1-[2-(5-Chloro-2-methoxybenzoylamino)ethyl]-1,6-dihydro-6-oxo-3-pyridinecarboxylic acid methyl ester

• 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: 1-[2-(5-Chloro-2-methoxybenzoylamino)ethyl]-1,6-dihydro-6-oxo-3-pyridinecarboxylic acid methyl ester
• 英文别名: methyl 1-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]-6-oxopyridine-3-carboxylate
• 化学式: C₁₇H₁₇ClN₂O₅
• 分子量: 364.785
• InChiKey: BNMKMYSBSNYYTR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  25
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  84.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  1-(2-aminoethyl)-1,6-dihydro-6-oxo-3-pyridinecarboxylic acid methyl ester 、 5-氯-2-甲氧基苯甲酰氯 在 silica gel 、 methanol-dichloromethane 作用下， 以 二氯甲烷 、 吡啶 为溶剂， 以gave the product, MP: 149°-150° C.的产率得到1-[2-(5-Chloro-2-methoxybenzoylamino)ethyl]-1,6-dihydro-6-oxo-3-pyridinecarboxylic acid methyl ester
  参考文献：
  名称：

  Arylcarbonylaminoalkyl-dihydro-oxo-pyridines, their production and their

  摘要：

  公开了公式I的芳基羰基氨基烷基二氢氧吡啶化合物，其中芳基是芳香或杂环芳香系统，n为0至5；R和R（1）为氢或低碳基；W为氢，（杂环）-（芳基）-低碳基；Z为氢，CH.sub.2 OR（2.sub.），CHO，（CO）OR（2），（CO）NR（2）.sub.2。还公开了化合物I的制备方法。化合物I适用于治疗心血管系统的疾病，例如高血压，心力衰竭或冠状动脉系统血流障碍，例如心绞痛。脑和周围血流的障碍也会受到有益的影响。此外，化合物I能够对子宫，支气管，肠道和胆道系统，尿路（输尿管，膀胱和尿道）的平滑肌器官产生影响，以实现平滑肌松弛。因此，它们也适用于治疗与这些器官痉挛有关的疾病，例如妊娠早产的治疗，输尿管或胆道绞痛，支气管哮喘，肠道运动障碍，例如肠易激综合征或膀胱失禁的治疗。此外，公式1的化合物可用作抗癫痫药物治疗癫痫病。

  公开号：

  US05360808A1

文献信息

• Pyridinylcarbonylaminoalkyl-dihydro-oxo-pyridines, their production and their use
  申请人：HOECHST AKTIENGESELLSCHAFT

  公开号：EP0556738A1

  公开（公告）日：1993-08-25

  Arylcarbonylaminoalkyl-dihydro-oxo-pyridines of Formula I are disclosed wherein aryl is an aromatic or heteroaromatic system, n is zero through 5; R and R(1), are hydrogen, or loweralkyl; W is hydrogen, (hetero)-(aryl)-loweralkyl; Z is hydrogen, CH₂OR(2), CHO, (CO)OR(2), (CO)NR(2)₂. Processes for the preparation of compound I are also disclosed. Compounds I are suitable for the treatment of disorders of the cardiovascular system, for example of hypertension, of cardiac insufficiency or of disturbances of blood flow in the coronary systems such as, for example, angina. Disturbances of cerebral and peripheral blood flow are likewise influenced beneficially. Furthermore, compounds I are able to influence smooth-muscle organs such as uterus, bronchi, intestines and biliary system, the urinary tract (ureter, bladder and urethra) in the sense of spasmolysis. They are therefore also suitable for the treatment of diseases associated with spasms of these organs, for example for the treatment of premature labor in pregnancy, of ureteral or biliary colic, of obstructive airway diseases such as asthma, of disturbances of intestinal motility such as, for example, of irritable colon or of bladder incontinence. Additionally, compounds of formula I can serve as anti-convulsants in the treatment of epilepsy and as hair growth inducers in the treatment of baldness.

