1-((tert-butyldimethylsilyl)oxy)-3-dimethylaminopropan-2-ol | 1003579-67-6

• 分子结构分类: 有机化合物 - 有机金属化合物 - 有机类金属化合物
• 英文名称: 1-((tert-butyldimethylsilyl)oxy)-3-dimethylaminopropan-2-ol
• 英文别名: 1-(t-Butyldimethylsilyloxy)-3-dimethylamino-2-propanol；1-[tert-butyl(dimethyl)silyl]oxy-3-(dimethylamino)propan-2-ol
• CAS: 1003579-67-6
• 化学式: C₁₁H₂₇NO₂Si
• 分子量: 233.426
• InChiKey: DOWHKEMBRQFDEG-UHFFFAOYSA-N

物化性质

• 沸点：
  269.3±30.0 °C(Predicted)
• 密度：
  0.906±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.93
• 重原子数：
  15
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  32.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-((tert-butyldimethylsilyl)oxy)-3-dimethylaminopropan-2-ol 在 盐酸 、 水 、 sodium hydride 作用下， 以 1,4-二氧六环 、 乙醇 、 甲苯 为溶剂， 反应 10.66h， 生成 2-{4-[(3b)-cholest-5-en-3-yloxy]butoxy}-N,N-dimethyl-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]propan-amine
  参考文献：
  名称：

  WO2008/103276

  摘要：

  公开号：
• 作为产物：
  描述：

  3-二甲胺基-1,2-丙二醇 、 叔丁基二甲基氯硅烷 在 咪唑 作用下， 以 二氯甲烷 为溶剂， 反应 2.25h， 生成 1-((tert-butyldimethylsilyl)oxy)-3-dimethylaminopropan-2-ol
  参考文献：
  名称：

  MODIFIED DRUGS FOR USE IN LIPOSOMAL NANOPARTICLES

  摘要：

  本文提供了适用于装载到脂质体纳米粒载体中的药物衍生物。在一些首选方面，这些衍生物包括一种水溶性较差的药物衍生物，其与一种弱碱基团衍生化，有助于通过LN跨膜pH或离子梯度将药物活性地装载到LN的水相内部。弱碱基团可以选择性地包括一个亲脂性结构域，有助于将药物活性地装载到脂质体膜的内单分子层。优点是，药物衍生物的LN配方相对于相应的游离药物表现出改善的溶解度、降低的毒性、增强的疗效和/或其他优点。

  公开号：

  US20180221279A1

文献信息

• Lipid Nanoparticle Based Compositions and Methods for the Delivery of Biologically Active Molecules
  申请人：Chen Tongqian

  公开号：US20090048197A1

  公开（公告）日：2009-02-19

  The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, dsRNA, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), short hairpin RNA (shRNA), and RNAi inhibitor molecules, to relevant cells and/or tissues, such as in a subject or organism. Such novel cationic lipids, microparticles, nanoparticles and transfection agents are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism. The compositions described herein are generally referred to as formulated molecular compositions (FMC) or lipid nanoparticles (LNP).

  本发明涉及新型阳离子脂质、转染剂、微粒、纳米粒子和短干扰核酸（siNA）分子。本发明还涉及组合物和使用方法，用于研究、诊断和治疗对基因表达和/或活性调节有反应的个体或生物的特征、疾病和状况。具体而言，本发明涉及新型阳离子脂质、微粒、纳米粒子和转染剂，可以有效地转染或传递生物活性分子，如抗体（例如单克隆、嵌合、人源化等）、胆固醇、激素、抗病毒药物、肽、蛋白质、化学治疗药物、小分子、维生素、辅因子、核苷、核苷酸、寡核苷酸、酶性核酸、反义核酸、三链体寡核苷酸、2,5-A嵌合体、dsRNA、异构酶、aptamers、诱饵和其类似物，以及小的核酸分子，如短干扰核酸（siNA）、短干扰RNA（siRNA）、双链RNA（dsRNA）、微RNA（miRNA）、短发夹RNA（shRNA）和RNAi抑制分子，传递到相关的细胞和/或组织中，例如在个体或生物中。这种新型阳离子脂质、微粒、纳米粒子和转染剂在提供组合物以预防、抑制或治疗细胞、个体或生物的疾病、状况或特征方面是有用的。本文所描述的组合物通常称为配方分子组合物（FMC）或脂质纳米粒子（LNP）。
• COMPOSITIONS AND METHODS FOR POTENTIATED ACTIVITY OF BIOLOGICALLY ACTIVE MOLECULES
  申请人：Jadhav Vasant

