N-甲酰基-4-(二苯基甲基)哌啶 | 72964-01-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-甲酰基-4-(二苯基甲基)哌啶
• 英文名称: 1-Formyl-4-(diphenylmethyl)-piperidine
• 英文别名: N-formyl-4-(diphenylmethyl)piperidine；4-benzhydrylpiperidine-1-carbaldehyde
• CAS: 72964-01-3
• 化学式: C₁₉H₂₁NO
• 分子量: 279.382
• InChiKey: IHQJXDLHKZENCY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  N-甲酰基-4-(二苯基甲基)哌啶 在 光气 、 lithium aluminium tetrahydride 、 potassium carbonate 、 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 7.0h， 生成 4-(diphenylmethyl)-1-<<(8-hydroxyoctyl)imino>methyl>piperidine
  参考文献：
  名称：

  Antisecretory activity of human, dog, and rat metabolites of fenoctimine

  摘要：

  Fenoctimine (1a), a nonanticholinergic inhibitor of gastric acid secretion in dogs and rats, was evaluated as a gastric antisecretory agent in humans. In humans it exhibited weak antisecretory activity and caused anticholinergic-like side effects such as dry mouth and nasal passages. Studies of the metabolic fate of fenoctimine in humans, dogs, and rats provided structures of the resultant metabolites. These were synthesized and tested for antisecretory and anticholinergic activity. The human metabolites were all less active than fenoctimine as antisecretory agents, and some displayed significant anticholinergic activity. These results suggest that the unexpectedly weak effect of fenoctimine as a gastric antisecretory agent in humans, as well as anticholinergic effects, may be due to its extensive metabolism, which is different from that seen in dog and rat.

  DOI：

  10.1021/jm00388a025
• 作为产物：
  描述：

  4-(二苯基甲基)哌啶 、 甲乙酐 以71%的产率得到N-甲酰基-4-(二苯基甲基)哌啶
  参考文献：
  名称：

  4-（二苯甲基）-1-[（亚氨基）甲基]哌啶作为胃类抗分泌剂。

  摘要：

  4-（二苯甲基）-1-哌啶甲亚胺（1）是大鼠中一种有效的口服胃抗分泌剂，但含有强大的抗胆碱能成分。由于非抗胆碱能的胃分泌药物可用于治疗消化性溃疡，因此我们启动了一个程序，以1为基础找到这种药物。化合物1包含抗胆碱药阿托品和荷马平的共同结构要素。对这些化合物及其衍生物的构效关系的研究表明，某些修饰会减弱或消除抗胆碱能活性。将这些修饰应用于1的类似物的设计中，得到了抗分泌化合物4-（二苯甲基）-1-[（辛基氨基）甲基]哌啶（3h，芬辛胺），其没有抗胆碱能活性。

  DOI：

  10.1021/jm00358a014

文献信息

• Antisecretory 4-diphenylmethyl-1-[(oxoalkyl)imino]methyl-piperidines and
  申请人：McNeilab, Inc.

  公开号：US04370335A1

  公开（公告）日：1983-01-25

  4-Diphenyl-1-[(oxo and oxo-related alkyl)imino]methyl-piperidine derivatives are disclosed which are useful for the inhibition of gastric acid secretion.

  本发明揭示了4-二苯基-1-[(氧化和氧化相关的烷基)亚胺基甲基]-哌啶衍生物，用于抑制胃酸分泌。
• Substituted N-iminomethylpiperidines
  申请人：McNeilab, Inc.

  公开号：US04251655A1

  公开（公告）日：1981-02-17

  Substituted N-iminomethylpiperidines are disclosed which are useful for the inhibition of gastric acid secretion.

  本发明公开了可用于抑制胃酸分泌的N-亚甲基吡啶烷酮衍生物。
• Heteroaromatic derivatives of iminomethyl piperidines and use to inhibit
  申请人：McNeilab, Inc.

  公开号：US04528293A1

  公开（公告）日：1985-07-09

  Compounds of the following formula (I): ##STR1## wherein Alk is a straight or branched chain alkylene of about 1 to 12 carbons and R.sup.1 is a heterocyclic ring system, have been found to possess potent antisecretory activity and are thus useful in the treatment of hyperacidity.

  以下化合物具有如下式(I)：##STR1## 其中，Alk是由约1到12个碳组成的直链或支链烷基，R.sup.1是一个杂环环系统，已被发现具有强效的抗分泌活性，因此可用于治疗胃酸过多。
• Furan or thiophene derivatives of iminomethyl piperidines and use to
  申请人：McNeilab, Inc.

  公开号：US04594351A1

  公开（公告）日：1986-06-10

  Compounds of the following formula (I): ##STR1## wherein Alk is a straight or branched chain alkylene of about 1 to 12 carbons and R.sup.1 is a heterocyclic ring system, have been found to possess potent antisecretory activity and are thus useful in the treatment of hyperacidity.

  以下化合物的公式（I）：##STR1## 其中Alk是大约1到12个碳的直链或支链烷基，R.sup.1是杂环环系，已被发现具有强效的抗分泌活性，因此在治疗酸过多方面是有用的。
• 4-Diphenylmethyl-1-(oxoalkyl)imino)methyl-piperidines and their derivatives
  申请人：McNeilab, Inc.

  公开号：EP0087853A2

  公开（公告）日：1983-09-07

  4-diphenyl-1-[(oxo and oxo-related alkyl)imino]methylpiperidine derivatives are disclosed which are useful for the inhibition of gastric acid secretion.

  本研究公开了可用于抑制胃酸分泌的 4-二苯基-1-[（氧代和氧代相关烷基）亚氨基]甲基哌啶衍生物。