(R)-(+)-N-t-butoxycarbonyl-N-2-amino-7-ethoxycarbonylmethoxytetralin | 158223-18-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (R)-(+)-N-t-butoxycarbonyl-N-2-amino-7-ethoxycarbonylmethoxytetralin
• 英文别名: (R)-2-tert-butoxycarbonylamino-7-carbethoxymethoxytetraline；ethyl 2-[[(7R)-7-[(2-methylpropan-2-yl)oxycarbonylamino]-5,6,7,8-tetrahydronaphthalen-2-yl]oxy]acetate
• CAS: 158223-18-8
• 化学式: C₁₉H₂₇NO₅
• 分子量: 349.427
• InChiKey: JMEDEGMZBHSWAA-OAHLLOKOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  25
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  73.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (R)-(+)-N-t-butoxycarbonyl-N-2-amino-7-ethoxycarbonylmethoxytetralin 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 生成 (R)-(+)-2-amino-7-ethoxycarbonylmethoxytetralin
  参考文献：
  名称：

  Synthesis and β-adrenergic activity of atypical β-adrenergic phenylethanolaminotetralin stereoisomers

  摘要：

  A series of substituted phenylethanolaminotetralins were synthesized as pure stereoisomers and their ability to stimulate atypical beta-adrenoceptors selectively was evaluated. The compounds in vitro relative potencies were assessed using the atypical beta response of inhibition of rat proximal colon motility and the typical beta 1 (increase in guinea-pig right atrial frequency) and beta 2 (guinea-pig tracheal relaxation and rat uterus motility inhibition) responses. Compound 42 (SR 58611A) was found to be the most potent and selective.

  DOI：

  10.1016/0223-5234(94)90095-7
• 作为产物：
  描述：

  (R)-2-氨基-7-羟基四氢化萘 在 TEA 、 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 、 丙酮 为溶剂， 反应 9.0h， 生成 (R)-(+)-N-t-butoxycarbonyl-N-2-amino-7-ethoxycarbonylmethoxytetralin
  参考文献：
  名称：

  Synthesis and β-adrenergic activity of atypical β-adrenergic phenylethanolaminotetralin stereoisomers

  摘要：

  A series of substituted phenylethanolaminotetralins were synthesized as pure stereoisomers and their ability to stimulate atypical beta-adrenoceptors selectively was evaluated. The compounds in vitro relative potencies were assessed using the atypical beta response of inhibition of rat proximal colon motility and the typical beta 1 (increase in guinea-pig right atrial frequency) and beta 2 (guinea-pig tracheal relaxation and rat uterus motility inhibition) responses. Compound 42 (SR 58611A) was found to be the most potent and selective.

  DOI：

  10.1016/0223-5234(94)90095-7

文献信息

• 2-amino-7-hydroxytetraline ethers
  申请人：Sanofi

  公开号：US05159103A1

  公开（公告）日：1992-10-27

  2-amino-7-hydroxytetraline ethers of formula ##STR1## wherein R' represents methyl substituted by a carboxy group or lower carbalkoxy group or a salt thereof; a process for their preparation starting from the 2-amino-7-hydroxytetraline, N-protection, O-alkylation and N-deprotection; N-protected intermediates; and use of the compounds I for the preparation of the corresponding phenylethanolaminotetralines.

  公式为##STR1##的2-氨基-7-羟基四氢萘醚，其中R'代表甲基，被羧基或较低的碳酰氧基取代，或其盐；一种从2-氨基-7-羟基四氢萘开始制备它们的方法，包括N-保护、O-烷基化和N-去保护步骤；N-保护中间体；以及使用化合物I制备相应的苯乙醇胺四氢萘。
• Ethers de la 2-amino-7-hydroxytétraline
  申请人：ELF SANOFI

  公开号：EP0347313A2

  公开（公告）日：1989-12-20

  Ethers de la 2-amino-7-hydroxytétraline de formule dans laquelle R′ représente un méthyle substitué par un groupe carboxy ou carbalcoxy inférieur; un procédé pour leur préparation à partir de la 2-amino-7-hydroxytétraline, N-protection, O-alkylation et N-déprotection; intermédiaires N-protégés; et utilisation des composés I pour la préparation des phényléthanolaminotétralines cor­respondantes.

  2-氨基-7-羟基四氢萘的醚类，其式为 其中 R′代表被羧基或低级烷氧基取代的甲基；由 2-氨基-7-羟基四氢萘，N-保护，O-烷基化和 N-脱保护制备它们的工艺；N-保护的中间体；以及使用化合物 I 制备相应的苯乙醇胺四氢萘。
• US5202466A
  申请人：——

  公开号：US5202466A

  公开（公告）日：1993-04-13
• US5159103A
  申请人：——

  公开号：US5159103A

  公开（公告）日：1992-10-27
• Synthesis and β-adrenergic activity of atypical β-adrenergic phenylethanolaminotetralin stereoisomers
  作者：R Cecchi、T Croci、R Boigegrain、S Boveri、M Baroni、G Boccardi、JP Guimbard、U Guzzi

  DOI：10.1016/0223-5234(94)90095-7

  日期：1994.1

  A series of substituted phenylethanolaminotetralins were synthesized as pure stereoisomers and their ability to stimulate atypical beta-adrenoceptors selectively was evaluated. The compounds in vitro relative potencies were assessed using the atypical beta response of inhibition of rat proximal colon motility and the typical beta 1 (increase in guinea-pig right atrial frequency) and beta 2 (guinea-pig tracheal relaxation and rat uterus motility inhibition) responses. Compound 42 (SR 58611A) was found to be the most potent and selective.