N-tritylmethoxyamine | 73962-45-5

• 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: N-tritylmethoxyamine
• 英文别名: N-trityl-O-methylhydroxylamine；O-methyl-N-trityl-hydroxylamine；[(Methoxyamino)(diphenyl)methyl]benzene；N-methoxy-1,1,1-triphenylmethanamine
• CAS: 73962-45-5
• 化学式: C₂₀H₁₉NO
• 分子量: 289.377
• InChiKey: ORWISSMNYBXGTE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-tritylmethoxyamine 在 次氯酸叔丁酯 作用下， 生成 N-diphenylmethylene-N-pheylnitrone
  参考文献：
  名称：

  1,2-rearrangement of N-Chloro-N-alkoxyamines in reactions with nucleophiles

  摘要：

  DOI：

  10.1007/bf00955293
• 作为产物：
  描述：

  3-氯苯甲酰乙腈 、 三苯基氯甲烷 在 苯 作用下， 生成 N-tritylmethoxyamine
  参考文献：
  名称：

  MOLECULAR REARRANGEMENT OF TRIPHENYLMETHYLALKOXYAMINES^*

  摘要：

  DOI：

  10.1021/jo01230a003

文献信息

• [EN] S-ANTIGEN TRANSPORT INHIBITING OLIGONUCLEOTIDE POLYMERS AND METHODS<br/>[FR] POLYMÈRES OLIGONUCLÉOTIDIQUES INHIBANT LE TRANSPORT DE L'ANTIGÈNE S ET MÉTHODES
  申请人：ALIGOS THERAPEUTICS INC

  公开号：WO2021119325A1

  公开（公告）日：2021-06-17

  Various embodiments provide STOPS™ polymers that are S-antigen transport inhibiting oligonucleotide polymers, processes for making them and methods of using them to treat diseases and conditions. In some embodiments the STOPS™ modified oligonucleotides include an at least partially phosphorothioated sequence of alternating A and C units having modifications as described herein. The sequence independent antiviral activity against hepatitis B of embodiments of STOPS™ modified oligonucleotides, as determined by HBsAg Secretion Assay, is an EC50 that is less than 100 nM.

  各种实施方式提供了STOPS™聚合物，这些聚合物是S-抗原转运抑制寡核苷酸聚合物，提供了制备它们的方法以及使用它们治疗疾病和症状的方法。在某些实施方式中，STOPS™修饰的寡核苷酸包括至少部分磷硫酸酯化的交替A和C单元序列，具有如本文所述的修饰。通过HBsAg分泌测定确定的STOPS™修饰的寡核苷酸对乙型肝炎的序列无关抗病毒活性，其EC50小于100 nM。
• N-Tritylhydroxylamines: preparations, structures, base strengths, and reactions with nitrous acid and perchloric acid
  作者：Moisés Canle L.、William Clegg、Ibrahim Demirtas、Mark R. J. Elsegood、Johanna Haider、Howard Maskill、Peter C. Miatt

  DOI：10.1039/b103569j

  日期：——

  N-Trityl, N-(4-methoxytrityl), N-(4,4′-dimethoxytrityl), and N-(4,4′,4″-trimethoxytrityl) derivatives of hydroxylamine, O-methylhydroxylamine, and O-benzylhydroxylamine have been prepared and characterised. Additionally, N,O-ditrityl- and N,O-bis(4,4′-dimethoxytrityl)-hydroxylamines have been made, and the X-ray crystal structure of the former has been determined. The pKa value of O-benzylhydroxylammonium in water (6.2) and of its N-trityl analogue in aqueous acetonitrile (7.5) have been measured. The N-tritylhydroxylamines all decompose under aqueous acidic conditions to give the corresponding trityl alcohols, and rate constants for uncatalysed and hydronium ion catalysed reactions of N-(4,4′-dimethoxytrityl)-O-methylhydroxylamine have been measured by stopped flow kinetics at 25 °C. This compound compares in reactivity with N-alkyl-N-(4,4′-dimethoxytrityl)amines rather than with 4,4′-dimethoxytritylamine. Attempted nitrosation of N-tritylhydroxylamine and its O-alkyl derivatives gave trityl alcohol, the intermediate N-nitroso compound being detectable but too unstable to isolate. From N-trityl-O-benzylhydroxylamine, attempted nitrosation led to the formation of triphenylmethane in addition to trityl alcohol, benzyl alcohol, and trityl benzyl ether. The mildly acidic conditions used for attempted nitrosation of methoxy-substituted N-tritylhydroxylamines led to deamination before addition of the nitrosating agent.

