tert-butyl [1-(5-aminopyridin-2-yl)pyrrolidin-3-yl](methyl)carbamate | 748183-15-5

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: tert-butyl [1-(5-aminopyridin-2-yl)pyrrolidin-3-yl](methyl)carbamate
• 英文别名: Tert-butyl (1-(5-aminopyridin-2-yl)pyrrolidin-3-yl)(methyl)carbamate；tert-butyl N-[1-(5-aminopyridin-2-yl)pyrrolidin-3-yl]-N-methylcarbamate
• CAS: 748183-15-5
• 化学式: C₁₅H₂₄N₄O₂
• 分子量: 292.381
• InChiKey: QFRRVRBQMHXWFP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  71.7
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tert-butyl [1-(5-aminopyridin-2-yl)pyrrolidin-3-yl](methyl)carbamate 在 盐酸 、 三乙胺 作用下， 以 乙醚 、 二氯甲烷 为溶剂， 反应 8.0h， 生成 Biphenyl-4-carboxylic acid [6-(3-methylamino-pyrrolidin-1-yl)-pyridin-3-yl]-amide
  参考文献：
  名称：

  1-(4-Amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine derivatives as melanin-concentrating hormone receptor-1 antagonists

  摘要：

  Derivatives of 1-(4-amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine were identified as potent and functionally active MCH-R1 antagonists. One compound with K-i = 2.3 nM demonstrated good oral bioavailability (32%) and in vivo efficacy in rats. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.05.130
• 作为产物：
  描述：

  3-N-Boc-N-甲基氨基吡咯烷 在 palladium on activated charcoal 氢气 作用下， 以 四氢呋喃 、 乙腈 为溶剂， 反应 5.0h， 生成 tert-butyl [1-(5-aminopyridin-2-yl)pyrrolidin-3-yl](methyl)carbamate
  参考文献：
  名称：

  1-(4-Amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine derivatives as melanin-concentrating hormone receptor-1 antagonists

  摘要：

  Derivatives of 1-(4-amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine were identified as potent and functionally active MCH-R1 antagonists. One compound with K-i = 2.3 nM demonstrated good oral bioavailability (32%) and in vivo efficacy in rats. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.05.130

文献信息

• Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
  申请人：Aventis Pharma Deutschland GmbH

  公开号：US20040220191A1

  公开（公告）日：2004-11-04

  The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I 1 in which the radicals have the stated meanings, the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.

  这项发明涉及取代N-芳基杂环化合物及其生理耐受盐和生理功能衍生物。式I的化合物 1 其中基团具有所述含义，其N-氧化物及其生理耐受盐以及其制备方法被描述。这些化合物例如适用作为厌食剂。
• [EN] QUINOLINE DERIVATIVES AND MELK INHIBITORS CONTAINING THE SAME<br/>[FR] DÉRIVÉS DE QUINOLINE ET INHIBITEURS DE MELK LES CONTENANT
  申请人：ONCOTHERAPY SCIENCE INC

  公开号：WO2012016082A1

  公开（公告）日：2012-02-02

  The present invention directs a compound represented by formula (I).

  本发明涉及一种由化学式（I）表示的化合物。
• Diacylglycerol Acyltransferase Inhibitors
  申请人：Bolin David Robert

  公开号：US20090093497A1

  公开（公告）日：2009-04-09

  Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

  本文提供的是公式(I)的化合物，以及其药物可接受的盐，其中取代基如规范中所述。这些化合物和含有它们的药物组合物对于治疗疾病，例如肥胖症、2型糖尿病和代谢综合征是有用的。
• AZOLOPYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
  申请人：Devasthale Pratik

  公开号：US20110195934A1

  公开（公告）日：2011-08-11

  The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable faints thereof according to wherein all of the variables are defined herein.

  本申请提供了化合物，包括所有立体异构体、溶剂化物、前药和药学上可接受的盐，其中所有变量在此定义。
• AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
  申请人：Devasthale Pratik

  公开号：US20110218185A1

  公开（公告）日：2011-09-08

  The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein the variables are defined herein.

  本申请提供了一些化合物，它们可用作MCHR1拮抗剂，特别适用于治疗肥胖症，包括所有立体异构体、溶剂合物、前药和药学上可接受的I式形式，其中变量在此定义。