1-(β-chloro-ethyl)-2,2,6,6-tetramethyl-piperidine hydrochloride | 18377-31-6

• 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-(β-chloro-ethyl)-2,2,6,6-tetramethyl-piperidine hydrochloride
• 英文别名: 1-(2-chloroethyl)-2,2,6,6-tetramethylpiperidine hydrochloride；1-(2-chloroethyl)-2,2,6,6-tetramethylpiperidine;hydrochloride
• CAS: 18377-31-6
• 化学式: C₁₁H₂₂ClN*ClH
• 分子量: 240.216
• InChiKey: DNMXJUDVHUYAAQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.69
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  1-(β-chloro-ethyl)-2,2,6,6-tetramethyl-piperidine hydrochloride 、 2-巯基-5-甲氧基苯并咪唑 在 potassium carbonate 作用下， 以 水 、 乙酸乙酯 、 N,N-二甲基甲酰胺 为溶剂， 以1.25 g (80%)的产率得到5-methoxy-2-[2-(2,2,6,6-tetramethylpiperidin-1-yl)ethylthio]benzimidazole
  参考文献：
  名称：

  Piperidine compounds and antiulcer composition containing the same

  摘要：

  一种由式（I）表示的哌啶化合物：##STR1## 其中，R.sup.1表示氢原子，具有1至4个碳原子的低碳基，具有1至4个碳原子的低烷氧基，羟甲基基团，--CO.sub.2 R.sup.3，或##STR2##其中，R.sup.3表示氢原子或具有1至4个碳原子的低碳基；R.sup.4表示羟基，具有1至4个碳原子的低烷氧基或--NR.sup.6 R.sup.7（其中，R.sup.6和R.sup.7可以相同也可以不同，分别表示氢原子或具有1至4个碳原子的低碳基）；R.sup.5表示氢原子，具有1至4个碳原子的低烷酰基，或氯苯甲酰基；R.sup.2表示氢原子，具有1至4个碳原子的烷基，取代或未取代的苄基，或（2,2,6,6-四甲基哌啶-1-基）乙基基团；n表示0或1或2的整数，以及含有所述哌啶化合物的抗溃疡组合物。

  公开号：

  US05185347A1

文献信息

• Novel compounds
  申请人：——

  公开号：US20040242573A1

  公开（公告）日：2004-12-02

  The invention relates to thiophene carboxanmides of formula (I). wherein A, R 1 , R 2 , R 3 , n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. 1

  本发明涉及公式（I）的噻吩羧酰胺，其中A，R1，R2，R3，n和X如规范中定义的，以及用于其制备的工艺和中间体，含有它们的制药组合物以及它们在治疗中的使用。
• 5-PYRIDINONE SUBSTITUTED INDAZOLES
  申请人：Guzzo Peter Robert

  公开号：US20100105679A1

  公开（公告）日：2010-04-29

  Various 5-substituted 1-substituted indazoles are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.

  本文介绍了各种5-取代的1-取代吲唑类化合物，以及含有这些化合物的药物组合物和使用这些化合物治疗疾病的方法。还介绍了其他实施例。
• Novel Compounds
  申请人：Faull Alan

  公开号：US20110152234A1

  公开（公告）日：2011-06-23

  The invention relates to thiophene carboxamides of formula (I), wherein A, R 1 , R 2 , R 3 , n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

  该发明涉及式(I)的噻吩羧酰胺，其中A、R1、R2、R3、n和X如规范中所定义，以及用于其制备的过程和中间体，含有它们的制药组合物以及它们在治疗中的使用。
• Piperidine derivatives and antiulcer composition containing the same
  申请人：MEIJI SEIKA KAISHA LTD.

  公开号：EP0457331A1

  公开（公告）日：1991-11-21

  A piperidine derivative represented by formula (I): wherein R¹ represents a hydrogen atom, a substituted or unsubstituted lower alkyl group having from 1 to 4 carbon atoms, a substituted or unsubstituted lower alkoxy group having from 1 to 4 carbon atoms, a hydroxymethyl group, -CO₂R³, or wherein R³ represents a hydrogen atom or a lower alkyl group having from 1 to 4 carbon atoms; R⁴ represents a hydroxyl group, a lower alkoxy group having from 1 to 4 carbon atoms or -NR⁶R⁷ (wherein R⁶ and R⁷, which may be the same or different, each represent a hydrogen atom or a lower alkyl group having from 1 to 4 carbon atoms); and R⁵ represents a hydrogen atom, a lower alkanoyl group having from 1 to 4 carbon atoms, or a substituted or unsubstituted benzoyl group; R² represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, a substituted or unsubstituted benzyl group, or a (2,2,6,6-tetramethylpiperidin-1-yl)ethyl group; and n represents 0 or an integer of 1 or 2, and an antiulcer composition containing said piperidine derivative.

  式 (I) 所代表的哌啶衍生物： 其中 R¹ 代表氢原子、具有 1 至 4 个碳原子的取代或未取代的低级烷基、具有 1 至 4 个碳原子的取代或未取代的低级烷氧基、羟甲基、-CO₂R³，或 其中 R³ 代表氢原子或具有 1 至 4 个碳原子的低级烷基；R⁴ 代表羟基、具有 1 至 4 个碳原子的低级烷氧基或-NR⁶R⁷（其中 R⁶ 和 R⁷ 可以相同或不同，各自代表氢原子或具有 1 至 4 个碳原子的低级烷基）；和 R⁵ 代表氢原子、具有 1 至 4 个碳原子的低级烷酰基或取代或未取代的苯甲酰基； R² 代表氢原子、具有 1 至 4 个碳原子的烷基、取代或未取代的苄基或 (2,2,6,6-四甲基哌啶-1-基)乙基；和 n 代表 0 或 1 或 2 的整数、 以及含有所述哌啶衍生物的抗溃疡组合物。
• Synthesis and evaluation of the permeability transition inhibitory characteristics of paramagnetic and diamagnetic amiodarone derivatives
  作者：Tamás Kálai、Gábor Várbiró、Zita Bognár、Anita Pálfi、Katalin Hantó、Balázs Bognár、Erzsébet Ősz、Balázs Sümegi、Kálmán Hideg

  DOI：10.1016/j.bmc.2005.01.028

  日期：2005.4

  Several amiodarone analogues were synthesized varying the 2-substituent on the benzofuran ring and diethylaminoethyl side chain of phenolether by introducing 2,2,5,5-tetramethyl-2,5-dihydro-1H-pyrrole and 1,2,5,6-tetrahydropyridine nitroxides or their amino or hydroxylamino precursors. The new compounds were screened on isolated mitochondria and perfused heart and their toxicity was evaluated on WRL-68 liver cells and H9C2 cardiomyocytes. Most of the newly synthesized derivatives exerted uncoupling effect on the mitochondrial oxidative phosphorilation at higher concentrations, compared to amiodarone and one of the modified amiodarone analogues showed an effect similar to that of arniodarone on the mitochondrial permeability transition and on restoring of mitochondrial high-energy phosphate metabolites in perfused hearts. This arniodarone analogue can be new leading compound among the experimental arniodarone analogues with the same or enhanced efficiency of amiodarone, but with less side effects. (c) 2005 Elsevier Ltd. All rights reserved.