2'-deoxy-5'-O-phthalimido-3'-O-tert-butyl(diphenyl)silyluridine | 161195-72-8

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘧啶核苷
• 英文名称: 2'-deoxy-5'-O-phthalimido-3'-O-tert-butyl(diphenyl)silyluridine
• 英文别名: 2'-deoxy-5'-O-phthalimido-3'-O-(t-butyldiphenylsilyl)uridine；2-[[(2R,3S,5R)-3-[tert-butyl(diphenyl)silyl]oxy-5-(2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy]isoindole-1,3-dione
• CAS: 161195-72-8
• 化学式: C₃₃H₃₃N₃O₇Si
• 分子量: 611.726
• InChiKey: TXBAFEVOOXAENC-YIKNKFAXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.0
• 重原子数：
  44
• 可旋转键数：
  9
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  115
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2′-deoxy-5′-O-phthalimidouridine 生成 2'-deoxy-5'-O-phthalimido-3'-O-tert-butyl(diphenyl)silyluridine
  参考文献：
  名称：

  Modified oligonucleotides

  摘要：

  提供模拟和/或调节野生型核酸活性的新化合物。这些新化合物具有修改的核苷酸间连接，最好用四原子连接基固定取代自然发生的磷酸二酯-5'-亚甲基连接。首选连接具有结构，例如，CH.sub.2 --R.sub.A --NR.sub.1 --CH.sub.2，CH.sub.2 --NR.sub.1 --R.sub.A --CH.sub.2，R.sub.A --NR.sub.1 --CH.sub.2 --CH.sub.2，CH.sub.2 --CH.sub.2 --NR.sub.1 --R.sub.A，CH.sub.2 --CH.sub.2 --R.sub.A --NR.sub.1，或NR.sub.1 --R.sub.A --CH.sub.2 --CH.sub.2，其中R.sub.A为O或NR.sub.2。这些连接是从适当功能化的核苷酸和寡核苷酸制备的。

  公开号：

  US05808023A1

文献信息

• Backbone modified oligonucleotide analogues
  申请人：Isis Pharmaceuticals, Inc.

  公开号：US05610289A1

  公开（公告）日：1997-03-11

  Therapeutic oligonucleotide analogues which have improved nuclease resistance and improved cellular uptake are provided. Replacement of the normal phosphorodiester inter-sugar linkages found in natural oligomers with four atom linking groups forms unique di- and poly- nucleosides and nucleotides useful in regulating RNA expression and in therapeutics. Methods of synthesis and use are also disclosed.

  提供了具有改善核酸酶抗性和细胞摄取能力的治疗性寡核苷酸类似物。用含有四个原子连接基团的连接取代天然寡聚物中发现的正常磷酸二酯间糖连接，形成了用于调节RNA表达和治疗的独特二核苷酸和多核苷酸。还公开了合成和使用方法。
• Backbone modified oligonucleotide analogs and preparation thereof
  申请人：Isis Pharmaceuticals

  公开号：US05386023A1

  公开（公告）日：1995-01-31

  Methods for preparing oligonucleotide analogs which have improved nuclease resistance and improved cellular uptake are provided. In preferred embodiments, the methods involve reductive coupling of 3'- and 4'-substituted or 4'- and 3'-substituted nucleosidic synthons.

  提供了一种制备具有改善核酸酶抗性和细胞摄取能力的寡核苷酸类似物的方法。在优选实施例中，该方法涉及3'-和4'-取代或4'-和3'-取代核苷合成子的还原偶联。
• Backbone modified oligonucleotide analogs
  申请人：ISIS Pharmaceuticals, Inc.

  公开号：US05378825A1

  公开（公告）日：1995-01-03

  Therapeutic oligonucleotide analogs which have improved nuclease resistance and improved cellular uptake are provided. Replacement of the normal phosphorodiester inter-sugar linkages found in wild type oligomers with four atom linking groups forms unique di- and poly- nucleosides and nucleotides useful in regulating RNA expression and in therapeutics. Methods of synthesis and use are also disclosed.

  提供了具有改善核酸酶抗性和细胞摄取能力的治疗性寡核苷酸类似物。用四个原子连接基取代野生型寡聚物中发现的正常磷酸二酯间糖连接，形成独特的二核苷酸和多核苷酸，可用于调节RNA表达和治疗。还公开了合成和使用的方法。
• Modified oligonucleotides
  申请人：ISIS Pharmaceuticals, Inc.

  公开号：US05808023A1

  公开（公告）日：1998-09-15

  Novel compounds that mimic and/or modulate the activity of wild-type nucleic acids are provided. The novel compounds have modified internucleoside linkages which preferably replace naturally-occurring phosphodiester-5'-methylene linkages with four atom linking groups. Preferred linkages have structures such as, for example, CH.sub.2 --R.sub.A --NR.sub.1 --CH.sub.2, CH.sub.2 --NR.sub.1 --R.sub.A --CH.sub.2, R.sub.A --NR.sub.1 --CH.sub.2 --CH.sub.2, CH.sub.2 --CH.sub.2 --NR.sub.1 --R.sub.A, CH.sub.2 --CH.sub.2 --R.sub.A --NR.sub.1, or NR.sub.1 --R.sub.A --CH.sub.2 --CH.sub.2 where R.sub.A is O or NR.sub.2. These linkages are prepared from appropriately functionalized nucleosides and oligonucleotides.

  提供模拟和/或调节野生型核酸活性的新化合物。这些新化合物具有修改的核苷酸间连接，最好用四原子连接基固定取代自然发生的磷酸二酯-5'-亚甲基连接。首选连接具有结构，例如，CH.sub.2 --R.sub.A --NR.sub.1 --CH.sub.2，CH.sub.2 --NR.sub.1 --R.sub.A --CH.sub.2，R.sub.A --NR.sub.1 --CH.sub.2 --CH.sub.2，CH.sub.2 --CH.sub.2 --NR.sub.1 --R.sub.A，CH.sub.2 --CH.sub.2 --R.sub.A --NR.sub.1，或NR.sub.1 --R.sub.A --CH.sub.2 --CH.sub.2，其中R.sub.A为O或NR.sub.2。这些连接是从适当功能化的核苷酸和寡核苷酸制备的。