4-(4-Fluorphenyl)-1-methylpiperidin | 6652-88-6

• 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: 4-(4-Fluorphenyl)-1-methylpiperidin
• 英文别名: 4-(4-Fluorophenyl)-1-methylpiperidine
• CAS: 6652-88-6
• 化学式: C₁₂H₁₆FN
• 分子量: 193.264
• InChiKey: WPULKDMHXQEULY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  4-Bromo-1-methylpiperidine;hydrochloride 、 4-氟苯基溴化镁 在 butylmethylimidazolium tetrachloroferrate 作用下， 以 乙醚 为溶剂， 以79%的产率得到4-(4-Fluorphenyl)-1-methylpiperidin
  参考文献：
  名称：

  An Iron-Containing Ionic Liquid as Recyclable Catalyst for Aryl Grignard Cross-Coupling of Alkyl Halides

  摘要：

  The ionic liquid butylmethylimidazolium tetrachloroferrate (bmim-FeCl4) was found to be a very effective and completely air stable catalyst for the biphasic Grignard cross-coupling with primary and secondary alkyl halides bearing beta-hydrogens. After simply decanting the product in the ethereal layer, the ionic liquid catalyst was successfully recycled four times.

  DOI：

  10.1021/ol052965z

文献信息

• [EN] AMIDO-ISOTHIAZOLE COMPOUNDS AND THEIR USE AS INHIBITORS OF 11BETA-HSD1 FOR THE TREATMENT OF METABOLIC SYNDROME AND RELATED DISORDERS<br/>[FR] COMPOSÉS AMIDO-ISOTHIAZOLE ET LEUR UTILISATION COMME INHIBITEURS DE LA 11 ?-HSD1 DANS LE TRAITEMENT DU SYNDROME MÉTABOLIQUE ET DES TROUBLES APPARENTÉS
  申请人：UNIV EDINBURGH

  公开号：WO2010146338A1

  公开（公告）日：2010-12-23

  The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-isothiazole compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

  本发明涉及治疗化合物领域。更具体地，本发明涉及某些酰胺异硫唑化合物，其中包括抑制11β-羟基类固醇脱氢酶1（11β-HSD1）。本发明还涉及包含这些化合物的药物组合物，以及使用这些化合物和组合物，无论在体外还是体内，来抑制11β-羟基类固醇脱氢酶1；治疗通过抑制11β-羟基类固醇脱氢酶1得到改善的疾病；治疗代谢综合征，其中包括疾病，如2型糖尿病和肥胖症，以及相关疾病，包括胰岛素抵抗、高血压、血脂紊乱和心血管疾病，如缺血性（冠状动脉）心脏病；治疗中枢神经系统疾病，如轻度认知障碍和早期痴呆，包括阿尔茨海默病等。
• [EN] AN IMPROVED PROCESS FOR THE PREPARATION OF PAROXETINE AND ITS INTERMEDIATE<br/>[FR] PROCÉDÉ AMÉLIORÉ DE PRÉPARATION DE PAROXÉTINE ET DE SON INTERMÉDIAIRE
  申请人：PIRAMAL ENTPR LTD

  公开号：WO2017037662A1

  公开（公告）日：2017-03-09

  The present invention provides an improved process for the preparation of N-protected ((3S,4R)- 4-(4-fluorophenyl)piperidin-3-yl)methanol (compound (A)) and further its transformation to Paroxetine and its pharmaceutically acceptable salts. The process comprises reaction of compound (II) with amido-malonate compound (C) in the presence of a chiral catalyst and optionally a dehydrating agent to obtain compound (B); followed by reduction of (B) in the presence of a reducing agent to provide compound (A).

  本发明提供了一种改进的制备N-保护基((3S,4R)-4-(4-氟苯基)哌啶-3-基)甲醇（化合物(A)）的方法，并进一步将其转化为帕罗西汀及其药用可接受的盐。该方法包括在手性催化剂和可选的脱水剂的存在下，将化合物(II)与酰胺-马隆酸酯化合物(C)反应，以获得化合物(B)；随后在还原剂的存在下还原(B)以提供化合物(A)。
• [EN] BENZYL AMINE-CONTAINING HETEROCYCLIC COMPOUNDS AND COMPOSITIONS USEFUL AGAINST MYCOBACTERIAL INFECTION<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES CONTENANT DE LA BENZYLAMINE ET COMPOSITIONS UTILES CONTRE UNE INFECTION MYCOBACTÉRIENNE
  申请人：MILLER MARVIN J

  公开号：WO2017049321A1

  公开（公告）日：2017-03-23

  Described herein are compounds and compositions, and methods of making and their use as effective agents against mycobacterial infections.

  本文描述了化合物和组合物，以及制备方法及其用作抗结核菌感染的有效药剂。
• CHEMOKINE RECEPTOR ACTIVITY REGULATOR
  申请人：Yamamoto Keisuke

  公开号：US20140221340A1

  公开（公告）日：2014-08-07

  The invention provides a chemokine receptor activity modulator containing a pyrazolopyrimidine derivative represented by the formula (I) wherein R 1 , R 2 , R 3 , and R 4 are as described herein.

  该发明提供了一种包含由式(I)表示的吡唑吡咯啉衍生物的趋化因子受体活性调节剂，其中R1、R2、R3和R4如本文所述。
• Process for preparing (+)trans-4-p-fluorophenyl-3-hydroxymethyl-1-methylpiperidine
  申请人：——

  公开号：US20040215020A1

  公开（公告）日：2004-10-28

  The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX′) methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine. 1

  本发明涉及一种制备式(I)的(±)-反式-4-对氟苯基-3-羟甲基-1-甲基哌啶的过程。本发明还涉及式(IX)和(IX')的新中间体、制备该中间体的方法以及使用该化合物制备帕罗西汀和奥米诺西汀的方法。