5-O-(4-chlorobenzoyl)-3-C-ethynyl-D-ribo-pentofuranose

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-O-(4-chlorobenzoyl)-3-C-ethynyl-D-ribo-pentofuranose
• 英文别名: 5-O-(4-chlorobenzoyl)-3-C-ethynyl-D-ribofuranose；[(2R,3S,4R)-3-ethynyl-3,4,5-trihydroxyoxolan-2-yl]methyl 4-chlorobenzoate
• 化学式: C₁₄H₁₃ClO₆
• 分子量: 312.707
• InChiKey: BHHWKAPNUFBDCK-ZZWXXDIBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  96.2
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  4-氯苯甲酰氯 、 5-O-(4-chlorobenzoyl)-3-C-ethynyl-D-ribo-pentofuranose 在 4-二甲氨基吡啶 、 三乙胺 作用下， 以 二氯甲烷 、 水 为溶剂， 以77%的产率得到1,2,3,5-tetra-O-(4-chlorobenzoyl)-3-C-ethynyl-D-ribo-pentofuranose
  参考文献：
  名称：

  D-pentofuranose derivatives and process for preparing the same

  摘要：

  本发明涉及通式(1)至(4)所示的D-戊呋喃糖衍生物：##STR1##（其中A代表氯苯甲酰基；R1代表氢原子、低级脂肪族酰基、取代或未取代的苯甲酰基；X和Y各自代表低级烷基；Z代表乙炔基或三低级烷基硅乙炔基；式(1)中的糖部分代表木糖；式(3)和(4)中的糖部分各自代表核糖）。本发明还涉及制备化合物(2)的方法，其特征在于在2,2,6,6-四甲基哌啶氧基化合物催化量的存在下，用次氯酸盐氧化式(1)的化合物，这些化合物作为合成具有优异抗肿瘤活性的3'-C-取代的核糖核苷衍生物的中间体是有用的。

  公开号：

  US05880294A1
• 作为产物：
  描述：

  5-O-(4-chlorobenzoyl)-1,2-O-isopropylidene-D-erythro-pentofuranose03-urose 在 甲酸 作用下， 以 四氢呋喃 为溶剂， 反应 3.42h， 生成 5-O-(4-chlorobenzoyl)-3-C-ethynyl-D-ribo-pentofuranose
  参考文献：
  名称：

  Nucleosides and nucleotides. Part 212: Practical large-scale synthesis of 1-(3-C-ethynyl-β-d-ribo-pentofuranosyl)cytosine (ECyd), a potent antitumor nucleoside. Isobutyryloxy group as an efficient anomeric leaving group in the Vorbrüggen glycosylation reaction

  摘要：

  A practical synthetic route to the antitumor nucleoside, 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)cytosine (ECyd, 1) from 1,2-O-isopropylidene-D-xylofuranose (3) has been developed. Since most of the compounds were obtained as crystals, the target ECyd was prepared without any chromatographic purification in 31% overall yield from compound 3. The isobutyryloxy group was found to be an effective leaving group at the anomeric position of the 3-beta-C-ethynyl glycosyl donors in the key Vorbruggen glycosylation reaction. Using a similar procedure without chromatographic purification, the uracil congener EUrd [1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)uracil (2), which also has a potent antitumor effect, was synthesized from 3 in 39% overall yield. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0040-4020(01)01249-2

文献信息

• Test kit, extraction device and method for the determination of streptococcus a antigen
  申请人：EASTMAN KODAK COMPANY (a New Jersey corporation)

  公开号：EP0280557A2

  公开（公告）日：1988-08-31

  A test kit useful for the determination of Streptococcus A antigen comprises: (i) an immunoreactive reagent comprising either Streptococcus A antigen or antibodies attached to water-insoluble particles, (ii) a substrate having thereon a dried, binder-free coating of a first extraction reagent, (iii) an aqueous solution of a second extraction reagent, and (iv) a neutralizing solution. Both extraction reagents combine to provide nitrous acid. In addition, an extraction device includes a water-insoluble container having affixed therein an extraction reagent and an applicator means for collecting and depositing a biological specimen within the container. The extraction device and test kit are useful for the determination of Streptococcus A antigen in a biological specimen.

  一种用于测定 A 型链球菌抗原的检测试剂盒包括：(i) 一种免疫反应试剂，该试剂由 A 型链球菌抗原或抗体组成，附着在不溶于水的颗粒上；(ii) 一种基质，该基质上有一层干燥的、不含粘合剂的第一萃取试剂涂层；(iii) 第二萃取试剂的水溶液；(iv) 一种中和溶液。 两种萃取试剂结合在一起可产生亚硝酸。 此外，一种萃取装置包括一个不溶于水的容器，该容器上附有一种萃取试剂和一种涂抹装置，用于收集生物标本并将其放入容器中。 该萃取装置和检测试剂盒可用于测定生物标本中的 A 型链球菌抗原。
• Agglutination reagent and method of preparing same
  申请人：EASTMAN KODAK COMPANY (a New Jersey corporation)

  公开号：EP0280561A2

  公开（公告）日：1988-08-31

  An agglutination reagent is prepared by covalently attaching an immunoreactive species to polymeric particles through reactive groups in the species. After attachment, the species is chemically modified with an acylating, alkylating or sulfonylating agent thereby modifying primary or secondary amino groups. The reagent can be used in agglutination assays for a number of analytes, including Streptococcus A antigen, human retroviruses or antibodies, human chorionic gonadotropin and other antibodies or antigens.

