4-chloro-N-ethyl-N-methylpyrimidin-2-amine | 771556-83-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 4-chloro-N-ethyl-N-methylpyrimidin-2-amine
• 英文别名: (4-chloro-pyrimidin-2-yl)-ethyl-methyl-amine
• CAS: 771556-83-3
• 化学式: C₇H₁₀ClN₃
• 分子量: 171.63
• InChiKey: BUEGJOMEDWRFNB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  29
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2,4-二氯嘧啶 、 N-乙基甲基胺 以 四氢呋喃 为溶剂， 反应 2.0h， 以59%的产率得到2-氯-N-乙基-N-甲基-4-嘧啶胺
  参考文献：
  名称：

  嘧啶基联苯脲：识别新的铅化合物作为大麻素受体CB 1的变构调节剂。

  摘要：

  变构调节剂1-（4-氯苯基）-3-（3-（6-（吡咯烷基-1-基）吡啶-2-基）苯基）脲（PSNCBAM- 1，2）结合了大麻素受体1（CB 1）和拮抗的G蛋白偶联。该化合物表现出有效的厌食作用，类似于曾经出售用于治疗肥胖症的CB 1拮抗剂利莫那班，这为发现抗肥胖药提供了新的化学实体。为了增加这类CB 1配体的结构多样性，我们设计并合成了两类新型类似物，其中2的吡啶环被嘧啶环取代。这些积极地调节了CB 1的结合正构激动剂CP55,940，同时表现出对G蛋白偶联活性的拮抗作用。有趣的是，化合物7d和8d表现出通过β-arrestin介导的ERK1 / 2磷酸化，而正构CP55940则以G蛋白依赖性方式发生。这些可以用作未来CB 1变构调节剂发展的新的先导化合物，它们通过新的机理表现出偏向激动性和潜在的抗肥胖行为。

  DOI：

  10.1021/acs.jmedchem.6b01448

文献信息

• Novel quinoline, tetrahydroquinazoline, and pyrimidine derivatives and methods of treatment related to the use thereof
  申请人：Sekiguchi Yoshinori

  公开号：US20050197350A1

  公开（公告）日：2005-09-08

  The present invention relates to novel compounds of the Formula (I): which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

  本发明涉及一种新的化合物，其化学式为(I)，该化合物作为MCH受体拮抗剂。这些组合物在制药组合物中的应用包括预防或治疗改善记忆功能、睡眠和觉醒、焦虑、抑郁、情绪障碍、癫痫、肥胖症、糖尿病、食欲和进食障碍、心血管疾病、高血压、血脂异常、心肌梗死、暴食症包括贪食症、厌食症、精神障碍包括躁郁症、精神分裂症、谵妄、痴呆、压力、认知障碍、注意力缺陷障碍、物质滥用障碍和运动障碍包括帕金森病、癫痫和成瘾等。
• PYRIMIDINE DERIVATIVES AND METHODS OF TREATMENT RELATED TO THE USE THEREOF
  申请人：Sekiguchi Yoshinori

  公开号：US20090036448A1

  公开（公告）日：2009-02-05

  The present invention encompasses novel substituted pyrimidine compounds of Formula (I): which act as MCH receptor antagonists. These compounds are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

  本发明涵盖了新型取代嘧啶化合物的公式（I）：这些化合物作为MCH受体拮抗剂。这些化合物在制药组合物中的用途包括预防或治疗改善记忆功能、睡眠和觉醒、焦虑、抑郁、情绪障碍、癫痫、肥胖症、糖尿病、食欲和进食障碍、心血管疾病、高血压、血脂异常、心肌梗死、暴食症（包括贪食症和厌食症）、精神障碍（包括躁郁症、精神分裂症、谵妄、痴呆、压力、认知障碍、注意力缺陷障碍、物质滥用障碍和运动障碍（包括帕金森病、癫痫和成瘾）。
• QUINOLINE, TETRAHYDROQUINOLINE AND PYRIMIDINE DERIVATIVES AS MCH ANTAGONIST
  申请人：Taisho Pharmaceutical Co. Ltd.

  公开号：EP1464335A2

  公开（公告）日：2004-10-06

  The present invention relates to compounds of the Formula (I) wherein Q is: which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

  本发明涉及式（I）化合物 其中 Q 为 作为 MCH 受体拮抗剂的化合物。这些组合物可用于药物组合物中，其用途包括预防或治疗改善记忆功能、睡眠和唤醒、焦虑、抑郁、情绪障碍、癫痫发作、肥胖、糖尿病、食欲和进食障碍、心血管疾病、高血压、血脂异常、心肌梗塞、暴饮暴食症（包括贪食症）、厌食症、心肌梗塞、暴食症（包括贪食症）、厌食症、精神障碍（包括躁狂抑郁症）、精神分裂症、谵妄、痴呆、压力、认知障碍、注意力缺陷障碍、药物滥用障碍和运动障碍（包括帕金森病）、癫痫和成瘾。
• [EN] PYRIMIDINE DERIVATIVES AND METHODS OF TREATMENT RELATED TO THE USE THEREOF<br/>[FR] DERIVES DE PYRIMIDINE ET PROCEDES DE TRAITEMENT LIES A L'UTILISATION DE CEUX-CI
  申请人：TAISHO PHARMA CO LTD

  公开号：WO2005095357A3

  公开（公告）日：2006-01-19
• [EN] NOVEL QUINOLINE, TETRAHYDROQUINAZOLINE, AND PYRIMIDINE DERIVATIVES AND METHODS OF TREATMENT RELATED TO THE USE THEREOF<br/>[FR] NOUVEAUX DERIVES QUINOLINE, TETRAHYDROQUINAZOLINE ET PYRIMIDINE, PROCEDES DE TRAITEMENT EN LIAISON AVEC L'UTILISATION DE CES DERNIERS
  申请人：TAISHO PHARMA CO LTD

  公开号：WO2004087669A1

  公开（公告）日：2004-10-14

  The present invention relates to novel compounds of the Formula (I): which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.