2-methyl-9-β-D-ribofuranosyl-6-chloropurine | 63709-15-9

• 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: 2-methyl-9-β-D-ribofuranosyl-6-chloropurine
• 英文别名: 1-(6-chloro-2-methyl-purin-9-yl)-β-D-1-deoxy-ribofuranose；6-chloro-2-methyl-9-(β-D-ribofuranosyl)-9H-purine；6-chloro-2-methyl-9-β-D-ribofuranosyl-9H-purine；2-methyl-6-chloropurine riboside；6-chloro-2-methyl-9-(beta-D-ribofuranosyl)-9H-purine；(2R,3R,4S,5R)-2-(6-chloro-2-methylpurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol
• CAS: 63709-15-9
• 化学式: C₁₁H₁₃ClN₄O₄
• 分子量: 300.702
• InChiKey: RPCUVBDPMOSUEW-IOSLPCCCSA-N

物化性质

• 沸点：
  516.5±60.0 °C(Predicted)
• 密度：
  1.92±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  114
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  2-methyl-9-β-D-ribofuranosyl-6-chloropurine 在 氢碘酸 作用下， 以 吡啶 为溶剂， 反应 0.03h， 生成 2-methyl-9-β-D-ribofuranosylpurine-6-carbonitrile
  参考文献：
  名称：

  某些9-β-D-呋喃核糖基嘌呤-6-羧酰胺的合成及其抗病毒活性。

  摘要：

  为了检查某些嘌呤核苷的抗病毒功效所必需的结构参数，已合成了几种9-β-D-呋喃核糖基嘌呤-6-羧酰胺。在路易斯酸存在下，嘌呤-6-羧酰胺的Me3Si衍生物与受保护的呋喃核糖的糖基化反应产生了被保护的核苷，该核苷酸在脱保护后提供了带有氰化物离子的9-β-D-核呋喃核糖基-6-碘嘌呤。还已经制备了某些2-氨基-和2-甲基-9-β-D-呋喃呋喃糖基嘌呤-6-羧酰胺。8-氨基甲酰基鸟苷（16）是通过母体核苷的均质酰化制备的。这些化合物针对细胞培养物中的几种RNA和DNA病毒进行了测试。9-β-D-呋喃核糖基嘌呤-6-羧酰胺（6a），相应的6-硫代羧酰胺（7b）和4-氨基-8-（β-D-呋喃核糖基氨基）嘧啶[5，4-d]嘧啶（8）在无毒剂量水平下显示出显着的体外抗病毒活性。以50（mg / kg）/天的剂量治疗裂谷热病毒感染的小鼠使用的6a在第21天的存活率为55％，而对照组为30％。

  DOI：

  10.1021/jm00140a006

文献信息

• 2,N-6-disubstituted adenosines and their antihypertensive methods of use
  申请人：Glaxo Group Limited

  公开号：US05032583A1

  公开（公告）日：1991-07-16

  Compounds of formula (I) ##STR1## wherein X represents a hydrogen or chlorine atom, or a methyl group; and R represents a cycloalkyl or cycloalkenyl ring containing 5 to 8 carbon atoms, which ring is substituted by a hydroxy group, and is optionally substituted by a C.sub.1-6 alkyl group and salts and solvates thereof. The new compounds have been found to exhibit activities such as an anti-lipolytic action. Processes for preparing the compounds of formula (I) and compositions containing them are also described.

  式(I)的化合物##STR1##其中X代表氢原子或氯原子，或甲基基团；R代表含有5至8个碳原子的环烷基或环烯基环，该环被一个羟基取代，并且可以被C.sub.1-6烷基基团取代，以及其盐和溶剂合物。发现这些新化合物具有抗脂肪分解作用等活性。还描述了制备式(I)化合物和含有它们的组合物的方法。
• Substituted 6-(Benzylamino) Purine Riboside Derivatives, Use Thereof and Compositions Containing These Derivatives
  申请人：Szucova Lucie

  公开号：US20120071433A1

  公开（公告）日：2012-03-22

  The invention relates to 2-substituted-6-(substituted benzylamino)purine riboside derivatives of the general formula I. These compounds possess antiapoptotic, anti-inflammatory and differentiating activities. The invention relates also to the compositions, which contain these derivatives as active ingredients.

  该发明涉及一般式I的2-取代-6-(取代苯基氨基)嘌呤核苷衍生物。这些化合物具有抗凋亡、抗炎和分化活性。该发明还涉及包含这些衍生物作为活性成分的组合物。
• [EN] SUBSTITUTED 6-(BENZYLAMINO) PURINE RIBOSIDE DERIVATIVES, USE THEREOF AND COMPOSITIONS CONTAINING THESE DERIVATIVES<br/>[FR] DÉRIVÉS DE RIBOSIDE DE 6-BENZYLAMINOPURINE SUBSTITUÉE, LEURS UTILISATIONS ET COMPOSITIONS CONTENANT CES DÉRIVÉS
  申请人：UNIVERZITA PALACKEHO V OLOMOUC

  公开号：WO2010130233A1

  公开（公告）日：2010-11-18

  The invention relates to 2-substituted-6-(substituted benzylamino)purine riboside derivatives of the general formula I. These compounds possess antiapoptotic, anti-inflammatory and differentiating activities. The invention relates also to the compositions, which contain these derivatives as active ingredients. ˙

  该发明涉及一般式I的2-取代-6-(取代苄胺基)嘌呤核苷衍生物。这些化合物具有抗凋亡、抗炎和分化活性。该发明还涉及含有这些衍生物作为活性成分的组合物。
• Substituted 6-(Benzylamino) Purine Riboside Derivatives, Use Thereof and Compositions Containing These Derivatives
  申请人：Biopatterns, S.R.O

  公开号：US20140066394A1

  公开（公告）日：2014-03-06

  A method of treatment using 2-substituted-6-(substituted benzylamino)purine riboside derivatives of the general formula I. These compounds possess antiapoptotic, anti-inflammatory and differentiating activities.

  使用通式I的2-取代-6-(取代苯基氨基)嘌呤核苷衍生物的治疗方法。这些化合物具有抗凋亡、抗炎和分化活性。
• Novel adenosine derivatives and pharmaceutical compositions containing them as an active ingredient
  申请人：NIPPON ZOKI PHARMACEUTICAL CO. LTD.

  公开号：EP0269574A2

  公开（公告）日：1988-06-01

  The present invention relates to novel adenosine derivatives having the formula (I): wherein each of R₁, R₂ and R₃, which may be the same or different, is hydrogen or a lower alkyl group; X is hydrogen, a lower alkyl group, an amino group or halogen; and Y is hydrogen or a lower alkyl group; and pharmaceutically acceptable salt thereof. These compounds are useful as antihypertensive agents, for example, for the treatments of hypertension and various diseases caused by hypertension, such as cerebrovascular diseases, cardiopathy or renal insufficiency.

  本发明涉及具有式(I)的新型腺苷衍生物：其中，R₁、R₂和R₃可以相同或不同，各自为氢或低级烷基；X为氢、低级烷基、氨基或卤素；Y为氢或低级烷基；及其药学上可接受的盐。 这些化合物可用作降压药，例如，用于治疗高血压和高血压引起的各种疾病，如脑血管疾病、心脏病或肾功能不全。