N-甲基-4-苯基-4-哌啶胺 | 182621-56-3

• 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: N-甲基-4-苯基-4-哌啶胺
• 英文名称: 4-methylamino-4-phenylpiperidine
• 英文别名: N-Methyl-4-phenyl-4-piperidinamine；N-methyl-4-phenylpiperidin-4-amine
• CAS: 182621-56-3
• 化学式: C₁₂H₁₈N₂
• mdl: MFCD09746173
• 分子量: 190.288
• InChiKey: UORMPYQLQRCWRN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  24.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-甲基-4-苯基-4-哌啶胺 在 TEA 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 122.0h， 生成 (S)-(N)-(1-(3-(1-benzoyl-3(3,4-dichlorophenyl)piperidin-3-yl)propyl)-4-phenylpiperidin-4-yl)-N-methylacetamide
  参考文献：
  名称：

  A reliable and efficient synthesis of SR 142801

  摘要：

  A convenient synthesis of the potent human NK-3 receptor antagonist SR 142801, (S)-(+)-N-{{3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1-yl}-4-phenylpiperidin-4-yl}-N-methylacetamide [(S)-(+)(15)], is described. Improvements over the previously reported procedure are the preparation of the intermediate 5 via the novel imide 3 and subsequent reaction with the nucleophile 14, which reacts, regioselectively, at the endocyclic nitrogen. Copyright (C) 1996 Elsevier Science Ltd

  DOI：

  10.1016/0960-894x(96)00419-2
• 作为产物：
  描述：

  4-(乙酰氨基)-1-苄基-4-苯基哌啶 在 palladium on activated charcoal 盐酸 、 lithium aluminium tetrahydride 、 氢气 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 反应 148.0h， 生成 N-甲基-4-苯基-4-哌啶胺
  参考文献：
  名称：

  A reliable and efficient synthesis of SR 142801

  摘要：

  A convenient synthesis of the potent human NK-3 receptor antagonist SR 142801, (S)-(+)-N-{{3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1-yl}-4-phenylpiperidin-4-yl}-N-methylacetamide [(S)-(+)(15)], is described. Improvements over the previously reported procedure are the preparation of the intermediate 5 via the novel imide 3 and subsequent reaction with the nucleophile 14, which reacts, regioselectively, at the endocyclic nitrogen. Copyright (C) 1996 Elsevier Science Ltd

  DOI：

  10.1016/0960-894x(96)00419-2
• 作为试剂：
  描述：

  1-Benzoyl-3-(3,4-dichlorophenyl)-3-[3-(methanesulfonyloxy)propyl]piperidine 、 N-甲基-4-苯基-4-哌啶胺 在 N-甲基-4-苯基-4-哌啶胺 作用下， 以85的产率得到[3-(3,4-Dichlorophenyl)-3-[3-[4-(methylamino)-4-phenylpiperidin-1-yl]propyl]piperidin-1-yl]-phenylmethanone
  参考文献：
  名称：

  Bioorganic Medicinal Chemistry Letters 1996, 6, 2307-2310

  摘要：

  DOI：

文献信息

• [EN] SUBSTITUTED 1H-BENZO[D]IMIDAZOLE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN AND PAIN RELATED CONDITIONS<br/>[FR] DÉRIVÉS DE 1H-BENZO[D]IMIDAZOLE SUBSTITUÉS AYANT UNE ACTIVITÉ MULTIMODALE DIRIGÉE CONTRE LA DOULEUR ET DES ÉTATS PATHOLOGIQUES ASSOCIÉS À LA DOULEUR
  申请人：ESTEVE PHARMACEUTICALS SA

  公开号：WO2020115045A1

  公开（公告）日：2020-06-11

  The present invention relates to new compounds that show pharmacological activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ- 1 subunit of voltage-gated calcium channels or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the μ-opiod receptor (MOR or mu-opioid). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

  本发明涉及对电压门控钙通道（VGCC）的亚单位α2δ，特别是对电压门控钙通道的α2δ-1亚单位或对电压门控钙通道的α2δ亚单位和μ-阿片受体（MOR或μ-阿片）显示药理活性的新化合物。该发明还涉及所述化合物的制备过程，以及包含它们的组合物，并将它们用作药物的用途。
• Method for preparing 4-methylamino-4-phenylpiperidine
  申请人：——

  公开号：US20040181071A1

  公开（公告）日：2004-09-16

  The invention relates to a process for preparing a 4-alkoxycarbonylamino-1-benzyl-4-phenylpiperidine of formula (I) 1 via hydrolysis of 1-benzyl-4-cyano-4-phenylpiperidine (II) in acidic medium and treatment of the 1-benzyl-4-phenyl-4-piperidinecarboxamide (III) thus obtained with bromine in the presence of an alkali metal alkoxide. The invention also relates to a process for preparing 4-methylamino-4-phenylpiperidine from compound (II).

  该发明涉及一种制备4-烷氧羰基氨基-1-苄基-4-苯基哌啶的方法，通过在酸性介质中水解1-苄基-4-氰基-4-苯基哌啶（II），并将得到的1-苄基-4-苯基-4-哌啶羧酰胺（III）与溴在碱金属碱中存在的条件下处理。该发明还涉及一种从化合物（II）制备4-甲氨基-4-苯基哌啶的方法。
• Method for preparing 4-amino-4-phenylpiperidines
  申请人：——

  公开号：US20040171837A1

  公开（公告）日：2004-09-02

  The invention relates to a process for preparing a 4-amino-4-phenylpiperidine (I): 1 in which R is hydrogen or a (C 1 -C 3 )alkyl group, characterized in that a 1-protected 4-piperidone (II): 2 in which Pr′ represents a removable N-protecting group, is treated sequentially first with an alkali metal cyanide and then with an amine ENHPr″ (III) in which E represents a group R′=(C 1 -C 3 )alkyl, or an N-protecting group and Pr″ is an N-protecting group, the protecting group(s) being removable under the same conditions as Pr′; then the compound thus obtained (IV) is subjected to a Grignard reaction with a phenylmagnesium halide, the two or three protecting groups are removed from the compound thus obtained (V) and compound (I) is isolated or in the form of the free base, which is converted into one of its salts.

  该发明涉及一种制备4-氨基-4-苯基哌啶(I)的过程：其中R是氢或(C1-C3)烷基基团，其特征在于首先处理一种1-保护的4-哌啶酮(II)：其中Pr'代表可去除的N-保护基团，然后依次与碱金属氰化物和胺ENHPr″(III)进行反应，其中E代表基团R′=(C1-C3)烷基，或N-保护基团，Pr″是N-保护基团，保护基团可在与Pr'相同的条件下去除；然后将得到的化合物(IV)进行格氏试剂反应，与苯基镁卤化物反应，从得到的化合物(V)中去除两个或三个保护基团，最终分离得到化合物(I)或其自由碱形式，随后将其转化为盐的其中一种形式。
• 3-phenyl-2, 6-dioxopiperidin-3-yl propionamide derivatives and method for preparing same
  申请人：Sanofi-Synthelabo

  公开号：US06342607B1

  公开（公告）日：2002-01-29

  This invention relates to 3-(3-phenyl-2,6-dioxopiperidin-3-yl)propionamide derivatives, and to processes for preparing the same.

  本发明涉及3-(3-苯基-2,6-二氧杂吡啶-3-基)丙酰胺衍生物，以及其制备方法。
• PROCESS FOR THE PREPARATION OF 3,3-DISUBSTITUTED PIPERIDINES
  申请人：Smithkline Beecham S.p.A.

  公开号：EP0915849A2

  公开（公告）日：1999-05-19