(S)-3-morpholinopyrrolidine | 216669-67-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: (S)-3-morpholinopyrrolidine
• 英文别名: 4-(3S)-3-Pyrrolidinyl-morpholine；4-[(3S)-pyrrolidin-3-yl]morpholine
• CAS: 216669-67-9
• 化学式: C₈H₁₆N₂O
• 分子量: 156.228
• InChiKey: OPJDRNMJJNFSNZ-QMMMGPOBSA-N

物化性质

• 沸点：
  241.6±30.0 °C(Predicted)
• 密度：
  1.063±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  24.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (S)-1-tosyl-3-morpholinopyrrolidine 在 sodium 、 叔丁醇 作用下， 以 四氢呋喃 、 氨 为溶剂， 以44%的产率得到(S)-3-morpholinopyrrolidine
  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

文献信息

• Hexahydro-cyclohepta-pyrrole oxindole as potent kinase inhibitors
  申请人：SUGEN, Inc.

  公开号：US20040186160A1

  公开（公告）日：2004-09-23

  The present invention is directed to a class indolinone compounds, hexahydro-cyclohepta-pyrrole oxindoles, which are useful as protein kinase inhibitors.

  本发明涉及一类吲哚酮化合物，即六氢-环庚-吡咯酮氧吲哚，其作为蛋白激酶抑制剂具有用途。
• 3-Imidazolyl-Indoles for the Treatment of Proliferative Diseases
  申请人：Boettcher Andreas

  公开号：US20100125064A1

  公开（公告）日：2010-05-20

  The invention relates to 3-heterocyclyl indolyl compounds capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, said compounds having the formula I, wherein R 1 , R 2 , R 3 , R 4 , R A , Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.

  本发明涉及能够抑制p53或其变体与MDM2和/或MDM4或其变体相互作用的3-杂环基吲哚化合物，其中所述化合物具有式I，其中R1、R2、R3、R4、RA、Y和Y的定义见说明书。由于其活性，这些化合物可用于治疗由MDM2和/或MDM4或其变体介导的各种疾病和疾病，例如炎症性或增殖性疾病或细胞保护。
• [EN] SPIRO RING-CONTAINING QUINAZOLINE COMPOUND<br/>[FR] COMPOSÉ DE QUINAZOLINE CONTENANT UN CYCLE SPIRO<br/>[ZH] 含螺环的喹唑啉化合物
  申请人：WIGEN BIOMEDICINE TECH SHANGHAI CO LTD

  公开号：WO2021129820A1

  公开（公告）日：2021-07-01

  本发明涉及一类含螺环的喹唑啉化合物，及其制备方法和该类化合物作为K-Ras G12C抑制剂在制备抗肿瘤药物中的用途。(1), (2), (3)
• US8053457B2
  申请人：——

  公开号：US8053457B2

  公开（公告）日：2011-11-08
• Structure-Selectivity Relationship in Alkyllithium−Aldehyde Condensations Using 3-Aminopyrrolidine Lithium Amides as Chiral Auxiliaries
  作者：Aline Corruble、Jean-Yves Valnot、Jacques Maddaluno、Pierre Duhamel

  DOI：10.1021/jo9810260

  日期：1998.11.1

  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.