(2-phenoxy-ethyl)-malonic acid | 74884-32-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: (2-phenoxy-ethyl)-malonic acid
• 英文别名: (2-Phenoxy-aethyl)-malonsaeure；4-Phenoxy-2-carboxy-buttersaeure；3-Phenoxy-propan-dicarbonsaeure-(1.1)；(β-Phenoxy-aethyl)-malonsaeure；2-Phenoxyethylmalonic acid；2-(2-phenoxyethyl)propanedioic acid
• CAS: 74884-32-5
• 化学式: C₁₁H₁₂O₅
• 分子量: 224.213
• InChiKey: NHWPMQFQPLNENF-UHFFFAOYSA-N

物化性质

• 熔点：
  148 °C
• 沸点：
  488.9±40.0 °C(Predicted)
• 密度：
  1.325±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  16
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  83.8
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (2-phenoxy-ethyl)-malonic acid 在 乙醚 、 溴 作用下， 生成 2-bromo-4-phenoxy-butyric acid
  参考文献：
  名称：

  Fischer,E.; Blumenthal, Chemische Berichte, 1907, vol. 40, p. 112

  摘要：

  DOI：
• 作为产物：
  描述：

  diethyl 2-phenoxyethyl-propanedioate 在 sodium hydroxide 作用下， 以 乙醇 、 水 为溶剂， 以64%的产率得到(2-phenoxy-ethyl)-malonic acid
  参考文献：
  名称：

  .beta.-thiopropionyl-aminoacid derivatives and their use as

  摘要：

  一种治疗人类或动物细菌感染的方法，包括与β-内酰胺类抗生素联合给药，给予公式(I)的氨基酸衍生物的治疗有效量或其药用可接受的盐、溶剂化合物或体内可水解酯的治疗有效量，其中：R为氢、形成盐的阳离子或体内可水解酯形成基团；R.sub.1为氢、(C.sub.1-6)烷基，可选地被高达三个卤素原子或巯基、(C.sub.1-6)烷氧基、羟基、氨基、硝基、羧基、(C.sub.1-6)烷基羰氧基、(C.sub.1-6)烷氧羰基、甲酰基或(C.sub.1-6)烷基羰基取代，(C.sub.3-7)环烷基，(C.sub.3-7)环烷基(C.sub.2-6)烷基，(C.sub.2-6)烯基，(C.sub.2-6)炔基，芳基，芳基(C.sub.1-6)烷基，杂环烷基或杂环烷基(C.sub.1-6)烷基；R.sub.2为氢，(C.sub.1-6)烷基或芳基(C.sub.1-6)烷基；R.sub.3为氢，(C.sub.1-6)烷基，可选地被高达三个卤素原子取代，(C.sub.3-7)环烷基，融合的芳基(C.sub.3-7)环烷基，(C.sub.3-7)环烷基(C.sub.2-6)烷基，(C.sub.2-6)烯基，(C.sub.2-6)炔基，芳基，芳基-(CHR.sub.10).sub.m --X--(CHR.sub.11).sub.n，杂环烷基或杂环烷基-(CHR.sub.10).sub.m --X--(CHR.sub.11).sub.n，其中m为0至3，n为1至3，每个R.sub.10和R.sub.11独立地为氢或(C.sub.1-4)烷基，X为O，S(O).sub.x，其中x为0-2，或键；R.sub.4为氢，或体内可水解的酰基；R.sub.5和R.sub.6独立地为氢和(C.sub.1-6)烷基，或一起代表(CH.sub.2).sub.p，其中p为2至5。一些化合物本身被要求。

  公开号：

  US06048852A1

文献信息

• Nanoparticulate bioactive agents
  申请人：Spherics, Inc.

  公开号：US20040220081A1

  公开（公告）日：2004-11-04

  Bioactive agents may be reproducibly converted into particles having diameters in the range of about 5 to about 2000 nanometers (nm). Conversion is accomplished by dissolving the bioactive agent in a solvent for the bioactive agent, and rapidly altering the polarity of the solution to make it a non-solvent for the bioactive agent, for example by diluting the bioactive agent solution with an excess of a liquid that is a non-solvent for the bioactive agent but is miscible with the solvent. Precipitated bioactive agent nanoparticles are collected by centrifugation, filtration or lyophilization. The nanoparticles have a relatively narrow size distribution, and the average diameter can be controlled by choice of solvent and non-solvent. The nanoparticles are typically amorphous. A surfactant may be added to ensure dispersion of the particles when administered. In the preferred embodiment, the bioactive agent is a drug with low aqueous solubility.

  生物活性物质可以被稳定地转化成直径在约5到2000纳米（nm）范围内的颗粒。转化是通过将生物活性物质溶解在其溶剂中，并迅速改变溶液的极性使其成为生物活性物质的非溶剂来完成的，例如通过将生物活性物质溶液与过量的非溶剂液体混合来稀释生物活性物质溶液。通过离心、过滤或冻干收集沉淀的生物活性物质纳米粒子。纳米粒子具有相对较窄的尺寸分布，平均直径可通过选择溶剂和非溶剂来控制。纳米粒子通常是无定形的。可以添加表面活性剂以确保在给药时颗粒的分散。在首选实施例中，生物活性物质是一种具有低水溶性的药物。
• Targeted delivery via biodegradable polymers
  申请人：FOCAL, INC.

