[1-(2-氨基乙基)-4-哌啶基]甲醇 | 129999-62-8

• 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: [1-(2-氨基乙基)-4-哌啶基]甲醇
• 中文别名: 1-(2-氨基乙基)-4-哌啶甲醇
• 英文名称: [1-(2-Aminoethyl)piperidin-4-yl]methanol
• CAS: 129999-62-8
• 化学式: C₈H₁₈N₂O
• mdl: MFCD09723205
• 分子量: 158.24
• InChiKey: GSPGIVPZQUNHRX-UHFFFAOYSA-N

物化性质

• 沸点：
  266℃
• 密度：
  1.005
• 闪点：
  115℃

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  49.5
• 氢给体数：
  2
• 氢受体数：
  3

安全信息

• 危险等级：
  IRRITANT
• 海关编码：
  2933399090
• WGK Germany：
  3

反应信息

• 作为反应物：
  描述：

  [1-(2-氨基乙基)-4-哌啶基]甲醇 、 2-氯-3-甲基吡嗪 、 在 silica gel 、 二氯甲烷 、 ammonia methanol 、 1-[2-[(3-Methyl-2-pyrazinyl)amino]-ethyl]4-piperidinemethanol 作用下， 反应 20.0h， 以yielding 2.3 g (29%) 1-[2-[(3-methyl-2-pyrazinyl)amino]-ethyl]-4-piperidinemethanol (intermediate 1)的产率得到1-[2-[(3-Methyl-2-pyrazinyl)amino]-ethyl]4-piperidinemethanol
  参考文献：
  名称：

  Novel N-substituted 4-((-4'-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties

  摘要：

  本发明涉及公式1的化合物，其N-氧化物形式，药学上可接受的酸加成盐和其立体化学异构体形式，其中R1是C1-6烷氧基，C2-6烯氧基或C2-6炔氧基; R2是氢或C1-6烷氧基，或当R1和R2一起取时，它们可以形成公式的二价基团，在所述的二价基团中，一个或两个氢原子可以被C1-6烷基取代，R3是氢或卤素; L是C3-6环烷基，C5-6环戊酮，C2-6烯基，可选地用芳基取代，或L是公式-Alk-R4，-Alk-NR5R6，1-R6-4-哌啶基，Alk-X-R7，-Alk-Y-C(═O)-R9，或-Alk-Y-C(═O)-NR11R12的基团，其中每个Alk是C1-12烷二基基；R4是氢，C1-6烷基磺酰胺基，C3-6环烷基，C5-6环戊酮，Ar-，二(Ar)甲基，Ar-氧基或Het1; R5是氢或C1-6烷基；R6是Het2; R7是氢，C1-6烷基，羟基C1-6烷基，C3-6环烷基，Ar或Het2; X是O，S，SO2或NR8; R8是氢，C1-6烷基或Ar; R9是氢，C1-6烷基，C3-6环烷基，Ar，ArC1-6烷基，二(Ar)甲基，C1-6烷氧基或羟基; Y是NR10或直接键; R10是氢，C1-6烷基或Ar; R11和R12各自独立地是氢，C1-6烷基，C3-6环烷基，Ar或ArC1-6烷基，或R11和R12与带R11和R12的氮原子结合，可以形成取代为C1-6烷基，氨基或单或二(C1-6烷基)氨基的吡咯啉基或哌啶基环，或R11和R12与带R11和R12的氮结合，可以形成取代为C1-6烷基的哌嗪基或4-吗啉基基团。公开了制备这些产品的过程，包括这些产品的制剂及其作为药物的用途，特别是用于治疗与胃排空障碍有关的疾病。

  公开号：

  US20030153573A1

文献信息

• [EN] BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS<br/>[FR] BIS-PYRIDYLPYRIDONES EN TANT QU'ANTAGONISTES DU RECEPTEUR 1 DE L'HORMONE DE MELANO-CONCENTRATION
  申请人：GLAXOSMITHKLINE LLC

  公开号：WO2010141539A1

  公开（公告）日：2010-12-09

  The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1 ), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.

  这项发明提供了新型的双吡啶基吡啉酮，它们是黑素浓缩激素受体1（MCHR1）的拮抗剂，包含它们的药物组合物，它们的制备方法，以及它们在治疗和治疗肥胖和糖尿病中的用途。
• Novel esters of 1, 4-disubstituted piperidine derivatives
  申请人：——

