1-trifluoroacetyl-4-trityl piperazine | 914361-73-2

• 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-trifluoroacetyl-4-trityl piperazine
• 英文别名: 1-trifluoroacetyl-4-tritylpiperazine；2,2,2-Trifluoro-1-[4-(triphenylmethyl)piperazin-1-yl]ethan-1-one；2,2,2-trifluoro-1-(4-tritylpiperazin-1-yl)ethanone
• CAS: 914361-73-2
• 化学式: C₂₅H₂₃F₃N₂O
• 分子量: 424.466
• InChiKey: RAZUQNZLWPEIIC-UHFFFAOYSA-N

物化性质

• 沸点：
  516.4±50.0 °C(Predicted)
• 密度：
  1.242±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  23.6
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  1-trifluoroacetyl-4-trityl piperazine 在 盐酸 作用下， 以 乙醚 、 二氯甲烷 为溶剂， 反应 4.0h， 以95%的产率得到2,2,2-三氟-1-(1-哌嗪基)乙酮盐酸盐(1:1)
  参考文献：
  名称：

  WO2006/121951

  摘要：

  公开号：
• 作为产物：
  描述：

  三氟乙酸乙酯 生成 1-trifluoroacetyl-4-trityl piperazine
  参考文献：
  名称：

  ANTISENSE MODULATION OF NUCLEAR HORMONE RECEPTORS

  摘要：

  提供了针对和调节核激素受体（NHRs）如糖皮质激素受体（GR）的反义寡核苷酸和其他药剂，包括这些药剂的组合物以及使用方法。

  公开号：

  US20110224283A1

文献信息

• Kinase inhibitor scaffolds and methods for their preparation
  申请人：IRM LLC, a Delaware Limited Liability Company

  公开号：US20030191312A1

  公开（公告）日：2003-10-09

  General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.

  已经展示了解决各种取代杂环烷基的溶液相和固相合成的一般方法。这些取代杂环烷基可以通过在高温下与胺发生芳香取代，或者通过钯催化的交叉偶联反应与苯胺、硼酸和酚进一步扩展。
• ANTISENSE ANTIVIRAL COMPOUND AND METHOD FOR TREATING INFLUENZA VIRAL INFECTION
  申请人：Iversen Patrick L.

  公开号：US20110118334A1

  公开（公告）日：2011-05-19

  The present invention relates to antisense antiviral compounds and methods of their use and production in inhibition of growth of viruses of the Orthomyxoviridae family and in the treatment of a viral infection. The compounds are particularly useful in the treatment of influenza virus infection in a mammal. Exemplary antisense antiviral compounds are substantially uncharged, or partially positively charged, morpholino oligonucleotides having 1) a nuclease resistant backbone, 2) 12-40 nucleotide bases, and 3) a targeting sequence of at least 12 bases in length that hybridizes to a target region selected from the following: a) the 5′ or 3′ terminal 25 bases of the negative sense viral RNA segment of Influenzavirus A, Influenzavirus B and Influenzavirus C; b) the terminal 30 bases of the 5′ or 3′ terminus of the positive sense vcRNA; c) the 45 bases surrounding the AUG start codon of an influenza viral mRNA and; d) 50 bases surrounding the splice donor or acceptor sites of influenza mRNAs subject to alternative splicing.

  本发明涉及反义抗病毒化合物及其使用和生产方法，用于抑制Orthomyxoviridae家族病毒的生长和治疗病毒感染。这些化合物特别适用于哺乳动物流感病毒感染的治疗。示例性的反义抗病毒化合物是具有以下特征的基本无电荷或部分正电荷的morpholino寡核苷酸：1）核酸酶耐受性骨架，2）12-40个核苷酸碱基，以及3）至少12个碱基的靶向序列，该序列与以下选定的目标区域杂交：a）Influenzavirus A，Influenzavirus B和Influenzavirus C负义病毒RNA片段的5'或3'端25个碱基; b）正义vcRNA的5'或3'端30个碱基；c）流感病毒mRNA的AUG起始密码子周围的45个碱基和；d）流感病毒mRNA的可选择剪接的剪接供体或受体位点周围的50个碱基。
• Antibacterial antisense oligonucleotide and method
  申请人：Weller Dwight D.

  公开号：US20080194463A1

  公开（公告）日：2008-08-14

  A method for enhancing, by at least 10 fold, the antibacterial activity of an antisense oligonucleotide composed of morpholino subunits linked by phosphorus-containing intersubunit linkages. The method includes one or both of: conjugating an arginine-rich carrier to a 3′ or 5′ end of the oligonucleotide and modifying the oligonucleotide to contain 20%-50% intersubunit linkages that are positively charged at physiological pH. Also disclosed is an antisense oligonucleotide having enhanced antibacterial activity by virtue of one or both modifications.

  一种增强抗菌活性的反义寡核苷酸方法，其由磷含量的亚单位连接的morpholino亚单位组成，至少增强了10倍的抗菌活性。该方法包括以下一项或两项：将富含精氨酸的载体与寡核苷酸的3'或5'端结合，并修改寡核苷酸，使其在生理pH下含有20％-50％的亚单位连接具有正电荷。此外，还披露了一种由于一项或两项修改而具有增强抗菌活性的反义寡核苷酸。
• 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。
• Antisense antiviral compounds and methods for treating foot and mouth disease
  申请人：Rieder E. Aida

  公开号：US20060293268A1

  公开（公告）日：2006-12-28

  An antiviral antisense composition and method for treating foot-and-mouth disease virus (FMDV) in veterinary animals is disclosed. The composition contains an antisense compound that has a sequence effective to target at least 12 contiguous bases of an FMDV RNA sequence within a region of the positive-strand genomic RNA defined by SEQ ID NO: 25, and preferably, one of the viral sequences within SEQ ID NO:25 identified by SEQ ID NOS: 26-28. The composition is administered in a therapeutically effective amount in treating FMDV.

  本发明公开了一种抗病毒反义组合物及其治疗兽医动物口蹄疫病毒（FMDV）的方法。该组合物含有一个反义化合物，其序列能够有效地靶向FMDV RNA序列中至少12个连续碱基，该RNA序列位于由SEQ ID NO: 25定义的正链基因组RNA的区域内，而且最好是在SEQ ID NOS: 26-28所确定的其中一个病毒序列中。该组合物以治疗性有效剂量给予，以治疗FMDV。