5-(4-吗啉)-2-吡啶胺 | 571189-78-1

• 物质功能分类: 化学试剂 - 有机试剂
• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 5-(4-吗啉)-2-吡啶胺
• 中文别名: 2-氨基-5-(4-吗啉基)吡啶
• 英文名称: 5-morpholinopyridin-2-amine
• 英文别名: 5-morpholin-4-ylpyridin-2-ylamine；5-(morpholin-4-yl)pyridin-2-amine；5-morpholin-4-ylpyridin-2-amine
• CAS: 571189-78-1
• 化学式: C₉H₁₃N₃O
• mdl: MFCD09388785
• 分子量: 179.222
• InChiKey: ACYSKLGOADDKAI-UHFFFAOYSA-N

物化性质

• 熔点：
  143 °C
• 沸点：
  389.7±42.0 °C(Predicted)
• 密度：
  1.208±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.444
• 拓扑面积：
  51.4
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2934999090
• 储存条件：
  室温且干燥环境下使用。

SDS

Material Safety Data Sheet

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Section 1. Identification of the substance
Product Name: 5-Morpholinopyridin-2-amine
Synonyms:

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Section 2. Hazards identification
Harmful by inhalation, in contact with skin, and if swallowed.

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Section 3. Composition/information on ingredients.
Ingredient name: 5-Morpholinopyridin-2-amine
CAS number: 571189-78-1

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Section 4. First aid measures
Skin contact: Immediately wash skin with copious amounts of water for at least 15 minutes while removing
contaminated clothing and shoes. If irritation persists, seek medical attention.
Eye contact: Immediately wash skin with copious amounts of water for at least 15 minutes. Assure adequate
flushing of the eyes by separating the eyelids with fingers. If irritation persists, seek medical
attention.
Inhalation: Remove to fresh air. In severe cases or if symptoms persist, seek medical attention.
Ingestion: Wash out mouth with copious amounts of water for at least 15 minutes. Seek medical attention.

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Section 5. Fire fighting measures
In the event of a fire involving this material, alone or in combination with other materials, use dry
powder or carbon dioxide extinguishers. Protective clothing and self-contained breathing apparatus
should be worn.

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Section 6. Accidental release measures
Personal precautions: Wear suitable personal protective equipment which performs satisfactorily and meets local/state/national
standards.
Respiratory precaution: Wear approved mask/respirator
Hand precaution: Wear suitable gloves/gauntlets
Skin protection: Wear suitable protective clothing
Eye protection: Wear suitable eye protection
Methods for cleaning up: Mix with sand or similar inert absorbent material, sweep up and keep in a tightly closed container
for disposal. See section 12.
Environmental precautions: Do not allow material to enter drains or water courses.

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Section 7. Handling and storage
Handling: This product should be handled only by, or under the close supervision of, those properly qualified
in the handling and use of potentially hazardous chemicals, who should take into account the fire,
health and chemical hazard data given on this sheet.
Store in closed vessels, refrigerated.
Storage:

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Section 8. Exposure Controls / Personal protection
Engineering Controls: Use only in a chemical fume hood.
Personal protective equipment: Wear laboratory clothing, chemical-resistant gloves and safety goggles.
General hydiene measures: Wash thoroughly after handling. Wash contaminated clothing before reuse.

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Section 9. Physical and chemical properties
Appearance: Not specified
Boiling point: No data
No data
Melting point:
Flash point: No data
Density: No data
Molecular formula: C9H13N3O
Molecular weight: 179.2

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Section 10. Stability and reactivity
Conditions to avoid: Heat, flames and sparks.
Materials to avoid: Oxidizing agents.
Possible hazardous combustion products: Carbon monoxide, nitrogen oxides.

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Section 11. Toxicological information
No data.

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Section 12. Ecological information
No data.

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Section 13. Disposal consideration
Arrange disposal as special waste, by licensed disposal company, in consultation with local waste
disposal authority, in accordance with national and regional regulations.

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Section 14. Transportation information
Non-harzardous for air and ground transportation.

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Section 15. Regulatory information
No chemicals in this material are subject to the reporting requirements of SARA Title III, Section
302, or have known CAS numbers that exceed the threshold reporting levels established by SARA
Title III, Section 313.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

2-氨基-5-(4-吗啉基)吡啶主要用于实验室研发和化工医药合成。

上下游信息

• 上游原料

  中文名称	英文名称	CAS号	化学式	分子量
  4-(6-硝基-3-吡啶)吗啉	4-(6-nitropyridin-3-yl)morpholine	491855-89-1	C9H11N3O3	209.205
  4-(6-氯-3-吡啶)吗啉	4-(6-chloropyridin-3-yl)morpholine	633283-57-5	C9H11ClN2O	198.652
  ——	3-morpholinopyridine 1-oxide	780802-29-1	C9H12N2O2	180.206
  4-(6-氨基吡啶-3-基)哌嗪-1-羧酸叔丁酯	tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate	571188-59-5	C14H22N4O2	278.354

• 下游产品

  中文名称	英文名称	CAS号	化学式	分子量
  5-吗啉代吡啶-3-胺	5-morpholinopyridine-3-amine	1008853-90-4	C9H13N3O	179.222

反应信息

• 作为反应物：
  描述：

  5-(4-吗啉)-2-吡啶胺 在 tris-(dibenzylideneacetone)dipalladium(0) 、 四(三苯基膦)钯 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 水 、 sodium carbonate 、 caesium carbonate 、 sodium hydroxide 作用下， 以 1,4-二氧六环 、 乙醇 、 水 为溶剂， 反应 18.0h， 生成 6-(1H-indazol-6-yl)-8-(5-morpholinopyridin-2-ylamino)imidazo[1,2-a]pyridine-5-carboxylic acid
  参考文献：
  名称：