  公开号：US20020042430A1

  公开（公告）日：2002-04-11

  This invention concerns the compounds of formula 1 the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R 1 is C 1-6 alkyloxy, C 2-6 alkenyloxy or C 2-6 alkynyloxy; R 2 is hydrogen or C 1-6 alkyloxy, or when taken together R 1 and R 2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C 1-6 alkyl, R 3 is hydrogen or halo; L is C 3-6 cycloalkyl, C 5-6 cycloalkanone, C 2-6 alkenyl optionally substituted with aryl, or L is a radical of formula —Alk—R 4 , —Alk—NR 5 R 6 , 1-R 6 -4-piperidinyl, Alk—X—R 7 , —Alk—Y—C(═O)—R 9 , or —Alk—Y—C(═O)—NR 11 R 12 wherein each Alk is C 1-12 alkanediyl; R 4 is hydrogen, C 1-6 alkylsulfonylamino, C 3-6 cycloalkyl, C 5-6 cycloalkanone, Ar—, di(Ar)methyl, Ar—oxy- or Het 1 ; R 5 is hydrogen or C 1-6 alkyl; R 6 is Het 2 ; R 7 is hydrogen, C 1-6 alkyl, hydroxyC 1-6 alkyl, C 3-6 cycloalkyl, Ar or Het 2 ; X is O, S, SO 2 or NR 8 ; said R 8 being hydrogen, C 1-6 alkyl or Ar; R 9 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, Ar, ArC 1-6 alkyl, di(Ar)methyl, C 1-6 alkyloxy or hydroxy; Y is NR 10 or a direct bond; said R 10 being hydrogen, C 1-6 alkyl or Ar; R 11 and R 12 each independently are hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, Ar or ArC 1-6 alkyl, or R 11 and R 12 combined with the nitrogen atom bearing R 11 and R 12 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C 1-6 alkyl, amino or mono or di(C 1-6 alkyl)amino, or said R 11 and R 12 combined with the nitrogen bearing R 11 and R 12 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C 1-6 alkyl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.

  本发明涉及公式1的化合物，其N-氧化物形式，药学上可接受的酸加成盐和立体化学异构体形式，其中R1是C1-6烷氧基，C2-6烯氧基或C2-6炔氧基；R2是氢或C1-6烷氧基，或当R1和R2一起取时，它们可以形成公式的双价基团，在所述双价基团中，一个或两个氢原子可以被C1-6烷基取代，R3是氢或卤素；L是C3-6环烷基，C5-6环烷酮，C2-6烯基，可选地取代芳基，或L是公式—Alk—R4，—Alk—NR5R6，1-R6-4-哌啶基，Alk—X—R7，—Alk—Y—C(═O)—R9或—Alk—Y—C(═O)—NR11R12的基团，其中每个Alk是C1-12烷二基；R4是氢，C1-6烷基磺酰胺基，C3-6环烷基，C5-6环烷酮，Ar—，二(Ar)甲基，Ar—氧基或Het1；R5是氢或C1-6烷基；R6是Het2；R7是氢，C1-6烷基，羟基C1-6烷基，C3-6环烷基，Ar或Het2；X是O，S，SO2或NR8；所述的R8是氢，C1-6烷基或Ar；R9是氢，C1-6烷基，C3-6环烷基，Ar，ArC1-6烷基，二(Ar)甲基，C1-6烷氧基或羟基；Y是NR10或直接键；所述的R10是氢，C1-6烷基或Ar；R11和R12各自独立地是氢，C1-6烷基，C3-6环烷基，Ar或ArC1-6烷基，或R11和R12与携带R11和R12的氮原子结合，可以形成一个吡咯啉基或哌啶基，两者都可以选择地取代C1-6烷基，氨基或单或双(C1-6烷基)氨基，或所述的R11和R12与携带R11和R12的氮原子结合，可以形成一个哌嗪基或4-吗啉基基团，两者都可以选择地取代C1-6烷基。公开了制备所述产品的过程，包括所述产品的配方以及它们作为药物的用途，特别是用于治疗与胃排空障碍有关的疾病。
• N-substituted 4-((-4′-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties
  申请人：Janssen Pharmaceutica N.V.

  公开号：US06800628B2

  公开（公告）日：2004-10-05

  This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-26alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula —Alk—R4, —Alk—NR5R6, 1-R6-4-piperidinyl, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar—, di(Ar)methyl, Ar-oxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, Ar or Het2; X is O, S, SO2 or NR8; said R8 being hydrogen, C1-6alkyl or Ar; R9 is hydrogen, C1-6alkyl, C3-6cyclo-alkyl, Ar, ArC1-6alkyl, di(Ar)methyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, C1-6alkyl or Ar; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, Ar or ArC1-6alkyl, or R11 and R12 combined with the nitrogen atom bearing R11 and R12 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C1-6alkyl, amino or mono or di(C1-6alkyl)amino, or said R11 and R12 combined with the nitrogen bearing R11 and R12 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C1-6alkyl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.

