formed with an adjacent heteroatom group can either remain stable or be degraded, and any one PEG segment in the molecule is discretely polydispersed or monodispersed. The multifunctional polyethylene glycol is flexible and diverse in terms of branch structures and the lengths of branching arms, has various parameters and performance indicators that are adjustable and easy to control, and has a broad applicability.

  本发明公开了一种多功能聚乙二醇衍生物及其制备方法。该衍生物具有由式（1）表示的 H 型结构，包括一个线性核心 LPEG 和四个 PEG 支链，其中 n1、n2、n3 和 n4 分别为支链的聚合度，U1 和 U2 为连接核心 LPEG 和两个 PEG 支链的三价支化基团、F1 和 F2 含有一个官能团或其保护形式 R01，可以含有或不含有支链基团 G，相应地，R01 的数目为一个或多个，F1 和 F2 要么相同要么不同，分子中的任何一个连接基团或与相邻杂原子基团形成的任何连接基团要么保持稳定，要么降解，分子中的任何一个 PEG 段离散多分散或单分散。多功能聚乙二醇的支链结构和支臂长度灵活多样，各种参数和性能指标可调且易于控制，具有广泛的适用性。