N-(β-Methoxyaethyl)-p-toluidin | 32382-69-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(β-Methoxyaethyl)-p-toluidin
• 英文别名: NoName_3111；N-(2-methoxyethyl)-4-methylaniline
• CAS: 32382-69-7
• 化学式: C₁₀H₁₅NO
• 分子量: 165.235
• InChiKey: LWFDKUZKEODOTF-UHFFFAOYSA-N

物化性质

• 沸点：
  269.7±23.0 °C(Predicted)
• 密度：
  1.004±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(β-Methoxyaethyl)-p-toluidin 、 3-环己基丙酰氯 在 三乙胺 作用下， 以 苯 为溶剂， 反应 2.0h， 以70.6%的产率得到N-(p-tolyl)-N-(2-methoxyethyl)-3-cyclohexylpropionamide
  参考文献：
  名称：

  Azimov, A. I.; Dustmukhamedov, T. T.; Abdullaev, U. A., Journal of Organic Chemistry USSR (English Translation), 1985, vol. 21, # 9, p. 1816 - 1819

  摘要：

  DOI：
• 作为产物：
  描述：

  2-甲氧基乙基甲基碳酸酯 、 乙烷,三氯氟- 在 碘化乙基三苯基瞵 作用下， 反应 0.5h， 生成 4-甲基乙酰苯胺 、 N-甲基-对甲基苯胺 、 N-(β-Methoxyaethyl)-p-toluidin 、 N,N-二甲基对甲苯胺
  参考文献：
  名称：

  Selective N,N-Dimethylation of Primary Aromatic Amines with Methyl Alkyl Carbonates in the Presence of Phosphonium Salts

  摘要：

  In the presence of onium salts, at 140-170 degrees C, methyl alkyl carbonates [1a-c, ROCO2Me, R) MeO(CH2) 2[O(CH2)(2)](n); n = 2-0, respectively] react with primary aromatic amines (XC6H4NH2, X = p-OMe, p-Me, H, p-Cl, p-CO2Me, o-Et, and 2,3-Me2C6H3NH2) to yield the corresponding N,N-dimethyl derivatives (ArNMe2) with high selectivity ( up to 96%) and good isolated yields (78-95%). Phosphonium salts ( e. g., Ph3PEtI and n-Bu4PBr) are particularly efficient catalysts. Overall, a solvent-free reaction is coupled with safe methylating agents (1a-c) made from nontoxic dimethyl carbonate.

  DOI：

  10.1021/jo060674d

文献信息

• [EN] NOVEL PYRIDINONE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2-RECEPTORS<br/>[FR] NOUVEAUX DERIVES DE PYRIDINONE ET LEUR UTILISATION EN TANT QUE MODULATEURS ALLOSTERIQUES POSITIFS DES RECEPTEURS MGLUR2
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2006030032A1

  公开（公告）日：2006-03-23

  The present invention relates to novel compounds, in particular novel pyridinone derivat ives according to Formula (I) X R1 N Y (I) R2 R3 wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subt ype 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新化合物，特别是根据式（I）X R1 N Y（I）R2 R3定义的新吡啶酮衍生物。根据本发明的化合物是代谢型受体-亚型2（'mGluR2'）的阳性变构调节剂，对于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及代谢型受体的mGluR2亚型的疾病具有用处。特别是，这些疾病是从焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统障碍组中选择的。该发明还涉及制备此类化合物和组合物的药物组合物和过程，以及利用这类化合物预防和治疗涉及mGluR2的这类疾病。
• [EN] NON-FUSED THIOPHENE DERIVATIVES AND THEIR USES<br/>[FR] DÉRIVÉS DE THIOPHÈNE NON FUSIONNÉS ET LEURS UTILISATIONS
  申请人：ENYO PHARMA

  公开号：WO2019154953A1

  公开（公告）日：2019-08-15

  The present invention relates to a new class of non-fused thiophene derivatives and their uses for treating diseases such as infection, cancer, metabolic diseases, cardiovascular diseases, iron storage disorders and inflammatory disorders.

  本发明涉及一类新型非融合噻吩衍生物及其用于治疗感染、癌症、代谢性疾病、心血管疾病、铁贮存紊乱和炎症性疾病等疾病的用途。
• NOVEL PYRIDINONE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2-RECEPTORS
  申请人：Imogai Julien Hassan

  公开号：US20070213323A1

  公开（公告）日：2007-09-13

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) X R1 N Y (I) R2 R3 wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新型化合物，特别是按照公式（I）X R1 N Y（I）R2 R3定义的新型吡啶酮衍生物。该发明的化合物是代谢型受体亚型2（“mGluR2”）的正向变构调节剂，适用于治疗或预防与谷氨酸功能障碍相关的神经系统和精神障碍以及涉及代谢型受体亚型2的疾病。特别是，这些疾病是选择自焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病的一组。本发明还涉及制备这种化合物和组合物的制药组合物和制备过程，以及利用这种化合物预防和治疗涉及mGluR2的这些疾病的用途。
• DE2732848
  申请人：——

  公开号：——

  公开（公告）日：——
• AZIMOV, A. I.;DUSTMUXAMEDOV, T. T.;ABDULLAEV, U. A.;SAFAEV, M. A., ZH. ORGAN. XIMII, 1985, 21, N 9, 1983-1986
  作者：AZIMOV, A. I.、DUSTMUXAMEDOV, T. T.、ABDULLAEV, U. A.、SAFAEV, M. A.

  DOI：——

  日期：——