2'-O-Trifluoroacetylaminopropyl-5'-O-dimethoxytrityl-5-methyl-2-thiouridine | 182495-94-9

• 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: 2'-O-Trifluoroacetylaminopropyl-5'-O-dimethoxytrityl-5-methyl-2-thiouridine
• 英文别名: N-[3-[(2R,3R,4R,5R)-5-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-4-hydroxy-2-(5-methyl-4-oxo-2-sulfanylidenepyrimidin-1-yl)oxolan-3-yl]oxypropyl]-2,2,2-trifluoroacetamide
• CAS: 182495-94-9
• 化学式: C₃₆H₃₈F₃N₃O₈S
• 分子量: 729.774
• InChiKey: JEVFYRNDGPAIAO-PBAMLIMUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  51
• 可旋转键数：
  14
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  160
• 氢给体数：
  3
• 氢受体数：
  12

文献信息

• Process for the synthesis of 2' -O-substituted pyrimidines and oligomeric compounds therefrom
  申请人：ISIS Pharmaceuticals, Inc.

  公开号：US20030050454A1

  公开（公告）日：2003-03-13

  oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2′ and 5′ positions. Monomeric sub-units having these modifications may be further modified at the 2′ position. Improved processes for the synthesis of 2′-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2′-anhydropyrimidine nucleoside or a 2S,2′-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.

  本文披露了含有嘧啶单体亚基的寡核苷酸类似物，其在2'和5'位置进行了修饰。具有这些修饰的单体亚基可以进一步在2'位置进行修饰。还提供了改进的2'-O-取代嘧啶核苷合成过程。该过程采用弱亲核试剂在Lewis酸存在下与2,2'-脱水嘧啶核苷或2S,2'-脱水嘧啶核苷烷基化的方法。
• Oligoribonucleotides and ribonucleases for cleaving RNA
  申请人：——

  公开号：US20030096287A1

  公开（公告）日：2003-05-22

  Oligomeric compounds including oligoribonucleotides and oligoribonucleosides are provided that have subsequences of 2′-pentoribofuranosyl nucleosides that activate dsRNase. The oligoribonucleotides and oligoribonucleosides can include substituent groups for increasing binding affinity to complementary nucleic acid strand as well as substituent groups for increasing nuclease resistance. The oligomeric compounds are useful for diagnostics and other research purposes, for modulating the expression of a protein in organisms, and for the diagnosis, detection and treatment of other conditions susceptible to oligonucleotide therapeutics. Also included in the invention are mammalian ribonucleases, i.e., enzymes that degrade RNA, and substrates for such ribonucleases. Such a ribonuclease is referred to herein as a dsRNase, wherein “ds” indicates the RNase's specificity for certain double-stranded RNA substrates. The artificial substrates for the dsRNases described herein are useful in preparing affinity matrices for purifying mammalian ribonuclease as well as non-degradative RNA-binding proteins.

  提供了包括寡核苷酸和寡核苷的寡聚化合物，其中包含2'-戊糖核苷酸亚序列，可以激活dsRNase。这些寡核苷酸和寡核苷可以包括取代基团，以增加与互补核酸链的结合亲和力，以及取代基团，以增加核酸酶抵抗力。这些寡聚化合物可用于诊断和其他研究目的，用于调节生物体内蛋白质的表达，以及用于诊断、检测和治疗其他易感于寡核苷酸治疗的疾病。本发明还包括哺乳动物核酸酶，即降解RNA的酶，以及这些核酸酶的底物。这样的核酸酶在本文中被称为dsRNase，其中“ds”表示RNase对某些双链RNA底物的特异性。本文所描述的dsRNases的人工底物可用于制备亲和力基质，以纯化哺乳动物核酸酶以及非降解的RNA结合蛋白。
• Processes for the synthesis of 2'-O-substituted pyrimidines and oligomeric compounds therefrom
  申请人：Cook Dan Phillip

  公开号：US20050059815A1

  公开（公告）日：2005-03-17

  Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at eh 2′ and 5′ positions. Monomeric sub-units having these modifications may be further modified at the 2′ position. Improved processes for the synthesis of 2′-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2′-anhydropyrimidine nucleoside or a 2S,2′-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.

  本文揭示了含有嘧啶单体亚基的寡核苷酸类似物，其在2'和5'位置被修饰。具有这些修饰的单体亚基可以在2'位置进一步修饰。还提供了改进的2'-O-取代嘧啶核苷的合成过程。该过程特点是在Lewis酸存在下，使用弱亲核试剂烷基化2,2'-苯并嘧啶核苷或2S,2'-苯并嘧啶核苷。
• Process For The Synthesis Of 2'-O-Substituted Pyrimidines And Oligomeric Compounds Therefrom
  申请人：Cook Dan Phillip

  公开号：US20070232798A1

  公开（公告）日：2007-10-04

  Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2′ and 5′ positions. Monomeric sub-units having these modifications may be further modified at the 2′ position. Improved processes for the synthesis of 2′-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2′-anhydropyrimidine nucleoside or a 2S,2′-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.

  本发明揭示了含有嘧啶单体亚单位的寡核苷酸类似物，其在2'和5'位置进行了修饰。具有这些修饰的单体亚单位可以在2'位置进一步修饰。还提供了改进的合成2'-O-取代嘧啶核苷的过程。该过程的特点是在弱亲核试剂存在下，与Lewis酸一起烷基化2,2'-无水嘧啶核苷或2S,2'-无水嘧啶核苷。
• OLIGORIBONUCLEOTIDES AND RIBONUCLEASES FOR CLEAVING RNA
  申请人：Crooke Stanley T.

  公开号：US20100151458A1

  公开（公告）日：2010-06-17

  Oligomeric compounds including oligoribonucleotides and oligoribonucleosides are provided that have subsequences of 2′-pentoribofuranosyl nucleosides that activate dsRNase. The oligoribonucleotides and oligoribonucleosides can include substituent groups for increasing binding affinity to complementary nucleic acid strand as well as substituent groups for increasing nuclease resistance. The oligomeric compounds are useful for diagnostics and other research purposes, for modulating the expression of a protein in organisms, and for the diagnosis, detection and treatment of other conditions susceptible to oligonucleotide therapeutics. Also included in the invention are mammalian ribonucleases, i.e., enzymes that degrade RNA, and substrates for such ribonucleases. Such a ribonuclease is referred to herein as a dsRNase, wherein “ds” indicates the RNase's specificity for certain double-stranded RNA substrates. The artificial substrates for the dsRNases described herein are useful in preparing affinity matrices for purifying mammalian ribonuclease as well as non-degradative RNA-binding proteins.

  本发明提供了包括寡核苷酸和寡核苷的寡聚化合物，其中包括2'-五糖基核苷酸的亚序列，可激活dsRNase。这些寡核苷酸和寡核苷可以包括取代基团，以增加与互补核酸链的结合亲和力，以及增加核酸酶抵抗力的取代基团。这些寡聚化合物可用于诊断和其他研究目的，用于调节生物体中蛋白质的表达，以及用于诊断、检测和治疗其他易感于寡核苷酸治疗的疾病。本发明还包括哺乳动物核酸酶，即降解RNA的酶，以及这种核酸酶的底物。这种核酸酶在此被称为dsRNase，其中“ds”表示RNase对某些双链RNA底物的特异性。本发明所描述的dsRNase的人工底物可用于制备亲和力基质，以纯化哺乳动物核酸酶以及非降解RNA结合蛋白。