2-ethoxymorpholine | 91259-04-0

• 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: 2-ethoxymorpholine
• 英文别名: 2-ethoxy-morpholine；2-Aethoxy-morpholin
• CAS: 91259-04-0
• 化学式: C₆H₁₃NO₂
• mdl: MFCD19217426
• 分子量: 131.175
• InChiKey: LCBNROLNCOHVID-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  9
• 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：
  30.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-ethoxymorpholine 、 3-(4-Iodobutyl)-6-(3-ethyl-4-methylanilino)uracil 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以51%的产率得到3-[4-(2-Ethoxy-morpholin-4-yl)-butyl]-6-(3-ethyl-4-methyl-phenylamino)-1H-pyrimidine-2,4-dione
  参考文献：
  名称：

  Synthesis of Substituted 6-Anilinouracils and Their Inhibition of DNA Polymerase IIIC and Gram-Positive Bacterial Growth

  摘要：

  Certain substituted 6-anilinouracils are potent and selective inhibitors of Gram+ bacterial DNA polymerase IIIC (pol IIIC). In addition, analogues with 3-substituents in the uracil ring have potent antibacterial activity against Gram+ organisms in culture. In an attempt to find optimal anilino substituents for pol IIIC binding and optimal 3-substituents for antibacterial activity, we have prepared several series of 3-substituted-6-aminouracils and assayed their activity against pol IIIC from Bacillus subtilis and a panel of Gram+ and Gram- bacteria in culture. The 6-(3-ethyl-4-methylanilino) group and closely related substituent patterns maximized pol IIIC inhibition potency. Among a series of 3-(substituted-butyl)-6-(3-ethyl-4-methylanilino)uracils, basic amino substituents increased pol IIIC inhibition, but decreased antibacterial activity. The most potent antibacterials were simple hydroxybutyl and methoxybutyl derivatives, and hydrophobically substituted piperidinylbutyl derivatives.

  DOI：

  10.1021/jm020591z
• 作为产物：
  描述：

  4-benzyl-2-ethoxymorpholine 在 palladium on activated charcoal 氢气 作用下， 以 甲醇 为溶剂， 生成 2-ethoxymorpholine
  参考文献：
  名称：

  5-溴-2-硝基噻唑动画中的意外重排产物

  摘要：

  虽然2-溴-5-硝基噻唑（2）与弱碱性仲脂肪胺反应可从溴的亲核取代反应获得预期的2-氨基产物，但异构5-溴-2-硝基噻唑（3）与此类胺反应得到预期的5-氨基产物与2-胺化的5-硝基噻唑重排产物的混合物。后者的身份通过替代合成和X射线晶体学测定衍生物确定。提出的机理是将5-溴-2-硝基噻唑（3）缓慢热异构化为反应性更高的2-溴-5-硝基异构体2 在较弱的胺亲核试剂的情况下，其与5-溴基团的直接（但缓慢）亲核取代竞争，形成正常的取代产物。

  DOI：

  10.1002/jhet.5570330431

文献信息

• [EN] N-PYRIDINYL ACETAMIDE DERIVATIVES AS WNT SIGNALLING PATHWAY INHIBITORS<br/>[FR] DÉRIVÉS N-PYRIDINYL ACÉTAMIDE COMME INHIBITEURS DE LA OIE DE SIGNALISATION WNT
  申请人：REDX PHARMA PLC

  公开号：WO2016055790A1

  公开（公告）日：2016-04-14

  This invention relates to compounds. More specifically, the invention relates to compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.

