3-t-butoxycarbonylamino-3-methyl-N-[2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-3(R)-yl]-butanamide | 145554-04-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 3-t-butoxycarbonylamino-3-methyl-N-[2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-3(R)-yl]-butanamide
• 英文别名: 3-t-butoxycarbonylamino-3-methyl-N-[2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-3-yl]-butanamide；tert-butyl N-[2-methyl-4-oxo-4-[(2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl)amino]butan-2-yl]carbamate
• CAS: 145554-04-7
• 化学式: C₂₀H₂₉N₃O₄
• 分子量: 375.468
• InChiKey: JTEPJIJJPBVTMB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  96.5
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-t-butoxycarbonylamino-3-methyl-N-[2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-3(R)-yl]-butanamide 在 盐酸 、 氢氧化钾 作用下， 以 二甲基亚砜 为溶剂， 生成 3-Amino-N-(1-biphenyl-4-ylmethyl-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-3-yl)-3-methyl-butyramide
  参考文献：
  名称：

  Naphtho-fused azepines as potent growth hormone secretagogues

  摘要：

  Computerguided improvements of known growth hormone secretagogues are reported. These are a new series of napthofused azepines. Structure-activity relationships are different than in the corresponding benzo-fused azepines. (C) 1997 Eisevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)10115-9
• 作为产物：
  描述：

  1,3,4,5-四氢-2H-1-苯并氮杂卓-2-酮 在 三甲基氯硅烷 、 氨 、 碘 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 sodium iodide 作用下， 生成 3-t-butoxycarbonylamino-3-methyl-N-[2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-3(R)-yl]-butanamide
  参考文献：
  名称：

  Naphtho-fused azepines as potent growth hormone secretagogues

  摘要：

  Computerguided improvements of known growth hormone secretagogues are reported. These are a new series of napthofused azepines. Structure-activity relationships are different than in the corresponding benzo-fused azepines. (C) 1997 Eisevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)10115-9

文献信息

• Benzo-fused lactams promote release of growth hormone
  申请人：Merck & Co., Inc.

  公开号：US05283241A1

  公开（公告）日：1994-02-01

  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. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed. ##STR1## Where L is ##STR2##

  已经披露了某些被识别为苯并融合内酰胺的新化合物，这些化合物促进人类和动物体内生长激素的释放。这种特性可以用来促进食用动物的生长，使可食用肉制品的生产更加高效，在人类中，可以增加那些患有正常生长激素分泌不足的人的身高。这些化合物是通过用取代酰胺功能取代氨内酰胺来制备的。含有这种苯并融合内酰胺作为活性成分的促生长组合物也已被披露。##STR1## 其中L是##STR2##
• Benzo-fused lactams that promote the release of growth hormone
  申请人：Merck & Co., Inc.

  公开号：US05206235A1

  公开（公告）日：1993-04-27

  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.

  已披露了一些新型化合物，被确定为苯并咪唑内酰胺，可促进人类和动物体内生长激素的释放。这种特性可以用于促进食用动物的生长，使可食用肉制品的生产更加高效，在人类身上，可以增加那些缺乏正常分泌天然生长激素的人的身高。还披露了含有苯并咪唑内酰胺作为活性成分的促生长组合物。
• A Novel 3-Substituted Benzazepinone Growth Hormone Secretagogue (L-692,429)
  作者：William R. Schoen、Judith M. Pisano、Kristine Prendergast、Matthew J. Wyvratt、Michael H. Fisher、Kang Cheng、Wanda W.-S. Chan、Bridget Butler、Roy G. Smith、Richard G. Ball

  DOI：10.1021/jm00033a006

  日期：1994.4

  The 3-substituted benzazepinone, L-692,429 (compound 1), is the prototype compound of a novel class of compounds that stimulate release of growth hormone (GH). The molecule evolved from efforts to identify a non-peptide mimic of the growth hormone-releasing hexapeptide, GHRP-6. Compound 1 is prepared by sequential attachment of dimethyl-beta-alanine and 2'-biphenylyltetrazole side chains to a chiral

  3-取代的苯并ze庚酮L-692,429（化合物1）是刺激生长激素（GH）释放的一类新型化合物的原型化合物。该分子是从努力确定释放生长激素的六肽GHRP-6的非肽模拟物演变而来的。通过将二甲基-β-丙氨酸和2'-联苯基基四唑侧链顺序连接到手性3-氨基苯并内酰胺核上来制备化合物1。1与相应的六元和八元内酰胺类似物的生物活性比较表明，七​​元苯并enza庚酮骨架是优选的。对结构多样的GH促分泌素L-692,429和GHRP-6进行了分子建模。
• Benzo-fused macrocycles promote release of growth hormone
  申请人：Merck & Co., Inc.

  公开号：US05438136A1

  公开（公告）日：1995-08-01

  There are disclosed certain novel compounds identified as benzo-fused macrocycles 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 macrocycles as the active ingredient thereof are also disclosed.

  本发明揭示了一些新型化合物，被确定为苯并螺环，可以促进人类和动物体内生长激素的释放。这种特性可以用来促进食用动物的生长，使可食用肉制品的生产更加高效，在人类中，可以增加那些缺乏正常分泌自然生长激素的人的身高。含有这些苯并螺环作为活性成分的促生长组合物也被揭示。
• 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。