(1R,2R,4S,5R,6R)-3,8,9-trioxatricyclo[4.2.1.02,4]nonan-5-ol | 3868-03-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氧环庚烷
• 英文名称: (1R,2R,4S,5R,6R)-3,8,9-trioxatricyclo[4.2.1.02,4]nonan-5-ol
• CAS: 3868-03-9；6893-59-0；26423-96-1；34147-05-2；90191-86-9
• 化学式: C₆H₈O₄
• 分子量: 144.127
• InChiKey: RXDFVNWKKAAOSK-VFUOTHLCSA-N

物化性质

• 熔点：
  67.0 to 71.0 °C

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  51.2
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2932999099

反应信息

• 作为产物：
  描述：

  苯磺酸,4-羟基-,盐(1:?:?)钙钾 生成 (1R,2R,4S,5R,6R)-3,8,9-trioxatricyclo[4.2.1.02,4]nonan-5-ol
  参考文献：
  名称：

  REHNBERG, NICOLA;MAGNUSSON, GORAN, J. ORG. CHEM., 55,(1990) N0, C. 5467-5476

  摘要：

  DOI：

文献信息

• DISACCHARIDE INTERMEDIATE AND SYNTHESIS METHOD THEREOF
  申请人：ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.

  公开号：US20160264609A1

  公开（公告）日：2016-09-15

  The present invention relates to a disaccharide intermediate and a synthesis method thereof, relates to the chemical pharmaceutical field, and more specifically relates to a method for preparing a disaccharide segment of a key intermediate for chemically synthesizing heparin and heparinoid compounds. Disclosed are a new disaccharide intermediate and three methods for synthesizing the disaccharide intermediate, that is, compounds of a formula (4) and glucopyranose protected by different anomeric carbon are made to react in the presence of an active agent, to obtain the disaccharide intermediate. According to the technical solutions of the present invention, synthetic raw materials are easy to obtain, have a mild reaction condition, and are suitable for industrialized production.

  本发明涉及一种二糖中间体及其合成方法，涉及化学制药领域，更具体地涉及一种用于制备肝素和肝素样化合物的关键中间体的二糖片段的方法。公开了一种新的二糖中间体和三种用于合成该二糖中间体的方法，即，在活性剂的存在下，使具有不同各向异性碳保护的化合物（4）和葡萄糖吡喃糖反应，以获得该二糖中间体。根据本发明的技术方案，合成原料易于获得，反应条件温和，适合工业化生产。
• METHOD FOR PREPARING 1,6:2,3-DIANHYDRO-BETA-D-MANNOPYRANOSE
  申请人：Grossi Pierre Jean

  公开号：US20110213141A1

  公开（公告）日：2011-09-01

  The invention relates to a method for preparing 1,6:2,3-dianhydro-â-D-mannopyranose and is characterized in that it includes a step of cyclizing the compound C, where R is an alykyl group and R′ is an activating agent, in an alcohol/alcoholate mixture under anhydrous conditions.

  本发明涉及一种制备1,6:2,3-二去氢-α-D-甘露糖的方法，其特征在于包括在无水条件下，在醇/醇酸盐混合物中环化化合物C的步骤，其中R为烷基，R'为活化剂。
• SHORT SYNTHETIC PATHWAY FOR 1,6:2,3-DIANHYDRO-BETA-D-MANNOPYRANOSE
  申请人：Bouvenot Laurent

  公开号：US20110224446A1

  公开（公告）日：2011-09-15

  The invention relates to a method for preparing 1,6:2,3-dianhydro-β-D-mannopyranose and is characterized in that it includes a step of cyclizing the compound B, where R is an activating agent, in the presence of a base selected from among ammonium hydroxides and mineral bases.

  本发明涉及一种制备1,6:2,3-二去水-β-D-甘露糖苷的方法，其特征在于，它包括在氨水和矿物质碱中选择一种碱的存在下，将化合物B环化的步骤，其中R是一种活性剂。
• Compositions for the regulation of cytokine activity
  申请人：YEDA RESEARCH AND DEVELOPMENT CO. LTD.

  公开号：EP1095657A2

  公开（公告）日：2001-05-02

  Substances comprising a N-sulfated or N-acetylated or non-sulfated N-acetylated 4-deoxy-4-en-iduronoglucosamine in substantially purified form, including compositions containing same and their uses are disclosed for the regulation of cytokine activity in a host. For instance, the secretion of Tumor Necrosis Factor Alpha (TNF-α) can be either inhibited or augmented selectively by administration to the host of effective amounts of substances or their compositions comprising specific oligosaccharides in substantially purified form. Thus, the present invention also relates to pharmaceutical compositions and their use for the prevention and/or treatment of pathological processes involving the induction of active cytokine secretion, such as TNF-α. The invention also relates to the initiation of a desirable immune system-related response by the host to the presence of activators, including pathogens. The substances and pharmaceutical compositions of the present invention may be administered daily, at very low effective doses, typically below 0.1 mg/kg human, or at intervals of up to about 5-8 days, preferably once a week.

  本发明公开了包含基本纯化形式的 N-硫酸化或 N-乙酰化或非硫酸化 N-乙酰化 4-脱氧-4-烯-尿嘧啶葡糖胺的物质，包括含有相同物质的组合物及其用途，用于调节宿主体内细胞因子的活性。例如，通过向宿主施用有效量的包含基本纯化形式的特定寡糖的物质或其组合物，可选择性地抑制或增加肿瘤坏死因子α（TNF-α）的分泌。因此，本发明还涉及药物组合物及其在预防和/或治疗涉及诱导活性细胞因子（如 TNF-α）分泌的病理过程中的用途。本发明还涉及宿主对活化剂（包括病原体）的存在启动理想的免疫系统相关反应。本发明的物质和药物组合物可以每天施用，有效剂量非常低，通常低于0.1毫克/千克人，或间隔长达约5-8天，最好每周一次。
• Disaccharide intermediate and synthesis method thereof
  申请人：Zhejiang Hisun Pharmaceutical Co., Ltd.

  公开号：US10287309B2

  公开（公告）日：2019-05-14

  The present invention relates to a disaccharide intermediate and a synthesis method thereof, relates to the chemical pharmaceutical field, and more specifically relates to a method for preparing a disaccharide segment of a key intermediate for chemically synthesizing heparin and heparinoid compounds. Disclosed are a new disaccharide intermediate and three methods for synthesizing the disaccharide intermediate, that is, compounds of a formula (4) and glucopyranose protected by different anomeric carbon are made to react in the presence of an active agent, to obtain the disaccharide intermediate. According to the technical solutions of the present invention, synthetic raw materials are easy to obtain, have a mild reaction condition, and are suitable for industrialized production.

  本发明涉及一种双糖中间体及其合成方法，涉及化学制药领域，更具体地说，涉及一种化学合成肝素和肝素化合物的关键中间体双糖段的制备方法。本发明公开了一种新的二糖中间体和合成该二糖中间体的三种方法，即在活性剂存在下，使式（4）化合物和被不同异构碳保护的葡吡喃糖发生反应，得到该二糖中间体。根据本发明的技术方案，合成原料易得，反应条件温和，适合工业化生产。