(2R)-2-pyrrolidino-butan-1-ol | 135711-17-0

• 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: (2R)-2-pyrrolidino-butan-1-ol
• 英文别名: (R)-2-Pyrrolidin-1-yl-butan-1-ol；(2R)-2-pyrrolidin-1-ylbutan-1-ol
• CAS: 135711-17-0
• 化学式: C₈H₁₇NO
• 分子量: 143.229
• InChiKey: MPOXJNRKFHZSFT-MRVPVSSYSA-N

物化性质

• 沸点：
  219.1±13.0 °C(Predicted)
• 密度：
  0.981±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  10
• 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：
  23.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (2R)-2-pyrrolidino-butan-1-ol 、 碘乙烷 以 乙腈 为溶剂， 生成 1-[(1R)-1-(hydroxymethyl)propyl]-1-ethylpyrrolidinium iodide
  参考文献：
  名称：

  Synthesis and Characterization of the First Pyrrolidine‐Based Chiral Ionic Liquids

  摘要：

  The first example of pyrrolidine-based room-temperature chiral ionic liquids using 2-aminobutanol as chiral auxiliary is described.

  DOI：

  10.1080/00397910801916140
• 作为产物：
  描述：

  1,4-二溴丁烷 、 2-氨基丁醇 在 sodium carbonate 作用下， 以 甲苯 为溶剂， 以73.5%的产率得到(2R)-2-pyrrolidino-butan-1-ol
  参考文献：
  名称：

  用（R）-（-）-2-氨基丁烷-1-醇的-二烷基衍生物改性的氢化锂铝不对称还原酮

  摘要：

  预先用2当量的（R）-（-）-2-（2-异吲哚基）丁-1-醇（一种容易获得的试剂）处理过的LiAlH 4将2-氯和2,4-二甲基二苯甲酮还原为相应的对映体过量100％对苯二酚。给出了酮还原的其他实例。

  DOI：

  10.1016/s0957-4166(00)82113-8

文献信息

• Substituted aryl or heteroarylpiperidine derivatives as melanocortin-4 receptor modulators
  申请人：Santhera Pharmaceuticals (Schweiz) AG

  公开号：EP2020405A1

  公开（公告）日：2009-02-04

  The present invention relates to substituted aryl or heteroarylpiperidine derivatives of structure (I) as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.

  本发明涉及结构式(I)的取代芳基或杂芳基哌啶衍生物，作为黑色素皮质素-4受体调节剂。根据结构和立体化学，本发明的化合物可以是人类黑色素皮质素-4受体(MC-4R)的选择性激动剂或选择性拮抗剂。激动剂可用于治疗肥胖、糖尿病和性功能障碍等疾病，而拮抗剂可用于治疗癌症恶病质、肌肉消耗、厌食症、焦虑和抑郁等疾病。一般来说，所有涉及MC-4R调节的疾病和疾病都可以用本发明的化合物进行治疗。
• Asymmetric reductions of ketones using lithium aluminium hydride modified with -dialkyl derivatives of (R)-(−)-2-aminobutan-1-ol
  作者：Eric Brown、Annie Penfornis、Joaquim Bayma、Joël Touet

  DOI：10.1016/s0957-4166(00)82113-8

  日期：1991.1

  LiAlH4 previously treated with 2 equivalents of (R)-(−)-2-(2-iso-indolinyl) butan-1-ol (a readily available reagent) reduced 2-chloro and 2,4-dimethyl benzophenones into the corresponding benzhydrols with 100% enantiomeric excess. Other examples of ketone reductions are given.

  预先用2当量的（R）-（-）-2-（2-异吲哚基）丁-1-醇（一种容易获得的试剂）处理过的LiAlH 4将2-氯和2,4-二甲基二苯甲酮还原为相应的对映体过量100％对苯二酚。给出了酮还原的其他实例。
• Pyrimidines as PLK inhibitors
  申请人：STADTMUELLER Heinz

  公开号：US20110086842A1

  公开（公告）日：2011-04-14

  The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1 , which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.

  本发明涵盖了一般式（1）的化合物，其中A、W、X、Y、Z、Ra、Rb、Rc、R1和R3如权利要求1所定义，适用于治疗以细胞过度或异常增殖为特征的疾病，并且用于制备具有上述特性的药物组合物。
• Substituted Heteroarylpiperidine Derivatives As Melanocortin-4 Receptor Modulators
  申请人：Henneböhle Marco

  公开号：US20100249093A1

  公开（公告）日：2010-09-30

  The present invention relates to substituted heteroarylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, amyotrophic lateral sclerosis (ALS), anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.

  本发明涉及取代杂环基哌啶衍生物作为黑色素-4受体调节剂。根据化合物的结构和立体化学，本发明的化合物可以是人类黑色素-4受体（MC-4R）的选择性激动剂或选择性拮抗剂。激动剂可用于治疗肥胖症、糖尿病和性功能障碍等疾病和疾病，而拮抗剂可用于治疗癌症消耗症、肌肉萎缩、厌食症、肌萎缩侧索硬化症（ALS）、焦虑和抑郁症等疾病和疾病。通常，涉及MC-4R调节的所有疾病和疾病都可以用本发明的化合物治疗。
• New amino-, imino- and oxazolinophosphites based on 1,1′-bi-2-naphtol: coordination and catalytic properties
  作者：K.N Gavrilov、O.G Bondarev、R.V Lebedev、A.I Polosukhin、A.A Shyryaev、S.E Lyubimov、P.V Petrovskii、S.K Moiseev、V.N Kalinin、N.S Ikonnikov、V.A Davankov、A.V Korostylev

  DOI：10.1016/s0022-328x(02)01561-9

  日期：2002.8

  A series of the new chiral BINOL-based phosphite P,N-hybrid ligands was prepared. The coordination behavior of all the ligands was studied and the neutral complexes [Rh(CO)Cl(P<^>N)] were synthesized in order to characterize a degree of the electronic non-symmetry of donating centers. Also the neutral and cationic complexes cis-[PdCl2(eta(2)-P<^>N=)], cis-[PdCl2(eta(1)-P<^>N=)(2)], cis-[PdCl(eta(2)-P<^>N=)(eta(1)-P<^>N=)]Cl-+(-), [Pd(allyl)(eta(2)-P<^>N=)]X-+(-) (X- = Cl-, BF4-) were obtained and characterized. The new P,N-hydrid ligands gave up to 81% ee in the enantioselective Pd-catalyzed alkylation of 3-penten-2-yl carbonate by dimethyl malonate and up to 60% ee in the Rh-catalyzed hydrosilylation of acetophenone and acetylferrocene by diphenylsilane. (C) 2002 Elsevier Science B.V. All rights reserved.