4-甲基-1-哌嗪羧酸酰肼 | 88701-65-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 4-甲基-1-哌嗪羧酸酰肼
• 英文名称: 4-methyl-piperazine-1-carboxylic acid hydrazide
• 英文别名: 4-Methylpiperazine-1-carbohydrazide
• CAS: 88701-65-9
• 化学式: C₆H₁₄N₄O
• mdl: MFCD09836367
• 分子量: 158.203
• InChiKey: TUXFLPICTVEGND-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.4
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.833
• 拓扑面积：
  61.6
• 氢给体数：
  2
• 氢受体数：
  3

安全信息

• 海关编码：
  2933599090

反应信息

• 作为反应物：
  描述：

  5-硝基噻吩-2-甲醛 、 4-甲基-1-哌嗪羧酸酰肼 在 对甲苯磺酸 作用下， 以 甲苯 为溶剂， 以40%的产率得到4-methyl-N-[(5-nitrothiophen-2-yl)methylideneamino]piperazine-1-carboxamide
  参考文献：
  名称：

  Synthesis and anti-trypanosomal activity of novel 5-nitro-2-furaldehyde and 5-nitrothiophene-2-carboxaldehyde semicarbazone derivatives

  摘要：

  Several novel semicarbazones derivatives were prepared from 5-nitro-2-furaldehyde or 5-nitrothiophene-2-carboxaldehyde, and tested in vitro as potential anti trypanosomal agents. The compounds were prepared in good to excellent yields in 2-3 steps from readily available starting materials. Some derivatives were found to be active against Trypanosoma cruzi with an activity similar to that of Nifurtimox. (C) 1998 Elsevier Science S.A. All rights reserved.

  DOI：

  10.1016/s0014-827x(97)00011-6
• 作为产物：
  描述：

  4-甲基哌嗪-1-甲酰氯盐酸盐 在 三乙胺 、 肼 作用下， 以 甲醇 、 苯 为溶剂， 以58%的产率得到4-甲基-1-哌嗪羧酸酰肼
  参考文献：
  名称：

  Sharma, Satyavan; Agarwal, V. K.; Dubey, S. K., Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1987, vol. 26, # 1-12, p. 748 - 751

  摘要：

  DOI：

文献信息

• Potential hypnotics and anxiolytics in the 4H-s-triazolo[4,3-a]-1,4-benzodiazepine series: 8-Chloro-6-(2-chlorophenyl)-1-[4-(2-methoxyethyl)piperazino]-4H-s-triazolo[4,3-a]-1,4-benzodiazepine and some related compounds
  作者：Zdeněk Polívka、Miroslav Ryska、Jiří Holubek、Emil Svátek、Jan Metyš、Miroslav Protiva

  DOI：10.1135/cccc19832395

  日期：——

  1-Bromo derivatives XIIa and XIIb were prepared by bromination of 8-chloro-6-phenyl-4H-s-triazolo[4,3-a]-1,4-benzodiazepine (XIa) and its 6-(2-chlorophenyl) analogue XIb with bromine in chloroform in the presence of pyridine. Substitution reactions with 1-(2-methoxyethyl)piperazine (XIVb), 1-(3-methoxypropyl)piperazine (XVb), 1-(2-ethoxyethyl)piperazine (XVIb) and 1-(2-methylthioethyl)piperazine (XVIIb) afforded the title compound IIb and analogues IIa and IIIb-Vb. A substitution reaction of the bromo derivative XIIb with piperazine gave the 1-piperazino derivative VIIIb which was alkylated with 2-phenoxyethyl bromide and 2-phenylthioethyl bromide to give compounds VIb and VIIb. The title compound IIb has very high anticonvulsant and discoordinating activities in mice. The enlargement of the substituent R¹ (compounds IIIb-VIIb) results in a gradual decrease of the effects mentioned.

