ethyl 4-(aminomethyl)-4-hydroxy-1-piperidinecarboxylic acid ester | 106244-76-2

• 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: ethyl 4-(aminomethyl)-4-hydroxy-1-piperidinecarboxylic acid ester
• 英文别名: ethyl 4-(aminomethyl)-4-hydroxy-1-piperidinecarboxylate；ethyl 4-(aminomethyl)-4-hydroxypiperidine-1-carboxylate；ethyl 4-aminomethyl-4-hydroxypiperidine-1-carboxylate
• CAS: 106244-76-2
• 化学式: C₉H₁₈N₂O₃
• 分子量: 202.254
• InChiKey: MEHDPHFVOFBZMT-UHFFFAOYSA-N

物化性质

• 熔点：
  82 °C
• 沸点：
  326.4±27.0 °C(Predicted)
• 密度：
  1.177±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  75.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  ethyl 4-(aminomethyl)-4-hydroxy-1-piperidinecarboxylic acid ester 在 盐酸 作用下， 以 P4 O10 为溶剂， 生成 4-Aminomethyl-4-hydroxypiperidine dihydrochloride
  参考文献：
  名称：

  Quinolone- and naphthyridone carboxylic acid derivatives, process for

  摘要：

  化学式为##STR1##的抗菌活性喹诺酮或萘啶酮羧酸衍生物，其中R1代表各种有机基团，R2代表氢、1至4个碳原子的烷基或(5-甲基-2-氧代-1,3-二氧杂环戊-4-基)甲基，R3代表氢或氨基，R4代表##STR2##的基团，A代表N或C-R5，其中R5代表氢、卤素甲基、氰基或硝基，或者与R1一起形成结构##STR3##的桥。当R2为氢时，该羧酸的药用水合物、酸加成盐、碱金属盐、碱土金属盐、银盐或胍啶盐。

  公开号：

  US05173484A1
• 作为产物：
  描述：

  ethyl 1-oxa-6-azaspiro[2.5]octane-6-carboxylate 在 氨 作用下， 生成 ethyl 4-(aminomethyl)-4-hydroxy-1-piperidinecarboxylic acid ester
  参考文献：
  名称：

  Quinolone- and naphthyridone carboxylic acid derivatives, process for

  摘要：

  化学式为##STR1##的抗菌活性喹诺酮或萘啶酮羧酸衍生物，其中R1代表各种有机基团，R2代表氢、1至4个碳原子的烷基或(5-甲基-2-氧代-1,3-二氧杂环戊-4-基)甲基，R3代表氢或氨基，R4代表##STR2##的基团，A代表N或C-R5，其中R5代表氢、卤素甲基、氰基或硝基，或者与R1一起形成结构##STR3##的桥。当R2为氢时，该羧酸的药用水合物、酸加成盐、碱金属盐、碱土金属盐、银盐或胍啶盐。

  公开号：

  US05173484A1

文献信息

• Bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives
  申请人：——

  公开号：US20020086879A1

  公开（公告）日：2002-07-04

  The present invention of compounds of formula (I) 1 a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R 1 and R 2 taken together 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; R 4 is hydrogen or C 1-6 alkyl; R 5 is hydrogen or C 1-6 alkyl; L is C 3-6 cycloalkyl, C 5-6 cycloalkanone, C 2-6 alkenyl, or L is a radical of formula —Alk—R 6 —, 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; and R 6 is hydrogen, cyano, C 1-6 alkylsulfonylamino, C 3-6 cycloalkyl, C 5-6 cycloalkanone, or a heterocyclic ringsystem; R 7 is hydrogen, C 1-6 alkyl, hydroxyC 1-6 alkyl, C 3-6 cycloalkyl, or a heterocyclic ringsystem; X is O, SO 2 or NR 8 ; said R 8 being hydrogen or C 1-6 alkyl; R 9 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxy or hydroxy; Y is NR 10 or a direct bond; said R 10 being hydrogen, or C 1-6 alkyl; R 11 and R 12 each independently are hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, or R 11 and R 12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. 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.