  本发明涉及式N-氧化物形式的化合物、药学上可接受的酸加成盐和其立体化学异构体形式，其中R1是C1-6烷氧基、C2-6烯氧基或C2-26炔氧基；R2是氢或C1-6烷氧基，或当R1和R2一起取时，它们可以形成式的二价基团，其中在所述的二价基团中，一个或两个氢原子可以被C1-6烷基取代，R3是氢或卤素；L是C3-6环烷基、C5-6环戊酮、C2-6烯基（可以选择地被芳基取代），或L是式的基团，其中每个Alk是C1-12烷二基；R4是氢、C1-6烷基磺酰氨基、C3-6环烷基、C5-6环戊酮、Ar-、二（Ar）甲基、Ar氧基或Het1；R5是氢或C1-6烷基；R6是Het2；R7是氢、C1-6烷基、羟基C1-6烷基、C3-6环烷基、Ar或Het2；X是O、S、SO2或NR8；其中R8是氢、C1-6烷基或Ar；R9是氢、C1-6烷基、C3-6环烷基、Ar、ArC1-6烷基、二（Ar）甲基、C1-6烷氧基或羟基；Y是NR10或直接键；其中R10是氢、C1-6烷基或Ar；R11和R12各自独立地是氢、C1-6烷基、C3-6环烷基、Ar或ArC1-6烷基，或R11和R12与携带R11和R12的氮原子结合，可以形成带有C1-6烷基、氨基或单个或双个（C1-6烷基）氨基的吡咯啉基环或哌啶基环，或者R11和R12与携带R11和R12的氮原子结合，可以形成带有C1-6烷基的哌嗪基或4-吗啉基基团，两者都可以选择地被C1-6烷基取代。公开了制备这些产品的方法、包含这些产品的配方以及它们作为药物的使用，特别是用于治疗与胃排空障碍有关的疾病。
• N-substituted 4-(4′-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties
  申请人：Janssen Pharmaceutica, N.V.

  公开号：US06291481B1

  公开（公告）日：2001-09-18

  Compounds of formula I the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the substituents are as described in the specification, and process for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.

  本发明揭示了I式化合物的制备方法，其中包括N-氧化物形式、药学上可接受的酸盐和其立体化学异构体形式，其中取代基如说明书所述。本发明还揭示了包含该产品的制剂及其作为药物的用途，特别是用于治疗与胃排空障碍有关的疾病。
• N-substituted 4-((4′-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties
  申请人：Janssen Pharmaceutica N.V.

  公开号：US06509339B2

  公开（公告）日：2003-01-21

  This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R4, -Alk-NR5R6, 1-R6-4-piperidinyl, Alk-X—R7, -Alk-Y—C(═O)—R9, or -Alk-Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar-, di(Ar)methyl, Ar-oxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, Ar or Het2; X is O, S, SO2 or NR8; said R8 being hydrogen, C1-6alkyl or Ar; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, Ar, ArC1-6alkyl, di(Ar)methyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, C1-6alkyl or Ar; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, Ar or ArC1-6alkyl, or R11 and R12 combined with the nitrogen atom bearing R11 and R12 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C1-6alkyl, amino or mono or di(C1-6alkyl)amino, or said R11 and R12 combined with the nitrogen bearing R11 and R12 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C1-6alkyl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.

  本发明涉及公式N-氧化物形式的化合物，药学上可接受的酸盐加成物和其立体化学异构体形式，其中R1是C1-6烷氧基，C2-6烯氧基或C2-6炔氧基；R2是氢或C1-6烷氧基，或当R1和R2一起取时，它们可以形成公式的二价基团，其中在该二价基团中，一个或两个氢原子可以被C1-6烷基取代，R3是氢或卤素；L是C3-6环烷基，C5-6环烷酮，C2-6烯基（可选地被芳基取代），或L是公式-Alk-R4，-Alk-NR5R6，1-R6-4-哌啶基，Alk-X—R7，-Alk-Y—C（═O）—R9，或-Alk-Y—C（═O）—NR11R12的基团，其中每个Alk是C1-12烷二基；R4是氢，C1-6烷基磺酰氨基，C3-6环烷基，C5-6环烷酮，Ar-，二（Ar）甲基，Ar-氧基或Het1；R5是氢或C1-6烷基；R6是Het2；R7是氢，C1-6烷基，羟基C1-6烷基，C3-6环烷基，Ar或Het2；X是O，S，SO2或NR8；其中R8是氢，C1-6烷基或Ar；R9是氢，C1-6烷基，C3-6环烷基，Ar，ArC1-6烷基，二（Ar）甲基，C1-6烷氧基或羟基；Y是NR10或直接键；其中R10是氢，C1-6烷基或Ar；R11和R12各自独立地是氢，C1-6烷基，C3-6环烷基，Ar或ArC1-6烷基，或R11和R12与携带R11和R12的氮原子结合，可以形成带有C1-6烷基，氨基或单或双（C1-6烷基）氨基的吡咯烷基或哌啶烷基环，或R11和R12与携带R11和R12的氮结合，可以形成带有C1-6烷基的哌嗪基或4-吗啉基基团，两者都可以选择地被C1-6烷基取代。公开了制备该产品的过程，包含该产品的制剂以及其作为药物的用途，特别是用于治疗与胃排空障碍有关的疾病。