N,N-二甲基(R-吗啉-2-基)甲酰胺 | 214273-19-5

• 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: N,N-二甲基(R-吗啉-2-基)甲酰胺
• 中文别名: N,N-二甲基-((R)-吗啉)甲胺；(R)-N,N-二甲基-2-吗啉甲胺
• 英文名称: (R)-N,N-dimethyl-1-(morpholin-2-yl)methanamine
• 英文别名: (R)-2-(N,N-dimethylaminomethyl)morpholine；N,N-dimethyl-1-[(2R)-morpholin-2-yl]methanamine
• CAS: 214273-19-5
• 化学式: C₇H₁₆N₂O
• 分子量: 144.217
• InChiKey: KNCQHMMKDOIHRT-SSDOTTSWSA-N

物化性质

• 沸点：
  198.8±15.0 °C(Predicted)
• 密度：
  0.931±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  24.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1,4-dihydro-3-quinoline carboxylic acid (O₃,O⁴)bis(acyloxy-O)borate 、 N,N-二甲基(R-吗啉-2-基)甲酰胺 在 三乙胺 作用下， 以39%的产率得到(S)-1-cyclopropyl-1,4-dihydro-7-[2-(N,N-dimethylaminomethyl)morpholino]-6-fluoro-8-methoxy-4-oxoquinoline-3-carboxylic acid
  参考文献：
  名称：

  Synthesis and structure-activity relationships of 7-(2-aminoalkyl)morpholinoquinolones as anti-Helicobacter pylori agents

  摘要：

  A series of the titled compounds was synthesized and tested for anti-Helicobacter pylori activities. We discovered Y-34867 having the most potent activity against Helicobacter pylori among the quinolones tested along with high photostability. Furthermore, Y-34867 showed an excellent therapeutic effect in the experimental Helicobacter pylori infected Mongolian gerbil model. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00390-4
• 作为产物：
  描述：

  (4-苄基-1,4-氧杂-2-基)甲胺 在 palladium on activated charcoal 甲酸 、 肼 作用下， 生成 N,N-二甲基(R-吗啉-2-基)甲酰胺
  参考文献：
  名称：

  Synthesis and structure-activity relationships of 7-(2-aminoalkyl)morpholinoquinolones as anti-Helicobacter pylori agents

  摘要：

  A series of the titled compounds was synthesized and tested for anti-Helicobacter pylori activities. We discovered Y-34867 having the most potent activity against Helicobacter pylori among the quinolones tested along with high photostability. Furthermore, Y-34867 showed an excellent therapeutic effect in the experimental Helicobacter pylori infected Mongolian gerbil model. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00390-4

文献信息

• [EN] COMPLEMENT MODULATORS AND RELATED METHODS<br/>[FR] MODULATEURS DU COMPLÉMENT ET PROCÉDÉS ASSOCIÉS
  申请人：RA PHARMACEUTICALS INC

  公开号：WO2020205501A1

  公开（公告）日：2020-10-08

  The present disclosure presents compounds and compositions that interact with complement components. Some compounds inhibit complement activity. Included are small molecule compounds and compositions that function as C5 inhibitor compounds. Methods for inhibiting complement activity and methods of treating complement-related indications with the C5 inhibitor compounds and compositions are provided.

  本公开涉及与补体成分相互作用的化合物和组合物。一些化合物抑制补体活性。包括作为C5抑制剂化合物的小分子化合物和组合物。提供了抑制补体活性的方法以及利用C5抑制剂化合物和组合物治疗与补体相关症状的方法。
• Prophylactic or therapeutic agent for diseases attributable to infection with helicobacters
  申请人：Welfide Corporation

  公开号：US06221864B1

  公开（公告）日：2001-04-24

  The present invention relates to an agent for the prophylaxis and treatment of diseases caused by Helicobacter infections, which comprises (S)-1-cyclopropyl-1,4-dihydro-7-[2-(N,N-dimethylaminomethyl)morpholino]-6-fluoro-8-methoxy-4-oxoquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof. The prophylactic and therapeutic agent of the present invention is effective even when used alone in a small dose for a short time, is almost free of problematic side effects such as tolerance and diarrhea, and is low toxic and capable of safe and ensured bacterial eradication. It is useful for the prophylaxis and treatment of diseases caused by Helicobacter infections, particularly, gastritis, gastric ulcer, duodenal ulcer, malignant lymphoma and gastric cancer.

