N-<2-<3,4-bis(benzyloxy)phenyl>ethyl>formamide | 84500-84-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: N-<2-<3,4-bis(benzyloxy)phenyl>ethyl>formamide
• 英文别名: N-[2-[3,4-bis(phenylmethoxy)phenyl]ethyl]formamide
• CAS: 84500-84-5
• 化学式: C₂₃H₂₃NO₃
• 分子量: 361.441
• InChiKey: PZHWCQGXUCLINS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  27
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  47.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-<2-<3,4-bis(benzyloxy)phenyl>ethyl>formamide 在 五氯化磷 作用下， 以 氯仿 为溶剂， 以65%的产率得到6,7-bis(benzyloxy)-3,4-dihydroisoquinoline
  参考文献：
  名称：

  Synthesis of 1-(aminomethyl)-1,2,3,4-tetrahydroisoquinolines and their actions at adrenoceptors in vivo and in vitro

  摘要：

  An improved synthesis of 1-(aminomethyl)-1,2,3,4-tetrahydroisoquinolines has been developed by using aluminum hydride reduction of 1-cyano-1,2,3,4-tetrahydroisoquinolines. Three 1-(aminomethyl)-6,7-dihydroxytetrahydroisoquinolines were tested for actions at beta adrenoceptors in order to examine a proposed similarity between this series and the related phenylethanolamines. The aminomethyl, (isopropylamino)methyl, and (tert-butylamino)methyl derivatives all showed weak partial agonist activity at beta adrenoceptors and the first also showed weak alpha adrenoceptor agonist activity in vivo. Their low potency implies that the catechol group of THIQ sympathomimetics, such as trimetoquinol, binds differently from that of the natural catecholamines. The protonation behavior of representative aminomethyl-THIQ's was investigated by pKa measurement and 1H and 13C NMR, and the compounds were shown to be substantially monoprotonated, on the exocyclic nitrogen, at physiological pH.

  DOI：

  10.1021/jm00358a010

文献信息

• Organocatalytic enantioselective synthesis of 1-vinyl tetrahydroisoquinolines through allenamide activation with chiral Brønsted acids
  作者：E. Manoni、A. Gualandi、L. Mengozzi、M. Bandini、P. G. Cozzi

  DOI：10.1039/c4ra14942d

  日期：——

  In this paper we present a new approach for the realization of tetrahydroisoquinoline scaffolds via stereoselective proto-activation of suitable allenamide precursors.

  在本文中，我们提出了一种新方法，通过对适当的亚砜前体进行立体选择性原位激活，实现四氢异喹啉骨架。
• Substituted pyridinone-containing trycyclic compounds, and methods using same
  申请人：ARBUTUS BIOPHARMA CORPORATION

  公开号：US10821103B2

  公开（公告）日：2020-11-03

  The present invention includes substituted pyridinone-containing tricyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infection in a patient. In certain embodiments, the compounds and compositions of the invention inhibit and/or reduce HBsAg secretion.

  本发明包括可用于治疗或预防患者乙型肝炎病毒（HBV）感染的含取代吡啶酮的三环化合物及其组合物。在某些实施方案中，本发明的化合物和组合物可以抑制和/或减少 HBsAg 的分泌。
• BEAUMONT, D.;WAIGH, R. D.;SUNBHANICH, METHI;NOTT, M. W., J. MED. CHEM., 1983, 26, N 4, 507-515
  作者：BEAUMONT, D.、WAIGH, R. D.、SUNBHANICH, METHI、NOTT, M. W.

  DOI：——

  日期：——
• SUBSTITUTED PYRIDINONE-CONTAINING TRYCYCLIC COMPOUNDS, AND METHODS USING SAME
  申请人：ARBUTUS BIOPHARMA CORPORATION

  公开号：US20190314347A1

  公开（公告）日：2019-10-17

  The present invention includes substituted pyridinone-containing tricyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infection in a patient. In certain embodiments, the compounds and compositions of the invention inhibit and/or reduce HBsAg secretion.