N'-[3-(乙胺基)丙基]丁烷-1,4-二胺 | 110539-43-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: N'-[3-(乙胺基)丙基]丁烷-1,4-二胺
• 英文名称: N1-(3-ethylaminopropyl)butane-1,4-diamine
• 英文别名: EtSPD；1,4-Butanediamine, N-[3-(ethylamino)propyl]-；N'-[3-(ethylamino)propyl]butane-1,4-diamine
• CAS: 110539-43-0
• 化学式: C₉H₂₃N₃
• 分子量: 173.302
• InChiKey: VNRFKJPUPRCQEV-UHFFFAOYSA-N

物化性质

• 熔点：
  >298 °C (decomp)(Solv: ethanol (64-17-5); ethyl acetate (141-78-6); water (7732-18-5))
• 沸点：
  271.2±8.0 °C(Predicted)
• 密度：
  0.873±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  12
• 可旋转键数：
  9
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  50.1
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  3-[4-(Trityl-amino)-butyrylamino]-propionic acid 2,5-dioxo-pyrrolidin-1-yl ester 在 三乙胺 、 三氟乙酸 作用下， 以 二氯甲烷 、 氯仿 、 N,N-二甲基甲酰胺 为溶剂， 反应 52.42h， 生成 N'-[3-(乙胺基)丙基]丁烷-1,4-二胺
  参考文献：
  名称：

  N-烷基化亚精胺片段和精胺生物碱苦瓜胺A类似物的简单合成

  摘要：

  通过琥珀酰亚胺基N-三苯甲基-β-丙氨酸酯与三甲基甲硅烷基γ-氨基丁酸酯的偶合可容易地将琥珀酰胺化N-三苯甲基-β-丙氨酰基-γ-氨基丁酸酯和N-三苯甲基-γ-氨基丁酰基-β-丙氨酸酰化各种胺用N-三苯甲基-γ-氨基丁酸和β-丙氨酸甲酯分别还原，然后用LiAlH 4还原，生成N-单烷基化亚精胺片段和精胺生物碱kukoamine A的类似物。该方法在固相上的适用性也是演示。

  DOI：

  10.1016/s0040-4039(00)02308-x

文献信息

• [EN] PHARMACEUTICAL OR COSMETIC COMPOSITION FOR TREATING ALOPECIA<br/>[FR] COMPOSITION PHARMACEUTIQUE OU COSMÉTIQUE DESTINÉE AU TRAITEMENT DE L'ALOPÉCIE
  申请人：GIULIANI SPA

  公开号：WO2014016407A1

  公开（公告）日：2014-01-30

  The present invention relates to a cosmetic or pharmaceutical composition for treating alopecia, and in general for counteracting excessive hair loss, comprising as an active ingredient a compound of formula (I) R-N1-spermidine, or 1,4-butanediamine,N-(3-aminopropyl)-N1-R. The compounds of general formula (I) are active in accordance with the objects of the present invention, and also sufficiently stable to allow effective application for topical use on the scalp without potentially being transformed into a different substance, which is no longer active, as a result of oxidation.

  本发明涉及一种用于治疗脱发，通常用于对抗过度脱发的化妆品或药用组合物，其活性成分为化合物R-N1-精胺，或1,4-丁二胺，N-(3-氨丙基)-N1-R的化合物。根据本发明的目的，通用式(I)的化合物是活性的，同时也足够稳定，可以有效地应用于头皮表面，而不会因为氧化而转化为不再活性的不同物质。
• PHARMACEUTICAL OR COSMETIC COMPOSITION FOR TREATING ALOPECIA
  申请人：GIULIANI S.P.A.

  公开号：US20150202132A1

  公开（公告）日：2015-07-23

  The present invention relates to a cosmetic or pharmaceutical composition for treating alopecia, and in general for counteracting excessive hair loss, comprising as an active ingredient a compound of formula (I) R—N 1 -spermidine, or 1,4-butane-diamine,N-(3-aminopropyl)-N 1 —R. The compounds of general formula (I) are active in accordance with the objects of the present invention, and also sufficiently stable to allow effective application for topical use on the scalp without potentially being transformed into a different substance, which is no longer active, as a result of oxidation.