  1-溴衍生物XIIa和XIIb是通过在氯仿中存在吡啶的情况下，用溴对8-氯-6-苯基-4H-s-三唑并[4,3-a]-1,4-苯二氮杂环己烷（XIa）及其6-(2-氯苯基)类似物XIb进行溴化制备的。用1-(2-甲氧基乙基)哌嗪（XIVb）、1-(3-甲氧基丙基)哌嗪（XVb）、1-(2-乙氧基乙基)哌嗪（XVIb）和1-(2-甲硫基乙基)哌嗪（XVIIb）进行取代反应，得到了标题化合物IIb及其类似物IIa和IIIb-Vb。溴衍生物XIIb与哌嗪的取代反应得到了1-哌嗪基衍生物VIIIb，它与2-苯氧基乙溴和2-苯硫基乙溴烷基化，得到化合物VIb和VIIb。标题化合物IIb在小鼠中具有非常高的抗惊厥和失调活性。取代基R1的扩大（化合物IIIb-VIIb）导致上述效应逐渐减弱。
• Polyene macrolide derivatives, use for vectoring molecules
  申请人：UNIVERSITE PIERRE ET MARIE CURIE

  公开号：US20040002465A1

  公开（公告）日：2004-01-01

  A composition having a negatively charged molecule and a cationic polyene macrolide compound having two to four positive charges that reacts with the negatively charged molecule is described. This compound can be used to vector molecules and especially nucleic acids into cells.

  描述了一种具有带负电荷的分子和带有两到四个正电荷的阳离子多烯大环化合物的组合物，该组合物与带负电荷的分子发生反应。这种化合物可用于将分子，尤其是核酸，导入细胞中。
• [EN] PYRAZOLOPYRIMIDINONE COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS DE PYRAZOLOPYRIMIDINONE ET LEURS UTILISATIONS
  申请人：ADURO BIOTECH INC

  公开号：WO2019055750A1

  公开（公告）日：2019-03-21

  The present invention relates to pyrazolopyrimidinone compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating autoimmune, inflammatory, and neurodegenerative diseases by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

  本发明涉及吡唑吡咪啉酮化合物。本发明还涉及含有这些化合物的药物组合物，以及通过向需要的受试者施用这些化合物和药物组合物来治疗自身免疫、炎症和神经退行性疾病的方法。本发明还涉及利用这些化合物进行研究或其他非治疗目的的用途。
• Avermectin derivatives
  申请人：MERCK & CO. INC.

  公开号：EP0343708A2

  公开（公告）日：1989-11-29

  There are disclosed novel avermectin compounds wherein the 4" or 4 hydroxy group is oxidized to an oxo group and replaced with a semicarbazone, carbonyl- or sulfonyl- hydrazone, hydrazone, or oxime, and optionally reduced to the corresponding semicarbazide, carbonyl- or sulfonylhydrazide or hydrazine. The semicarbazones and hydrazones are prepared from the 4 or 4 oxo compound using the corresponding semicarbazides or hydrazines. The compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests. Compositions for such uses are also disclosed.

  本发明公开了新型阿维菌素化合物，其中 4 "或 4-羟基被氧化成氧代基团，并被半咔唑、羰基或磺酰基腙、腙或肟取代，还可选择还原成相应的半咔唑、羰基或磺酰基肼或肼。缩氨基脲和肼是用相应的缩氨基脲或肼从 4 或 4 氧代化合物中制备出来的。这些化合物可用作抗寄生虫药剂，其组合物也已公开。这些化合物也是针对农业害虫的高效杀虫剂。还公开了用于这种用途的组合物。
• ANTIVIRAL COMPOUNDS
  申请人：Gilead Pharmasset LLC

  公开号：EP3699176A2

  公开（公告）日：2020-08-26

  The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

  本发明涉及抗病毒化合物、含有此类化合物的组合物、包括施用此类化合物的治疗方法，以及制备此类化合物的工艺和中间体。