(R)-3-Boc-aminopiperidine | 948549-39-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (R)-3-Boc-aminopiperidine
• 英文别名: 3-Boc-amino piperidine；tert-butyl 1-aminopiperidine-3-carboxylate
• CAS: 948549-39-1
• 化学式: C₁₀H₂₀N₂O₂
• 分子量: 200.281
• InChiKey: BXHWWPNRUOHACS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  55.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2,4-二氯-3-硝基吡啶-6-羧酸 、 (R)-3-Boc-aminopiperidine 以 乙醇 为溶剂， 反应 48.0h， 生成 (R)-1-[2-hydroxycarbonyl-5-nitro-6 chloropyridin-4-yl]piperidine-3-carbamic acid tert-butyl ester
  参考文献：
  名称：

  FUSED PYRIDINE DERIVATIVES

  摘要：

  揭示了作为一般式(I)显示的融合吡啶衍生物以及它们的药用可接受盐、立体异构体或溶剂化物，属于药物技术领域。在式(I)中，R1、R2、R3、Q、X和Y的取代基的定义如描述中所述。还揭示了该化合物的制备方法、包含该化合物的药物组合物以及用于制造治疗和/或预防非胰岛素依赖性糖尿病、高血糖、高脂血症和胰岛素抵抗的药物的用途。

  公开号：

  US20120289497A1

文献信息

• [EN] FUNCTIONALIZED HETEROCYCLIC COMPOUNDS AS MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES FONCTIONNALISÉS UTILISÉS EN TANT QUE MODULATEURS DU STIMULATEUR DES GÈNES DE L'INTERFÉRON (STING)
  申请人：RYVU THERAPEUTICS S A

  公开号：WO2021116446A1

  公开（公告）日：2021-06-17

  The present invention relates to compound-linker constructs and antibody-drug-conjugates of compounds of formula (I) that are useful as modulators of STING (Stimulator of Interferon Genes).

  这项发明涉及化合物-连接物构造和化合物的抗体药物偶联物，其化学式为(I)，可用作STING（干扰素基因刺激剂）调节剂。
• [EN] HETEROCYCLIC COMPOUNDS AS MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES EN TANT QUE MODULATEURS DU STIMULATEUR DES GÈNES DE L'INTERFÉRON (STING)
  申请人：RYVU THERAPEUTICS S A

  公开号：WO2021116451A1

  公开（公告）日：2021-06-17

  The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.

  本发明涉及公式（I）的化合物及其盐、立体异构体、互变异构体或N-氧化物，这些化合物可用作STING（干扰素基因刺激剂）的调节剂。本发明还涉及公式（I）的化合物用作药物以及包含该类化合物的药物组合物。
• [EN] LIBRARIES OF PYRIDINE-CONTAINING MACROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING THE SAME<br/>[FR] BIBLIOTHÈQUES DE COMPOSÉS MACROCYCLIQUES CONTENANT DE LA PYRIDINE ET LEURS PROCÉDÉS DE PRÉPARATION ET D'UTILISATION
  申请人：CYCLENIUM PHARMA INC

  公开号：WO2018232506A1

  公开（公告）日：2018-12-27

  The present disclosure relates to novel pyridine-containing macrocyclic compounds and libraries thereof that are useful as research tools for drug discovery efforts. This disclosure also relates to methods of preparing these compounds and libraries and methods of using these libraries, such as in high throughput screening. In particular, these libraries are useful for evaluation of bioactivity at existing and newly identified pharmacologically relevant targets, including G protein-coupled receptors, nuclear receptors, enzymes, ion channels, transporters, transcription factors, protein-protein interactions and nucleic acid-protein interactions. As such, these libraries can be applied to the search for new pharmaceutical agents for the treatment and prevention of a range of medical conditions.

  本公开涉及新型含吡啶的大环化合物及其库，这些化合物对药物发现工作是有用的研究工具。本公开还涉及制备这些化合物和库的方法，以及使用这些库的方法，例如在高通量筛选中。特别是，这些库对评估现有和新鉴定的药理学相关靶点的生物活性是有用的，包括G蛋白偶联受体、核受体、酶、离子通道、转运蛋白、转录因子、蛋白质相互作用和核酸-蛋白质相互作用。因此，这些库可应用于寻找用于治疗和预防各种医疗状况的新药物。
• XANTHINE DERIVATIVE
  申请人：Chengdu Easton Pharmaceutical Co., Ltd.

  公开号：US20150183788A1

  公开（公告）日：2015-07-02

  The present invention discloses a xanthine derivative having the structure of the following general formula (I) or a pharmaceutically acceptable salt thereof; further discloses a preparation method for the xanthine derivative or a pharmaceutically acceptable salt thereof; and further discloses the use of the xanthine derivative or a pharmaceutically acceptable salt thereof. Through experiments of DPP-IV activity inhibition experiments in vitro, impact on glucose tolerance in normal mice and impact on blood glucose in spontaneous diabetic mice, it proves that the compounds and pharmaceutically acceptable salts thereof show good DPP-IV inhibition activity, can be applied to prepare medicines for treating dipeptidyl peptidase IV-related diseases, and more particularly, can be applied to the use of medicines for treating type II diabetes or diseases of abnormal glucose tolerance.

  本发明公开了具有以下一般式（I）的黄嘌呤衍生物或其药学上可接受的盐；进一步公开了该黄嘌呤衍生物或其药学上可接受的盐的制备方法；并进一步公开了该黄嘌呤衍生物或其药学上可接受的盐的用途。通过体外DPP-IV活性抑制实验、对正常小鼠葡萄糖耐量的影响以及对自发性糖尿病小鼠血糖的影响实验证明，这些化合物及其药学上可接受的盐表现出良好的DPP-IV抑制活性，可用于制备治疗二肽基肽酶IV相关疾病的药物，更具体地说，可用于治疗II型糖尿病或异常葡萄糖耐量疾病的药物的应用。
• METHOD FOR PREPARING AN IMPORTANT INTERMEDIATE OF LINAGLIPTIN
  申请人：2Y-CHEM, LTD.

  公开号：US20150274728A1

  公开（公告）日：2015-10-01

  The present invention discloses an improved process for preparing an important intermediate of linagliptin. In particular, disclosed are a process for preparing a compound V which is an important intermediate of linagliptin and has the structure V, and an industrial process of preparing linagliptin having excellent chemical and optical purities, which is an inhibitor of dipeptidyl peptidase-4 (DPP-IV), from the compound V. The process employs a phase-transfer catalyst, is high in yield, easy and simple to handle, environmentally friendly, suitable for industrial mass production, and can be implemented by a “one-pot process”.

  本发明公开了一种改进的制备利那格列汀重要中间体的工艺。具体公开了一种制备化合物V的工艺，该化合物V是利那格列汀的重要中间体，具有结构V，并且从化合物V中制备出具有优异化学和光学纯度的利那格列汀的工业工艺，利那格列汀是二肽基肽酶-4（DPP-IV）的抑制剂。该工艺采用相转移催化剂，产率高，易于操作和简单处理，环保，适合工业大规模生产，并且可以通过“一锅法”实施。