  本发明涉及一种用于治疗脱发的化妆品或药用组合物，一般用于对抗过度脱发，包括作为活性成分的化合物，其化学式为(I) R—N1-精胺，或1,4-丁二胺，N-(3-氨基丙基)-N1-R。根据本发明的目的，一般式(I)的化合物是活性的，同时也足够稳定，可以在头皮上有效应用于局部使用，而不会由于氧化而可能转化为不再活性的不同物质。
• [EN] NOVEL POLYAMINE ANALOG CONJUGATES AND QUINONE CONJUGATES AS THERAPIES FOR CANCERS AND PROSTATE DISEASES<br/>[FR] NOUVEAUX CONJUGUES D'ANALOGUE DE POLYAMINE ET CONJUGUES DE QUINONE, UTILISES POUR LE TRAITEMENT DE CANCERS ET DE MALADIES DE LA PROSTATE
  申请人：SLIL BIOMEDICAL CORP

  公开号：WO2000066175A2

  公开（公告）日：2000-11-09

  Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.

  提供一种肽共轭物，其中将细胞毒性和细胞增殖抑制剂，如多胺类似物或萘醌类化合物，与多肽共轭，该多肽可以被酶如前列腺特异性抗原（PSA）和半胱氨酸蛋白酶B识别和剪切，以及包含这些共轭物的组合物。还提供了使用这些共轭物治疗前列腺疾病的方法。
• Biologically active spermidine analogues, pharmaceutical compositions and methods of treatment
  申请人：——

  公开号：US20020045780A1

  公开（公告）日：2002-04-18

  Polyamines having the formula: 1 or a salt thereof with a pharmaceutically acceptable acid wherein: R 1 -R 5 may be the same or different and are alkyl, aryl, aryl alkyl, cycloalkyl or hydrogen; at least one of R 1 and R 2 and at least one of R 4 and R 5 are not hydrogen, and any of the alkyl chains may optionally be interrupted by at least one etheric oxygen atom, excluding N 1 ,N 3 -diethylspermidine and N 1 ,N 3 -dipropylspermidine; and A and B are bridging groups which effectively maintain the distance between the nitrogen atoms such that the polyamine: (i) is capable of uptake by a target cell upon administration of the polyamine to a human or non-human animal; and (ii) upon uptake by the target cell, competitively binds via an electrostatic interaction between the positively charged nitrogen atoms to substantially the same biological counter-anions as the intracellular natural polyamines in the target cell.

  具有以下公式1或其药学上可接受的酸盐的多胺，其中：R1-R5可以相同或不同，且为烷基，芳基，芳基烷基，环烷基或氢；R1和R2中至少有一个，以及R4和R5中至少有一个不是氢，任何烷基链都可以选择性地被至少一个醚氧原子中断，但不包括N1，N3-二乙基亚精胺和N1，N3-二丙基亚精胺；A和B是桥接基团，有效地保持氮原子之间的距离，使得多胺：（i）在将多胺用于人类或非人类动物的治疗时，能够被目标细胞吸收；（ii）在被目标细胞吸收后，通过正电荷氮原子之间的静电相互作用与目标细胞中的细胞内天然多胺基本相同地竞争性结合生物计数离子。
• RNA POLYMERASE TRANSCRIPTION PROMOTERS AND METHOD FOR DETERMINING BASE SEQUENCE
  申请人：Riken

  公开号：EP1061130A1

  公开（公告）日：2000-12-20

  An RNA polymerase transcription accelerator comprising a compound represented by the following Formula (I) or salts thereof. A method of sequencing DNA in which nucleic acid transcripts are obtained using an RNA polymerase and a DNA fragment as a template, the resulted nucleic acid transcripts are separated, the nucleic acid sequence is determined from the separated fractions wherein the nucleic acid transcription reaction is carried out in the presence of a compound selected from a group of compounds represented by the above formula (I). The polyamine compounds above have outstanding accelerating activity on transcription activity of RNA polymerase. Therefore, use of the polyamine compounds in a DNA sequencing method using RNA polymerase can make a length of DNA sequence that can be determined in one sequencing longer.

  一种 RNA 聚合酶转录促进剂，包括下式 (I) 所代表的化合物或其盐类。 一种 DNA 测序方法，其中使用 RNA 聚合酶和 DNA 片段作为模板获得核酸转录本，分离得到的核酸转录本，从分离的部分确定核酸序列，其中核酸转录反应是在选自上式（I）所代表的一组化合物的存在下进行的。 上述多胺化合物对 RNA 聚合酶的转录活性具有突出的加速活性。因此，在使用 RNA 聚合酶的 DNA 测序方法中使用这些多胺化合物，可使一次测序确定的 DNA 序列长度更长。