2,2-dimethylcyclopropylamine | 73434-10-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2,2-dimethylcyclopropylamine
• 英文别名: 2,2-Dimethylcyclopropan-1-amine
• CAS: 73434-10-3
• 化学式: C₅H₁₁N
• mdl: MFCD13368192
• 分子量: 85.149
• InChiKey: IVYCMLREPMLLEO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  6
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2,2-dimethylcyclopropylamine 在 sodium hydride 作用下， 以 1,4-二氧六环 、 乙醇 为溶剂， 反应 3.0h， 生成
  参考文献：
  名称：

  Fluoronaphthyridines and quinolones as antibacterial agents. 1. Synthesis and structure-activity relationship of new 1-substituted derivatives

  摘要：

  A series of novel 7-piperazinyl-1-substituted-6-fluoroquinolones and naphthyridines have been prepared and their antibacterial activities evaluated. These derivatives are characterized by having alkyl, alkenyl, arylalkyl, cycloalkyl, and cycloalkenyl groups at the 1-position. As a result of this study, derivatives 7 and 26, which are substituted with tert-butyl groups at N-1, were found to possess excellent in vitro and in vivo potency, particularly against Staphylococcus aureus, comparable to that of norfloxacin or ciprofloxacin. Structure-activity relationships of N-1 substituted alkyls and cycloalkyls are also discussed.

  DOI：

  10.1021/jm00123a005
• 作为产物：
  描述：

  N-(3-chloro-2,2-dimethylpropylidene)-1-phenylmethanamine 在 potassium tert-butylate 、 草酸 作用下， 以 四氢呋喃 、 甲醇 、 水 为溶剂， 反应 2.0h， 生成 2,2-dimethylcyclopropylamine
  参考文献：
  名称：

  Synthesis of 2,2-dialkylcyclopropylamines from β-chloroimines and application towards the synthesis of1-amino-2,2-dialkylcyclopropane-carboxylic acids

  摘要：

  DOI：

  10.1016/s0040-4020(01)86403-6

文献信息

• [EN] 2-QUINOLONE DERIVED INHIBITORS OF BCL6<br/>[FR] INHIBITEURS DE BCL6 DÉRIVÉS DE 2-QUINOLONE
  申请人：CANCER RESEARCH TECH LTD

  公开号：WO2018215798A1

  公开（公告）日：2018-11-29

  The present invention relates to compounds of formula I that function as inhibitors of BCL6(B- cell lymphoma 6) activity: Formula I wherein X1, X2, X3, R1, R2, R3, R4 and R5 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer,as well as other diseases or conditions in which BCL6 activity is implicated.

  本发明涉及作为BCL6（B细胞淋巴瘤6）活性抑制剂的I式化合物：式中X1、X2、X3、R1、R2、R3、R4和R5分别如本文所定义。本发明还涉及制备这些化合物的方法，包括含有它们的药物组合物，以及它们在治疗增生性疾病（如癌症）以及其他BCL6活性所涉及的疾病或病况中的用途。
• A new method for the preparation of 2,2-dialkylcyclopropylamines
  作者：Paul Sulmon、Norbert De Kimpe、Niceas Schamp

  DOI：10.1039/c39860001677

  日期：——

  2,2-Dialkylcyclopropylamines have been prepared by a new synthetic method involving base-induced cyclization of β-chloroimines and subsequent hydrolysis.

  已经通过一种新的合成方法制备了2，2-二烷基环丙胺，该方法涉及碱诱导的β-氯亚胺的环化和随后的水解。
• 6-SUBSTITUTED IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS
  申请人：Koppitz Marcus

  公开号：US20140135319A1

  公开（公告）日：2014-05-15

  The present invention relates to substituted imidazopyrazine compounds of general formula (I): in which R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

  本发明涉及通式（I）的取代咪唑吡嗪化合物，其中R1、R2、R3、R4和R5如权利要求所定义，以及制备该化合物的方法和中间体，包括该化合物的药物组合物和组合物，以及使用该化合物制造用于治疗或预防疾病的药物组合物，特别是用于治疗或预防增生性和/或血管生成异常的药物组合物，作为唯一的活性成分或与其他活性成分组合使用。
• 10.1021/acsmedchemlett.4c00249
  作者：Capstick, Rory A.、Bollinger, Sean R.、Engers, Julie L.、Long, Madeline F.、Chang, Sichen、Luscombe, Vincent B.、Rodriguez, Alice L.、Niswender, Colleen M.、Bridges, Thomas M.、Boutaud, Olivier、Conn, P. Jeffrey、Engers, Darren W.、Lindsley, Craig W.、Temple, Kayla J.

  DOI：10.1021/acsmedchemlett.4c00249

  日期：——

  details our efforts to develop novel tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM) scaffolds with improved pharmacological properties. This endeavor involved a “tie-back” strategy to replace the 3-amino-5-chloro-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide core, which led to the discovery of two novel tricyclic cores: an 8-chloro-9-methylpyrido[3′

  这封信详细介绍了我们开发新型三环毒蕈碱乙酰胆碱受体亚型 4 (M 4 ) 正变构调节剂 (PAM) 支架的努力，该支架具有改进的药理学特性。这项工作涉及“回接”策略来取代 3-氨基-5-氯-4,6-二甲基噻吩并[2,3- b ]吡啶-2-甲酰胺核心，从而发现了两个新型三环核心：8-氯-9-甲基吡啶并[3',2':4,5]噻吩并[3,2- d ]嘧啶-4-胺核心和8-氯-7,9-二甲基吡啶并[3',2' :4,5]呋喃[3,2- d ]嘧啶-4-胺核心。与母体化合物ML253相比，两种三环核心均表现出针对人 M 4 的低纳摩尔效力，并且大大降低了细胞色素 P450 抑制。
• Azetidines. 5. Reaction of 1,1,3,3-tetramethyl- and 1-benzyl-1,3,3-trimethylazetidinium ions with butyllithium and phenyllithium. Deuterium labeling as a mechanistic probe
  作者：Max. T. Wills、Irene E. Wills、Lawrence Von Dollen、Barry L. Butler、John Porter、Arthur G. Anderson

  DOI：10.1021/jo01300a046

  日期：1980.6