4-(2-iodophenoxy)butanoic acid | 957040-08-3

• 英文名称: 4-(2-iodophenoxy)butanoic acid
• 英文别名: 4-(2-Iodophenoxy)-butyric acid
• CAS: 957040-08-3
• 化学式: C₁₀H₁₁IO₃
• 分子量: 306.1
• InChiKey: PBYVZSKWMWEABM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  14
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  46.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(2-iodophenoxy)butanoic acid 在 盐酸 、 4-二甲氨基吡啶 、 氯化亚砜 作用下， 以 乙醚 、 二氯甲烷 为溶剂， 反应 23.25h， 生成 N-(2-(N,N-diethylamino)ethyl)-6-(2-(2-iodophenoxy)acetamido)quinoxaline-2-carboxamide dihydrochloride
  参考文献：
  名称：

  Synthesis and Biological Evaluation of New Quinoxaline Derivatives of ICF01012 as Melanoma-Targeting Probes

  摘要：

  The aim of this study was the synthesis and pharmacokinetic selection of a best melanin-targeting ligand for addressing anticancer agents to pigmented melanoma. Seven quinoxaline carboxamide derivatives were synthesized and radiolabeled with iodine-125. Biodistribution studies of compounds [I-125]1a-g performed in melanoma-bearing mice tumor showed significant tumor uptake (range 2.43-5.68%ID/g) within 1 h after i.v. injection. Fast clearance of the radioactivity from the nontarget organs mainly via the urinary system gave high tumor-to-blood and tumor-to-muscle ratios. Given its favorable clearance and high tumor-melanoma uptake at 72 h, amide 1d was the most promising melanoma-targeting ligand in this series. Compound Id will be used as building block for the design of new melanoma-selective drug delivery systems.

  DOI：

  10.1021/ml400468x
• 作为产物：
  描述：

  2-碘苯酚 在 lithium hydroxide monohydrate 、 potassium carbonate 作用下， 以 四氢呋喃 、 甲醇 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 生成 4-(2-iodophenoxy)butanoic acid
  参考文献：
  名称：

  使用烷基羧甲基戊烷的烷基化封端的Catellani反应。

  摘要：

  Catellani反应已经引起了广泛的关注，因为它能够快速进行芳香族化合物的多重衍生。当使用烷基亲电子来实现邻烷基化是Catellani反应的最早的应用之一，本位与烷基化-封端的反应β -H-含有反应物还没有实现更新。在本文中，我们报道了使用烷基碳霉菌素（缩写为烷基Ge）作为亲核试剂的烷基化终止的Catellani反应。讨论了该反应中烷基Ge和烷基B（OH）2的反应性。该方法可实现与β的有效二烷基化含H的反应物，以前是Catellani反应无法获得的。

  DOI：

  10.1002/anie.202008482

文献信息

• Leukotriene-B4 derivatives, process for their production and their use
  申请人：Schering Aktiengesellschaft

  公开号：US05183925A1

  公开（公告）日：1993-02-02

  The invention relates to leukotriene-B.sub.4 derivatives of formula I, ##STR1## in which n=1-10, R.sub.1 means radical CH.sub.2 OH, radical COOR.sub.4, radical CONHR.sub.5 or radical CONR.sub.6 R.sub.7, A means a cis, trans or trans, trans--CH.dbd.CH--CH.dbd.CH group or tetramethylene group, B means an alkylene group with up to 10 C atoms, D means a direct compound, oxygen, sulfur, a --C.tbd.C group or a --CH.dbd.CR.sub.8 group, B and D together mean a direct bond, R.sub.2 means a hydrogen atom or an acid radical of an organic acid with 1-15 C atoms and R.sub.3 means a hydrogen atom, an optionally substituted alkyl radical with 1-10 C atoms, a cycloalkyl radical with 3-10 C atoms, an optionally substituted aryl radical with 6-10 C atoms or a 5-6 member heterocyclic radical and if R.sub.4 means a hydrogen atom, their salts with physiologically compatible bases and their cyclodextrin clathrates, process for their production and their pharmaceutical use.

  本发明涉及化合物I的白三烯-B.sub.4衍生物，其中：##STR1## 其中n = 1-10，R.sub.1表示基团CH.sub.2 OH、基团COOR.sub.4、基团CONHR.sub.5或基团CONR.sub.6R.sub.7，A表示顺式、反式或反式，反式-CH.dbd.CH-CH.dbd.CH基团或四亚甲基基团，B表示最多有10个C原子的烷基基团，D表示直接化合物、氧、硫、-C.tbd.C基团或-CH.dbd.CR.sub.8基团，B和D一起表示直接键，R.sub.2表示氢原子或具有1-15个C原子的有机酸的酸基基团，R.sub.3表示氢原子、可选择取代的1-10个C原子的烷基基团、3-10个C原子的环烷基团、6-10个C原子的可选择取代的芳基基团或5-6个成员的杂环基团，如果R.sub.4表示氢原子，则它们与生理兼容的碱盐和它们的环糊精包合物，以及它们的制备方法和药物用途。
• Development of new recyclable reagents and catalytic systems based on hypervalent iodine compounds
  作者：Mekhman S. Yusubov、Viktor V. Zhdankin

  DOI：10.1016/j.mencom.2010.06.001

  日期：2010.7

  Recent advances in the development of polymer-supported iodine(V) oxidants, recyclable monomeric hypervalent iodine(III) reagents and catalytic systems based on hypervalent iodine compounds are discussed. These efficient and environmentally friendly reagents and catalysts are particularly useful for oxidative transformations of alcohols to carbonyl compounds and for oxidations at the benzylic position.
• Preparation and Reactivity of Polymer-Supported 2-Iodylphenol Ethers, an Efficient Recyclable Oxidizing System
  作者：Rashad R. Karimov、Zeinul-Gabiden M. Kazhkenov、Matthew J. Modjewski、Eric M. Peterson、Viktor V. Zhdankin

  DOI：10.1021/jo7015746

  日期：2007.10.1

  [GRAPHICS]Preparation of new recyclable polymer-supported oxidizing reagents based on 2-iodylphenol ethers is described. The synthesis employs commercially available aminomethylated polystyrene or Merrifield resin and affords polymer-supported 2-iodylphenol ethers with loading up to 0.86 mmol/g with respect to 102 groups. The new reagents effect clean and efficient conversion of a wide range of alcohols, including heteroatomic and unsaturated structures, to the corresponding carbonyl compounds. Recycling of the resins is possible with minimal loss of activity after several reoxidations.
• US5183925A
  申请人：——

  公开号：US5183925A

  公开（公告）日：1993-02-02