1-(6-(Hydroxymethyl)-4-tritylmorpholin-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione | 1265140-28-0

• 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: 1-(6-(Hydroxymethyl)-4-tritylmorpholin-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione
• 英文别名: 1-[6-(hydroxymethyl)-4-tritylmorpholin-2-yl]-5-methylpyrimidine-2,4-dione
• CAS: 1265140-28-0
• 化学式: C₂₉H₂₉N₃O₄
• 分子量: 483.567
• InChiKey: SINOYLIIFJJPCM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  36
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  82.1
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  1-(6-(Hydroxymethyl)-4-tritylmorpholin-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione 在 2,6-二甲基吡啶 、 三氯氧磷 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 生成 phosphodichloridate
  参考文献：
  名称：

  FUNCTIONALLY-MODIFIED OLIGONUCLEOTIDES AND SUBUNITS THEREOF

  摘要：

  提供了包含修改的亚单位间连接和/或修改的3'和/或5'-末端基团的功能修饰寡核苷酸类似物。所公开的化合物对于治疗需要抑制蛋白质表达或纠正异常mRNA剪接产物以产生有益治疗效果的疾病是有用的。

  公开号：

  US20140330006A1

文献信息

• Synthesis of phosphorodiamidate morpholino oligonucleotides by H-phosphonate method
  作者：Jhuma Bhadra、Jayanta Kundu、Keshab Ch. Ghosh、Surajit Sinha

  DOI：10.1016/j.tetlet.2015.05.080

  日期：2015.7

  Synthesis of T-containing phosphorodiamidate morpholino oligomers (PMO) by H-phosphonate method on solid support has been reported for the first time. Initially, 5-mer then 15-mer of T-containing PMO using H-phosphonate-T monomer was synthesized on polystyrene resin bead. The phosphonamidate backbone was oxidized by iodine–dimethylamine mixture followed by the cleavage from solid support by aqueous

  首次报道了在固体载体上通过H-膦酸酯方法合成含T的二氨基磷酸二酰胺吗啉代低聚物（PMO）。最初，在聚苯乙烯树脂珠上合成了使用H-膦酸酯-T单体的5聚体然后15聚体的含T PMO。碘化二甲胺混合物将膦酰胺的骨架氧化，然后用氨水从固相载体上裂解，得到含15-mer T的PMO。
• OLIGONUCLEOTIDE ANALOGUES HAVING MODIFIED INTERSUBUNIT LINKAGES AND/OR TERMINAL GROUPS
  申请人：Hanson Gunnar J.

  公开号：US20120065169A1

  公开（公告）日：2012-03-15

  Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.

  提供了包含修改的亚单位连接和/或修改的3'和/或5'-末端基团的寡核苷酸类似物。所披露的化合物对于治疗需要抑制蛋白质表达或纠正异常mRNA剪接产物以产生有益治疗效果的疾病非常有用。
• PEPTIDE OLIGONUCLEOTIDE CONJUGATES
  申请人：Hanson Gunnar J.

  公开号：US20120289457A1

  公开（公告）日：2012-11-15

  Oligonucleotide analogues conjugated to carrier peptides are provided. The disclosed compounds are useful for the treatment of various diseases, for example diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.

  提供了与载体肽共轭的寡核苷酸类似物。所公开的化合物可用于治疗各种疾病，例如抑制蛋白质表达或校正异常的mRNA剪接产物可产生有益的治疗效果的疾病。
• OLIGONUCLEOTIDES FOR TREATING EXPANDED REPEAT DISEASES
  申请人：Sarepta Therapeutics, Inc.

  公开号：US20140303238A1

  公开（公告）日：2014-10-09

  The invention provides for a method for selectively reducing the expression of a mutant mRNA and/or protein having an expanded nucleotide repeat relative to a wild-type mRNA, comprising contacting a cell with an antisense oligonucleotide of sufficient length and complementarity to the expanded nucleotide repeat. More particularly it relates to selectively reducing the expression of mutant Huntington protein associated with Huntington's disease. The antisense oligonucleotide comprising either a nucleotide or a repeated three nucleotide sequence as defined in the claims.

  该发明提供了一种选择性减少具有扩展核苷酸重复相对于野生型mRNA的突变型mRNA和/或蛋白质表达的方法，包括将长度和互补性足够的反义寡核苷酸与细胞接触。更具体地，它涉及选择性减少与亨廷顿病相关的突变亨廷顿蛋白的表达。反义寡核苷酸包括在权利要求中定义的核苷酸或重复的三核苷酸序列。
• INDUCED EXON INCLUSION IN SPINAL MUSCLE ATROPHY
  申请人：Sarepta Therapeutics, Inc.

  公开号：US20140329772A1

  公开（公告）日：2014-11-06

  The invention relates to the use of an antisense compound for inducing exon inclusion as a treatment for Spinal Muscle Atrophy (SMA). More particularly it relates to inducing inclusion of exon 7 to restore levels of Survival Motor Neuron (SMN) protein encoded by the Survival Motor Neuron (SMN) gene.

  本发明涉及使用反义化合物作为诱导外显子包含的治疗脊髓肌肉萎缩症（SMA）的方法。更具体地，它涉及诱导包含外显子7以恢复由Survival Motor Neuron（SMN）基因编码的Survival Motor Neuron（SMN）蛋白质水平。