  公开号：EP1004293A2

  公开（公告）日：2000-05-31

  Delivery of bioactive molecules such as nucleic acid molecules encoding a protein can be significantly enhanced by immobilization of the bioactive molecule in a polymeric material adjacent to the cells where delivery is desired, where the bioactive molecule is encapsulated in a vehicle such as liposomes which facilitates transfer of the bioactive molecules into the targeted tissue. Targeting of the bioactive molecules can also be achieved by selection of an encapsulating medium of an appropriate size whereby the medium serves to deliver the molecules to a particular target. For example, encapsulation of nucleic acid molecules or biologically active proteins within biodegradable, biocompatible polymeric microparticles which are appropriately sized to infiltrate, but remain trapped within, the capillary beds and alveoli of the lungs can be used for targeted delivery to these regions of the body following administration to a patient by infusion or injection.

  将生物活性分子（如编码蛋白质的核酸分子）固定在需要递送的细胞附近的聚合物材料中，可以大大提高生物活性分子（如编码蛋白质的核酸分子）的递送效果，其中生物活性分子被包裹在脂质体等载体中，有利于将生物活性分子转移到目标组织中。生物活性分子的靶向性还可以通过选择适当大小的封装介质来实现，介质的作用是将分子输送到特定的靶点。例如，将核酸分子或生物活性蛋白质封装在可生物降解、生物相容性好的聚合物微粒中，这种微粒大小适当，可渗入肺部的毛细血管床和肺泡，但仍被困在其中，通过输液或注射给病人用药后，可将核酸分子或生物活性蛋白质定向输送到身体的这些区域。
• Bioadhesive drug delivery systems comprising poly(fumaric-co-sebacic acid)
  申请人：BROWN UNIVERSITY RESEARCH FOUNDATION

  公开号：EP1518550A2

  公开（公告）日：2005-03-30

  Bioadhesive polymers in the form of, or as a coating on, microcapsules containing drugs or bioactive substances which may serve for therapeutic, or diagnostic purposes in diseases of the gastrointestinal tract, are described. The polymeric microspheres all have a bioadhesive force of at least 11 mN/cm2 (110 N/m2). Techniques for the fabrication of bioadhesive microspheres, as well as a method for measuring bioadhesive forces between microspheres and selected segments of the gastrointestinal tract in vitro are also described. The quantitative method provides a means to establish a correlation between the chemical nature, the surface morphology and the dimensions of drug-loaded microspheres on one hand and bioadhesive forces on the other, allowing the screening of the most promising materials from a relatively large group of natural and synthetic polymers which, from theoretical consideration, should be used for making bioadhesive microspheres.

  本文描述了生物粘性聚合物以微胶囊的形式或作为微胶囊的涂层，微胶囊中含有可用于治疗或诊断胃肠道疾病的药物或生物活性物质。所有聚合物微球的生物粘附力至少为 11 mN/cm2（110 N/m2）。此外，还介绍了生物黏附微球的制造技术，以及在体外测量微球与所选胃肠道片段之间生物黏附力的方法。这种定量方法提供了一种手段，可以在载药微球的化学性质、表面形态和尺寸与生物粘附力之间建立联系，从而从相对较多的天然和合成聚合物中筛选出最有前途的材料，从理论上考虑，这些材料应被用于制造生物粘附微球。
• Method for peroral delivery of insulin and its analogues for therapeutic usage
  申请人：Kollipara Koteswara Rao

  公开号：US10143754B2

  公开（公告）日：2018-12-04

  A method for treating type 1 and type 2 diabetes by administering an oral pharmaceutical formulation which comprises of insulin or its analogs amalgamated with suitable encapsulating agents and pharmaceutical excipients. The encapsulated pharmaceutical oral formulation protects insulin or its analogs from harsh milieu of the gastrointestinal tract and facilitates efficient delivery of insulin at targeted sites with sustained hypoglycemic activity.

  一种治疗 1 型和 2 型糖尿病的方法，通过给药口服药物制剂，该制剂由胰岛素或其类似物与合适的封装剂和药用辅料混合而成。这种封装的口服药物制剂可保护胰岛素或其类似物免受胃肠道恶劣环境的影响，并有助于将胰岛素有效地输送到具有持续降糖活性的目标部位。
• Local delivery forms of acriflavine for treating tumors
  申请人：The Johns Hopkins University

  公开号：US10195190B2

  公开（公告）日：2019-02-05

  Local delivery formulations of the antineoplastic and microbicide agent acriflavine, and methods of making and using thereof are significantly more efficacious at increasing the median survival of subjects with proliferative disease than systemic administrations of acriflavine. The local delivery formulations of acriflavine show a dose-dependent increase in the median survival of subjects. The local delivery forms provide the increased efficacy without the toxicity associated with systemic administration of the agent.

  抗肿瘤药和杀微生物剂炔雌醇的局部给药制剂及其制造和使用方法在提高增殖性疾病患者的中位存活率方面的疗效明显优于炔雌醇的全身给药。局部给药的阿西黄嘌呤制剂显示，受试者的中位存活率呈剂量依赖性增长。局部给药形式在提高疗效的同时，不会产生与全身给药相关的毒性。