(2S,3S)-isoleucinol | 152786-10-2

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (2S,3S)-isoleucinol
• 英文别名: D-isoleucinol；D-erythro-2-amino-3-methyl-pentan-1-ol；(2R,3R)-2-Amino-3-methyl-pentan-1-ol；(2R,3R)-2-Amino-3-methylpentan-1-ol
• CAS: 152786-10-2
• 化学式: C₆H₁₅NO
• 分子量: 117.191
• InChiKey: VTQHAQXFSHDMHT-RITPCOANSA-N

物化性质

• 沸点：
  196.9±0.0 °C(Predicted)
• 密度：
  0.904±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  8
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (2S,3S)-isoleucinol 、 2-(三氟甲基)-3,3,3-三幅丙酸甲酯 以 N,N-二甲基甲酰胺 为溶剂， 生成 (Z)-methyl 2-((R)-4-((R)-sec-butyl)oxazolidin-2-ylidene)-3,3,3-trifluoropropanoate
  参考文献：
  名称：

  Palladium-catalyzed allylation of trifluoromethylated ketene aminoacetals

  摘要：

  A new development in the palladium-catalyzed allylation reaction of trifluoromethylated ketene aminoacetals was reported. These nucleophilic reagents were prepared by adding aminoalcohols to methyl 3,3,3-trifluoro-2-trifluoromethylpropanoate. The asymmetric version of the allylation reaction was investigated using chiral oxazolidine-based starting materials or chiral palladium catalysts. Asymmetric allylic alkylation was carried out with up to 74% ee using a chiral catalyst. However, no improvement was observed using double stereodifferentiation. These results provided a novel access for trifluoromethylated all-carbon quaternary carbon centers. (C) 2014 Elsevier B.V. All rights reserved.

  DOI：

  10.1016/j.jfluchem.2014.10.002
• 作为产物：
  描述：

  D-异亮氨酸 在 lithium aluminium tetrahydride 、 sodium hydroxide 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 18.0h， 生成 (2S,3S)-isoleucinol
  参考文献：
  名称：

  [EN] SUBSTITUTED PHENYLSULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION
  [FR] INHIBITEURS A SUBSTITUTION PHENYLSULFONAMIDE DE LA PRODUCTION DE BETA-AMYLOIDES

  摘要：

  提供了符合以下式I的化合物，其中R1-R8在此处定义，以及其药用盐、水合物、代谢物和/或前药。描述了这些化合物用于抑制β淀粉样蛋白的产生以及预防和治疗阿尔茨海默病和唐氏综合征的用途。

  公开号：

  WO2003103660A1

文献信息

• Catalyst-Free, Metal-Free, and Chemoselective Transamidation of Activated Secondary Amides
  作者：Srinivasan Chandrasekaran、Rajagopal Ramkumar

  DOI：10.1055/s-0037-1610664

  日期：2019.2

  well. The present methodology appears to be better than the other catalyzed transamidations reported recently. A simple protocol, which is catalyst-free, metal-free, and chemoselective, for transamidation of activated secondary amides in ethanol as solvent under mild conditions is reported. A wide range of amines, amino acids, amino alcohols, and the substituents, which are problematic in catalyzed transamidation

  摘要 据报道，在温和条件下，无溶剂，无金属和化学选择性的简单方案可用于乙醇中作为溶剂的活化仲酰胺的氨基转移。在该方法学中容许在催化的转酰胺基化中有问题的各种各样的胺，氨基酸，氨基醇和取代基。转酰胺基反应也成功地扩展到水作为介质。本方法学似乎比最近报道的其他催化的转酰胺作用更好。 据报道，在温和条件下，无溶剂，无金属和化学选择性的简单方案可用于乙醇中作为溶剂的活化仲酰胺的氨基转移。在该方法学中容许在催化的转酰胺基化中有问题的各种各样的胺，氨基酸，氨基醇和取代基。转酰胺基反应也成功地扩展到水作为介质。本方法学似乎比最近报道的其他催化的转酰胺作用更好。
• Functionalized Iminium Salt Systems for Catalytic Asymmetric Epoxidation
  作者：Philip C. Bulman Page、Gerasimos A. Rassias、David Barros、Adel Ardakani、Benjamin Buckley、Donald Bethell、Timothy A. D. Smith、Alexandra M. Z. Slawin

  DOI：10.1021/jo010258n

  日期：2001.10.1

  A range of dihydroisoquinolinium salts containing alcohol, ether, and acetal functionalities in the nitrogen substituent has been prepared and tested as asymmetric epoxidation catalysts, providing ee's of up to ca. 60%.

  制备了一系列在氮取代基中含有醇，醚和乙缩醛官能团的二氢异喹啉鎓盐，并作为不对称环氧化催化剂进行了测试，可提供的电子最高可达约。60％。
• SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS
  申请人：CZECHTIZKY Werngard

  公开号：US20130065859A1

  公开（公告）日：2013-03-14

  The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的取代2-(色甘醇-6-氧基)-噻唑衍生物，其中Ar、R2、R3和R4如权利要求中所定义。式I的化合物是钠-钙交换蛋白（NCX）的抑制剂，特别是亚型1的钠-钙交换蛋白（NCX1），适用于处理细胞内钙离子稳态受扰的各种疾病，如心律失常、心力衰竭和中风。本发明还涉及制备式I的化合物的方法，它们作为药物的用途，以及包含它们的药物组合物。
• [EN] SUBSTITUTED PHENYLSULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION<br/>[FR] INHIBITEURS A SUBSTITUTION PHENYLSULFONAMIDE DE LA PRODUCTION DE BETA-AMYLOIDES
  申请人：WYETH CORP

  公开号：WO2003103660A1

  公开（公告）日：2003-12-18

  Compounds of Formula I, wherein R1-R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer’s Disease and Down’s syndrome are described.

  提供了符合以下式I的化合物，其中R1-R8在此处定义，以及其药用盐、水合物、代谢物和/或前药。描述了这些化合物用于抑制β淀粉样蛋白的产生以及预防和治疗阿尔茨海默病和唐氏综合征的用途。
• COMPOUNDS AND METHODS OF TREATING OBESITY
  申请人：Katzhendler Jehoshua

  公开号：US20110178151A1

  公开（公告）日：2011-07-21

  The present invention relates to novel fatty acid derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as agents for the treatment of obesity and related disorders, and for improving cognition.

  本发明涉及一种新型脂肪酸衍生物、其制备方法、包括这些化合物的制药组合物，以及使用这些化合物和组合物的方法，特别是作为治疗肥胖和相关疾病的药物和改善认知能力的药物。