尤普罗辛 | 1301-42-4

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 金鸡纳生物碱
• 中文名称: 尤普罗辛
• 中文别名: 优扑罗兴
• 英文名称: (8S,9R)-6'-Isopentyloxy-10,11-dihydro-cinchonan-9-ol
• 英文别名: euprocin；(R)-[(2S,4S,5R)-5-ethyl-1-azabicyclo[2.2.2]octan-2-yl]-[6-(3-methylbutoxy)quinolin-4-yl]methanol
• CAS: 1301-42-4
• 化学式: C₂₄H₃₄N₂O₂
• 分子量: 382.546
• InChiKey: CAFOIGUDKPQBIO-BYIOMEFUSA-N

物化性质

• 熔点：
  152°
• 沸点：
  535.4±35.0 °C(Predicted)
• 密度：
  1.13±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  28
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  45.6
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  2 5-噻吩二羰酰二摧毁 、 尤普罗辛 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 6.0h， 以59%的产率得到2-((1S)-((2S)-5-ethylquinuclidin-2-yl)(6-(isopentyloxy)quinolin-4-yl)methyl) 5-((1S)-((2S,4S,5R)-5-ethylquinuclidin-2-yl)(6-(isopentyloxy)quinolin-4-yl)methyl) thiophene-2,5-dicarboxylate
  参考文献：
  名称：

  新型 C 2-对称硫基催化剂的合成：卤基和硒基官能化的正常和中等尺寸环的不对称形成

  摘要：

  开发了新型、高度官能化的 C 2 对称硫基催化剂的合成，并探索了它们在烯酸的不对称溴、碘和硒官能化中的催化应用。该方案以高达 98% 的产率和 83% 的立体选择性提供相应的正常和中等大小的溴、碘和硒内酯。

  DOI：

  10.1055/s-0037-1610715
• 作为产物：
  描述：

  异戊醇 在 氢氧化钾 、 戊醇 作用下， 生成 尤普罗辛
  参考文献：
  名称：

  Slotta; Behnisch, Chemische Berichte, 1933, vol. 66, p. 360,363

  摘要：

  DOI：

文献信息

• GLUTATHIONE-CHOLESTEROL DERIVATIVES AS BRAIN TARGETING AGENTS
  申请人：South Dakota Board of Regents

  公开号：US20200048305A1

  公开（公告）日：2020-02-13

  The present invention describes compositions containing cholesterol-linker-glutathione conjugates for targeting the brain by overcoming barrier entry to the CNS through the blood brain barrier (BBB), including micelle and liposome forms of such compositions. In addition, methods for treating subjects by administering such compositions are also disclosed.

  本发明描述了含有胆固醇-连接剂-谷胱甘肽共轭物的组合物，通过克服血脑屏障（BBB）进入中枢神经系统的屏障入口，包括这些组合物的胶束和脂质体形式。此外，还公开了通过给予这些组合物治疗受试者的方法。
• Nitric Oxide Releasing Prodrugs of Therapeutic Agents
  申请人：SATYAM Apparao

  公开号：US20110263526A1

  公开（公告）日：2011-10-27

  The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

  本发明涉及已知药物或治疗剂的一氧化氮释放前药，其在此处表示为式(I)的化合物，其中药物或治疗剂包含一个或多个功能基团，独立地选自羧酸、氨基、羟基和巯基。该发明还涉及制备一氧化氮释放前药（式(I)的化合物）的方法，含有它们的药物组合物以及使用这些前药的方法。
• Crosslinked hyaluronic acid compositions for tissue augmentation
  申请人：Sadozai K. Khalid

  公开号：US20050136122A1

  公开（公告）日：2005-06-23

  A hyaluronic acid (HA) composition includes crosslinked, water-insoluble, hydrated HA gel particles. The HA includes crosslinks represented by the following structural formula: HA—U—R 2 —U—HA The variables are defined herein. A method of augmenting tissue in a subject includes inserting a needle into a subject at a location in the subject that is in need of tissue augmentation, wherein the needle is coupled to a syringe loaded with the HA composition, and applying force to the syringe, to deliver the HA composition into the subject. A method of preparing the HA composition, includes forming water-insoluble, dehydrated crosslinked HA particles, separating the water-insoluble, dehydrated particles by average diameter, selecting a subset of particles by average diameter, and hydrating the subset of dehydrated particles with a physiologically compatible aqueous solution. Another method of preparing the crosslinked HA composition includes crosslinking a precursor of the crosslinked HA with a biscarbodiimide in the presence of a pH buffer and dehydrating the crosslinked HA. Also included is a method of augmenting tissue in a subject that is in need of tissue augmentation. A method of stabilizing crosslinked HA includes hydrating water-insoluble, dehydrated crosslinked HA with a physiologically compatible aqueous solution that includes a local anesthetic, wherein the value of storage modulus G′ for the stabilized composition is at least about 110% of the value of G′ for a non-stabilized composition,. Also included is the stabilized HA composition.

  一种透明质酸（HA）组合物包括交联的、不溶于水的、水合的HA凝胶颗粒。HA包括由以下结构式表示的交联：HA—U—R2—U—HA。变量在此定义。一种在受试者中增强组织的方法包括将针插入受试者体内需要组织增强的位置，其中针连接到装有HA组合物的注射器，并施加力量到注射器，将HA组合物注入受试者体内。一种制备HA组合物的方法包括形成不溶于水的、脱水的交联HA颗粒，通过平均直径分离不溶于水的、脱水的颗粒，通过平均直径选择颗粒的子集，并用生理兼容的水溶液使脱水的颗粒子集水化。另一种制备交联HA组合物的方法包括在pH缓冲剂存在下用双异氰酸酯交联交联HA的前体，并脱水交联HA。还包括一种在需要组织增强的受试者中增强组织的方法。一种稳定交联HA的方法包括用含有局部麻醉剂的生理兼容水溶液水化不溶于水的、脱水的交联HA，其中稳定组合物的存储模量G′的值至少为非稳定组合物G′值的约110%。还包括稳定的HA组合物。
• [EN] MACROMOLECULES FOR TREATING ATHEROSCLEROSIS<br/>[FR] MACROMOLÉCULES POUR LE TRAITEMENT DE L'ATHÉROSCLÉROSE
  申请人：UNIV RUTGERS

  公开号：WO2013188882A1

  公开（公告）日：2013-12-19

  The invention includes compounds of the formula I and formula II and salts thereof, as well as methods for using the compounds of formula I and formula II for treating atherosclerosis. The invention also includes compounds of formula III and (21) and salts thereof, as well as methods of using the compounds of formula III and (21) for treating atherosclerosis. The invention also includes methods of encapsulating molecules using the compounds of the invention.

  该发明包括公式I和公式II的化合物及其盐，以及使用公式I和公式II的化合物治疗动脉粥样硬化的方法。该发明还包括公式III和(21)的化合物及其盐，以及使用公式III和(21)的化合物治疗动脉粥样硬化的方法。该发明还包括使用该发明的化合物对分子进行封装的方法。
• Technology for the Preparation of Microparticles
  申请人：Malakhov Michael

  公开号：US20090098207A1

  公开（公告）日：2009-04-16

  Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

  微球是通过将溶液中的大分子或小分子与抗溶剂和对离子接触，并冷却溶液而制备的。这些微球可用于制备具有明确定义尺寸的药物、营养保健品、化妆品等产品。