  式 I 的芳基羰基氨基烷基二氢氧代吡啶 公开了式 I 的芳基羰基氨基烷基-二氢-氧代吡啶，其中芳基是芳香族或杂芳香族系统，n 是 0 到 5；R 和 R(1)是氢或低级烷基；W 是氢、（杂）-（芳基）-低级烷基；Z 是氢、CH₂OR(2)、CHO、(CO)OR(2)、(CO)NR(2)₂。 还公开了化合物 I 的制备工艺。 化合物 I 适用于治疗心血管系统疾病，例如高血压、心功能不全或冠状动脉系统血流紊乱，如心绞痛。大脑和外周血流的紊乱也同样会受到有益的影响。此外，I 号化合物还能影响平滑肌器官，如子宫、支气管、肠道和胆道系统、泌尿道（输尿管、膀胱和尿道）的痉挛溶解。因此，它们也适用于治疗与这些器官痉挛有关的疾病，例如治疗妊娠早产、输尿管或胆道绞痛、阻塞性气道疾病（如哮喘）、肠道蠕动紊乱（如结肠易激症）或膀胱失禁。此外，式 I 化合物还可作为抗惊厥药治疗癫痫，以及作为毛发生长促进剂治疗秃头。
• US5360808A
  申请人：——

  公开号：US5360808A

  公开（公告）日：1994-11-01
• Arylcarbonylaminoalkyl-dihydro-oxo-pyridines, their production and their
  申请人：Hoechst Aktiengesellschaft

  公开号：US05360808A1

  公开（公告）日：1994-11-01

  Arylcarbonylaminoalkyl-dihydro-oxo-pyridines of Formula I ##STR1## are disclosed wherein aryl is an aromatic or heteroaromatic system, n is zero through 5; R and R(1), are hydrogen, or loweralkyl; W is hydrogen, (hetero)-(aryl)-loweralkyl; Z is hydrogen, CH.sub.2 OR(2.sub.), CHO, (CO)OR(2), (CO)NR(2).sub.2. Processes for the preparation of compound I are also disclosed. Compounds I are suitable for the treatment of disorders of the cardiovascular system, for example of hypertension, of cardiac insufficiency or of disturbances of blood flow in the coronary systems such as, for example, angina. Disturbances of cerebral and peripheral blood flow are likewise influenced beneficially. Furthermore, compounds I are able to influence smooth-muscle organs such as uterus, bronchi, intestines and biliary system, the urinary tract (ureter, bladder and urethra) in the sense of spasmolysis. They are therefore also suitable for the treatment of diseases associated with spasms of these organs, for example for the treatment of premature labor in pregnancy, of ureteral or biliary colic, of obstructive airway diseases such as asthma, of disturbances of intestinal motility such as, for example, of irritable colon or of bladder incontinence. Additionally, compounds of formula 1 can serve as anticonvulsants in the treatment of epilepsy.

  公开了化合物I的结构，其中aryl是芳香或杂芳系统，n为0到5；R和R(1)为氢或低烷基；W为氢，(杂)－(芳基)－低烷基；Z为氢，CH.sub.2 OR(2.sub.)，CHO，(CO)OR(2)，(CO)NR(2).sub.2。还公开了化合物I的制备方法。化合物I适用于治疗心血管系统的疾病，例如高血压、心力衰竭或冠状动脉系统的血液流动障碍，如心绞痛等。脑部和周围血液流动障碍也会受到良好的影响。此外，化合物I能够影响子宫、支气管、肠道和胆道系统、泌尿道（输尿管、膀胱和尿道）的平滑肌器官，具有解痉作用。因此，它们也适用于治疗与这些器官痉挛相关的疾病，例如妊娠早产的治疗、输尿管或胆道绞痛、哮喘等梗阻性气道疾病、肠道蠕动障碍，如肠易激综合征或膀胱失禁等的治疗。此外，公式1的化合物也可作为抗癫痫药物治疗癫痫。