4-amino-1-(2-naphthalenylmethyl)piperidine | 80349-38-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 4-amino-1-(2-naphthalenylmethyl)piperidine
• 英文别名: 4-amino-1-(2-naphthyl)methylpiperidine；4-amino-1-(naphth-2-ylmethyl)piperidine；4-amino-1-(naphthalen-2-ylmethyl)piperidine；1-(naphthalen-2-ylmethyl)piperidin-4-amine
• CAS: 80349-38-8
• 化学式: C₁₆H₂₀N₂
• mdl: MFCD11199102
• 分子量: 240.348
• InChiKey: MIQDSUXICBIPQN-UHFFFAOYSA-N

物化性质

• 沸点：
  379.2±35.0 °C(Predicted)
• 密度：
  1.104±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.375
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-amino-1-(2-naphthalenylmethyl)piperidine 在 三乙酰氧基硼氢化钠 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 12.0h， 生成 5-Chloro-N-(1-naphthalen-2-ylmethyl-piperidin-4-yl)-2-[(thiazol-2-ylmethyl)-amino]-benzamide
  参考文献：
  名称：

  Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists

  摘要：

  Several potent and efficacious MCHr1 antagonists containing an ortho-amino benzamide or nicotinamide chemotype have been identified, exemplified by 28 and 50. (c) 2005 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2005.06.089
• 作为产物：
  描述：

  1-[(Naphthalen-2-yl)methyl]piperidine-4-carboxamide 在 [双(三氟乙酰氧基)碘]苯 作用下， 以 水 、 乙腈 为溶剂， 生成 4-amino-1-(2-naphthalenylmethyl)piperidine
  参考文献：
  名称：

  THE DESIGN AND SYNTHESIS OF PURINE INHIBITORS OF CDK2. III

  摘要：

  Cyclin-dependent kinases (CDKs) belong to a class of enzymes that control the ability of a cell to enter into and proceed through the cell division cycle. Using purine as a scaffold, we have synthesized a number of nanomolar inhibitors of CDK-2/cyclin E. In this report, the synthesis of a series of piperidine-substituted purine analogs will be presented, as well as some of their in vitro and in vivo biological effects.

  DOI：

  10.1081/ncn-100002493

文献信息

• Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists
  作者：Christopher Blackburn、Matthew J. LaMarche、James Brown、Jennifer Lee Che、Courtney A. Cullis、Sujen Lai、Martin Maguire、Thomas Marsilje、Bradley Geddes、Elizabeth Govek、Vivek Kadambi、Colleen Doherty、Brian Dayton、Sevan Brodjian、Kennan C. Marsh、Christine A. Collins、Philip R. Kym

  DOI：10.1016/j.bmcl.2006.02.044

  日期：2006.5

  Several potent, functionally active MCHr1 antagonists derived from quinolin-2(1H)-ones and quinazoline-2(1H)-ones have been synthesized and evaluated. Pyridylmethyl substitution at the quinolone 1-position results in derivatives with low-nM binding potency and good selectivity with respect to hERG binding.

  已合成和评估了几种衍生自喹啉2（1H）-和喹唑啉-2（1H）-的功能强大的功能性MCHr1拮抗剂。喹诺酮1位上的吡啶基甲基取代导致衍生物具有较低的nM结合力和相对于hERG结合的良好选择性。
• SUBSTITUTED ISOQUINOLINE DERIVATIVE
  申请人：Hidaka Hiroyoshi

  公开号：US20120035159A1

  公开（公告）日：2012-02-09

  The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt: wherein X and Y each independently represent a direct bond, NH, CH═CH, O, or S; R 1 and R 2 each independently represent a hydrogen atom, a halogen atom, a cyano group, an alkyl group, or the like; R 3 and R 4 each independently represent a hydrogen atom, an alkyl group, or the like, or R 3 and R 4 together form an alkylene group or an alkenylene group, which may be bridged between two carbon atoms to an arbitrary position; and l, m, and n represent an integer number of 1 to 4.

