[1-[(diphenylmethyl)amino]-2-phenylethyl]phosphinic acid | 65577-31-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: [1-[(diphenylmethyl)amino]-2-phenylethyl]phosphinic acid
• 英文别名: (1-(benzhydrylamino)-2-phenylethyl)phosphinic acid；[1-(benzhydryl-amino)-2-phenyl-ethyl]-phosphinic acid；1-(benzhydrylamino)-2-phenylethylphosphinic acid
• CAS: 65577-31-3
• 化学式: C₂₁H₂₂NO₂P
• 分子量: 351.385
• InChiKey: GEPPLBMHKLSXDF-UHFFFAOYSA-N

物化性质

• 沸点：
  535.7±60.0 °C(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  25.0
• 可旋转键数：
  7.0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  49.33
• 氢给体数：
  2.0
• 氢受体数：
  2.0

反应信息

• 作为反应物：
  描述：

  [1-[(diphenylmethyl)amino]-2-phenylethyl]phosphinic acid 在 R(+)-alpha-甲基苄胺 、 氢溴酸 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 、 六甲基二硅氮烷 、 sodium hydroxide 作用下， 以 甲醇 、 乙醇 、 二氯甲烷 、 水 为溶剂， 反应 90.67h， 生成 (2-benzyl-3-(((R)-1-(((benzyloxy)carbonyl)amino)-2-phenylethyl)(hydroxy)phosphoryl)propanoyl)-L-alanine
  参考文献：
  名称：

  Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration

  摘要：

  Lamin A contributes to the structure of nuclei in all mammalian cells and plays an important role in cell division and migration. Mature lamin A is derived from a farnesylated precursor protein, known as prelamin A, which undergoes post-translational cleavage catalyzed by the zinc metalloprotease STE24 (ZPMSTE24). Accumulation of farnesylated prelamin A in the nuclear envelope compromises cell division, impairs mitosis and induces an increased expression of inflammatory gene products. ZMPSTE24 has been proposed as a potential therapeutic target in oncology. A library of peptidomimetic compounds were synthesized and screened for their ability to induce accumulation of prelamin A in cancer cells and block cell migration in pancreatic ductal adenocarcinoma cells. The results of this study suggest that inhibitors of lamin A maturation may interfere with cell migration, the biological process required for cancer metastasis.

  DOI：

  10.1016/j.bmc.2018.10.001
• 作为产物：
  描述：

  benzylmethylidenediphenylmethylamine 在 乙醇 作用下， 以 苯 为溶剂， 生成 [1-[(diphenylmethyl)amino]-2-phenylethyl]phosphinic acid
  参考文献：
  名称：

  A New Synthetic Route to 1-Aminoalkylphosphonous Acids

  摘要：

  将双（三甲基硅基）亚磷酸加到 N-（二苯基甲基）亚胺 1 中，可得到双（三甲基硅基）1-（二苯基甲基氨基）烷基膦酸 2，用水性醇处理后，可轻松将其转化为 1-（二苯基甲基氨基）烷基膦酸 3。

  DOI：

  10.1055/s-1987-28133

文献信息

• Phosphinic Amino Acid Compounds
  申请人：Dive Vincent

  公开号：US20080153890A1

  公开（公告）日：2008-06-26

  Compounds of formula (I): wherein: R 1 represents hydrogen, alkylcarbonyloxyalkyl or alkylcarbonylthioalkyl, R 2 represents hydrogen, alkylcarbonyloxyalkyl, arylcarbonylthioalkyl or optionally substituted arylalkyl, R 3 represents phenyl, which is optionally substituted, or indolyl, their isomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful in the treatment of arterial hypertension and complications thereof.

