3-(N-Acetyl-N-phenylamino)-pyridine | 13020-86-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 3-(N-Acetyl-N-phenylamino)-pyridine
• 英文别名: N-phenyl-N-pyridin-3-yl-acetamide；N-(3-pyridyl)-acetanilide；N-phenyl-N-pyridin-3-ylacetamide
• CAS: 13020-86-5
• 化学式: C₁₃H₁₂N₂O
• 分子量: 212.251
• InChiKey: UDKIANVDMDXXIK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  33.2
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  3-乙酰氨基吡啶 、 溴苯 在 potassium carbonate 、 copper(l) chloride 作用下， 以 xylene 为溶剂， 反应 22.0h， 以74%的产率得到3-(N-Acetyl-N-phenylamino)-pyridine
  参考文献：
  名称：

  An Improvement of theN-Arylation of Amides; Application to the Synthesis of Substituted 3-(N-Acetyl-N-phenylamino)-pyridines

  摘要：

  在催化量的三(3,6-二氧杂庚基)胺（TDA-1）和氯化铜(I)的存在下，通过共沸分离反应水，羧酰胺的N-芳基化反应得到了简化，现在可以在较为温和的条件下进行，使用准化学计量的取代溴苯作为芳基化剂，在沸腾的二甲苯中进行，或者使用氯苯作为芳基化剂和反应溶剂，在回流条件下进行。该反应在制备各种二芳基胺方面展示了其普遍适用性。

  DOI：

  10.1055/s-1989-27238

文献信息

• 3-piperidyl-4-oxoquinazoline derivatives and pharmaceutical compositions comprising the same
  申请人：Japan Tobacco, Inc.

  公开号：US06235730B1

  公开（公告）日：2001-05-22

  3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.

  本发明提供了3-哌啶基-4-氧喹唑啉衍生物，其由式（I）表示：其中R代表氨基或环氨基，例如二苯并氮杂环，每个都被取代或未取代的芳基基团，取代或未取代的杂环基团或类似物所取代，n是1到3的整数，R3和R4独立地表示氢原子，低碳基或类似物，或其药学上可接受的盐。本发明化合物（I）具有出色的MTP抑制活性。因此，这些化合物不仅抑制了导致动脉硬化疾病的LDL的形成，还通过调节MTP活性来调节血液中的TG，胆固醇和脂蛋白如LDL，并通过调节细胞脂质来使用作为新型的高脂血症或动脉硬化疾病的预防或治疗药物。此外，它们还可以用作胰腺炎，肥胖症，高胆固醇血症和高三酰甘油血症的治疗或预防剂。
• 3-PIPERIDYL-4-OXOQUINAZOLINE DERIVATIVES AND MEDICINCAL COMPOSITIONS CONTAINING THE SAME
  申请人：Japan Tobacco Inc.

  公开号：EP0970954A1

  公开（公告）日：2000-01-12

  3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 4, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.

  提供了3-哌啶基-4-氧代喹唑啉衍生物，由式(I)表示： 其中 R 代表氨基或环状氨基，如二苯并氮杂卓，它们各自被取代或未被取代的芳基、取代或未被取代的杂芳基或类似基团取代，n 是 1 至 4 的整数，R3 和 R4 独立地代表氢原子、低级烷基或类似基团，或其药学上可接受的盐。本发明的化合物（I）具有优异的 MTP 抑制活性。因此，这些化合物不仅能抑制导致动脉硬化疾病的低密度脂蛋白的形成，还能调节血液中的总胆固醇、胆固醇和脂蛋白（如低密度脂蛋白），并通过调节 MTP 活性来调节细胞脂质。它们还可用作高脂血症或动脉硬化疾病的新型预防或治疗药物。此外，它们还可用作胰腺炎、肥胖症、高胆固醇血症和高甘油三酯血症的治疗或预防药物。
• TDA-1 catalysis in Smiles rearrangement of N-arylphenoxyamides. Accelerating effect of the 2,4,6-trichloro substitution
  作者：A Greiner

  DOI：10.1016/s0040-4039(00)95282-1

  日期：1989.1
• GREINER, ALFRED, SYNTHESIS,(1989) N, C. 312-313
  作者：GREINER, ALFRED

  DOI：——

  日期：——
• US6235730B1
  申请人：——

  公开号：US6235730B1

  公开（公告）日：2001-05-22