4-吗啉磺酰氯 | 1828-66-6

• 物质功能分类: 有机原料 - 羧酸类化合物及衍生物 - 羧酸酰卤化物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 中文名称: 4-吗啉磺酰氯
• 中文别名: 吗啉-4-磺酰氯；吗啉磺酰氯
• 英文名称: Morpholine-4-sulfonyl chloride
• CAS: 1828-66-6
• 化学式: C₄H₈ClNO₃S
• mdl: MFCD03249981
• 分子量: 185.631
• InChiKey: KXIBCCFSAMRWIC-UHFFFAOYSA-N

物化性质

• 熔点：
  72.36° C (Predicted)
• 沸点：
  300℃
• 密度：
  1.53
• 闪点：
  135℃

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  55
• 氢给体数：
  0
• 氢受体数：
  4

安全信息

• 危险等级：
  IRRITANT
• 危险品标志：
  Xi
• 安全说明：
  S26
• 危险类别码：
  R36/37/38
• 海关编码：
  2934999090
• 包装等级：
  III
• 危险类别：
  8
• 危险性防范说明：
  P260,P280,P303+P361+P353,P301+P330+P331,P304+P340+P310,P305+P351+P338+P310
• 危险品运输编号：
  3265
• 危险性描述：
  H314
• 储存条件：
  2-8°C

SDS

Material Safety Data Sheet

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Section 1. Identification of the substance
Product Name: Morpholine-4-sulfonyl chloride
Synonyms:

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Section 2. Hazards identification
Harmful by inhalation, in contact with skin, and if swallowed.
H318: Causes serious eye damage
P305+P351+P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present
and easy to do – continue rinsing

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Section 3. Composition/information on ingredients.
Ingredient name: Morpholine-4-sulfonyl chloride
CAS number: 1828-66-6

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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.
Storage: Store in closed vessels, refrigerated.

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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
Melting point: No data
Flash point: No data
Density: No data
Molecular formula: C4H8ClNO3S
Molecular weight: 185.6

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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, hydrogen chloride, sulfur 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
UN Number: UN3265 Class: 8 Packing group: III
Proper shipping name: CORROSIVE LIQUID, ACIDIC, ORGANIC, N.O.S. (Morpholine-4-sulfonyl chloride)

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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

反应信息

• 作为反应物：
  描述：

  4-吗啉磺酰氯 在 四丁基氟化铵 、 三乙胺 、 4-二甲氨基吡啶 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 1.67h， 以68%的产率得到
  参考文献：
  名称：

  [EN] PRE-ORGANIZED TRICYCLIC INTEGRASE INHIBITOR COMPOUNDS
  [FR] COMPOSÉS TRICYCLIQUES PRÉORGANISÉS INHIBITEURS D'INTÉGRASE

  摘要：

  公开号：

  WO2004035576A3
• 作为产物：
  描述：

  吗啉 在 磺酰氯 、 三乙胺 作用下， 以 乙腈 为溶剂， 反应 0.5h， 生成 4-吗啉磺酰氯
  参考文献：
  名称：

  三组分磺酰胺合成中的S（VI）：使用氯化硫作为钯催化的Suzuki-Miyaura偶联中的关键

  摘要：

  在钯催化的三组分磺酰胺合成中，氯化硫被用作-SO 2-基团的来源。原位生成的氨磺酰氯与硼酸之间的Suzuki-Miyaura偶联以中等至高收率产生了多种磺酰胺，并具有出色的反应选择性。尽管此转化不适用于伯胺或苯胺，但结果表明官能团耐受性高。通过解决脱磺酰化问题并利用廉价且容易获得的氯化硫作为二氧化硫的来源，首先实现了氧化还原中性三组分合成的磺酰胺。

  DOI：

  10.1039/d1sc01351c
• 作为试剂：
  描述：

  二丁基二硫代次磷酸 在 4-吗啉磺酰氯 作用下， 以 苯 为溶剂， 生成 bis-(dibutylthiophosphoryl)trisulfane
  参考文献：
  名称：

  �ber heteroorganische Verbindungen, 39. Mitt.: Neue Darstellungsmethoden f�r Bis-(dialkylthiophosphinyl)-trisulfide. Reaktionsmechanismus

  摘要：

  DOI：

  10.1007/bf00909881

文献信息

• Benzene Sulfonamide Thiazole and Oxazole Compounds
  申请人：Adams Jerry Leroy

  公开号：US20090298815A1

  公开（公告）日：2009-12-03

  The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.

