N'-Pentanoyl-N-methyl-piperazin | 10001-06-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: N'-Pentanoyl-N-methyl-piperazin
• 英文别名: 1-(4-methylpiperazin-1-yl)pentan-1-one；1-methyl-4-pentanoyl-piperazine
• CAS: 10001-06-6
• 化学式: C₁₀H₂₀N₂O
• mdl: MFCD03385971
• 分子量: 184.282
• InChiKey: JDNGEKSTTQZLHP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  23.6
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  N-甲基哌嗪 、 正戊酸正戊酯 在 (6-(di-tert-butylphosphinomethylene)-2-(N,N-diethylaminomethyl)-1,6-dihydropyridine)Ru(H)(CO) 作用下， 以 甲苯 、 苯 为溶剂， 反应 24.0h， 以94%的产率得到N'-Pentanoyl-N-methyl-piperazin
  参考文献：
  名称：

  中性条件下释放H2的酯和胺合成酰胺

  摘要：

  直接由酯和胺有效合成酰胺是在温和的中性条件下实现的，并释放出分子氢。伯胺和仲胺都可以使用。这种前所未有的、普遍的、对环境无害的反应在中性条件下由脱芳构化的钌-钳形 PNN 络合物均匀催化，并在惰性气氛下在甲苯中进行，具有高周转数（高达 1000）。PNP 类似物不催化这种转化，强调了钳形配体的胺臂的重要性。提出了一种机制，涉及通过吡啶部分的芳构化-脱芳构化和胺臂的半可溶性进行金属-配体合作。

  DOI：

  10.1021/ja109944n

文献信息

• [EN] N-ACYL-N'-PHENYLPIPERAZINE DERIVATIVES AS SRBP MODULATORS FOR USE IN THE TREATMENT OF DIABETES AND OBESITY<br/>[FR] DÉRIVÉS DE N-ACYL-N'-PHÉNYLPIPÉRAZINE UTILISÉS COMME MODULATEURS DE LA SRBP DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT DU DIABÈTE ET DE L'OBÉSITÉ
  申请人：NAT UNIVERSITY OF IRELAND MAYNOOTH

  公开号：WO2013060860A1

  公开（公告）日：2013-05-02

  The present invention relates to compounds having the general formula (I) as described herein; methods of preparing said compounds; and their use in treating Type 1 and/or Type 2 Diabetes Mellitus. The compounds were assayed for binding to serum retinol binding protein (sRBP) and for disruption of the sRBP:transthyretin (TTR) and sRBP:sRBP receptor interaction. The compounds were also assayed for their ability to induce glucose uptake into mouse muscle cells. Also described is a pharmaceutical composition comprising a compound according to the first aspect of the present invention, and use thereof in treating Type 1 and Type 2 Diabetes.

  本发明涉及具有如下所述的一般式（I）的化合物；制备该化合物的方法；以及它们在治疗1型和/或2型糖尿病中的应用。对这些化合物进行了与血清视黄醇结合蛋白（sRBP）的结合和对sRBP：甲状腺素转运蛋白（TTR）和sRBP：sRBP受体相互作用的破坏的测定。这些化合物还被检测其促进小鼠肌肉细胞中葡萄糖摄取的能力。还描述了包含根据本发明第一方面的化合物的药物组合物，以及其在治疗1型和2型糖尿病中的用途。
• (2E,4E)-5-PHENYL-PENTA-2,4-DIEN-1-ONE DERIVATIVE
  申请人：BIOWAY., INC

  公开号：US20200157048A1

  公开（公告）日：2020-05-21

  The present application relates to a novel pentadienoyl compound and a pharmaceutical composition including the same. The pentadienoyl compound of the present application may be used to prevent or treat fatty liver and fatty liver-related disease by inhibiting lipogenesis and lipid accumulation in cells and activating lipid metabolism. In addition, the pentadienoyl compound of the present application may increase a SIRT1 expression level in cells or SIRT1 activity, and thus may be used to prevent or treat a SIRT1-mediated disease. In addition, the pentadienoyl compound of the present application may reduce a CK2 expression level in cells or CK2 activity, and thus may be used to prevent or treat a CK2-mediated disease.

  本申请涉及一种新型的戊二烯酰化合物和包括该化合物的药物组合物。本申请的戊二烯酰化合物可用于通过抑制细胞内脂肪生成和脂质积累，激活脂质代谢，预防或治疗脂肪肝和脂肪肝相关疾病。此外，本申请的戊二烯酰化合物可能增加细胞中SIRT1的表达水平或SIRT1的活性，因此可用于预防或治疗SIRT1介导的疾病。此外，本申请的戊二烯酰化合物可能降低细胞中CK2的表达水平或CK2的活性，因此可用于预防或治疗CK2介导的疾病。
• [EN] COMPOUNDS<br/>[FR] COMPOSÉS
  申请人：RESPIVERT LTD

  公开号：WO2011048111A1

  公开（公告）日：2011-04-28

  The present invention relates to compounds of formula (I) and to compositions comprising the same and to the use of the compounds and their 10 compositions in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making said compounds.

  本发明涉及公式（I）的化合物，以及包含该化合物的组合物，以及化合物及其组合物在治疗中的使用，例如在治疗炎症性疾病，特别是呼吸道炎症性疾病的治疗中的使用。该发明还涉及制备上述化合物的方法。
• [EN] SUBSTITUTED UREA EIF2α KINASE ACTIVATORS<br/>[FR] ACTIVATEURS SUBSTITUÉS DE L'URÉE-KINASE EIF2&Agr;
  申请人：BRIGHAM & WOMENS HOSPITAL

  公开号：WO2015038778A1

  公开（公告）日：2015-03-19

  This disclosure relates to substituted urea eIF2α kinase activators including methods of making and using the same. For example, such activators can include cycloalkyl aryl ureas, which activate at least one eIF2α kinase. These compounds may be useful for treatment of diseases such as, for example, cancer, hemolytic anemia not caused by infectious agents, Wolcott-Rallison syndrome, neurodegenerative disease, tuberous sclerosis complex, fragile-X syndrome, autism spectrum disorder, and ribosomal defect disease.

  本公开涉及替代脲eIF2α激酶激活剂，包括其制备和使用方法。例如，这些激活剂可以包括环烷基芳基脲，其激活至少一种eIF2α激酶。这些化合物可能对治疗疾病有用，例如癌症、非感染性溶血性贫血、沃尔科特-拉里森综合征、神经退行性疾病、结节性硬化症、脆性X综合征、自闭症谱系障碍和核糖体缺陷疾病。
• USE OF RUTHENIUM COMPLEXES FOR FORMATION AND/OR HYDROGENATION OF AMIDES AND RELATED CARBOXYLIC ACID DERIVATIVES
  申请人：Milstein David

  公开号：US20120253042A1

  公开（公告）日：2012-10-04

  A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.

  一种制备酰胺的方法，包括在Ruthenium配合物的存在下，通过反应一种一级胺和一种一级醇生成酰胺和分子氢。直接用等摩尔量的醇对一级胺进行酰化反应，可以高产率、高周转数地生成酰胺和分子氢（唯一的副产物）。此外，还揭示了将酰胺氢化为醇和胺的方法；将有机碳酸酯氢化为醇的方法；将氨基甲酸酯或尿素衍生物氢化为醇和胺的方法；酯的酰胺化反应；使用酯对醇进行酰化反应；将醇与水和碱偶联形成羧酸；将β-氨基醇脱氢生成吡嗪和环肽；以及将二级醇脱氢生成酮的方法。这些反应由基于A1式或A2式或A3式的去芳香的PNN型配体的Ruthenium配合物催化。