(2R,6R)-2-methyl-6-[[(2S)-2-(sulfanyloxymethyl)-2H-furan-5-yl]oxy]-2,6-dihydropyran | 74135-10-7

• 物质功能分类: 生物化工 - 糖类化合物 - 寡糖
• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (2R,6R)-2-methyl-6-[[(2S)-2-(sulfanyloxymethyl)-2H-furan-5-yl]oxy]-2,6-dihydropyran
• 英文别名: Sucrose octasulfate sodium salt；sucrose octasulphate sodium salt；sodium salt of sucrose octasulfate；sodium sucrose octasulfate；sucrose octasulfate sodium；sucrose octasulfate
• CAS: 74135-10-7；127930-09-0
• 化学式: C₁₂H₁₄O₃₅S₈*8Na
• 分子量: 1158.67
• InChiKey: AUAYLRSBUXJFCP-AKSHDPDZSA-F

物化性质

• 熔点：
  159-164°C
• 密度：
  2.097 at 20℃
• 溶解度：
  可微溶于水（微溶，超声处理）
• 表面张力：
  75.1mN/m at 1g/L and 20℃

计算性质

• 辛醇/水分配系数(LogP)：
  -12.52
• 重原子数：
  56.0
• 可旋转键数：
  21.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  559.13
• 氢给体数：
  0.0
• 氢受体数：
  35.0

安全信息

• 安全说明：
  S24/25
• 海关编码：
  28331900
• 危险性防范说明：
  P261,P280,P301+P312,P302+P352,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

制备方法与用途

产品特点

蔗糖酯（SE)是由蔗糖与高级脂肪酸合成的一类非离子表面 活性剂的总称，一般为白色至象牙色粉状、块状、蜡状固体，或无色至微黄色粘稠状或树脂 状液体。无臭味与异味，具有良好的乳化、分散、润湿、起泡和洗涤性能，以及粘度调节、防止 老化、防止析晶等作用。

反应信息

• 作为反应物：
  描述：

  (2R,6R)-2-methyl-6-[[(2S)-2-(sulfanyloxymethyl)-2H-furan-5-yl]oxy]-2,6-dihydropyran 以 水 为溶剂， 生成 硫糖酯
  参考文献：
  名称：

  Drug salts

  摘要：

  已经发现糖酸盐代表了基本有机药物化合物有益的控释形式。适当的盐的例子包括单糖，双糖，寡糖和多糖聚糖硫酸盐，例如四环素类和氨基糖苷类抗生素。

  公开号：

  US06077822A1
• 作为产物：
  描述：

  蔗糖 在 三乙胺三氧化硫 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 24.0h， 以65%的产率得到(2R,6R)-2-methyl-6-[[(2S)-2-(sulfanyloxymethyl)-2H-furan-5-yl]oxy]-2,6-dihydropyran
  参考文献：
  名称：

  摘要：

  Purpose. Aluminum sucrose octasulfate (SOS) is used clinically to prevent ulcers. Under physiologic conditions, the sodium salt of this drug can be formed. Our objective was to determine whether sodium SOS was absorbed when administered orally. In addition to furthering our understanding of aluminum SOS, this study also aimed to clarify how other polyanionic drugs, such as heparin and low-molecular-weight heparins, are absorbed.Methods.[C-14]-labeled and cold sodium SOS (60 mg/kg) were given to rats by stomach tube. Radioactivity was counted in gut tissue, gut washes, and nongut tissue (i.e., lung, liver, kidney, spleen, endothelial, and plasma samples) at 3 min, 6 min, 15 min, 30 min, 60 min, 4 h, and 24 h, and in urine and feces accumulated over 4 h and 24 h.Results. Peak radioactivity was found in the tissue and washes of the stomach, ileum, and colon at 6 min, 60 min, and 4 h, respectively, showing progression through the gut. Gut recovery accounted for 84% of the dose at 6 min but only 12% of the dose at 24 h, including counts from feces. Radioactivity was recovered from nongut tissue (averaging 8.6% of the dose) and accumulated urine (18% of the dose at 24 h). When total body distribution was considered, the recovery of radioactivity was greater for the endothelium than for plasma (peak percentage of the dose was 65% at 15 min, 20% at 3 min, 5% from 20 to 240 min for the vena cava, aortic endothelium, and plasma, respectively).Conclusions. Results indicate that sodium SOS is absorbed, agreeing with previous studies demonstrating the oral absorption of other sulfated polyanions. Endothelial concentrations must be considered when assessing the pharmacokinetics of these compounds. The measured plasma drug concentrations reflect the much greater amounts of drug residing with the endothelium.

