DMT(-5)Xylf2Me(b)-uracil-1-yl

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: DMT(-5)Xylf2Me(b)-uracil-1-yl
• 英文别名: 1-[(2R,3R,4S,5R)-5-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-4-hydroxy-3-methoxyoxolan-2-yl]pyrimidine-2,4-dione
• 化学式: C₃₁H₃₂N₂O₈
• 分子量: 560.604
• InChiKey: MFDHAVFJDSRPKC-KKAKYAENSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  41
• 可旋转键数：
  10
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  116
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  DMT(-5)Xylf2Me(b)-uracil-1-yl 在 吡啶 、 甲醇 、 sodium methylate 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 反应 39.0h， 生成
  参考文献：
  名称：

  Modified Short Interfering Nucleic Acid (siNA) Molecules and Uses Thereof

  摘要：

  本文披露了包含修饰核苷酸的短干扰核酸（siNA）分子及其用途。siNA分子可以是双链的，并包括从2'-O-甲基核苷酸和2'-氟核苷酸中选择的修饰核苷酸。本文还披露了包含（a）磷酸化阻断剂、共轭基团或5'-稳定端盖；以及（b）短干扰核酸（siNA）的siNA分子。

  公开号：

  US20220177888A1
• 作为产物：
  描述：

  1-((2R,3r,4r,5r)-5-((双(4-甲氧基苯基)(苯基)甲氧基)甲基)-4-羟基-3-甲氧基四氢呋喃-2-基)嘧啶-2,4(1h,3h)-二酮 在 吡啶 、 sodium hydroxide 作用下， 以 四氢呋喃 为溶剂， 反应 23.5h， 生成 DMT(-5)Xylf2Me(b)-uracil-1-yl
  参考文献：
  名称：

  Modified Short Interfering Nucleic Acid (siNA) Molecules and Uses Thereof

  摘要：

  本文披露了包含修饰核苷酸的短干扰核酸（siNA）分子及其用途。siNA分子可以是双链的，并包括从2'-O-甲基核苷酸和2'-氟核苷酸中选择的修饰核苷酸。本文还披露了包含（a）磷酸化阻断剂、共轭基团或5'-稳定端盖；以及（b）短干扰核酸（siNA）的siNA分子。

  公开号：

  US20220177888A1

文献信息

• Phosphoramidite synthones for the synthesis of self-neutralizing oligonucleotide compounds
  申请人：ZATA PHARMACEUTICALS, INC.

  公开号：US10723755B2

  公开（公告）日：2020-07-28

  Compositions and compounds of nucleoside phosphoramidites and modified oligonucleotides, each comprising one or more charge-neutralizing moieties according to the formula V wherein represents the point of attachment to the nucleoside phosphoramidite or the oligonucleotide, optionally through a spacer group. The nucleoside phosphoramidites permit facile attachment of the neutralizing moieties on the backbones of the modified oligonucleotides. The modified oligonucleotides can be used as therapeutic agents (i.e., oligotherapeutics) for the treatment of cancer, autoimmune disorders, genetic diseases, infectious diseases, neurological diseases, inflammatory diseases, metabolic diseases and others.

  核苷磷酸酰胺和修饰的寡核苷酸的组合物和化合物，每种核苷磷酸酰胺和修饰的寡核苷酸都包含一个或多个电荷中和分子，根据式 V 其中表示与核苷磷酰胺或寡核苷酸的连接点，可选择通过间隔基团连接。核苷磷酰胺可以方便地将中和分子附着在修饰寡核苷酸的骨架上。经修饰的寡核苷酸可用作治疗剂（即寡治疗剂），用于治疗癌症、自身免疫性疾病、遗传性疾病、传染性疾病、神经性疾病、炎症性疾病、代谢性疾病等。
• PHOSPHORAMIDITE SYNTHONES FOR THE SYNTHESIS OF SELF-NEUTRALIZING OLIGONUCLEOTIDE COMPOUNDS
  申请人：ZATA PHARMACEUTICALS, INC.

  公开号：US20170320902A1

  公开（公告）日：2017-11-09

  Compositions and compounds having nucleoside phosphoramidites, and methods of making the same are provided. The compounds can also have one or more amino groups that each can be positively charged. The compounds described permit facile attachment of certain neutralizing moieties with positive charges at their terminal ends on the backbones of oligonucleotides. The compounds can be used for the treatment of cancer, autoimmune, genetic and infectious diseases.
• [EN] PNPLA3-TARGETING SHORT INTERFERING RNA (SIRNA) MOLECULES AND USES THEREOF<br/>[FR] MOLÉCULES D'ARN INTERFÉRENT COURT (ARNSI) CIBLANT PNPLA3 ET LEURS UTILISATIONS
  申请人：[en]ALIGOS THERAPEUTICS, INC.

  公开号：WO2023034937A1

  公开（公告）日：2023-03-09

  Disclosed herein are short interfering RNA (siRNA) molecules that downregulate expression of PNPLA3 or variants thereof. The siRNA molecules comprise modified nucleotides and uses thereof. The siRNA molecules may be double stranded and comprise modified nucleotides, such as 2'-O-methyl nucleotides and 2'-fluoro nucleotides, and ligands.
• [EN] MODIFIED SHORT INTERFERING NUCLEIC ACID (SINA) MOLECULES AND USES THEREOF<br/>[FR] MOLÉCULES D'ACIDE NUCLÉIQUE INTERFÉRENT COURT MODIFIÉES (SINA) ET LEURS UTILISATIONS
  申请人：[en]ALIGOS THERAPEUTICS, INC.

  公开号：WO2023039076A1

  公开（公告）日：2023-03-16

  Disclosed herein are short interfering nucleic acid (siNA) molecules comprising modified nucleotides and uses thereof. The siNA molecules may be double stranded and comprise modified nucleotides selected from 2'-O-methyl nucleotides and 2'-fluoro nucleotides. Further disclosed herein are siNA molecules comprising additional modification including a phosphorylation blocker, conjugated moiety, or 5'-stabilized end cap. The siNA molecules may reduce or inhibit the production of hydroxysteroid dehydrogenase.