3-(2-Tetrahydropyranyloxyethyl)-3-(3,4-dichlorophenyl)piperidine | 146395-81-5

• 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: 3-(2-Tetrahydropyranyloxyethyl)-3-(3,4-dichlorophenyl)piperidine
• 英文别名: 3-tetrahydropyranyloxyethyl-3-(3,4-dichlorophenyl)piperidine；3-(3,4-Dichlorophenyl)-3-(2-[tetrahydropyran-2-yloxy]ethyl)piperidine；3-(3,4-Dichlorophenyl)-3-[2-(tetrahydro-2-pyranyloxy)ethyl]piperidine；3-(3,4-dichlorophenyl)-3-[2-(oxan-2-yloxy)ethyl]piperidine
• CAS: 146395-81-5
• 化学式: C₁₈H₂₅Cl₂NO₂
• 分子量: 358.308
• InChiKey: MOEXBGWSMFSVPB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  30.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(2-Tetrahydropyranyloxyethyl)-3-(3,4-dichlorophenyl)piperidine 在 盐酸 、 sodium hydroxide 、 sodium chloride 作用下， 以 甲醇 、 水 为溶剂， 生成 3-(3,4-dichloro-phenyl)-3-(2-hydroxy-ethyl)-piperidine
  参考文献：
  名称：

  Polycyclic amine compounds and their enantiomers, their method of

  摘要：

  该发明涉及公式（I）的多环胺化合物 其中Y、m、Ar'、n、p、Q、T、q和Z在此处被定义。该发明还涉及制备公式（I）化合物的方法和含有公式（I）化合物的药物组合物。这些创新化合物可用作神经激肽受体拮抗剂，适用于治疗任何物质P依赖性和神经激肽依赖性的病理状况。

  公开号：

  US05340822A1
• 作为产物：
  描述：

  2-(2-溴乙氧基)四氢吡喃 在 镍 dimethyl sulfide borane 、 氢气 、 sodium hydride 、 lithium diisopropyl amide 作用下， 以 四氢呋喃 、 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 生成 3-(2-Tetrahydropyranyloxyethyl)-3-(3,4-dichlorophenyl)piperidine
  参考文献：
  名称：

  4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK2) receptor

  摘要：

  A library, evaluating a range of piperazines, piperidines and acyclic amines, as replacements for the 4-hydroxy-4-phenylpiperidine moiety in lead (1b) was prepared. These efforts identified the 4-((N)-benzimidazolone)piperidine analogue (2a) which was further optimised using classical single-compound synthesis to yield the 3-((N)-morpholino)azetidine (2j). Conformationally constrained analogues of (2j), generally offered no potency advantage in this particular series. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00343-3

文献信息

• 3-Azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists
  申请人：Pfizer Inc.

  公开号：US06242438B1

  公开（公告）日：2001-06-05

  The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.

  本发明提供了式(I)的化合物及其药用盐。这些化合物和盐是催吐肽拮抗剂。
• 1-azoniabicyclo[2.2.1] heptanes and pharmaceutical compositions in which
  申请人：Sanofi

  公开号：US05554763A1

  公开（公告）日：1996-09-10

  The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tri-cyclic aromatic or heteroaromatic group; T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C.sub.1 -C.sub.4, or a C.sub.1 -C.sub.5 -alkylene group; Ar' is an unsubstituted or mono- or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl; R is hydrogen or a C.sub.1 -C.sub.4 -alkyl, or a .omega.-C.sub.1 -C.sub.4 -alkoxy(C.sub.2 -C.sub.4)alkyl, or a .omega.-C.sub.2 -C.sub.4 -alkanoyloxy (C.sub.1 -C.sub.4)alkyl;. Q is hydrogen; or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group; Am.sup..sym. is the radical ##STR2## in which X.sub.1, X.sub.2 and X.sub.3, together with the nitrogen atom to which they are bonded, form an azabicyclic or azatricyclic system optionally substituted by a phenyl or benzyl group; and A.sup..crclbar. is a pharmaceutically acceptable anion. These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachykinin system.

