(S)-1-ethyl-3-aminopyrrolidine | 216667-65-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: (S)-1-ethyl-3-aminopyrrolidine
• 英文别名: (S)-1-ethylpyrrolidin-3-ylamine；(3S)-1-ethylpyrrolidin-3-amine；(3S)-1-ethyl-3-aminopyrrolidine
• CAS: 216667-65-1
• 化学式: C₆H₁₄N₂
• 分子量: 114.191
• InChiKey: GOLVGZOPWLLUSF-LURJTMIESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  8
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 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：

  (S)-1-ethyl-3-aminopyrrolidine 在 lithium aluminium tetrahydride 、 4 A molecular sieve 作用下， 以 四氢呋喃 为溶剂， 反应 3.0h， 生成 (S)-1-ethyl-3-(cyclohexylamino)pyrrolidine
  参考文献：
  名称：

  Structure-Selectivity Relationship in Alkyllithium−Aldehyde Condensations Using 3-Aminopyrrolidine Lithium Amides as Chiral Auxiliaries

  摘要：

  A nonracemizing route to a set of chiral 3-aminopyrrolidines, based on 4-hydroxy-(L)-proline, is described. The induction potential of the lithium amides derived from these diamines has then been investigated in the asymmetric addition of alkyllithium compounds onto various aldehydes. Enantiomeric excesses up to 76% have been obtained in the case of the condensation of n-butyllithium onto o-tolualdehyde under standard experimental conditions (THF, -78 degrees C). Interestingly, the presence of a second asymmetric center, such as an alpha-methylbenzyl group, on the lateral 3-amino group gives access, according to its configuration, to one or the other of the 1-o-tolylpentan-1-ol enantiomers.

  DOI：

  10.1021/jo9810260
• 作为产物：
  描述：

  tert-butyl ((S)-1-ethylpyrrolidin-3-yl)carbamate 在 盐酸 、 氨 作用下， 以 甲醇 为溶剂， 反应 18.0h， 生成 (S)-1-ethyl-3-aminopyrrolidine
  参考文献：
  名称：

  [EN] PHENYL SULFONYL DERIVATIVES AND THEIR USE AS HISTAMINE H3 ANTAGONISTS
  [FR] DÉRIVÉS PHÉNYLSULFONYLE ET LEUR UTILISATION COMME ANTAGONISTES DE L'HISTAMINE H3

  摘要：

  具有以下式子（1）的化合物：其中W代表N或CH; R1代表H或C1-3烷基; R2代表一个含氮杂环环或-C1-3烷基-含氮杂环基团;其中R2上包含或存在的任何含氮杂环均可选择性地被取代;或者，当W代表N时，R1和R2以及它们附着的N原子可以连接形成一个可选择性取代的氮杂环环，其中该氮杂环环可以选择性地被取代; R3代表H或C1-3烷基; R4代表可选择性取代的C3-6环烷基，杂环芳基或杂环基;或R3和R4以及它们附着的N原子可以连接形成一个可选择性取代的杂环基环;或其药学上可接受的盐。该发明的化合物已被发现可以调节组胺H3受体。

  公开号：

  WO2011121309A1

文献信息

• [EN] BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS<br/>[FR] BIS-PYRIDYLPYRIDONES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR 1 DE L'HORMONE DE CONCENTRATION DE LA MÉLANINE
  申请人：GLAXO GROUP LTD

  公开号：WO2009076387A1

  公开（公告）日：2009-06-18

  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/or diabetes.

  这项发明提供了新型的双吡啶基吡啉酮，它们是黑素浓集激素受体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/或糖尿病中的用途。
• [EN] TROPANE COMPOUNDS<br/>[FR] COMPOSÉS DE TROPANE
  申请人：EXELIXIS INC

  公开号：WO2009055077A1

  公开（公告）日：2009-04-30

  A compound according to Formula I or II: (I) or (II) wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.

  根据公式I或II的化合物：（I）或（II），其中R1、R1b、R2、L1和L2以及L2b的定义如规范中所述，以及其药物组合物和使用方法。
• THIAZOLOPYRIMIDINE MODULATORS AS IMMUNOSUPPRESSIVE AGENTS
  申请人：Herdewijn Piet

  公开号：US20120046278A1

  公开（公告）日：2012-02-23

  The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 11 , and R 12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.

  本发明涉及式I、II、III或IV的化合物，及/或其药用可接受的加合盐和/或其立体异构体和/或其溶剂化合物，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、R11和R12如权利要求1所定义。本发明还涉及它们的制备方法，以及其药物组合物。本发明进一步涉及所述化合物作为生物活性成分的用途，更具体地作为治疗疾病和病理状况的药物，例如但不限于免疫和自身免疫性疾病、器官和细胞移植排斥反应。
• PYRIDINES AND PYRIMIDINES AND USE THEREOF
  申请人：Purdue Pharma L.P.

  公开号：US20170008882A1

  公开（公告）日：2017-01-12

  The present disclosure provides pyridines and pyrimidines of Formula I and pharmaceutically acceptable salts and solvates thereof: wherein A, G, W 1 , W 2 , W 3 , and R 5 are defined as set forth in the specification. The present disclosure also provides uses of the compounds of Formula I and pharmaceutically acceptable salts and solvates thereof. In certain embodiments, Compounds of the present disclosure are useful for treating pain. In another embodiment, Compounds of the present disclosure are useful for treating a disorder responsive to blockade of sodium channels, or alleviating symptoms of the disorder.

  本公开提供了Formula I的吡啶和嘧啶以及其药用可接受的盐和溶剂化合物：其中A、G、W1、W2、W3和R5如规范中所述。本公开还提供了Formula I化合物及其药用可接受的盐和溶剂的用途。在某些实施例中，本公开的化合物对治疗疼痛有用。在另一实施例中，本公开的化合物对治疗对钠通道阻滞有反应的疾病，或缓解该疾病的症状有用。
• [EN] 2-PHENYL-3H-IMIDAZO[4,5-B]PYRIDINE DERIVATES USEFUL AS INHIBITORS OF MAMMALIAN TYROSINE KINASE ROR1 ACTIVITY<br/>[FR] DÉRIVÉS DE 2-PHÉNYL-3H-IMIDAZO[4,5-B]PYRIDINE UTILISÉS COMME INHIBITEURS DE L'ACTIVITÉ DE LA TYROSINE KINASE DE MAMMIFÈRE ROR1
  申请人：KANCERA AB

  公开号：WO2016124553A1

  公开（公告）日：2016-08-11

  A compound of formula (I´) or (I´´) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of mammalian kinase enzyme activity, including ROR1 tyrosine kinase activity and may be used in the treatment of disorders associated with such activity.

  化合物的化学式（I´）或（I´´）或其药学上可接受的盐。该化合物是哺乳动物激酶酶活性的抑制剂，包括ROR1酪氨酸激酶活性，并可用于治疗与该活性相关的疾病。