2-cyclopentylamino-1,9-dihydro-purin-6-one | 1236152-01-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: 2-cyclopentylamino-1,9-dihydro-purin-6-one
• 英文别名: Cyclopentyl guanine；2-(cyclopentylamino)-1,7-dihydropurin-6-one
• CAS: 1236152-01-4
• 化学式: C₁₀H₁₃N₅O
• 分子量: 219.246
• InChiKey: MYNLFDZUGRGJES-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  82.2
• 氢给体数：
  3
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  (6-chloro-9-trityl-9H-purin-2-yl)-cyclopentyl-amine 在 甲酸 作用下， 以 水 为溶剂， 反应 4.0h， 以95%的产率得到2-cyclopentylamino-1,9-dihydro-purin-6-one
  参考文献：
  名称：

  Concise access to N9-mono-, N2-mono- and N2,N9-di-substituted guanines via efficient Mitsunobu reactions

  摘要：

  Guanine poses several problems to the synthetic chemist owing to its polyfunctional nature and poor solubility. Over the past few decades, synthetic guanines have found applications as anti-cancer and anti-viral agents. Coupled with the ever-growing interest in designer PNAs and G-quartets, simple and efficient synthetic routes to novel guanines would be of significant benefit. We herein report that, upon simple protection and/or activation step(s), the guanine precursor 2-amino-6-chloropurine is rendered an excellent substrate for Mitsunobu chemistry, furnishing, after subsequent hydrolytic dechlorination and appropriate deprotection step(s), the desired N9-mono-, N2-mono- or N2,N9-di-substituted guanines in excellent yields (>= 80%). Importantly, we demonstrate that N9-functionalization proceeds with very good N9/N7 regioselectivity and with complete inversion of stereochemistry. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2010.03.118

文献信息

• Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)
  申请人：CHEN Han-Min

  公开号：US20140303112A1

  公开（公告）日：2014-10-09

  The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.

  本发明涉及一种治疗疾病或病情的方法，该疾病或病情容易通过AMPK激活剂和公式化合物得到改善，这些化合物有助于激活AMP激活蛋白激酶（AMPK），并将这些化合物用于预防或治疗疾病，包括糖尿病前期、2型糖尿病、X综合症、代谢综合征和肥胖症。
• [EN] PEPTIDE OLIGONUCLEOTIDE CONJUGATES<br/>[FR] CONJUGUÉS PEPTIDES/OLIGONUCLÉOTIDES
  申请人：SAREPTA THERAPEUTICS INC

  公开号：WO2016187425A1

  公开（公告）日：2016-11-24

  Provided herein are oligonucleotides, peptides, and peptide-oligonucleotide-conjugates. Also provided herein are methods of treating a muscle disease, a viral infection, or a bacterial infection in a subject in need thereof, comprising administering to the subject oligonucleotides, peptides, and peptide-oligonucleotide-conjugates described herein.

  本文提供寡核苷酸、肽和肽-寡核苷酸共轭物。本文还提供了治疗肌肉疾病、病毒感染或细菌感染的方法，包括向需要治疗的受试者注射本文所描述的寡核苷酸、肽和肽-寡核苷酸共轭物。
• Peptide oligonucleotide conjugates
  申请人：Sarepta Therapeutics, Inc.

  公开号：US10675356B2

  公开（公告）日：2020-06-09

  Provided herein are oligonucleotides, peptides, and peptide-oligonucleotide-conjugates. Also provided herein are methods of treating a muscle disease, a viral infection, or a bacterial infection in a subject in need thereof, comprising administering to the subject oligonucleotides, peptides, and peptide-oligonucleotide-conjugates described herein.

  本文提供的是寡核苷酸、肽和肽-寡核苷酸-共轭物。本文还提供了治疗有需要的受试者的肌肉疾病、病毒感染或细菌感染的方法，包括对受试者施用本文所述的寡核苷酸、多肽和多肽-寡核苷酸-结合物。
• OLIGONUCLEOTIDE FOR THE TREATMENT OF MUSCULAR DYSTROPHY PATIENTS
  申请人：Prosensa Technologies B.V.

  公开号：EP2870246A2

  公开（公告）日：2015-05-13
• METHODS AND MODIFICATIONS THAT PRODUCE ssRNAi COMPOUNDS WITH ENHANCED ACTIVITY, POTENCY AND DURATION OF EFFECT
  申请人：Smith, Larry J.

  公开号：EP3137606A1

  公开（公告）日：2017-03-08