1-(2-aminoethyl)-4-hydroxy-4-phenyl-piperidine | 56079-76-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-(2-aminoethyl)-4-hydroxy-4-phenyl-piperidine
• 英文别名: 1-(2-Aminoethyl)-4-phenylpiperidin-4-ol
• CAS: 56079-76-6
• 化学式: C₁₃H₂₀N₂O
• 分子量: 220.315
• InChiKey: RVRCVAKZCDNBIT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  49.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(2-aminoethyl)-4-hydroxy-4-phenyl-piperidine 以 苯 为溶剂， 生成 3-[2-(4-羟基-4-苯基哌啶-1-基)乙基]-2-(4-硝基苯基)-1,3-噻唑烷-4-酮
  参考文献：
  名称：

  Diurno; Mazzoni; Capasso, Il Farmaco, 1997, vol. 52, # 4, p. 237 - 241

  摘要：

  DOI：
• 作为产物：
  描述：

  4-苯基-4-羟基哌啶 在 一水合肼 、 三乙胺 作用下， 以 甲醇 、 乙腈 为溶剂， 反应 54.0h， 生成 1-(2-aminoethyl)-4-hydroxy-4-phenyl-piperidine
  参考文献：
  名称：

  Diurno; Mazzoni; Capasso, Il Farmaco, 1997, vol. 52, # 4, p. 237 - 241

  摘要：

  DOI：

文献信息

• Therapeutic method of treating cardiac arrhythmias utilizing
  申请人：Miles Laboratories, Inc.

  公开号：US04006232A1

  公开（公告）日：1977-02-01

  3-substituted-5,5-diphenylhydantoin derivatives in which the 5,5-diphenylhydantoin moiety is attached at C.sub.3 by a loweralkylene bridge to a 4-phenyl-1-piperidyl, 4-hydroxy-4-phenyl-1-piperidyl, 4-phenyl-1,2,3,6-tetrahydropyridyl, 4-phenyl-1-piperazinyl, or loweralkylamino group are useful in the treatment of cardiac arrhythmias in mammals. One or both of the 5,5-diphenyl substituents optionally can be substituted in the ortho-, meta-, or para-positions with halogeno, lowerakyl, loweralkoxy, amino or nitro groups.

  3-取代-5,5-二苯基海达嗪衍生物，其中5,5-二苯基海达嗪基团通过较低的烷基桥连接到C.sub.3处，形成4-苯基-1-哌啶基、4-羟基-4-苯基-1-哌啶基、4-苯基-1,2,3,6-四氢吡啶基、4-苯基-1-哌嗪基或较低的烷基氨基团，在哺乳动物心律失常的治疗中是有用的。其中一个或两个5,5-二苯基取代基可以选择性地在邻位、间位或对位与卤素、较低烷基、较低烷氧基、氨基或硝基团进行取代。
• 3-Imidazolyl-Indoles for the Treatment of Proliferative Diseases
  申请人：Boettcher Andreas

  公开号：US20100125064A1

  公开（公告）日：2010-05-20

  The invention relates to 3-heterocyclyl indolyl compounds capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, said compounds having the formula I, wherein R 1 , R 2 , R 3 , R 4 , R A , Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.

  本发明涉及能够抑制p53或其变体与MDM2和/或MDM4或其变体相互作用的3-杂环基吲哚化合物，其中所述化合物具有式I，其中R1、R2、R3、R4、RA、Y和Y的定义见说明书。由于其活性，这些化合物可用于治疗由MDM2和/或MDM4或其变体介导的各种疾病和疾病，例如炎症性或增殖性疾病或细胞保护。
• N-[(Amino)Alkyl]-1-pyrrolidine, 1-piperidine and 1-homopiperidinecarboxamides (and thiocarboxamides) with sulphur linked substitution in the 2, 3 or 4-position
  申请人：A.H. ROBINS COMPANY, INCORPORATED

  公开号：EP0160436A2

  公开（公告）日：1985-11-06

  Pyrrolidine, piperidine and homopiperidine- carboxamide and thiocarboxamide compounds of the formula: wherein X is -S-, -S(0)- or -S(0)2-; A is a loweralkalene chain and A1 and A2 are alkalene chains when p and d are one; R, R1 and R2 are hydrogen, loweralkyl, phenyl cycloalkyl or phenylalkyl and R1 and R2 may form a heterocyclic residue with the adjacent nitrogen atom; Q is a selected aromatic radical, and the pharmaceutically acceptable acid addition salts are useful as cardiac antiarrhythmia agents. Chemical intermediates, unsubstituted on pyrrolidine, piperidine and homopiperidine nitrogen but with the -(A2)p-X-(A2)d-Q side chain are also disclosed.

  式中的吡咯烷、哌啶和均哌啶-羧酰胺和硫代羧酰胺化合物： 其中，X 是-S-、-S(0)- 或-S(0)2-；A 是低级烯烃链，当 p 和 d 为 1 时，A1 和 A2 是烯烃链；R、R1 和 R2 是氢、低级烷基、苯基环烷基或苯基烷基，R1 和 R2 可与相邻的氮原子形成杂环残基；Q 是选定的芳香基，药学上可接受的酸加成盐可用作抗心律失常剂。 还公开了吡咯烷、哌啶和高哌啶氮上未取代但具有-(A2)p-X-(A2)d-Q 侧链的化学中间体。
• 1-[(Aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl]-alpha,alpha-diarylpyrrolidine, piperidine and homopiperidineacetamides and acetonitriles
  申请人：A.H. ROBINS COMPANY, INCORPORATED

  公开号：EP0178947A2

  公开（公告）日：1986-04-23

  1-(Aminoalkyl and aminoalkylamino) carbonyl and thiocarbonyl-a, α-diaryl-pyrrolidine, piperidine and homopiperidineacetamides and acetonitriles having the formula: wherein: n is zero, one or two; X is oxygen or sulphur; Z is p is 0 to 5 inclusive with the proviso that when Z is p is at least one; Y is aminocarbonyl or cyano; Ar' and Ar2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl; R is hydrogen or loweralkyl; R1, R2 and R3 are hydrogen, cycloalkyl, loweralkyl, phenyl, substituted phenyl, phenyl-loweralkyl, and R2 and R3 taken with the adjacent nitrogen may form a heterocyclic residue, (including diastereoisomers when possible) and pharmaceutical salts; are disclosed as having cardiac antiarrhythmic activity.

  式中的 1-(氨基烷基和氨基烷基氨基)羰基和硫代羰基-a、α-二基吡咯烷、哌啶和均哌啶乙酰胺和乙腈： 其中 n 为 0、1 或 2； X 是氧或硫 Z 是 p 为 0 至 5（包括 5），但当 Z 是 p 至少为 1； Y 是氨基羰基或氰基； Ar'和Ar2是2、3或4-吡啶基、苯基或取代苯基； R 是氢或低级烷基； R1、R2 和 R3 是氢、环烷基、低级烷基、苯基、取代苯基、苯基-低级烷基，R2 和 R3 与相邻的氮可形成杂环残基（可能时包括非对映异构体）和药用盐。
• 3-IMIDAZOLYL-INDOLES FOR THE TREATMENT OF PROLIFERATIVE DISEASES
  申请人：Novartis AG

  公开号：EP2142535A2

  公开（公告）日：2010-01-13