4-[(Naphthalene-1-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester | 192130-27-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 4-[(Naphthalene-1-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester
• 英文别名: Tert-butyl 4-[(naphthalen-1-ylsulfonylamino)methyl]piperidine-1-carboxylate
• CAS: 192130-27-1
• 化学式: C₂₁H₂₈N₂O₄S
• 分子量: 404.53
• InChiKey: GLCJNOJTHYYRRL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  84.1
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-[(Naphthalene-1-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester 在 盐酸 、 三乙胺 作用下， 以 乙酸乙酯 为溶剂， 生成 {4-[(Naphthalene-1-sulfonylamino)-methyl]-piperidin-1-yl}-acetic acid ethyl ester
  参考文献：
  名称：

  Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: substituted benzo[a]cycloheptene derivatives

  摘要：

  Novel berizo[a]cycloheptene derivatives were prepared for the purpose of searching new neuropeptide Y-Y5 (NPY-Y5) receptor antagonists, The structure activity relationships Lire described and compound 2o (FR226928) showed the most potent affinity for Y5 receptor of all we prepared and was found to have higher potency and better selectivity for Y5 over Y1 receptor affinities when compared with the known lead compound 1. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00002-1
• 作为产物：
  描述：

  1-叔丁氧羰基-4-哌啶甲酰胺 在 lithium aluminium tetrahydride 、 三乙胺 作用下， 生成 4-[(Naphthalene-1-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester
  参考文献：
  名称：

  Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: substituted benzo[a]cycloheptene derivatives

  摘要：

  Novel berizo[a]cycloheptene derivatives were prepared for the purpose of searching new neuropeptide Y-Y5 (NPY-Y5) receptor antagonists, The structure activity relationships Lire described and compound 2o (FR226928) showed the most potent affinity for Y5 receptor of all we prepared and was found to have higher potency and better selectivity for Y5 over Y1 receptor affinities when compared with the known lead compound 1. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00002-1

文献信息

• [EN] HETEROARYL COMPOUNDS<br/>[FR] COMPOSES HETEROARYLES
  申请人：NOVARTIS AG

  公开号：WO1997020820A1

  公开（公告）日：1997-06-12

  (EN) The invention relates to a method of treatment of disorders and diseases associated with NPY receptor subtype Y5 comprising administering to a warm-blooded animal, including man, in need of such treatment a therapeutically effective amount of a compound of formula (I) in which the variables are as defined and relates to new compounds of formula (I) or a salt thereof, to pharmaceutical compositions, and to the manufacture of new compounds of formula (I) and salts thereof.(FR) L'invention concerne une méthode de traitement de troubles et maladies associés au sous-type Y5 du récepteur du neuropeptide Y, laquelle consiste à administrer à un animal à sang chaud nécessitant un tel traitement, notamment à l'homme, une dose efficace sur le plan thérapeutique d'un composé de la formule (I) dans laquelle les variables sont telles que définies. L'invention se rapporte également à des nouveaux composés de la formule (I) ou à un sel de ceux-ci, à des compositions pharmaceutiques ainsi qu'à la production de ces nouveaux composés et des sels de ceux-ci.
• Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: substituted benzo[a]cycloheptene derivatives
  作者：Hiromichi Itani、Harunobu Ito、Yoshihiko Sakata、Yoshifumi Hatakeyama、Hiroko Oohashi、Yoshinari Satoh

  DOI：10.1016/s0960-894x(02)00002-1

  日期：2002.3

  Novel berizo[a]cycloheptene derivatives were prepared for the purpose of searching new neuropeptide Y-Y5 (NPY-Y5) receptor antagonists, The structure activity relationships Lire described and compound 2o (FR226928) showed the most potent affinity for Y5 receptor of all we prepared and was found to have higher potency and better selectivity for Y5 over Y1 receptor affinities when compared with the known lead compound 1. (C) 2002 Elsevier Science Ltd. All rights reserved.