  公开号：US20100015218A1

  公开（公告）日：2010-01-21

  The present invention relates to novel compositions and methods for potentiating the activity of biologically active molecules in conjunction with one or more delivery vehicles and one or more carrier molecules. Specifically, the invention features the use of a carrier molecule in combination with a delivery vehicle and a biologically active molecule of interest to potentiate the activity of the biologically active molecule. The carrier molecule can be biologically inert, inactive, or attenuated; or can alternately be biologically active in the same or different manner than the biologically active molecule of interest. Specifically, the invention features novel particle forming delivery agents including cationic lipids, microparticles, and nanoparticles that are useful for delivering various biologically active molecules to cells in conjunction with a carrier molecule. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism that are delivered intracellularly in conjunction with a carrier molecule. In various embodiments, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules, to relevant cells and/or tissues, such as in a subject or organism, in conjunction with one or more carrier molecules. Such novel cationic lipids, microparticles, nanoparticles and transfection agents that are used in conjunction with one or more carrier molecules are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism.

  本发明涉及一种新型组合物和方法，用于增强生物活性分子的活性，结合一个或多个传递载体和一个或多个载体分子。具体而言，本发明涉及使用载体分子与传递载体和感兴趣的生物活性分子结合，以增强生物活性分子的活性。载体分子可以是生物惰性、不活跃或减弱的；或者可以是与生物活性分子以相同或不同的方式活跃的。具体而言，本发明涉及新型形成颗粒的传递剂，包括阳离子脂质、微粒和纳米粒子，它们对于传递各种生物活性分子到细胞中与载体分子结合是有用的。本发明还涉及组合物和使用方法，用于研究、诊断和治疗在主体或有机体中对基因表达和/或活性调节有反应的特征、疾病和情况，这些组合物和方法是与载体分子一起递送到细胞内的。在各种实施例中，本发明涉及新型阳离子脂质、微粒、纳米粒子和转染剂，它们有效地转染或递送生物活性分子，如抗体（例如单克隆、嵌合、人源化等）、胆固醇、激素、抗病毒药物、肽、蛋白质、化学治疗药物、小分子、维生素、辅因子、核苷、核苷酸、寡核苷酸、酶核酸、反义核酸、三链体寡核苷酸、2,5-A嵌合体、异构酶、适配体、诱饵和其类似物以及小核酸分子，如短干扰核酸（siNA）、短干扰RNA（siRNA）、双链RNA（dsRNA）、微RNA（miRNA）和短发夹RNA（shRNA）分子，递送到相关的细胞和/或组织中，例如在主体或有机体中，与一个或多个载体分子结合。这种与一个或多个载体分子一起使用的新型阳离子脂质、微粒、纳米粒子和转染剂是有用的，例如提供组合物以预防、抑制或治疗细胞、主体或有机体中的疾病、情况或特征。
• Lipid nanoparticle based compositions and methods for the delivery of biologically active molecules
  申请人：Chen Tongqian

  公开号：US20080020058A1

  公开（公告）日：2008-01-24

  The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, dsRNA, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), short hairpin RNA (shRNA), and RNAi inhibitor molecules, to relevant cells and/or tissues, such as in a subject or organism. Such novel cationic lipids, microparticles, nanoparticles and transfection agents are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism. The compositions described herein are generally referred to as formulated molecular compositions (FMC) or lipid nanoparticles (LNP).

