4,6-dichloro-5-cyclopropylpyrimidine | 832754-14-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4,6-dichloro-5-cyclopropylpyrimidine
• CAS: 832754-14-0
• 化学式: C₇H₆Cl₂N₂
• 分子量: 189.044
• InChiKey: QYJUWWNELQCTCV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4,6-dichloro-5-cyclopropylpyrimidine 在 palladium 10% on activated carbon 、 盐酸羟胺 、 甲酸铵 、 sodium acetate 、 palladium diacetate 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 、 N,N-二异丙基乙胺 、 sodium t-butanolate 作用下， 以 N-甲基吡咯烷酮 、 甲醇 为溶剂， 反应 40.0h， 生成
  参考文献：
  名称：

  Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA

  摘要：

  We describe the design and synthesis of novel bicyclic spiro sulfonamides as potent Akt inhibitors. Through structure-based rational design, we have successfully improved PKA selectivity of previously disclosed spirochromanes. Representative compounds showed favorable Akt potency while exhibiting up to 1000-fold selectivity against PKA. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.02.098
• 作为产物：
  描述：

  5-Cyclopropyl-4,6-pyrimidindiol 在 N,N-二异丙基乙胺 、 三氯氧磷 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 48.0h， 以78%的产率得到4,6-dichloro-5-cyclopropylpyrimidine
  参考文献：
  名称：

  [EN] AKT PROTEIN KINASE INHIBITORS
  [FR] INHIBITEURS DE LA PROTEINE KINASE AKT

  摘要：

  公开号：

  WO2005051304A3

文献信息

• [EN] TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO<br/>[FR] DERIVES ARYLES ET HETEROARYLES TRISUBSTITUES UTILISES EN TANT QUE MODULATEURS DU METABOLISME ET PROPHYLAXIE ET TRAITEMENT DE TROUBLES AFFERENTS
  申请人：ARENA PHARM INC

  公开号：WO2005007647A1

  公开（公告）日：2005-01-27

  The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及公式（I）的某些三取代芳基和杂环芳基衍生物，它们是代谢调节剂。因此，本发明的化合物在预防或治疗代谢紊乱及其并发症，如糖尿病和肥胖方面是有用的。
• [EN] BRIDGED BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF<br/>[FR] DÉRIVÉS D'HÉTÉROCYCLES BICYCLIQUES PONTÉS ET LEURS PROCÉDÉS D'UTILISATION
  申请人：SCHERING CORP

  公开号：WO2010114958A1

  公开（公告）日：2010-10-07

  The present invention relates to Bridged Bicyclic Heterocycle Derivatives, compositions comprising a Bridged Bicyclic Heterocycle Derivative, and methods of using the Bridged Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.

  本发明涉及桥环双环杂环衍生物，包含桥环双环杂环衍生物的组合物，以及利用桥环双环杂环衍生物治疗或预防肥胖、糖尿病、代谢紊乱、心血管疾病或与患者GPCR活性有关的疾病的方法。
• AKT protein kinase inhibitors
  申请人：Mitchell S. Ian

  公开号：US20050130954A1

  公开（公告）日：2005-06-16

  The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

  本发明提供化合物，包括已解决的对映体、二对映异构体、溶剂化物和药学上可接受的盐，其包括公式：A-L-CR，其中CR是一个环核心基团，L是一个连接基团，A如此处所定义。同时提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗增殖性疾病如癌症的方法。
• Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
  申请人：Jones M. Robert

  公开号：US20050070562A1

  公开（公告）日：2005-03-31

  The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及公式（I）的某些三取代芳基和杂环芳基衍生物，其是代谢调节剂。因此，本发明的化合物对于预防或治疗代谢性疾病及其并发症（如糖尿病和肥胖症）是有用的。
• Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the phophylaxis and treatment of disorders related thereto
  申请人：Jones M. Robert

  公开号：US20070155763A1

  公开（公告）日：2007-07-05

  The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及公式（I）的某些三取代芳基和杂环芳基衍生物，它们是代谢调节剂。因此，本发明的化合物在预防或治疗代谢性疾病及其并发症方面是有用的，如糖尿病和肥胖症。