  这项发明涉及化合物。更具体地，该发明涉及作为Wnt信号通路抑制剂的化合物。具体来说，该发明考虑了Porcupine（Porcn）的抑制剂。此外，该发明考虑了制备这些化合物的过程以及这些化合物的用途。因此，该发明的化合物可用于治疗由Wnt信号通路介导的疾病，例如治疗癌症、肉瘤、黑色素瘤、皮肤癌、血液肿瘤、淋巴瘤、癌症和白血病；或增强抗癌治疗的有效性。
• [EN] N-PYRIDINYL ACETAMIDE DERIVATIVES AS INHIBITORS OF THE WNT SIGNALLING PATHWAY<br/>[FR] DÉRIVÉS DE N-PYRIDYL ACÉTAMIDE UTILISÉS COMME INHIBITEURS DE LA VOIE DE SIGNALISATION WNT
  申请人：REDX PHARMA PLC

  公开号：WO2016055786A1

  公开（公告）日：2016-04-14

  This invention relates to compounds. More specifically, the invention relates to compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.

  这项发明涉及化合物。更具体地，该发明涉及作为Wnt信号通路抑制剂的化合物。具体来说，该发明考虑了Porcupine（Porcn）的抑制剂。此外，该发明考虑了制备这些化合物的过程以及这些化合物的用途。因此，该发明的化合物可用于治疗由Wnt信号通路介导的疾病，例如治疗癌症、肉瘤、黑色素瘤、皮肤癌、血液肿瘤、淋巴瘤、癌症和白血病；或增强抗癌治疗的有效性。
• PURINE DERIVATIVE AND ANTITUMOR AGENT USING SAME
  申请人：Suzuki Toshiaki

  公开号：US20120088765A1

  公开（公告）日：2012-04-12

  Disclosed are: a novel purine derivative, a composition thereof, a method for treating tumor using the purine derivative, and an antitumor agent using the purine derivative. Specifically disclosed is a compound represented by formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, or a prodrug thereof.

  本发明公开了一种新型嘌呤衍生物、其组合物、使用该嘌呤衍生物治疗肿瘤的方法以及使用该嘌呤衍生物的抗肿瘤剂。具体公开了一种由式（I）表示的化合物，或其药学上可接受的盐、溶剂或水合物，或其前药。
• NOVEL BETULINIC ACID DERIVATIVES AS HIV INHIBITORS
  申请人：HETERO RESEARCH FOUNDATION

  公开号：US20150119373A1

  公开（公告）日：2015-04-30

  The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.

  本发明涉及新型苦杏仁酸衍生物及相关化合物，以及用于治疗病毒性疾病，特别是HIV介导的疾病的药物组合物。
• New benzene derivatives having (NGF) production-promoting activity
  申请人：Sankyo Company Limited

  公开号：EP0501656A2

  公开（公告）日：1992-09-02

  Novel benzene derivatives are provided of the general formula (I): [wherein R¹ represents an amino group, a substituted amino group, a protected amino group, or a nitro group;    R² represents an amino group, a substituted amino group, a protected amino group, a hydroxy group, a substituted hydroxy group, or a protected hydroxy group;    R³ represents an amino group, a substituted amino, a heterocyclyl group having a ring nitrogen atom as the point of binding, or a substituted heterocyclyl group having a ring nitrogen atom as the point of binding; m is 0 to 2; n is 0 to 6; with the proviso that when m is 0, then n represents an integer from 2 to 6] and salts thereof. Compounds of formula (I) except those wherein R¹ is a nitro group have activity in promoting production of nerve growth factor. Compounds of formula (I) wherein R¹ is a nitro group are intermediates for compounds of formula (I) wherein R¹ is an amino group.

  提供了通式 (I) 的新型苯衍生物： [其中 R¹ 代表氨基、取代氨基、受保护氨基或硝基； R² 代表氨基、取代的氨基、受保护的氨基、羟基、取代的羟基或受保护的羟基； R³ 代表氨基、取代氨基、以环状氮原子为结合点的杂环基，或以环状氮原子为结合点的取代杂环基；m 为 0 至 2；n 为 0 至 6；但当 m 为 0 时，n 代表 2 至 6 的整数]及其盐。 式（I）化合物（其中 R¹ 为硝基的化合物除外）具有促进神经生长因子产生的活性。其中 R¹ 为硝基的式 (I) 化合物是其中 R¹ 为氨基的式 (I) 化合物的中间体。