  DOI：

  10.1023/a:1016161001013

文献信息

• [EN] EPHRIN RECEPTOR A2 (EPHA2)-TARGETED DOCETAXEL-GENERATING NANO-LIPOSOME COMPOSITIONS<br/>[FR] COMPOSITIONS DE NANOLIPOSOMES GÉNÉRANT DU DOCÉTAXEL ET CIBLANT LE RÉCEPTEUR DE L'ÉPHRINE A2 (EPHA2)
  申请人：MERRIMACK PHARMACEUTICALS INC

  公开号：WO2017161067A1

  公开（公告）日：2017-09-21

  EphA2-targeted immunoliposomes for delivering docetaxel are useful in the treatment of certain types of cancer. The immunoliposomes can include an EphA2 targeting moiety (e.g., a scFv) and encapsulate a docetaxel prodrug in a stable salt form within a liposome having an average size of about 100 nm. Novel docetaxel prodrugs suitable for loading into nanoliposomes (including immunoliposomes) are provided, along with novel and other useful EphA2 targeting moieties for preparation of EphA2-targeted doxorubicin-generating immunoliposome therapies. Pharmaceutical compositions can be prepared that include nanoliposomes encapsulating one or more docetaxel prodrugs, and/or immunoliposomes or nanoparticles comprising an EphA2 binding moiety and encapsulating one or more docetaxel prodrugs. The pharmaceutical compositions are useful for administration to a patient for the treatment of cancer.

  EphA2靶向免疫脂质体用于输送紫杉醇在治疗某些类型的癌症中是有用的。这些免疫脂质体可以包括EphA2靶向基团（例如，scFv），并在平均大小约为100纳米的脂质体内以稳定的盐形式封装紫杉醇前药。提供了适合装载到纳米脂质体（包括免疫脂质体）中的新型紫杉醇前药，以及用于制备EphA2靶向阿霉素生成免疫脂质体疗法的新型和其他有用的EphA2靶向基团。可以制备包含封装一个或多个紫杉醇前药的纳米脂质体和/或包含EphA2结合基团并封装一个或多个紫杉醇前药的免疫脂质体或纳米粒子的药物组合物。这些药物组合物对于用于治疗癌症的患者是有用的。
• Stabilizing Camptothecin Pharmaceutical Compositions
  申请人：Ipsen Biopharm Ltd.

  公开号：US20170319573A1

  公开（公告）日：2017-11-09

  Irinotecan phospholipid liposomes with improved storage stability are provided, with related methods of treatment and manufacture. The irinotecan liposomes can have reduced formation of lyso-phosphatidylcholine (lyso-PC) during storage, and prior to administration to a patient.

  提供具有改善储存稳定性的伊立替康磷脂脂质体，以及相关的治疗和制造方法。伊立替康脂质体在储存期间和在给患者之前可以减少溶血磷脂酰胆碱（lyso-PC）的形成。
• HYPERSULFATED GLUCOPYRANOSIDES
  申请人：AHMED Tahir

  公开号：US20110245197A1

  公开（公告）日：2011-10-06

  Hypersulfated disaccharides, preferably octasulfated sucrose, with utility in asthma or asthma related disorders are disclosed. The compounds may optionally be formulated with pharmaceutically acceptable excipients or delivery agents. The delivery agents are selected from the group consisting of natural or synthetic polymers, aerosols or other vehicles that facilitate the delivery or administration of the drug. The hypersulfated disaccharides are made from carbohydrate starting materials. Ion exchange or other suitable synthetic processes may be utilized to prepare the pharmaceuticals. The hypersulfated disaccharides are useful as anti-inflammatory agents.

  本发明涉及用于哮喘或哮喘相关疾病的高度硫酸化二糖，优选为八硫酸化蔗糖。该化合物可以选择性地与药学上可接受的辅料或给药剂配制。给药剂可以选择自然或合成聚合物、气雾剂或其他有助于药物输送或给药的载体。高度硫酸化二糖是由碳水化合物起始材料制成的。离子交换或其他适当的合成过程可用于制备药品。高度硫酸化二糖可用作抗炎剂。
• Crystalline salts of sucrose octasulfate.
  作者：KIYOSHIGE OCHI、YOSHIHIKO WATANABE、KIYOSHI OKUI、MINORU SHINDO

  DOI：10.1248/cpb.28.638

  日期：——

  Sulfation of sucrose with pyridine-sulfur trioxide was carried out in dimethylformamide and pyridine, and the degree of sulfation of the sodium salt of sucrose sulfate thus obtained was estimated from the ratio of sulfur to carbon content (S/C). The sulfates prepared with 9-15 molar equivalents of pyridine-sulfur trioxide in dimethylformamide and those prepared with 5 and 9 equivalents in pyridine were identified as sucrose octasulfate. Potassium, cesium, rubidium, and ammonium salts of sucrose octasulfate were obtained as crystals.

  在二甲基甲酰胺和吡啶中用吡啶三氧化硫对蔗糖进行硫化，并根据硫含量与碳含量之比（S/C）估算出由此得到的蔗糖硫酸钠盐的硫化程度。在二甲基甲酰胺中用 9-15 摩尔当量的吡啶-三氧化硫制备的硫酸盐，以及在吡啶中用 5 和 9 摩尔当量的吡啶-三氧化硫制备的硫酸盐被鉴定为蔗糖八硫酸盐。蔗糖八硫酸钾、铯、铷和铵盐均以晶体形式存在。
• CN116874540
  申请人：——

  公开号：——

  公开（公告）日：——