  本发明涉及一种用于预防和治疗由幽门螺杆菌感染引起的疾病的制剂，包括（S）-1-环丙基-1,4-二氢-7-[2-(N,N-二甲基氨甲基)吗啉基]-6-氟-8-甲氧基-4-氧代喹啉-3-羧酸或其药学上可接受的盐。本发明的预防和治疗剂即使在小剂量和短时间内单独使用也有效，几乎没有耐受性和腹泻等问题性副作用，毒性低且能够安全有效地根除细菌。它对于预防和治疗由幽门螺杆菌感染引起的疾病特别有效，包括胃炎、胃溃疡、十二指肠溃疡、恶性淋巴瘤和胃癌。
• [EN] NEW PYRAZOLO[3,4-D]PYRIMIDINES INHIBITING H. PYLORI INFECTIONS<br/>[FR] PYRAZOLO[3,4-D]PYRIMIDINES INHIBANT LES INFECTIONS PAR H. PYLORI
  申请人：ASTRAZENECA AB

  公开号：WO2003002567A1

  公开（公告）日：2003-01-09

  Compounds having the general formula , and pharmaceutical compositions containing them, and their use in the treatment or prophylaxis of H. pylori infection.

  具有一般式的化合物，以及含有它们的制药组合物，以及它们在治疗或预防H. pylori感染中的用途。
• PROPHYLACTIC OR THERAPEUTIC AGENT FOR DISEASES ATTRIBUTABLE TO INFECTION WITH HELICOBACTERS
  申请人：YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

  公开号：EP0995746A1

  公开（公告）日：2000-04-26

  The present invention relates to an agent for the prophylaxis and treatment of diseases caused by Helicobacter infections, which comprises (S)-1-cyclopropyl-1,4-dihydro-7-[2-(N,N-dimethylaminomethyl)morpholino]-6-fluoro-8-methoxy-4-oxoguinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof. The prophylactic and therapeutic agent of the present invention is effective even when used alone in a small dose for a short time, is almost free of problematic side effects such as tolerance and diarrhea, and is low toxic and capable of safe and ensured bacterial eradication. It is useful for the prophylaxis and treatment of diseases caused by Helicobacter infections, particularly, gastritis, gastric ulcer, duodenal ulcer, malignant lymphoma and gastric cancer.

  本发明涉及一种用于预防和治疗由螺旋杆菌感染引起的疾病的药剂，它包括(S)-1-环丙基-1,4-二氢-7-[2-(N,N-二甲基氨基甲基)吗啉基]-6-氟-8-甲氧基-4-氧代谷氨酰胺-3-羧酸或其药学上可接受的盐。本发明的预防和治疗药物即使在短时间内小剂量单独使用也有效，几乎没有耐受性和腹泻等副作用问题，而且毒性低，能够安全地确保根除细菌。它可用于预防和治疗由螺旋杆菌感染引起的疾病，特别是胃炎、胃溃疡、十二指肠溃疡、恶性淋巴瘤和胃癌。
• Polyurethane catalyst and application thereof
  申请人：JIANGSU OSIC PERFORMANCE MATERIALS CO. LTD.

  公开号：US10889681B2

  公开（公告）日：2021-01-12

  A polyurethane catalyst comprises a sodium compound, the sodium compound being 1 to 60 wt % of the polyurethane catalyst by the mass percent, and further comprises a tertiary amine and/or pyridine compound. The sodium compound and the tertiary amine and/or pyridine compound achieve a synergistic effect; during the catalysis of the polymerization of isocyanate and polyalcohol, the speed of the polymerization reaction is increased; and the prepared polyurethane material has excellent physical properties, does not contain any heavy metal element at all, is an environment-friendly catalyst, solves the technical problem of ensuring environmental protection, safety and the catalytic efficiency of the polyurethane catalyst, and is particularly applicable to the preparation of polyurethane synthetic leather resin slurry, a polyurethane elastomer (prepolymer), a polyurethane coating, a polyurethane adhesive, a polyurethane composite material, flexible polyurethane foam, and a rigid polyurethane material.

  一种聚氨酯催化剂包括钠化合物，钠化合物占聚氨酯催化剂的质量百分比为 1 至 60 wt%，还包括叔胺和/或吡啶化合物。钠化合物和叔胺和/或吡啶化合物具有协同效应；在催化异氰酸酯和多元醇聚合的过程中，聚合反应的速度得到提高；本发明制备的聚氨酯材料物理性能优异，不含任何重金属元素，属于环境友好型催化剂，解决了确保聚氨酯催化剂环保、安全和催化效率的技术难题，特别适用于制备聚氨酯合成革树脂浆料、聚氨酯弹性体（预聚物）、聚氨酯涂料、聚氨酯胶粘剂、聚氨酯复合材料、软质聚氨酯泡沫塑料和硬质聚氨酯材料。