5-(6-Amino-2-chloro-9-purinyl)-4-fluoro-2-(hydroxymethyl)-3-oxolanol

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘌呤核苷
• 英文名称: 5-(6-Amino-2-chloro-9-purinyl)-4-fluoro-2-(hydroxymethyl)-3-oxolanol
• 英文别名: 5-(6-amino-2-chloropurin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol
• 化学式: C₁₀H₁₁ClFN₅O₃
• 分子量: 303.68
• InChiKey: WDDPHFBMKLOVOX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  119
• 氢给体数：
  3
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  克罗拉滨 生成 5-(6-Amino-2-chloro-9-purinyl)-4-fluoro-2-(hydroxymethyl)-3-oxolanol
  参考文献：
  名称：

  J. Med. Chem. 2009, 52, 688-699

  摘要：

  DOI：

文献信息

• METHOD FOR THE SYNTHESIS OF CLOFARABINE
  申请人：SYNBIAS PHARMA AG

  公开号：US20170044204A1

  公开（公告）日：2017-02-16

  The present invention relates to a method for the high yield production of the anticancer nucleoside clofarabine, the method comprising the preparation of 2-chloroadenosine by enzymatic transglycosylation between 2-chloroadenine and nucleosides, benzoylation, isomerization, sulfonate ester formation, fluorination, and deprotection.

  本发明涉及一种高产抗癌核苷类药物克洛法滨的生产方法，该方法包括通过酶促转糖基反应在2-氯腺苷和核苷类化合物之间制备2-氯腺苷，然后进行苯甲酰化、异构化、磺酸酯形成、氟化和去保护等步骤。
• Method for the synthesis of clofarabine
  申请人：Synbias Pharma AG

  公开号：EP2937420A1

  公开（公告）日：2015-10-28

  The present invention relates to a method for the high yield production of the anticancer nucleoside clofarabine, the method comprising the preparation of 2-chloroadenosine by enzymatic transglycosylation between 2-chloroadenine and nucleosides, benzoylation, isomerization, sulfonate ester formation, fluorination, and deprotection.

  本发明涉及一种高产抗癌核苷类药物克拉法滨的生产方法，该方法包括通过2-氯腺嘌呤和核苷之间的酶促转基因作用制备2-氯腺苷，然后进行苯甲酰化、异构化、磺酸酯形成、氟化和去保护等步骤。
• [EN] METHOD FOR THE SYNTHESIS OF CLOFARABINE<br/>[FR] PROCÉDÉ DE SYNTHÈSE DE CLOFARABINE
  申请人：SYNBIAS PHARMA AG

  公开号：WO2015162175A1

  公开（公告）日：2015-10-29

  Method for the production of the anticancer nucleoside clofarabine in high yield, the method comprising the preparation of 2- chloroadenosine by enzymatic transglycosylation between 2- chloroadenine and nucleosides, benzoylation, isomerization, sulfonate ester formation, fluorination, and deprotection.

  高产抗癌核苷类药物克拉法滨的生产方法，包括通过2-氯腺嘌呤和核苷之间的酶促转糖基化反应制备2-氯腺苷，进行苯甲酰化、异构化、磺酸酯形成、氟化和去保护反应。
• Compositions Containing Antiviral Compounds and Methods of Using the Same
  申请人：Cantrell Gary L.

  公开号：US20090258843A1

  公开（公告）日：2009-10-15

  The present invention is directed to compositions and methods for the treatment of various diseases, pathological disorders, and medical conditions such as viral infections and cancer. The compositions include (A) an antiviral compound or a pharmaceutically acceptable salt thereof; and (B) an agent selected from the group consisting of a substituted or unsubstituted imidazole or a pharmaceutically acceptable salt thereof; a non-steroidal anti-inflammatory agent or a pharmaceutically acceptable salt thereof; an amino acid or a pharmaceutically acceptable salt thereof; a carboxylic acid or a pharmaceutically acceptable salt thereof; a sulfonic acid or a pharmaceutically acceptable salt thereof; and a combination thereof.

  本发明涉及用于治疗各种疾病、病理障碍和医疗条件，如病毒感染和癌症的组合物和方法。所述组合物包括（A）抗病毒化合物或其药学上可接受的盐；和（B）从以下组中选择的药剂：取代或未取代的咪唑或其药学上可接受的盐；非甾体抗炎药或其药学上可接受的盐；氨基酸或其药学上可接受的盐；羧酸或其药学上可接受的盐；磺酸或其药学上可接受的盐；或其组合物。
• DOUBLE-LIVER-TARGETING PHOSPHORAMIDATE AND PHOSPHONOAMIDATE PRODRUGS
  申请人：NANJING MOLECULAR RESEARCH, INC.

  公开号：US20130210757A1

  公开（公告）日：2013-08-15

  This application discloses phosphoramidate and phosphonoamidate prodrugs of alcohol-based therapeutic agents, such as nucleosides, nucleotides, acyclonucleosides, C-nucleosides, and C-nucleotides, and use of these prodrugs for treatment of diseases or disorders, including infectious diseases and cancers. This application also discloses a general method for enhancing bioavailability and/or liver-targeting property of alcohol drugs through converting the alcohol drugs to phosphoramidate or phosphonoamidate prodrugs, and methods of preparation of these prodrugs.

  本申请公开了醇类治疗剂的磷酰胺酸和磷酸胺酯前药，例如核苷、核苷酸、非环核苷、C-核苷和C-核苷酸，以及使用这些前药治疗疾病或疾病的方法，包括传染病和癌症。本申请还公开了一种通用方法，通过将醇类药物转化为磷酰胺酸或磷酸胺酯前药，增强醇类药物的生物利用度和/或肝靶向性，以及这些前药的制备方法。