5-[4-(4-Methylphenyl)phenyl]-1-trityltetrazole | 1429045-73-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: 5-[4-(4-Methylphenyl)phenyl]-1-trityltetrazole
• CAS: 1429045-73-7
• 化学式: C₃₃H₂₆N₄
• 分子量: 478.596
• InChiKey: VZWDAFNBVCCHTJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8
• 重原子数：
  37
• 可旋转键数：
  6
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  43.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-[4-(4-Methylphenyl)phenyl]-1-trityltetrazole 在 盐酸 、 N-溴代丁二酰亚胺(NBS) 、 水 、 potassium carbonate 、 过氧化苯甲酰 作用下， 以 四氢呋喃 、 四氯化碳 、 N,N-二甲基甲酰胺 为溶剂， 反应 30.0h， 生成 4-[[4-[4-(2H-tetrazol-5-yl)phenyl]phenyl]methylsulfanyl]quinazoline
  参考文献：
  名称：

  Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors

  摘要：

  The latest scientific findings concerning PDE7 and PDE4 inhibition suggest that selective small-molecule inhibitors of both enzymes could provide a novel approach to treat a variety of immunological diseases. In this context, we describe a new series of quinazoline derivatives from quinazolin-4-thiones which include a substituted biphenyl fragment. Some of these compounds show inhibitory potencies at sub-micromolar levels against the catalytic domain of PDE7. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2013.01.067
• 作为产物：
  描述：

  三丁基(对甲苯基)锡烷 在 bis-triphenylphosphine-palladium(II) chloride 、 sodium azide 、 三丁基氯化锡 、 lithium chloride 作用下， 以 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 73.0h， 生成 5-[4-(4-Methylphenyl)phenyl]-1-trityltetrazole
  参考文献：
  名称：

  Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors

  摘要：

  The latest scientific findings concerning PDE7 and PDE4 inhibition suggest that selective small-molecule inhibitors of both enzymes could provide a novel approach to treat a variety of immunological diseases. In this context, we describe a new series of quinazoline derivatives from quinazolin-4-thiones which include a substituted biphenyl fragment. Some of these compounds show inhibitory potencies at sub-micromolar levels against the catalytic domain of PDE7. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2013.01.067

文献信息

• Novel benzo-fused lactams that promote the release of growth hormone
  申请人：MERCK & CO. INC.

  公开号：EP0513974A1

  公开（公告）日：1992-11-19

  There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositiors containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

  已公开的某些新型化合物被确定为苯并融合内酰胺，可促进人和动物体内生长激素的释放。这种特性可用于促进食用动物的生长，使可食用肉类产品的生产更有效率，也可用于提高那些缺乏正常天然生长激素分泌的人的身材。此外，还公开了以此类苯并内酰胺为活性成分的促进生长复合剂。
• US5206235A
  申请人：——

  公开号：US5206235A

  公开（公告）日：1993-04-27
• US5310737A
  申请人：——

  公开号：US5310737A

  公开（公告）日：1994-05-10
• [EN] BENZO-FUSED LACTAMS PROMOTE RELEASE OF GROWTH HORMONE
  申请人：——

  公开号：WO1992016524A1

  公开（公告）日：1992-10-01

  [FR] L'invention concerne de nouveaux composés identifiés comme étant des lactames à fusion benzo, qui favorisent la sécrétion de l'hormone de croissance chez les hommes et les animaux. Cette propriété peut être utilisée pour stimuler la croissance d'animaux destinés à la production de produits alimentaires, pour rendre la production de produit à base de viande plus efficace, et chez les hommes, pour développer la taille de ceux affligés par un manque de sécrétion normale de l'hormone de croissance naturelle. L'invention concerne également des compositions favorisant la croissance contenant de tels lactames à fusion benzo comme ingrédient actif.
  [EN] There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
• Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors
  作者：Ana I. Sánchez、Valentín Martínez-Barrasa、Carolina Burgos、Juan J. Vaquero、Julio Alvarez-Builla、Emma Terricabras、Víctor Segarra

  DOI：10.1016/j.bmc.2013.01.067

  日期：2013.4

  The latest scientific findings concerning PDE7 and PDE4 inhibition suggest that selective small-molecule inhibitors of both enzymes could provide a novel approach to treat a variety of immunological diseases. In this context, we describe a new series of quinazoline derivatives from quinazolin-4-thiones which include a substituted biphenyl fragment. Some of these compounds show inhibitory potencies at sub-micromolar levels against the catalytic domain of PDE7. (C) 2013 Elsevier Ltd. All rights reserved.