  本发明提供了噻唑磺胺和噁唑磺胺化合物，含有这些化合物的组合物，以及用作药物制剂的制备方法和使用方法。
• Cu-Catalyzed Photoredox Chlorosulfonation of Alkenes and Alkynes
  作者：Murat Alkan-Zambada、Xile Hu

  DOI：10.1021/acs.joc.9b00238

  日期：2019.4.5

  Visible-light photoredox chlorosulfonation of alkenes and alkynes is achieved using a Cu photocatalyst. The reactions occur under mild conditions, have broad scope, and have high functional group tolerance.

  使用铜光催化剂实现烯烃和炔烃的可见光光氧化还原氯磺化。反应在温和的条件下发生，范围广，对官能团的耐受性高。
• NEW HSL INHIBITORS USEFUL IN THE TREATMENT OF DIABETES
  申请人：Ackermann Jean

  公开号：US20110065707A1

  公开（公告）日：2011-03-17

  The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein A 1 , A 2 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 have the significance given herein.

  本发明涉及式(I)的化合物以及其药学上可接受的盐，其中A1、A2、R1、R2、R3、R4、R5和R6具有本文中给出的含义。
• [EN] HSL INHIBITORS USEFUL IN THE TREATMENT OF DIABETES<br/>[FR] INHIBITEURS DE HSL UTILES DANS LE TRAITEMENT DU DIABÈTE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2011029808A1

  公开（公告）日：2011-03-17

  Compounds of formula (I), as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1,R2 R3,R4 R5 and R6 have the significance given in claim 1. Objects of the present invention are the compounds of formula (I) and their aforementioned salts and esters and their use as therapeutically active substances, a process for the manufacture of the said compounds, intermediates, pharmaceutical compositions, medicaments containing the said compounds, their pharmaceutically acceptable salts or esters, the use of the said compounds, salts or esters for the treatment or prophylaxis of illnesses, especially in the treatment or prophylaxis of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis or obesity and the use of the said compounds, salts or esters for the production of medicaments for the treatment or prophylaxis of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis or obesity.

  化合物的化学式（I），以及其药学上可接受的盐可以用作药物组合物的形式，其中A1，A2，R1，R2，R3，R4，R5和R6具有权利要求1中给定的含义。本发明的目的是化学式（I）的化合物及其上述的盐和酯，以及它们作为治疗活性物质的用途，制造所述化合物的方法，中间体，含有所述化合物的药物组合物，含有所述化合物、其药学上可接受的盐或酯的药物，所述化合物、盐或酯的用途用于治疗或预防疾病，特别是用于治疗或预防糖尿病、代谢综合征、血脂异常、动脉粥样硬化或肥胖症，以及所述化合物、盐或酯的用途用于生产用于治疗或预防糖尿病、代谢综合征、血脂异常、动脉粥样硬化或肥胖症的药物。
• Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists
  作者：Martin Cooper、Antonio Llinas、Peter Hansen、Moya Caffrey、Asim Ray、Stina Sjödin、Igor Shamovsky、Hiroki Wada、Tina Jellesmark Jensen、Ulf Sivars、Leif Hultin、Ulf Andersson、Sara Lundqvist、Karin Gedda、Lisa Jinton、Nina Krutrök、Richard Lewis、Paul Jansson、Cristina Gardelli

  DOI：10.1021/acs.jmedchem.0c00828

  日期：2020.9.10

  adipogenesis and therefore has been considered a promising therapeutic target for catabolic conditions. We previously reported on the synthesis and properties of an indane based series of ghrelin receptor full agonists which led to a sustained increase of insulin-like growth factor-1 in a dog pharmacodynamic study. Herein we report on the identification of a series of pyrrolidine or piperidine based

  肌肉萎缩和恶病质是罹患癌症，慢性阻塞性肺疾病和其他几种慢性疾病的患者中的常见合并症。肽激素生长激素释放肽发挥多效性作用，包括刺激生长激素分泌和随后增加胰岛素样生长因子-1水平，这是肌肉生长和修复的重要介质。Ghrelin还作用于炎症，食欲和脂肪形成，因此被认为是分解代谢疾病的有希望的治疗靶标。我们先前曾报道过基于茚满的系列生长素释放肽受体完全激动剂的合成和性质，该合成和性质在狗药效学研究中导致胰岛素样生长因子-1的持续增加。