  [EN] IMIDAZOPYRIDINES SYK INHIBITORS
  [FR] INHIBITEURS DE SYK À BASE D'IMIDAZOPYRIDINES

  摘要：

  本文提供了某些咪唑吡啶(I)及其药物组合物。提供了治疗对Syk活性抑制敏感的患者患有某些疾病和疾病的方法，包括向这些患者施用至少一种有效减轻疾病或疾病症状的化学实体。还提供了一种确定样本中Syk激酶存在或不存在的方法。

  公开号：

  WO2011112995A1
• 作为产物：
  描述：

  4-(6-硝基-3-吡啶)吗啉 在 水 、 tin(ll) chloride 作用下， 以 乙醇 为溶剂， 反应 5.0h， 生成 5-(4-吗啉)-2-吡啶胺
  参考文献：
  名称：

  一系列双环HIV-1整合酶抑制剂的设计。第1部分：脚手架的选择

  摘要：

  提出了一种基于新型双环嘧啶酮核心的HIV整合酶抑制剂。评价了核心支架的九种变异，从而优化了6：6核心，从而得到了针对野生型HIV感染T细胞的EC 50为3 nM的化合物48。

  DOI：

  10.1016/j.bmcl.2010.07.079
• 作为试剂：
  描述：

  2-氨基-5-溴吡啶 、 吗啉 、 2-二环己膦基-2'-(N,N-二甲胺)-联苯 、 、 lithium hexamethyldisilazane 、 四氢呋喃 在 (1E,4E)-1,5-diphenylpenta-1,4-dien-3-one;palladium 氮气 、 乙酸乙酯 、 水 、 Sodium sulfate-III 、 crude material 、 5-(4-吗啉)-2-吡啶胺 、 A7 作用下， 以 叔丁醇 、 水 为溶剂， 反应 2.08h， 生成 5-(4-吗啉)-2-吡啶胺
  参考文献：
  名称：

  Benzonitrile derivatives as kinase inhibitors

  摘要：

  公式I中的化合物，其中R1，R2，X和Y具有声明1中指示的含义，是TBK1和IKKε的抑制剂，可用于治疗癌症和炎症性疾病等。

  公开号：

  US08969335B2

文献信息

• [EN] PYRROLOTRIAZINES AS ALK AND JAK2 INHIBITORS<br/>[FR] PYRROLOTRIAZINES EN TANT QU'INHIBITEURS D'ALK ET DE JAK2
  申请人：CEPHALON INC

  公开号：WO2010071885A1

  公开（公告）日：2010-06-24

  The present invention provides a compound of formula (I) or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula (I) has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.

  本发明提供了一种式（I）的化合物或其盐形式，其中Q1、Q2、Q3和Q4如本文所定义。式（I）的化合物具有ALK和/或JAK2抑制活性，并可用于治疗增殖性疾病。
• TYK2 INHIBITORS AND USES THEREOF
  申请人：Nimbus Lakshmi, Inc.

  公开号：US20160251376A1

  公开（公告）日：2016-09-01

  The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

  本发明提供了化合物、其组合物以及使用这些化合物来抑制TYK2并治疗TYK2介导的疾病的方法。
• [EN] COMBINATIONS AND DOSING REGIMES TO TREAT RB-POSITIVE TUMORS<br/>[FR] COMBINAISONS ET RÉGIMES POSOLOGIQUES POUR TRAITER DES TUMEURS RB-POSITIVES
  申请人：G1 THERAPEUTICS INC

  公开号：WO2016040858A1

  公开（公告）日：2016-03-17

  This invention directed to methods for treating select RB-positive cancers and other Rb- positive abnormal cellular proliferative disorders using CDK4/6 inhibitors in specific dosing and combination or alternation regimes. In one aspect, treatments of select RB-positive cancers are disclosed using specific CDK4/6 inhibitors in combination or alternation with another chemotherapeutic, for example, an additional kinase inhibitor, PD-1 inhibitor, or BCL-2 inhibitor, or combination thereof.

  这项发明涉及使用特定剂量和组合或交替方案中的CDK4/6抑制剂治疗选择性RB阳性癌症和其他RB阳性异常细胞增殖紊乱疾病的方法。在一个方面，揭示了使用特定CDK4/6抑制剂与另一种化疗药物（例如，额外的激酶抑制剂、PD-1抑制剂或BCL-2抑制剂，或其组合）组合或交替治疗选择性RB阳性癌症。
• IMIDAZO[1',2':1,6]PYRIDO[2,3-D]PYRIMIDINE COMPOUND AS PROTEIN KINASE INHIBITOR
  申请人：SHENGKE PHARMACEUTICALS (JIANGSU) LTD.

  公开号：US20200270251A1

  公开（公告）日：2020-08-27

  Provided is an imidazo[1′;2′:1,6]pyrido[2,3-d]pyrimidine compound of general formula (I). The compound can be used in treating a cell proliferative disorder and is a cyclin-dependent kinase (CDK) inhibitor with broad-spectrum and strong activity.

  提供的是一种通式为(I)的咪唑[1′;2′:1,6]吡啶[2,3-d]嘧啶化合物。该化合物可用于治疗细胞增殖紊乱，是一种具有广谱和强活性的周期蛋白依赖性激酶（CDK）抑制剂。
• COMPOUNDS AND METHODS FOR TREATING CANCER
  申请人：ANTIDOTE IP HOLDINGS, LLC

  公开号：US20200299282A1

  公开（公告）日：2020-09-24

  Substituted cinnamamide compounds and analogs, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or ameliorate cancer are provided.

  提供了替代肉桂酰胺化合物和类似物、制备这类化合物的方法、包含这类化合物的药物组合物和药物、以及使用这类化合物治疗、预防或改善癌症的方法。