  本发明涉及新型阳离子脂质、转染剂、微粒子、纳米粒子和短干扰核酸（siNA）分子。该发明还涉及组合物和使用方法，用于研究、诊断和治疗对基因表达和/或活性调节有反应的个体或生物的特征、疾病和状况。具体而言，该发明涉及新型阳离子脂质、微粒子、纳米粒子和转染剂，这些转染剂能够有效地转染或传递生物活性分子，如抗体（例如单克隆、嵌合、人源化等）、胆固醇、激素、抗病毒药物、肽、蛋白质、化疗药物、小分子、维生素、辅因子、核苷、核苷酸、寡核苷酸、酶性核酸、反义核酸、三链形成寡核苷酸、2,5-A嵌合体、dsRNA、异构酶、适配体、诱饵和其类似物以及小核酸分子，如短干扰核酸（siNA）、短干扰RNA（siRNA）、双链RNA（dsRNA）、微RNA（miRNA）、短发夹RNA（shRNA）和RNAi抑制分子，传递到相关的细胞和/或组织中，例如在个体或生物中。这些新型阳离子脂质、微粒子、纳米粒子和转染剂在提供组合物以预防、抑制或治疗细胞、个体或生物的疾病、状况或特征方面是有用的。所述组合物通常被称为配制分子组合物（FMC）或脂质纳米粒子（LNP）。
• LIPID NANOPARTICLE BASED COMPOSITIONS AND METHODS FOR THE DELIVERY OF BIOLOGICALLY ACTIVE MOLECULES
  申请人：Chen Tongqian

  公开号：US20100105933A1

  公开（公告）日：2010-04-29

  The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, dsRNA, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), short hairpin RNA (shRNA), and RNAi inhibitor molecules, to relevant cells and/or tissues, such as in a subject or organism. Such novel cationic lipids, microparticles, nanoparticles and transfection agents are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism. The compositions described herein are generally referred to as formulated molecular compositions (FMC) or lipid nanoparticles (LNP).

  本发明涉及新型阳离子脂质体、转染剂、微粒、纳米粒子和短干扰核酸（siNA）分子。本发明还涉及用于研究、诊断和治疗对基因表达和/或活性调节有响应的特征、疾病和情况的组合物和使用方法。具体而言，本发明涉及新型阳离子脂质体、微粒、纳米粒子和转染剂，可以有效地转染或传递生物活性分子，例如抗体（例如单克隆、嵌合、人源化等）、胆固醇、激素、抗病毒药物、肽、蛋白质、化疗药物、小分子、维生素、辅因子、核苷、核苷酸、寡核苷酸、酶性核酸、反义核酸、三股形成寡核苷酸、2,5-A嵌合体、dsRNA、等位酶、适配体、诱饵和其类似物以及小核酸分子，例如短干扰核酸（siNA）、短干扰RNA（siRNA）、双链RNA（dsRNA）、微RNA（miRNA）、短发夹RNA（shRNA）和RNAi抑制剂分子，传递到相关的细胞和/或组织中，例如在一个主体或生物体内。这种新型阳离子脂质体、微粒、纳米粒子和转染剂在提供组合物以预防、抑制或治疗细胞、主体或生物体中的疾病、情况或特征方面非常有用。本文所述的组合物通常称为配制分子组合物（FMC）或脂质纳米粒子（LNP）。
• Modified Drugs for Use in Liposomal Nanoparticles
  申请人：Cullis Peter

  公开号：US20110165225A1

  公开（公告）日：2011-07-07

  Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.

  本文提供了适用于载入脂质体纳米粒子载体的拖曳导数。在某些优选方面，这些导数包括一种难溶于水的拖曳经过弱碱基团衍生化，该弱碱基团促进通过LN跨膜pH或离子梯度将拖曳活性负载到LN的水内部。弱碱基团可以选择包括一个亲脂性域，该亲脂性域促进将拖曳活性负载到脂质体膜的内单层。优点是，与相应的自由拖曳相比，拖曳导数的LN配方表现出改善的溶解度、降低的毒性、增强的功效和/或其他益处。