  该发明涉及以下结构的四元碱性酰胺：其中Ar是可选择取代的单、双或三环芳香族或杂芳族基团；T是直接键、羟甲亚基、烷氧基甲亚基（其中烷氧基是C.sub.1 -C.sub.4）、或C.sub.1 -C.sub.5 烷基亚基；Ar'是未取代或单或多取代的苯基、噻吩基、苯并噻吩基、萘基或吲哚基；R是氢或C.sub.1 -C.sub.4 烷基，或.ω.-C.sub.1 -C.sub.4 烷氧基(C.sub.2 -C.sub.4)烷基，或.ω.-C.sub.2 -C.sub.4 烷酰氧基(C.sub.1 -C.sub.4)烷基；Q是氢；或者Q和R一起形成1,2-乙烯基、1,3-丙烷基或1,4-丁烷基；Am.sup..sym.是基团：其中X.sub.1、X.sub.2和X.sub.3与它们连接的氮原子一起形成一个可能被苯基或苄基取代的氮杂双环或氮杂三环系统；A.sup..crclbar.是一种药用可接受的阴离子。这些化合物可用于制备用于治疗涉及缓激肽系统的病理状况的药物。
• Polycyclic amine compounds and their enantiomers, their method of
  申请人：Elf Sanofi

  公开号：US05340822A1

  公开（公告）日：1994-08-23

  The invention relates to polycyclic amine compounds of formula (I) ##STR1## where Y. m. Ar', n, p, Q, T, q and Z are defined herein. The invention also relates to methods of making the compounds of formula (I) and pharmaceutical compositions which contain the compounds of formula (I). The inventive compounds are useful as neurokinin receptor antagonists, and are useful for the treatment of any substance P-dependent and neurokinin-dependent pathological condition.

  该发明涉及公式（I）的多环胺化合物 其中Y、m、Ar'、n、p、Q、T、q和Z在此处被定义。该发明还涉及制备公式（I）化合物的方法和含有公式（I）化合物的药物组合物。这些创新化合物可用作神经激肽受体拮抗剂，适用于治疗任何物质P依赖性和神经激肽依赖性的病理状况。
• Quaternary basic amides, method of preparing them and pharmaceutical
  申请人：Sanofi

  公开号：US05712288A1

  公开（公告）日：1998-01-27

  The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tri-cyclic aromatic or heteroaromatic group; T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C.sub.1 -C.sub.4, or a C.sub.1 -C.sub.5 -alkylene group; Ar' is an unsubstituted or mono- or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl; R is hydrogen or a C.sub.1 -C.sub.4 -alkyl, or a C.sub.1 -C.sub.4 -.omega.-alkoxy(C.sub.2 -C.sub.4)alkyl, or a C.sub.2 -C.sub.4 -.omega.-alkanoyloxy (C.sub.1 -C.sub.4)alkyl; Q is hydrogen; or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group; Am.sup..sym. is the radical ##STR2## in which X.sub.1, X.sub.2 and X.sub.3, together with the nitrogen atom to which they are bonded, form a 1-azoniabicyclo\x9b2.2.2!octane optionally substituted by a phenyl or benzyl group; and A.sup..crclbar. is a pharmaceutically acceptable anion. These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachykinin system.

  本发明涉及公式##STR1##中的季铵基酰胺，其中Ar是一个可选的取代的单环、双环或三环芳香或杂芳基团；T是直接键，羟甲基烷基，其中烷氧基是C.sub.1-C.sub.4，或C.sub.1-C.sub.5-烷基烷基；Ar'是未取代或单取代或多取代的苯基、噻吩基、苯并噻吩基、萘基或吲哚基；R是氢或C.sub.1-C.sub.4-烷基，或C.sub.1-C.sub.4-ω-烷氧基(C.sub.2-C.sub.4)烷基，或C.sub.2-C.sub.4-ω-酰氧基(C.sub.1-C.sub.4)烷基；Q是氢；或者Q和R一起形成1,2-乙烯基、1,3-丙烯基或1,4-丁烷基；Am.sup..sym.是基团##STR2##其中X.sub.1、X.sub.2和X.sub.3与它们连接的氮原子一起形成一个可选取代的苯基或苄基的1-氮杂双环[2.2.2]辛烷；A.sup..crclbar.是一种药学上可接受的阴离子。这些化合物可用于制备用于治疗涉及Tachykinin系统的病理状况的药物。
• 1-azoniabicyclo[2.2.2] octanes and pharmaceutical compositions in which
  申请人：Sanofi

  公开号：US05583134A1

  公开（公告）日：1996-12-10

  The present invention relates to quaternary basic amides of the formula: ##STR1## These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachkinin system.

  本发明涉及公式为：##STR1## 的季铵基酰胺。这些化合物可用于制备用于治疗涉及缩氨酸系统的病理状况的药物。