1-(3,5-dichloropyridin-4-yl)-4-methylpiperazine | 1221567-29-8

• 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: 1-(3,5-dichloropyridin-4-yl)-4-methylpiperazine
• CAS: 1221567-29-8
• 化学式: C₁₀H₁₃Cl₂N₃
• 分子量: 246.139
• InChiKey: FNSGBKHKJNAQQX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  19.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(3,5-dichloropyridin-4-yl)-4-methylpiperazine 在 三氟乙酸 、 溶剂黄146 作用下， 以 二氯甲烷 、 异丙醇 为溶剂， 反应 13.0h， 生成
  参考文献：
  名称：

  A traceless solid-supported synthesis of novel pyrazinediazepinedione derivatives

  摘要：

  A simple, convenient, six-step synthesis of novel, tricyclic pyrazinebenzodiazepinedione derivatives has been described. The strategy is based on the use of the orthogonally-protected, optically pure, (S)-piperazine-2-carboxylic acid, in a Petasis reaction, followed by coupling with anthranilic acid and finally cyclizing cleavage. The investigated method was applied for the synthesis of novel bicyclic pyrazinediaze-pinedione derivatives. This traceless, solid-supported approach allows the preparation of a wide variety of compounds in moderate yields from commercially available or easily obtainable reagents. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2010.01.064
• 作为产物：
  描述：

  N-甲基哌嗪 、 3,4,5-三氯吡啶 在 三乙胺 作用下， 以 N-甲基吡咯烷酮 为溶剂， 反应 1.0h， 以65%的产率得到1-(3,5-dichloropyridin-4-yl)-4-methylpiperazine
  参考文献：
  名称：

  Microwave-assisted synthesis of 4-amino-3,5-dihalopyridines

  摘要：

  4-Amino-3,5-dihalopyridines have been efficiently prepared via microwave-assisted nucleophilic aromatic substitution of 3,4,5-trihalopyridines using 1-1.1 equiv of primary and secondary amines. The reaction is also applicable to electron rich arylamines. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2010.01.101

文献信息

• [EN] PYRIDINE AND PYRIMIDINE BASED COMPOUNDS AS WNT SIGNALING PATHWAY INHIBITORS FOR THE TREATMENT OF CANCER<br/>[FR] COMPOSÉS À BASE DE PYRIDINE ET DE PYRIMIDINE EN TANT QU'INHIBITEURS DE LA VOIE DE SIGNALISATION WNT POUR LE TRAITEMENT DU CANCER
  申请人：CANCER REC TECH LTD

  公开号：WO2010041054A1

  公开（公告）日：2010-04-15

  The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and / or prevention of cancer.

  本发明涉及以吡啶和嘧啶为基础的化合物，包括这些化合物的药物组合物，以及它们作为治疗和/或预防癌症的潜在用途。
• PYRIDINE AND PYRIMIDINE BASED COMPOUNDS AS WNT SIGNALING PATHWAY INHIBITORS FOR THE TREATMENT OF CANCER
  申请人：McDonald Edward

  公开号：US20110190297A1

  公开（公告）日：2011-08-04

  The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.

  本发明涉及以吡啶和嘧啶为基础的化合物，包括这些化合物的药物组合物以及它们作为治疗和/或预防癌症的治疗剂的潜在用途。
• Pyridine and pyrimidine based compounds as Wnt signaling pathway inhibitors for the treatment of cancer
  申请人：McDonald Edward

  公开号：US08778925B2

  公开（公告）日：2014-07-15

  The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.

  本发明涉及以吡啶和嘧啶为基础的化合物、包含这些化合物的药物组合物以及它们作为治疗和/或预防癌症的潜在治疗剂的用途。
• Proline derivatives and use thereof as drugs
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP1930319A1

  公开（公告）日：2008-06-11

  The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

  本发明旨在提供因具有 DPP-IV 抑制作用而具有治疗效果的化合物，并提供令人满意的药物产品。 本发明者发现，在式 (I) 所代表的脯氨酸的 γ 位上引入取代基的衍生物 其中各符号如说明书中所定义，具有强效的 DPP-IV 抑制活性，并通过提高稳定性完成了本发明。
• US8778925B2
  申请人：——

  公开号：US8778925B2

  公开（公告）日：2014-07-15