  已经制备并表征了羟胺、O-甲基羟胺和O-苄基羟胺的N-三苯甲基、N-(4-甲氧基三苯甲基)、N-(4,4'-二甲氧基三苯甲基)和N-(4,4',4''-三甲氧基三苯甲基)衍生物。此外，还制备了N,O-二三苯甲基和N,O-双(4,4'-二甲氧基三苯甲基)羟胺，并测定了前者的X射线晶体结构。测量了O-苄基羟胺盐在水中(pKa 6.2)及其N-三苯甲基类似物在乙腈水溶液中(pKa 7.5)的pKa值。所有N-三苯甲基羟胺在酸性水溶液条件下均分解生成相应的三苯甲基醇，通过停流动力学在25°C下测量了N-(4,4'-二甲氧基三苯甲基)-O-甲基羟胺的无催化反应和质子催化反应的速率常数。该化合物的反应性介于N-烷基-N-(4,4'-二甲氧基三苯甲基)胺和4,4'-二甲氧基三苯甲基胺之间。试图对N-三苯甲基羟胺及其O-烷基衍生物进行亚硝化反应，生成三苯甲基醇，中间体N-亚硝基化合物可检测到但过于不稳定而无法分离。从N-三苯甲基-O-苄基羟胺出发，试图进行亚硝化反应除了生成三苯甲基醇外，还形成了三苯甲烷、苄醇和三苯甲基苄基醚。对甲氧基取代的N-三苯甲基羟胺试图进行亚硝化反应时的轻微酸性条件，在加入亚硝化试剂之前先发生了脱氨反应。
• Oligomeric compounds for the modulation survivin expression
  申请人：Hansen Bo

  公开号：US20050014712A1

  公开（公告）日：2005-01-20

  Oligonucleotides directed against the survivin gene are provided for modulating the expression of survivin. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the survivin. Methods of using these compounds for modulation of survivin expression and for the treatment of diseases associated with either overexpression of survivin, expression of mutated survivin or both are provided. Examples of diseases are cancer such as lung, breast, colon, prostate, pancreas, lung, liver, thyroid, kidney, brain, testes, stomach, intestine, bowel, spinal cord, sinuses, bladder, urinary tract or ovaries cancers. The oligonucleotides may be composed of deoxyribonucleosides or a nucleic acid analogue such as for example locked nucleic acid or a combination thereof.

  提供针对survivin基因的寡核苷酸，用于调节survivin的表达。这些组合物包括寡核苷酸，特别是针对编码survivin的核酸的反义寡核苷酸。提供使用这些化合物调节survivin表达和治疗与survivin过度表达，表达突变survivin或两者都有关的疾病的方法。疾病的例子是癌症，如肺癌，乳腺癌，结肠癌，前列腺癌，胰腺癌，肝癌，甲状腺癌，肾癌，脑癌，睾丸癌，胃癌，肠道癌，脊髓癌，鼻窦癌，膀胱癌，泌尿道或卵巢癌。寡核苷酸可以由脱氧核糖核苷或核酸类似物组成，例如锁定核酸酸或两者的组合。
• Oligomeric compounds for the modulation of thioredoxin expression
  申请人：Santaris Pharma A/S

  公开号：US20040241717A1

  公开（公告）日：2004-12-02

  Oligonucleotides directed against the TRX gene are provided for modulating the expression of TRX. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the TRX. Methods of using these compounds for modulation of TRX expression and for the treatment of diseases associated with either overexpression of TRX, expression of mutated TRX or both are provided. Examples of diseases are cancer such as lung, breast, colon, prostate, pancreas, lung, liver, thyroid, kidney, brain, testes, stomach, intestine, bowel, spinal cord, sinuses, bladder, urinary tract or ovaries cancers. The oligonucleotides may be composed of deoxyribonucleosides or a nucleic acid analogue such as for example locked nucleic acid or a combination thereof.

  提供针对TRX基因的寡核苷酸，用于调节TRX的表达。这些组合物包括寡核苷酸，特别是针对编码TRX的核酸的反义寡核苷酸。提供了使用这些化合物调节TRX表达和治疗与TRX过度表达、突变TRX表达或两者都相关的疾病的方法。疾病的例子包括肺癌、乳腺癌、结肠癌、前列腺癌、胰腺癌、肝癌、甲状腺癌、肾癌、脑癌、睾丸癌、胃癌、肠癌、脊髓癌、鼻窦癌、膀胱癌、泌尿道癌或卵巢癌等。这些寡核苷酸可以由脱氧核苷酸或核酸类似物组成，例如锁定核酸或二者的组合。
• Oligomeric compounds for the modulation of ras expression
  申请人：Santaris Pharma A/S

  公开号：US20040248840A1

  公开（公告）日：2004-12-09

  Oligonucleotides directed against the Ha-ras gene are provided for modulating the expression of Ha-ras. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the Ha-ras. Methods of using these compounds for modulation of Ha-ras expression and for the treatment of diseases associated with either overexpression of Ha-ras, expression of mutated Ha-ras or both are provided. Examples of diseases are cancer such as lung, breast, colon, prostate, pancreas, lung, liver, thyroid, kidney, brain, testes, stomach, intestine, bowel, spinal cord, sinuses, bladder, urinary tract or ovaries cancers. The oligonucleotides may be composed of deoxyribonucleosides or a nucleic acid analogue such as for example locked nucleic acid or a combination thereof.

  提供了针对Ha-ras基因的寡核苷酸，用于调节Ha-ras的表达。该组成物包括针对编码Ha-ras的核酸的寡核苷酸，特别是反义寡核苷酸。提供了使用这些化合物调节Ha-ras表达和治疗与Ha-ras过度表达、突变Ha-ras表达或两者都有关的疾病的方法。疾病的例子包括肺癌、乳腺癌、结肠癌、前列腺癌、胰腺癌、肝癌、甲状腺癌、肾癌、脑癌、睾丸癌、胃癌、肠癌、脊髓癌、鼻窦癌、膀胱癌、泌尿道癌或卵巢癌。寡核苷酸可以由脱氧核苷酸或核酸类似物组成，例如锁定核酸或两者的组合。