哌啶,4-[2-(1-甲基乙氧基)苯基]- | 148583-58-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 哌啶,4-[2-(1-甲基乙氧基)苯基]-
• 英文名称: 4-(2-isopropoxy-phenyl)-piperidine
• 英文别名: 4-(2-Isopropoxyphenyl)piperidine；4-(2-propan-2-yloxyphenyl)piperidine
• CAS: 148583-58-8
• 化学式: C₁₄H₂₁NO
• 分子量: 219.327
• InChiKey: AOLUCIWIXNUYDZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  哌啶,4-[2-(1-甲基乙氧基)苯基]- 在 三乙酰氧基硼氢化钠 、 sodium carbonate 、 溶剂黄146 、 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 20.0h， 生成 JNJ-26218127
  参考文献：
  名称：

  (Phenylpiperidinyl)cyclohexylsulfonamides: Development of α1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS)

  摘要：

  Although alpha(1), adrenergic receptor blockers can be very effective for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS), their usage is limited by CV-related side-effects that are caused by the subtype non-selective nature of the current drugs. To overcome this problem, it was hypothesized that a alpha(1a/1d) subtype selective antagonist would bring more benefit for the therapy of BPH/LUTS. In developing such selective alpha(1a/1d) ligands, a series of (phenylpiperidinyl)cyclohexylsulfonamides has been synthesized and evaluated for binding to three cloned human alpha(1)-adrenergic receptor subtypes. Many compounds showed equal affinity for both alpha(1a) and alpha(1d) subtypes with good selectivity versus the alpha(1b) subtype. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.04.098
• 作为产物：
  描述：

  1-溴-2-异丙氧基苯 在 palladium on activated charcoal 正丁基锂 、 氢气 、 甲基磺酰氯 、 三乙胺 、 三氟乙酸 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， -78.0~20.0 ℃ 、310.27 kPa 条件下， 反应 24.0h， 生成 哌啶,4-[2-(1-甲基乙氧基)苯基]-
  参考文献：
  名称：

  (Phenylpiperidinyl)cyclohexylsulfonamides: Development of α1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS)

  摘要：

  Although alpha(1), adrenergic receptor blockers can be very effective for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS), their usage is limited by CV-related side-effects that are caused by the subtype non-selective nature of the current drugs. To overcome this problem, it was hypothesized that a alpha(1a/1d) subtype selective antagonist would bring more benefit for the therapy of BPH/LUTS. In developing such selective alpha(1a/1d) ligands, a series of (phenylpiperidinyl)cyclohexylsulfonamides has been synthesized and evaluated for binding to three cloned human alpha(1)-adrenergic receptor subtypes. Many compounds showed equal affinity for both alpha(1a) and alpha(1d) subtypes with good selectivity versus the alpha(1b) subtype. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.04.098

文献信息

• Indol-3-y-carbonyl-piperidin and piperazin-derivatives
  申请人：Bissantz Caterina

  公开号：US20070027163A1

  公开（公告）日：2007-02-01

  The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R 1 to R 3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.

  本发明涉及作为V1a受体拮抗剂的吲哒-3-基甲酰哌啶和哌嗪衍生物，其由以下式I表示：其中残基R1至R3如本文所定义。该发明还涉及含有这种化合物的药物组合物，以及制备这些化合物和组合物的方法。该发明还涉及治疗痛经、高血压、慢性心力衰竭、抗利尿素过度分泌、肝硬化、肾病综合征、强迫症、焦虑和抑郁症的方法。
• Piperidinyl substituted cyclohexane-1,4-diamines
  申请人：Chiu George

  公开号：US20060217419A1

  公开（公告）日：2006-09-28

  The present invention relates to piperidine substituted cyclohexane-1,4-diamine compounds of Formula (I) and pharmaceutically acceptable forms thereof, as α 1a /α 1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as method of treatments.

  本发明涉及式(I)的哌啶取代的环己烷-1,4-二胺化合物及其药学上可接受的形式，作为α1a/α1d肾上腺素受体调节剂，用于治疗良性前列腺肥大和下尿路症状。本发明还涉及包含所述新化合物的药物组合物，制备这些新化合物的新方法以及作为药物的新用途和治疗方法。
• Dihydroindolyl methanones as alpha 1a/1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms
  申请人：Baxter W. Ellen

  公开号：US20060183902A1

  公开（公告）日：2006-08-17

  The present invention relates to new compounds of Formula (I): and pharmaceutically acceptable forms thereof, use of the compounds as α 1a and/or α 1d adrenoreceptor modulators, including use of a pharmaceutical composition, medicine or medicament comprising said compounds, a process to prepare said compounds and a method for treating an α 1a and/or α 1d adrenoreceptor mediated disorder.

  本发明涉及公式（I）的新化合物及其药用可接受形式，所述化合物用作α1a和/或α1d肾上腺受体调节剂，包括使用含有该化合物的药物组合物、药品或药剂，制备该化合物的过程以及治疗α1a和/或α1d肾上腺受体介导的疾病的方法。
• Serotonin 5-HT1A and dopamin D2 receptor ligands
  申请人：H. Lundbeck A/S

  公开号：US20030120070A1

  公开（公告）日：2003-06-26

  The present invention relates to a series of 4-phenylpiperazines of formula (I) 1 wherein A is alkylene, alkenylene, alkynylene, and C 3-7 cycloalkylene; R 1 is a C 3-10 alkyl, alkenyl, or alkynyl group, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl, trifluoromethylsulfonyl, or alkylsulfonyl, R 2 -R 5 are optional substituents; R 9 and R 10 are hydrogen, alkyl or together form an ethylene or propylene bridge, W is O or S; V is O, S, CR 6 R 7 , or NR 8 wherein R 6 , R 7 , and R 8 are hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, optionally substituted arylalkyl or aryl, or R 6 and R 7 constitute a 3-7 membered spiro ring; Z is—(CH 2 ) m —; m being 2 or 3 or Z is —CH═CH—; which show effects on central serotonin 5-HT 1A and dopamine D 2 receptors. Thus the novel compounds are useful in the treatment of certain psychic and neurologic disorders, in particular psychosis.

  本发明涉及一系列4-苯基哌嗪化合物，其化学式为(I)1，其中A为烷基、烯基、炔基和C3-7环烷基；R1为C3-10烷基、烯基或炔基、环烷(烯)基、环烷(烯)基-烷(炔)基、三氟甲磺酰基或烷基磺酰基，R2-R5为可选取代基；R9和R10为氢、烷基或共同形成乙烯或丙烯桥；W为O或S；V为O、S、CR6R7或NR8，其中R6、R7和R8为氢或烷基、烯基、环烷基、环烷基烷基、可选取代芳基烷基或芳基，或R6和R7构成一个3-7成员的螺环；Z为—(CH2)m—，其中m为2或3，或Z为—CH=CH—，这些化合物对中枢血清素5-HT1A和多巴胺D2受体具有作用。因此，这些新的化合物在治疗某些精神和神经疾病，特别是精神病方面具有应用价值。
• BENZIMIDAZOLYL COMPOUNDS
  申请人：Efremov Ivan

  公开号：US20080280933A1

  公开（公告）日：2008-11-13

  Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  本文披露了化合物及其药学上可接受的盐，其中化合物的结构如规范中所定义的I式。还披露了相应的制药组合物、治疗方法、合成方法和中间体。