Piperidin-4-amine, 1-(6-fluoro-2-naphthylmethyl)-

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: Piperidin-4-amine, 1-(6-fluoro-2-naphthylmethyl)-
• 英文别名: 1-[(6-fluoronaphthalen-2-yl)methyl]piperidin-4-amine
• 化学式: C₁₆H₁₉FN₂
• 分子量: 258.33
• InChiKey: VORWTFWMZCRIGW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Piperidin-4-amine, 1-(6-fluoro-2-naphthylmethyl)- 、 isonicotinoyl-urea 生成 N-[[[1-[(6-Fluoro-2-naphthalenyl)methyl]-4-piperidinyl]amino]carbonyl]-4-pyridinecarboxamide
  参考文献：
  名称：

  ARCHIBALD, JOHN LEHEUP;WARD, TERENCE JAMES

  摘要：

  DOI：

文献信息

• Pyridyl-and/or pyridoyl-(piperid-4-yl) ureas and analogues thereof
  申请人：John Wyeth & Brother, Limited

  公开号：US04985438A1

  公开（公告）日：1991-01-15

  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 --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 substitutent 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.

  本发明涉及公式##STR1##化合物及其酸加成物和季铵盐的制备方法，其中点线表示可选键，Ar表示公式##STR2##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；当存在时，R.sup.7和R.sup.8各自表示氢或从下列取出的取代基：低烷基、低烯基、低烷氧基、NO.sub.2、NH.sub.2、卤代低烷基、羟基低烷基、氨基低烷基、取代氨基、卤素、低烷氧羰基、氰基、CONH.sub.2和羟基；并且在相邻的R.sup.4和R.sup.5或R.sup.6和R.sup.8之间，连同它们附着的碳原子，也表示一个融合的五元或六元碳环或杂环，可选地携带一个或多个上述定义的取代基；R是一个可选取代的芳基或杂环芳基基团或含有5到7个碳原子的环烷基基团；R.sup.1、R.sup.2、R.sup.3和R.sup.9各自表示氢或低烷基；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 --，但前提是当Ar为未取代的苯基且R.sup.9为氢时，y为--O--。公式I的化合物表现出精神活性并可用作抗抑郁剂。
• Piperidine derivatives
  申请人：John Wyeth and Brother Limited

  公开号：US05212179A1

  公开（公告）日：1993-05-18

  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 --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.

  本发明涉及制备式为 ##STR1## 的化合物及其酸加成物和季铵盐，其中虚线表示可选键，Ar代表式为 ##STR2## 的环系，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；当存在时，R.sup.7和R.sup.8各自表示氢或从下列低烷基，低烯基，低烷氧基，NO.sub.2，NH.sub.2，卤代低烷基，羟基低烷基，氨基低烷基，取代氨基，卤素，低烷氧羰基，氰基，CONH.sub.2和羟基中选择的取代基；此外，当相邻的R.sup.4和R.sup.5或R.sup.6和R.sup.8，连同它们所附着的碳原子，也表示一个融合的五元或六元环族或杂环族，可选地带有一个或多个上述定义的取代基；R为可选取代的芳基或杂芳基基团或含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各自为氢或低烷基；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--，但当Ar为未取代的苯基且R.sup.9为氢时，Y为--O--。式I的化合物表现出精神活性，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.

  本发明涉及公式##STR1##的化合物及其酸加成物和季铵盐的制备，其中虚线表示可选键，Ar表示公式##STR2##的环系统，其中Q为O，S，--CR.sup.7 .dbd.CR.sup.8 --，--N.dbd.CR.sup.8 --和--NM.dbd.N--；R.sup.4，R.sup.5和R.sup.6；当存在时，R.sup.7和R.sup.8分别表示氢或从下面选取的取代基：低烷基，低烯基，低烷氧基，NO.sub.2，NH.sub.2，卤代低烷基，羟基低烷基，氨基低烷基，取代氨基，卤素，低烷氧羰基，氰基，CONH.sub.2和羟基；并且当相邻的R.sup.4和R.sup.5或R.sup.6和R.sup.8存在时，它们与它们所连接的碳原子一起也表示一个融合的五元或六元碳环或杂环，可选地携带一个或多个上述定义的取代基；R是一个可选地取代的芳基或杂芳基基团或含有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分别为氢或低烷基；n为0或1；X为.dbd.O，.dbd.S或.dbd.NY；Y为--O--或直接键，Z为--CO--或--CH.sub.2 --，但当Ar为未取代的苯基且R.sup.9为氢时，则v为--O--。公式I的化合物表现出精神活性，并且可用作抗抑郁剂。
• Piperidine derivatives having a psychotropic activity
  申请人：JOHN WYETH & BROTHER LIMITED

  公开号：EP0228795A1

  公开（公告）日：1987-07-15

  The invention relates to compounds of formula wherein R represents hydrogen or fluorine and R' represents 3-pyridyl or 4-pyridyl or a salt thereof which compounds exhibit psychotropic activity and are useful as antidepressants.

  本发明涉及式中 R 代表氢或氟和 R' 代表 3-吡啶基或 4-吡啶基的化合物或其盐，这些化合物具有精神活性，可用作抗抑郁药。
• N-[piperidylaminocarbonyl]quinolinecarboxamide derivatives having psychotropic activity
  申请人：JOHN WYETH & BROTHER LIMITED

  公开号：EP0234098A1

  公开（公告）日：1987-09-02

  The invention relates to compounds of formula or a salt thereof, wherein =X- is =CH- or =N-, R and R1 independently represent hydrogen, halogen or lower alkoxy and R2 is hydrogen or a substituent selected from halogen, lower alkyl, lower alkoxy or halolower alkyl which compounds exhibit psychotropic activity and are useful as anti-depressants.

  本发明涉及如下式的化合物 或其盐，其中 =X- 是 =CH- 或 =N-，R 和 R1 分别代表氢、卤素或低级烷氧基，R2 是氢或选自卤素、低级烷基、低级烷氧基或卤代低级烷基的取代基，这些化合物具有精神活性，可用作抗抑郁药。