[4-(Trifluoroacetyl)piperazin-1-yl]phosphonic dichloride | 914361-74-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: [4-(Trifluoroacetyl)piperazin-1-yl]phosphonic dichloride
• 英文别名: 1-(4-dichlorophosphorylpiperazin-1-yl)-2,2,2-trifluoroethanone
• CAS: 914361-74-3
• 化学式: C₆H₈Cl₂F₃N₂O₂P
• 分子量: 299.017
• InChiKey: MXNASHSZUXNRBC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  40.6
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  [4-(Trifluoroacetyl)piperazin-1-yl]phosphonic dichloride 、 1-[(2R,6S)-6-(羟基甲基)-4-(三苯基甲基)-2-吗啉基]-5-甲基-2,4(1H,3H)-嘧啶二酮 在 N-甲基咪唑 、 2,6-二甲基吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 6.0h， 以71%的产率得到((2S,6R)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-tritylmorpholin-2-yl)methyl (4-(2,2,2-trifluoroacetyl)piperazin-1-yl)phosphonochloridate
  参考文献：
  名称：

  WO2006/121951

  摘要：

  公开号：
• 作为产物：
  描述：

  2,2,2-三氟-1-(1-哌嗪基)乙酮盐酸盐(1:1) 在 N,N-二异丙基乙胺 、 三氯氧磷 作用下， 以 甲苯 为溶剂， 反应 4.0h， 以50%的产率得到[4-(Trifluoroacetyl)piperazin-1-yl]phosphonic dichloride
  参考文献：
  名称：

  WO2006/121951

  摘要：

  公开号：

文献信息

• ANTISENSE COMPOSITION AND METHOD FOR INHIBITION OF miRNA BIOGENESIS
  申请人：Rasko John E. J.

  公开号：US20080199961A1

  公开（公告）日：2008-08-21

  The present disclosure relates to compounds and methods for inhibiting the formation of miRNAs that inhibit translation of one or more identified proteins. The compounds comprise antisense oligonucleotides targeting the pri-miRNA precursor of miRNAs.

  本公开涉及抑制miRNA形成的化合物和方法，以抑制对一个或多个已确定的蛋白质的翻译有抑制作用的miRNAs的形成。该化合物包括针对miRNA的pri-miRNA前体的反义寡核苷酸。
• Oligonucleotide compound and method for treating nidovirus infections
  申请人：Stein A. David

  公开号：US20070037763A1

  公开（公告）日：2007-02-15

  A method and oligonucleotide compound for inhibiting replication of a nidovirus in virus-infected animal cells are disclosed. The compound (i) has a nuclease-resistant backbone, (ii) is capable of uptake by the infected cells, (iii) contains between 8-25 nucleotide bases, and (iv) has a sequence capable of disrupting base pairing between the transcriptional regulatory sequences in the 5′ leader region of the positive-strand viral genome and negative-strand 3′ subgenomic region. In practicing the method, infected cells are exposed to the compound in an amount effective to inhibit viral replication.
• Antisense antiviral compound and method for treating picornavirus infection
  申请人：Stein A. David

  公开号：US20070066556A1

  公开（公告）日：2007-03-22

  The invention provides antisense antiviral compounds and methods of their use and production in inhibition of growth of viruses of the Picornaviridae family and in the treatment of a viral infection. The compounds are particularly useful in the treatment of Enterovirus and/or Rhinovirus infection in a mammal. The antisense antiviral compounds are substantially uncharged, morpholino oligonucleotides have a sequence of 12-40 subunits, including at least 12 subunits having a targeting sequence that is complementary to a region associated with viral RNA sequences within a 32 nucleotide region of the viral 5′ untranslated region identified by SEQ ID NO:7.
• Antisense composition and method for treating muscle atrophy
  申请人：Iversen L. Patrick

  公开号：US20070122821A1

  公开（公告）日：2007-05-31

  A method and compound for treating skeletal muscle mass deficiency in a human subject are disclosed. The composition is an oligomer of morpholino subunits and phosphorus-containing intersubunit linkages joining a morpholino nitrogen of one subunit to a 5′ exocyclic carbon of an adjacent subunit, contains between 10-40 nucleotide bases, has a base sequence effective to hybridize to an expression-sensitive region of processed or preprocessed human myostatin RNA transcript, identified, in its processed form, by SEQ ID NO:6, and is capable of uptake by target muscle cells in the subject. In practicing the method, the compound is administered in an amount and at a dosage schedule to produce an overall reduction in the level of serum myostatin measured in the patient, and preferably to bring the myostatin level within the a range determined for normal, healthy individuals.
• Immunosuppression compound and treatment method
  申请人：Mourich V. Dan

  公开号：US20070111962A1

  公开（公告）日：2007-05-17

  A method and compound for suppressing an immune response in a mammalian subject, for the treatment or prevention of an autoimmune condition or transplantation rejection are disclosed. The compound is an antisense oligonucleotide analog compound having a targeting sequence complementary to a preprocessed CTLA-4 mRNA region identified by SEQ ID NO: 1, spanning the splice junction between intron 1 and exon 2 of the preprocessed mRNA of the subject. The compound is effective, when administered to a subject, to form within host cells, a heteroduplex structure (i) composed of the preprocessed CTLA-4 mRNA and the oligonucleotide compound, (ii) characterized by a Tm of dissociation of at least 45° C., and (iii) resulting in an increased ratio of processed mRNA encoding ligand-independent CTLA-4 to processed mRNA encoding full-length CTLA-4.