  本发明提供了一种作为新型药物剂的异喹啉-6-磺酰胺衍生物。本发明提供了由式（1）表示的异喹啉-6-磺酰胺衍生物，其盐或该衍生物或盐的溶剂：其中X和Y分别独立表示直接键，NH，CH═CH，O或S；R1和R2分别独立表示氢原子，卤素原子，氰基，烷基或类似物；R3和R4分别独立表示氢原子，烷基或类似物，或R3和R4共同形成烷基或烯基，可以在两个碳原子之间被桥接到任意位置；l，m和n表示1到4的整数。
• Piperid-4-yl ureas and thio ureas used as antidepressant agents
  申请人：——

  公开号：US04563466A1

  公开（公告）日：1986-01-07

  The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammoniun salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocylic or heterocyclic ring optionally carrying one or more substituents as defined above; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is -- CO-- or --CH.sub.2 --, with the proviso that when Ar is unsubstituted phenyl and R.sup.9 is hydrogen then Y is --O--. The compounds of formula I exhibit psychotropic activity and are useful as antidepressants.

  该发明涉及化合物的制备的公式##STR1##以及其酸盐和季铵盐，其中虚线代表可选键，Ar代表公式##STR2##中的环系统，其中Q为O、S、--CR.sup.7 .dbd.CR.sup.8 --、--N.dbd.CR.sup.8 --和--N.dbd.N--; R.sup.4、R.sup.5和R.sup.6，以及R.sup.7和R.sup.8（存在时），每个代表氢或从较低烷基、较低烯基、较低烷氧基、NO.sub.2、NH.sub.2、卤代较低烷基、羟基较低烷基、氨基较低烷基、取代氨基、卤素、较低烷氧羰基、氰基、CONH.sub.2和羟基中选择的取代基；另外，当相邻时，R.sup.4和R.sup.5或R.sup.6和R.sup.8也代表与它们连接的碳原子一起表示一个融合的五元或六元碳环或杂环，该环可以携带一个或多个上述定义的取代基；R是一个可选择取代的芳基或杂环芳基基团或含有5至7个碳原子的环烷基基团；R.sup.1、R.sup.2、R.sup.3和R.sup.9分别是氢或较低烷基基团；n为0或1；X为.dbd.O、.dbd.S或.dbd.NH；Y为--O--或直接键，Z为--CO--或--CH.sub.2--，但如果Ar为未取代的苯基且R.sup.9为氢，则Y为--O--。公式I的化合物具有精神活性并可用作抗抑郁剂。
• Pyridyl- and/or pyridoyl-(piperid-4-yl) ureas and analogues thereof
  申请人：John Wyeth & Brother, Limited

  公开号：US04806552A1

  公开（公告）日：1989-02-21

  The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --NM.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocylic or heterocyclic ring optionally carrying one or more substituents as defined above; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S, or .dbd.NY; Y is --O-- or a direct bond and Z is -- CO-- or --CH.sub.2 --, with the proviso that when Ar is unsubstituted phenyl and R.sup.9 is hydrogen then v is --O--. The compounds of formula I exhibit psychotropic activity and are useful as antidepressants.

  该发明涉及化合物的制备，其化学式为##STR1##以及其酸加成物和季铵盐，其中虚线代表一个可选键，Ar代表一个化学式为##STR2##的环系统，其中Q为O、S、--CR^7.dbd.CR^8--、--N.dbd.CR^8--和--NM.dbd.N--; R^4、R^5和R^6; 当R^7和R^8存在时，每个都代表氢或从较低烷基、较低烯基、较低烷氧基、NO2、NH2、卤代较低烷基、羟基较低烷基、氨基较低烷基、取代氨基、卤素、较低烷氧羰基、氰基、CONH2和羟基中选择的取代基; 此外，当相邻时，R^4和R^5或R^6和R^8，连同它们所连接的碳原子，也代表一个融合的五元或六元碳环或杂环，可选择携带一个或多个上述定义的取代基; R是一个可选择取代的芳基或杂环芳基基团或含有5至7个碳原子的环烷基基团; R^1、R^2、R^3和R^9分别是氢或较低烷基基团; n为0或1; X是.dbd.O、.dbd.S或.dbd.NY; Y是--O--或直接键，Z是--CO--或--CH2--，但当Ar为未取代的苯丙烯基且R^9为氢时，则v为--O--。化合物I的表现出精神活性，并可用作抗抑郁剂。
• 1-AMINO-PHTHALAZINE DERIVATIVES, THE PREPARATION AND THE THERAPEUTIC USE THEREOF
  申请人：Augereau Michel Jean

  公开号：US20070099895A1

  公开（公告）日：2007-05-03

  A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments using the compounds of formula (I).

  通用式（I）的1-氨基邻苯二酮衍生物，其中取代基如本文所定义。还披露了制备这类化合物的方法，用于该方法的中间体以及使用式（I）化合物进行医疗治疗的方法。