N,N-di-tert-butyl-isobutylamine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N,N-di-tert-butyl-isobutylamine
• 英文别名: N,N-ditert-butyl-2-methylpropan-1-amine
• 化学式: C₁₂H₂₇N
• 分子量: 185.353
• InChiKey: VJRZKKYEBUAJIJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  N-chloro-di(tert-butyl)amine 、 (2-methylpropyl)lithium 在 四甲基乙二胺 作用下， 以 正庚烷 为溶剂， 以62%的产率得到N,N-di-tert-butyl-isobutylamine
  参考文献：
  名称：

  极高位阻性三烷基胺的合成及其通过霍夫曼样消除反应的衰变

  摘要：

  通过使用不同的合成方法，制备了许多在氮上具有三个大烷基的胺，这些胺大大超过了三异丙胺的空间拥挤。原来，对氮的治疗-氯二烷基胺与有机金属化合物（例如格氏试剂）在大量过量的四亚甲基二胺的存在下提供了最有效的目标化合物。还测试了该方法的局限性。即使在环境温度下，取决于空间应力的程度，三烷基胺也经历脱烷基反应。因为在此转化过程中形成了烯烃，所以它与霍夫曼消除法有一些相似之处。但是，碱不能促进空间上拥挤的叔胺的热衰变。相反，质子条件甚至微量水强烈促进了该反应。建议通过量子化学计算来分析反应机理来解释实验结果。

  DOI：

  10.1021/acs.joc.0c01790

文献信息

• Antimicrobials and methods of making and using same
  申请人：BIOVERSYS AG

  公开号：US10815237B2

  公开（公告）日：2020-10-27

  The present disclosure relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, reducing the risk of, and delaying the onset of microbial infections in humans and animals. In some embodiments, the present disclosure provides a compound of Formula (I) or a tautomer thereof or a pharmaceutically acceptable salt of the compound or tautomer.

  本公开内容一般涉及抗微生物化合物领域及其制造和使用方法。这些化合物可用于治疗、预防、降低人和动物微生物感染的风险并延缓其发生。在一些实施方案中，本公开提供了式(I)化合物或其同系物或该化合物或同系物的药学上可接受的盐。
• Aminoalcohol lipidoids and uses thereof
  申请人：Massachusetts Institute of Technology

  公开号：US10844028B2

  公开（公告）日：2020-11-24

  Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

  本文介绍了通过胺与环氧化物封端化合物反应制备氨基醇脂质的方法。还提供了从市售起始原料制备氨基醇类脂质的方法。氨基醇脂质可由外消旋或立体化学纯环氧化物制备。氨基醇类脂质或其盐类最好具有生物降解性和生物相容性，可用于各种给药系统。考虑到这些氨基醇类脂化合物的氨基，它们特别适合用于多核苷酸的给药。现已制备出含有本发明类脂化合物和多核苷酸的复合物、胶束、脂质体或颗粒。本发明的类脂质还可用于制备给药微粒。由于本发明脂质具有缓冲周围环境 pH 值的能力，因此在递送易变药剂方面特别有用。
• Aryl, heteroaryl, and heterocyclic pharmaceutical compounds for treatment of medical disorders
  申请人：Achillion Pharmaceuticals, Inc.

  公开号：US11084800B2

  公开（公告）日：2021-08-10

  Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

  本发明提供了补体因子 D 抑制剂、药物组合物及其用途以及制造工艺。所提供的化合物包括式I、式II、式III、式IV和式V，或其药学上可接受的盐、原药、同位素类似物、N-氧化物或分离异构体，可选药学上可接受的组合物。本文所述的抑制剂以因子 D 为靶点，抑制或调节补体级联。
• Synthesis of backbone modified morpholino oligonucleotides and chimeras using phosphoramidite chemistry
  申请人：THE REGENTS OF THE UNIVERSITY OF COLORADO

  公开号：US11230565B2

  公开（公告）日：2022-01-25

  Amine substituted morpholino oligonucleotides, other than the classical N,N-dimethylamino PMO analogue, and methods of efficiently synthesizing these oligonucleotides with high yield are provided. Morpholino oligonucleotides having thiophosphoramidate, phosphoramidate, and alkyl phosphoramidate linkers. Chimeras containing unmodified DNA/RNA and other analogs of DNA/RNA can be prepared. These oligonucleotides form duplexes with complementary DNA or RNA that are more stable than natural DNA or DNA/RNA complexes, are active with RNAse H1, and may be transfected into cells using standard lipid reagents. These analogues are therefore useful for numerous applications.

  除了经典的 N,N-二甲基氨基 PMO 类似物之外，本研究还提供了胺取代的吗啉寡核苷酸，以及高效高产合成这些寡核苷酸的方法。具有硫代磷酰胺、磷酰胺和烷基磷酰胺连接体的吗啉寡核苷酸。可以制备含有未修饰 DNA/RNA 和其他 DNA/RNA 类似物的嵌合体。这些寡核苷酸与互补 DNA 或 RNA 形成双链，比天然 DNA 或 DNA/RNA 复合物更稳定，对 RNAse H1 有活性，可使用标准脂质试剂转染细胞。因此，这些类似物可用于多种用途。
• AMINOALCOHOL LIPIDOIDS AND USES THEREOF
  申请人：Massachusetts Institute of Technology

  公开号：US20190177289A1

  公开（公告）日：2019-06-13

  Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.