[2-[(2-chloroethoxy)(para-(N,N-dimethylamino)phenyl)phosphoryl]acetyl]hydrazine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: [2-[(2-chloroethoxy)(para-(N,N-dimethylamino)phenyl)phosphoryl]acetyl]hydrazine
• 英文别名: 2-[[4-(dimethylamino)phenyl]-(2-chloroethoxy)phosphoryl]acetohydrazide；2-{[4-(dimethylamino)phenyl](2-chloroethoxy)phosphoryl}acetohydrazide；2-chloroethoxy-para-N-dimethylaminophenylphosphoryl-acetohydrazide；2-chloroethoxy-p-N-dimethylaminophenyl phosphoryl acetohydrazide；CAPAH；2-[2-chloroethoxy-[4-(dimethylamino)phenyl]phosphoryl]acetohydrazide
• 化学式: C₁₂H₁₉ClN₃O₃P
• 分子量: 319.728
• InChiKey: DIZVDQGIOGULHT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  20
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  84.7
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  [2-[(2-chloroethoxy)(para-(N,N-dimethylamino)phenyl)phosphoryl]acetyl]hydrazine 在 sodium tetrahydroborate 作用下， 以 甲醇 、 乙醇 为溶剂， 生成 (N'-Benzyl-hydrazinocarbonylmethyl)-(4-dimethylamino-phenyl)-phosphinic acid 2-chloro-ethyl ester
  参考文献：
  名称：

  摘要：

  DOI：

  10.1023/a:1020872422070

文献信息

• [EN] ARYL IMIDAZOLE COMPOUNDS AND THEIR USE AS BETA AMYLOID PRODUCTION INHIBITORS<br/>[FR] COMPOSÉ ARYLIMIDAZOLE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE PRODUCTION DE LA PROTÉINE AMYLOÏDE BÊTA
  申请人：EISAI R&D MAN CO LTD

  公开号：WO2010098488A1

  公开（公告）日：2010-09-02

  A compound represented by the formula (I): or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a triazolyl group or the like which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by Aβ.

  一种由化学式(I)表示的化合物，或其药理学上可接受的盐或酯，其中环A代表可能被取代的三唑基团或类似物，环B代表可能被取代的苯基团或类似物，X1代表单键或类似物，R1和R2分别代表C1-6烷基或类似物，m代表0到3的整数，n代表0到2的整数，对于由Aβ引起的疾病具有治疗作用。
• MULTI-CYCLIC COMPOUNDS
  申请人：KIMURA Teiji

  公开号：US20090062529A1

  公开（公告）日：2009-03-05

  A compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar 1 represents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Ar 2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, X 1 represents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by Aβ.

  一种由化学式(I)表示的化合物或其药理学可接受的盐，其中Ar1代表可用C1-6烷基基团取代的咪唑基团或类似基团，Ar2代表可用C1-6烷氧基团取代的苯基团或类似基团，X1代表双键或类似基团，Het代表可用C1-6烷基基团或类似基团取代的三唑基团或类似基团，对由Aβ引起的疾病具有治疗或预防作用。
• [EN] IMIDAZOLYLPYRAZINE DERIVATIVES<br/>[FR] DÉRIVÉS D'IMIDAZOLYLPYRAZINE
  申请人：EISAI R&D MAN CO LTD

  公开号：WO2010098495A1

  公开（公告）日：2010-09-02

  To provide a novel low-molecular-weight compound that inhibits the production of amyloid-β (Aβ ). A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein R1 and R2 are the same or different and each represent a substituent selected from the following Substituent Group a1; m represents an integer of 0 to 3; n represents an integer of 0 to 2; X1 represents a single bond or the like; X2 represents a single bond or the like; Ring A represents a five-membered aromatic heterocyclic group or the like which contains two or more nitrogen atoms and may have 1 to 3 substituents selected from the following Substituent Group b1; and Ring B represents a monocyclic or fused cyclic aromatic ring group such as the formula [2] which may have 1 to 3 substituents selected from the following Substituent Group c1, is effective as a therapeutic agent for a disease such as Alzheimer's disease. Substituent Group a1: a C1-6 alkyl group and the like Substituent Group b1: a C1-6 alkyl group and the like Substituent Group c1: an amino group and the like

  提供一种新型低分子量化合物，该化合物能够抑制淀粉样蛋白-β（Aβ）的产生。表示为化学式[I]的化合物，或其药理学上可接受的盐或酯，其中R1和R2相同或不同，每个代表以下取代基团a1中选择的取代基；m代表0到3的整数；n代表0到2的整数；X1代表单键或类似物；X2代表单键或类似物；环A代表含有两个或更多氮原子并且可能具有1到3个取代基团b1中选择的取代基的五元芳香杂环基团或类似物；环B代表可能具有1到3个取代基团c1中选择的取代基的单环或融合环芳香环基团，如化学式[2]所示，对于阿尔茨海默病等疾病具有治疗作用。取代基团a1：C1-6烷基基团等；取代基团b1：C1-6烷基基团等；取代基团c1：氨基团等。
• Synthesis of novel “hybrid” structures based on phosphorylacetic acid hydrazides and sterically hindered phenols
  作者：S. V. Bukharov、Yu. N. Oludina、R. A. Khabibullina、A. R. Burilov、E. L. Gavrilova、I. A. Krutov、R. G. Tagasheva

  DOI：10.1080/10426507.2018.1515205

  日期：2018.12.2

  Abstract The insertion of fragments of sterically hindered phenols into the structure of phosphorylacetic acids hydrazides in their reactions with 3,5-di-tert-butyl-4-hydroxybenzylacetates and sterically hindered 2- and 4-hydroxybenzaldehydes has been carried out. The synthesis of 3,5-di-tert-butyl-4-benzyl derivatives of 5-[(diphenylphosphoryl) methyl]-2,4-dihydro-3H-1,2,4-triazol-3-thiones was also

  摘要 在磷酸酰肼与 3,5-二叔丁基-4-羟基苄基乙酸酯和位阻 2- 和 4- 羟基苯甲醛的反应中，将位阻酚片段插入到磷酸酰肼的结构中。还进行了5-[(二苯基磷酰基)甲基]-2,4-二氢-3H-1,2,4-三唑-3-硫酮的3,5-二-叔丁基-4-苄基衍生物的合成. 图形概要
• Nitrogen-Containing Fused Heterocyclic Compounds and Their use as Beta Amyloid Production Inhibitors
  申请人：Kitazawa Noritaka

  公开号：US20120053171A1

  公开（公告）日：2012-03-01

  A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by Aβ.

  化合物的化学式为[I]，或其药理学上可接受的盐或酯，其中环A代表一个五元芳香杂环基团或类似物，与非芳香环基团融合，可以被取代，环B代表苯基或类似物，可以被取代，X1代表单键或类似物，R1和R2各代表C1-6烷基或类似物，m代表0至3的整数，n代表0至2的整数，该化合物对由Aβ引起的疾病具有治疗作用。