  本发明涉及化合物的一种以及其立体化学异构体形式，N-氧化物形式或药学上可接受的酸加合物盐，其中R1和R2结合在一起形成以下式的二价基团，其中在所述二价基团中一个或两个氢原子可被C1-6烷基取代；R3为氢或卤素；R4为氢或C1-6烷基；R5为氢或C1-6烷基；L为C3-6环烷基，C5-6环戊酮，C2-6烯基，或L为以下式的基团—Alk—R6—，Alk—X—R7，—Alk—Y—C(═O)—R9或—Alk—Y—C(═O)—NR11R12，其中每个Alk为C1-12烷二基；R6为氢，氰基，C1-6烷基磺酰氨基，C3-6环烷基，C5-6环戊酮或杂环环系；R7为氢，C1-6烷基，羟基C1-6烷基，C3-6环烷基或杂环环系；X为O，SO2或NR8；R8为氢或C1-6烷基；R9为氢，C1-6烷基，C3-6环烷基，C1-6烷氧基或羟基；Y为NR10或直接键；R10为氢或C1-6烷基；R11和R12各自独立地为氢，C1-6烷基，C3-6环烷基，或R11和R12与氮原子结合可形成可选择取代的吡咯烷基，哌啶基，哌嗪基或4-吗啉基环。公开了制备所述产品的过程，包括所述产品的制剂以及它们作为药物的用途，特别用于治疗与胃排空障碍有关的病症。
• Antidepressive substituted N-[(4-piperidinyl)alkyl] bicyclic condensed
  申请人：Janssen Pharmaceutica N.V.

  公开号：US04689330A1

  公开（公告）日：1987-08-25

  Novel substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines useful as anti-depressives, in the treatment of Parkinson's disease and in the treatment of diseases related with disturbed enterokinesia.

  新型替代N-[(4-哌啶基)烷基]的环状氧唑和噻唑胺类化合物可用作抗抑郁药，在帕金森病的治疗以及与肠动力紊乱相关疾病的治疗中有用。
• 4-(aminomethyl)-piperidine benzamides for treating gastrointestinal disorders
  申请人：——

  公开号：US20030181456A1

  公开（公告）日：2003-09-25

  The present invention of compounds of formula (I) 1 a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, —R 1 —R 2 — is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C 1-6 alkyl or hydroxy; R 3 is hydrogen or halo; R 4 is hydrogen or C 1-6 alkyl; R 5 is hydrogen or C 1-6 alkyl; L is C 3-6 cycloalkyl, oxoC 5-6 cycloalkyl, C 2-6 alkenyl, or L is a radical of formula -Alk-R 6 —, 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; and R 6 is hydrogen, amino, cyano, C 1-6 alkylsulfonylamino, C 3-6 cycloalkyl, oxoC 5-6 cycloalkyl, aryl or a heterocyclic ringsystem; R 7 is hydrogen, C 1-6 alkyl, hydroxyC 1-6 alkyl, C 3-6 cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO 2 or NR 8 ; said R 8 being hydrogen or C 1-6 alkyl; R 9 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxy, hydroxy or aryl; Y is a direct bond or NR 10 ; said R 10 being hydrogen, or C 1-6 alkyl; R 11 and R 12 each independently are hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, or R 11 and R 12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4 -morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating or preventing gastrointestinal disorders.

  本发明涉及一种化合物，其化学式为（I）1a立体化学异构体形式，其N-氧化物形式或药学上可接受的酸盐形式，其中-R1-R2-是一个化学式的二价基团，在所述的二价基团中，一个或两个氢原子可以被C1-6烷基或羟基取代；R3是氢或卤素；R4是氢或C1-6烷基；R5是氢或C1-6烷基；L是C3-6环烷基，氧代C5-6环烷基，C2-6烯基，或L是化学式-Alk-R6-，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烷基二亚基；R6是氢，氨基，氰基，C1-6烷基磺酰氨基，C3-6环烷基，氧代C5-6环烷基，芳基或杂环环系统；R7是氢，C1-6烷基，羟基C1-6烷基，C3-6环烷基，芳基或杂环环系统；X是O，S，SO2或NR8；其中R8是氢或C1-6烷基；R9是氢，C1-6烷基，C3-6环烷基，C1-6烷氧基，羟基或芳基；Y是直接键或NR10；其中R10是氢或C1-6烷基；R11和R12各自独立地是氢，C1-6烷基，C3-6环烷基，或R11和R12与氮原子结合可以形成一个可选取代的吡咯烷基，哌啶基，哌嗪基或4-吗啉基环。本发明还公开了制备所述产品的方法，包含所述产品的制剂以及其作为药物的用途，特别是用于治疗或预防胃肠道疾病。
• Monocyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives
  申请人：——

