N-(diethyl-2-phosphono)ethyl-ethoxyethylamine

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机膦酸及其衍生物
• 英文名称: N-(diethyl-2-phosphono)ethyl-ethoxyethylamine
• 英文别名: N-(2-diethoxyphosphorylethyl)-2-methoxyethanamine
• 化学式: C₉H₂₂NO₄P
• 分子量: 239.252
• InChiKey: RDJLXIBOMGXSML-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  15
• 可旋转键数：
  10
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  56.8
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N-(diethyl-2-phosphono)ethyl-ethoxyethylamine 、 乙烯基磷酸二乙酯 在 lithium perchlorate 作用下， 反应 7.0h， 以89%的产率得到N-methoxyethyl-N,N-bis(2-diethoxyphosphorylethyl)amine
  参考文献：
  名称：

  WO2007/83395

  摘要：

  公开号：
• 作为产物：
  描述：

  2-溴乙基膦酸二乙酯 、 2-甲氧基乙胺 在 sodium hydroxide 作用下， 以 水 为溶剂， 反应 3.0h， 以55%的产率得到N-(diethyl-2-phosphono)ethyl-ethoxyethylamine
  参考文献：
  名称：

  WO2007/83395

  摘要：

  公开号：

文献信息

• INTERMEDIATE COMPOUND OF TECHNETIUM NITRIDE COMPLEX FOR RADIODIAGNOSTIC IMAGING
  申请人：Tisato Francesco

  公开号：US20100160615A1

  公开（公告）日：2010-06-24

  A bisphosphonoaminc compound represented by the following formula (I): wherein R1, R2, R3, R4 and R5 are independently an alkyl group having 1 to 6 carbon atoms, and n is an integer of 1 to 6, is extremely useful as an intermediate for preparing a technetium nitride complex for radiodiagnostic imaging.

  一种由以下化学式（I）表示的双膦氨基化合物：其中R1、R2、R3、R4和R5分别是具有1至6个碳原子的烷基基团，n是1至6的整数，作为制备用于放射诊断成像的锝氮化物配合物的中间体非常有用。
• WO2007/83395
  申请人：——

  公开号：——

  公开（公告）日：——
• US8182789B2
  申请人：——

  公开号：US8182789B2

  公开（公告）日：2012-05-22
• Biological <i>in Vitro</i> and <i>in Vivo</i> Studies of a Series of New Asymmetrical Cationic [^99mTc(N)(DTC-Ln)(PNP)]⁺ Complex (DTC-Ln = Alicyclic Dithiocarbamate and PNP = Diphosphinoamine)
  作者：Cristina Bolzati、Mario Cavazza-Ceccato、Stefania Agostini、Fiorenzo Refosco、Yoshihiro Yamamichi、Shinji Tokunaga、Davide Carta、Nicola Salvarese、Daniele Bernardini、Giuliano Bandoli

  DOI：10.1021/bc900493e

  日期：2010.5.19

  Tc-99m(N)-DBODC5 is a cationic mixed compound under clinical investigation as potential myocardial imaging agent. In spite of this, analogously to the other cationic Tc-99m-agents, presents a relatively low first-pass extraction. Thus, modification of Tc-99m(N)-DBODC(5) direct to increase its first-pass extraction keeping unaltered the favorable imaging properties would be desirable. This work describes the synthesis and biological evaluation of a series of novel cationic Tc-99m-nitrido complexes, of general formula [(TcN)-Tc-99m(DTC-Ln)(PNP)](+) (DTC-Ln= alicyclic dithiocarbamates; PNP = diphosphinoamine), as potential radiotracers for myocardial perfusion imaging. The synthesis of cationic Tc-99m-(N)-complexes were accomplished in two steps. Biodistribution studies were performed in rats and compared with the distribution profiles of Tc-99m(N)-DBODC5 and Tc-99m-Sestamibi. The metabolisms of the roost promising compounds were evaluated by HPLC methods. Biological studies revealed that most of the complexes have a high initial and persistent heart uptake with rapid clearance from nontarget tissues. Among tested compounds. 2 and 12 showed improved heart uptake with respect to the gold standard Tc-99m-complexes with favorable heart-to-liver and slightly lower heart-to-lung ratios. Chromatographic profiles of Tc-99m(N)radioactivity extracted from tissues and fluids were coincident with the native compound evidencing remarkable in vivo stability of these agents. This study shows that the incorporation of alicyclic dithiocarbamate in the [Tc-99m(N)(PNP)](+) building block yields to a significant increase of the heart uptake at early injection point suggesting that the first-pass extraction fraction of these novel complexes may he increased with respect to the other cationic Tc-99m-agents keeping almost unaltered the favorable target/nontarget ratios.