N-(3-iodophenyl)morpholine | 291533-82-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: N-(3-iodophenyl)morpholine
• 英文别名: 4-(3-iodo-phenyl)-morpholine；4-(3-Iodophenyl)morpholine
• CAS: 291533-82-9
• 化学式: C₁₀H₁₂INO
• 分子量: 289.116
• InChiKey: ZACIRAVARVYABO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(3-iodophenyl)morpholine 、 tert-butylcarbazate 在 copper(l) iodide 、 1,10-菲罗啉 、 caesium carbonate 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 18.0h， 以62%的产率得到N-(3-morpholin-4-yl-phenyl)-hydrazinecarboxylic acid tert-butyl ester
  参考文献：
  名称：

  [EN] DIAMINOTRIAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES
  [FR] DIAMINOTRIAZOLES CONVENANT COMME INHIBITEURS DE PROTEINE KINASES

  摘要：

  公开号：

  WO2004046120A3
• 作为产物：
  描述：

  lithium morpholide 、 1,3-二碘苯 以59%的产率得到N-(3-iodophenyl)morpholine
  参考文献：
  名称：

  多官能芳基和杂芳基氨基铜酸盐氧化偶联制备叔胺

  摘要：

  高度官能化的叔胺可以通过使用四氯苯醌作为氧化剂的多官能氨基铜酸锂的氧化偶联来制备。这种通用胺化反应具有高官能团耐受性和对空间位阻不敏感的特点。在此，我们报告了一种制备芳基和杂芳基叔胺的实用程序。

  DOI：

  10.1055/s-2007-965941

文献信息

• [EN] PHTHALAZINONE AND RELATED ANALOGS AS SIRTUIN MODULATORS<br/>[FR] PHTALAZINONE ET ANALOGUES APPARENTÉS EN TANT QUE MODULATEURS DE LA SIRTUINE
  申请人：SIRTRIS PHARMACEUTICALS INC

  公开号：WO2010077947A1

  公开（公告）日：2010-07-08

  Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin- modulating compound in combination with another therapeutic agent.

  本文提供了新颖的去乙酰化酶调节化合物及其使用方法。这些去乙酰化酶调节化合物可用于延长细胞的寿命，并用于治疗和/或预防各种疾病和紊乱，包括与老化或压力、糖尿病、肥胖、神经退行性疾病、心血管疾病、血液凝块紊乱、炎症、癌症、潮红等相关的疾病或紊乱，以及那些可能受益于增加线粒体活性的疾病或紊乱。还提供了包含去乙酰化酶调节化合物与另一治疗剂组合的组合物。
• [EN] AZABENZIMIDAZOLES AND RELATED ANALOGS AS SIRTUIN MODULATORS<br/>[FR] AZABENZIMIDAZOLES ET ANALOGUES APPARENTÉS EN TANT QUE MODULATEURS DE LA SIRTUINE
  申请人：SIRTRIS PHARMACEUTICALS INC

  公开号：WO2010088574A1

  公开（公告）日：2010-08-05

  Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin- modulating compound in combination with another therapeutic agent.

  本文提供了一种新颖的调节sirtuin的化合物及其使用方法。这些调节sirtuin的化合物可用于增加细胞的寿命，并治疗和/或预防各种疾病和紊乱，包括与老化或压力、糖尿病、肥胖、神经退行性疾病、心血管疾病、血液凝块紊乱、炎症、癌症、潮红以及那些会受益于增加线粒体活性的疾病或紊乱。此外，还提供了包含一种sirtuin调节化合物与另一种治疗剂结合的组合物。
• [EN] ALKENYL- AND ALKYNYL-CONTAINING METALLOPROTEASE INHIBITORS<br/>[FR] INHIBITEURS DE METALLOPROTEASES, CONTENANT ALCENYLE ET ALCYNALE
  申请人：PROCTER & GAMBLE

  公开号：WO2000051975A1

  公开（公告）日：2000-09-08

  Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to Formula (I) where X, W, Z, A, G, R?1, R2, R3, R4, R5, R5'¿ and k have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of said formula, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.

  本发明涉及一种金属蛋白酶抑制剂化合物，其能够有效治疗由这些酶过度活性引起的疾病。特别地，该化合物具有如公式（I）所示的结构，其中X，W，Z，A，G，R1，R2，R3，R4，R5，R5'和k具有规范中描述的含义。本发明还包括该公式的光学异构体、对映异构体和对映体，以及其药学上可接受的盐、生物水解酰胺、酯和亚酰胺。还描述了包含这些化合物的药物组合物，以及使用这些化合物或药物组合物治疗或预防金属蛋白酶相关疾病的方法。
• ANTIPROLIFERATIVE COMPOUNDS AND METHODS OF USE THEREOF
  申请人：Celgene Corporation

  公开号：US20200163948A1

  公开（公告）日：2020-05-28

  Compounds of formula I for treating, preventing or managing cancer are disclosed. Also disclosed are methods of treating, preventing or managing cancer, such as leukemia, comprising administering the compounds. In certain embodiments, the method of treatment comprise administering a compound provided herein in combination with a second agent. Pharmaceutical compositions and single unit dosage forms comprising the compounds are also disclosed.

  本文揭示了化学式I的化合物，用于治疗、预防或管理癌症。还揭示了治疗、预防或管理癌症的方法，例如治疗白血病，包括给予这些化合物。在某些实施例中，治疗方法包括与第二药物联合给药。此外，还揭示了包含这些化合物的药物组合物和单剂量形式。
• [EN] ANTIPROLIFERATIVE COMPOUNDS AND METHODS OF USE THEREOF<br/>[FR] COMPOSÉS ANTIPROLIFÉRATIFS ET MÉTHODES D'UTILISATION DESDITS COMPOSÉS
  申请人：CELGENE CORP

  公开号：WO2016007848A1

  公开（公告）日：2016-01-14

  Compounds of formula (I) for treating, preventing or managing cancer are disclosed. Also disclosed are methods of treating, preventing or managing cancer, such as leukemia, comprising administering the compounds. In certain embodiments, the method of treatment comprise administering a compound provided herein in combination with a second agent. Pharmaceutical compositions and single unit dosage forms comprising the compounds are also disclosed. In Formula (I) R1 is optionally substituted cycloalkyi, aryl, heteroaryl or heterocyclyl; and R2 and R3 are each halo.

  本发明揭示了化学式(I)的化合物，用于治疗、预防或管理癌症。同时，还揭示了治疗、预防或管理癌症的方法，例如白血病，包括给予该化合物。 在某些实施例中，治疗方法包括联合给予本文提供的化合物和第二药物。还揭示了包含该化合物的制药组合物和单剂量形式。 在化学式(I)中，R1是可选的取代环烷基，芳基，杂芳基或杂环烷基；R2和R3均为卤素。