  凝集试剂的制备方法是通过免疫活性物质中的反应基团将其共价连接到聚合微粒上。附着后，用酰化剂、烷基化剂或磺化剂对免疫活性物质进行化学修饰，从而修饰伯氨基或仲氨基。该试剂可用于多种分析物的凝集试验，包括链球菌 A 抗原、人类逆转录病毒或抗体、人类绒毛膜促性腺激素和其他抗体或抗原。
• Use of immobilized biotinylated receptor in test device, kit and method for determining a ligand
  申请人：EASTMAN KODAK COMPANY (a New Jersey corporation)

  公开号：EP0321261A1

  公开（公告）日：1989-06-21

  A device useful for the determination of a ligand in an aqueous liquid comprises a water-insoluble substrate. Immobilized in at least one location on that substrate is a biotinylated receptor for the ligand. This receptor is in dried form and immobilized with one or more dried water-soluble acrylamide homo- or copolymer binder materials. When the immobilized receptor is contacted with an aqueous sample, the binder material is dissolved and the receptor is released for reaction with the ligand. The resulting reaction product is determined in a suitable manner. The device can be included in a kit having other components useful for ligand determination. The device and method of its use are particularly useful for the determination of human chorionic gonadotropin (hCG) as an early indicator of pregnancy.

  一种用于测定水性液体中配体的装置包括一个不溶于水的基质。该底物上至少有一个位置固定着配体的生物素化受体。这种受体呈干燥状态，并与一种或多种干燥的水溶性丙烯酰胺均聚物或共聚物粘合剂材料固定在一起。当固定化受体与水样接触时，粘合剂材料溶解，受体释放出来与配体反应。由此产生的反应产物以适当的方式进行测定。该装置可以包含在一个试剂盒中，试剂盒中还有其他对配体测定有用的组件。该装置及其使用方法尤其适用于测定作为怀孕早期指标的人绒毛膜促性腺激素（hCG）。
• Method of preparing a polymeric latex composition
  申请人：EASTMAN KODAK COMPANY (a New Jersey corporation)

  公开号：EP0308233A2

  公开（公告）日：1989-03-22

  A polymeric latex composition having a hydrophobe incorporated therein can be prepared using a novel method for incorporating the hydrophobe into the latex particles. This method includes providing a loadable latex, providing a hydrophobe dissolved in a water-miscible organic solvent, heating the loadable latex to 30 to 90°C and gradually adding the hydrophobe solution to the heated loadable latex under conditions to keep the hydrophobe in solution and to "load" or incorporate it into the latex particles. The latex can be surfactant-free and have particles which have outer reactive groups which are capable of reacting with free amine or sulfhydryl groups of a biological compound. Such latices can be used to prepare water-insoluble biological reagents having a biological compound attached to the particles.

  使用一种将憎水剂掺入胶乳颗粒的新方法，可以制备出含有憎水剂的聚合物胶乳组合物。该方法包括提供一种可负载胶乳，提供一种溶于水溶性有机溶剂中的憎水剂，将可负载胶乳加热至 30 至 90°C，并在使憎水剂保持在溶液中的条件下逐渐将憎水剂溶液添加到加热的可负载胶乳中，以将其 "负载 "或掺入胶乳颗粒中。这种胶乳可以不含表面活性剂，其颗粒的外部活性基团能够与生物化合物的游离胺或巯基发生反应。这种胶乳可用于制备水不溶性生物试剂，其颗粒上附有生物化合物。
• Dye-providing composition, diagnostic test kit and their use in method for ligand determination using peroxidase labeled-receptor
  申请人：Johnson & Johnson Clinical Diagnostics, Inc.

  公开号：EP0308236A2

  公开（公告）日：1989-03-22

  A dye-providing composition comprises a water-soluble or -dispersible polymer, such as a vinylpyrrolidone polymer, and an imidazole leuco dye capable of providing a dye in the presence of hydrogen peroxide and a peroxidative substance. The weight ratio of polymer to leuco dye is from 10,000:1 to 100:1. The dye-providing composition can be included with a peroxidase substrate in a diagnostic test kit. A method for the determination of a ligand can be carried out using a peroxidase labeled-receptor for the ligand and the dye-providing composition described above. The method is particularly useful for the determination of human chorionic gonadotropin.

  一种提供染料的组合物由水溶性或可分散性聚合物（如乙烯基吡咯烷酮聚合物）和在过氧化氢和过氧化物存在下能提供染料的咪唑白胺染料组成。聚合物与白兰地染料的重量比为 10,000:1 至 100:1。提供染料的组合物可与过氧化物酶底物一起加入诊断试剂盒中。使用过氧化物酶标记的配体受体和上述提供染料的组合物，可以进行配体的测定方法。该方法尤其适用于测定人绒毛膜促性腺激素。