  公开号：US20030078427A1

  公开（公告）日：2003-04-24

  The present invention of compounds of formula (I) 1 a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R 1 is C 1-6 alkyloxy, C 2-6 alkenyloxy or C 2-6 alkynyl-oxy; R 2 is hydrogen, C 1-6 alkyl C 1-6 alkyloxy; R 3 is hydrogen or halo; R 4 is hydrogen or C 1-6 alkyl; R 5 is hydrogen or C 1-6 alkyl; L is C 3-6 cycloalkyl, C 5-6 cycloalkanone, C 2-6 alkenyl, or L is a radical of formula-Alk-R 6 —, 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; and R 6 is hydrogen, cyano, C 1-6 alkylsulfonylamino, C 3-6 cycloalkyl, C 5-6 cyclo-alkanone, or a heterocyclic ringsystem; R 7 is hydrogen, C 1-6 alkyl, hydroxyC 1-6 alkyl, C 3-6 cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO 2 or NR 8 ; said R 8 being hydrogen or C 1-6 alkyl; R 9 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxy or hydroxy; Y is NR 10 or a direct bond; said R 10 being hydrogen, or C 1-6 alkyl; R 11 and R 12 each independently are hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, or R 11 and R 12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. 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（I）化合物，其立体化学异构体形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中R1为C1-6烷氧基，C2-6烯氧基或C2-6炔氧基；R2为氢，C1-6烷基或C1-6烷氧基；R3为氢或卤素；R4为氢或C1-6烷基；R5为氢或C1-6烷基；L为C3-6环烷基，C5-6环戊酮，C2-6烯基，或L为式-Alk-R6—，Alk-X—R7，—Alk-Y—C(═O)—R9或—Alk-Y—C(═O)—NR11R12的基团，其中每个Alk为C1-12烷二基；R6为氢，氰基，C1-6烷基磺酰氨基，C3-6环烷基，C5-6环戊酮或杂环环系；R7为氢，C1-6烷基，羟基C1-6烷基，C3-6环烷基或杂环环系；X为O，S，SO2或NR8；其中R8为氢或C1-6烷基；R9为氢，C1-6烷基，C3-6环烷基，C1-6烷氧基或羟基；Y为NR10或直接键；其中R10为氢或C1-6烷基；R11和R12各自独立地为氢，C1-6烷基，C3-6环烷基，或R11和R12与氮原子结合可以形成可选择取代的吡咯烷基，哌啶基，哌嗪基或4-吗啉基环。公开了制备所述产品的过程，包含所述产品的配方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。
• Quinolone- and naphthridone carboxylic acid derivatives, process for
  申请人：Bayer Aktiengesellschaft

  公开号：US05284842A1

  公开（公告）日：1994-02-08

  An antibacterially active quinolone or naphthyridonecarboxylic acid derivative of the formula ##STR1## in which R.sup.1 stands for various organic radical, R.sup.2 stands for hydrogen, alkyl having 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl, R.sup.3 stands for hydrogen or amino, R.sup.4 stands for a radical of the formula ##STR2## A stands for N or C--R.sup.5, wherein R.sup.5 stands for hydrogen, halogen methyl, cyano or nitro or else together with R.sup.1 can form a bridge of the structure ##STR3## or a pharmaceutically utilizable hydrate, acid addition salt, alkali metal salt, alkaline earth metal salt, silver salt or guanidinium salt of the carboxylic acid when R.sup.2 is hydrogen.

  一种具有抗菌活性的喹诺酮或萘啶酮羧酸衍生物的化学式为##STR1##其中R.sup.1代表各种有机基团，R.sup.2代表氢，1至4个碳原子的烷基或（5-甲基-2-氧代-1,3-二氧杂环戊-4-基）甲基，R.sup.3代表氢或氨基，R.sup.4代表式##STR2##A代表N或C--R.sup.5，其中R.sup.5代表氢，卤素甲基，氰基或硝基，或者与R.sup.1一起形成结构的桥梁##STR3##或药物可利用的羧酸的水合物，酸加成盐，碱金属盐，碱土金属盐，银盐或羟基胍盐，当R.sup.2为氢时。