  式(I)的化合物：其中：R1代表氢、烷基羰基氧烷基或烷基羰基硫烷基，R2代表氢、烷基羰基氧烷基、芳基羰基硫烷基或可选择取代的芳基烷基，R3代表苯基（可选择取代）或吲哚基，它们的异构体以及与药学上可接受的酸或碱形成的加合物。含有这些化合物的药物，用于治疗动脉高血压及其并发症。
• (&agr;-aminophosphino) peptide derivatives, method for making same and therapeutic applications thereof
  申请人：Institut National de la Sante et de la Recherche Medicale (Inserm)

  公开号：US06518260B1

  公开（公告）日：2003-02-11

  The invention concerns compounds derived from (&agr;-aminophosphino) peptides, of general formula (I), in which R1 and R2 each represents a hydrogen atom or taken together form an imine with the adjacent nitrogen atom; R3 represents an alkyl group, an alkenyl group, a phenyl group, a benzyl group, all these groups capable of being substituted or not, a hydrogen atom, a cycloalkyl group, a cycloalkylmethyl group or finally, a methyl group substituted by a heterocyclic, aromatic or saturated group; R4 represents a phenyl group, a benzyl group, these groups capable of being substituted or not, a hydrogen atom, an alkyl group, analkenyl group or a cycloalkyl group; R5 represents an alkyl group, an alkenyl group, a phenyl group, a benzyl group, all these groups capable of being substituted or not, a hydrogen atom, a cycloalkyl, cycloalkylmethyl group or finally a methyl group substituted by a heterocyclic, aromatic or saturated group; R6, R7 and R8 can in particular represent a hydrogen atom, an alkyl group, a phenyl group substituted or not . . . n is equal to 0 or 1, in the form of enantiomers, diastereoisomers or racemic mixtures, their salts, their method of preparation and their therapeutic applications.

  本发明涉及由(&agr;-氨基膦)肽衍生的化合物，通式为(I)，其中R1和R2分别表示氢原子或与相邻氮原子形成亚胺基; R3表示烷基、烯基、苯基、苄基，所有这些基团都可以被取代或不被取代，氢原子、环烷基、环烷基甲基或最后，被杂环、芳香或饱和基团取代的甲基基团; R4表示苯基、苄基，这些基团可以被取代或不被取代，氢原子、烷基、烯基或环烷基; R5表示烷基、烯基、苯基、苄基，所有这些基团都可以被取代或不被取代，氢原子、环烷基、环烷基甲基或最后，被杂环、芳香或饱和基团取代的甲基基团; R6、R7和R8特别可以表示氢原子、烷基、取代或不取代的苯基......n等于0或1，以对映异构体、顺异构体或混合物的形式存在，它们的盐、制备方法及其治疗应用。
• Phosphinic amino acid compounds
  申请人：Les Laboratoires Servier

  公开号：US07521469B2

  公开（公告）日：2009-04-21

  Compounds of formula (I): wherein: R1 represents hydrogen, alkylcarbonyloxyalkyl or alkylcarbonylthioalkyl, R2 represents hydrogen, alkylcarbonyloxyalkyl, arylcarbonylthioalkyl or optionally substituted arylalkyl, R3 represents phenyl, which is optionally substituted, or indolyl, their isomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful in the treatment of arterial hypertension and complications thereof.

  式(I)的化合物：其中：R1代表氢、烷基羰基氧烷基或烷基羰基硫烷基，R2代表氢、烷基羰基氧烷基、芳基羰基硫烷基或可选地取代的芳基烷基，R3代表苯基，可选地取代，或吲哚基，它们的异构体和与药学上可接受的酸或碱的加合物。含有这些化合物的药物产品在治疗动脉高血压及其并发症方面有用。
• Baylis, E. Keith; Campbell, Colin D.; Dingwall, John G., Journal of the Chemical Society. Perkin transactions I, 1984, p. 2845 - 2853
  作者：Baylis, E. Keith、Campbell, Colin D.、Dingwall, John G.

  DOI：——

  日期：——
• DE2722162
  申请人：——

  公开号：——

  公开（公告）日：——