N-methoxyethyl-N,N-bis(2-diethoxyphosphorylethyl)amine

• 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-methoxyethyl-N,N-bis(2-diethoxyphosphorylethyl)amine
• 英文别名: N-(2-methoxyethyl)-N,N-bis(2-diethoxyphosphorylethyl)amine；N,N-bis[(diethyl 2-phosphono)ethyl]methoxyethylamine；N,N-bis(2-diethoxyphosphorylethyl)-2-methoxyethanamine
• 化学式: C₁₅H₃₅NO₇P₂
• 分子量: 403.393
• InChiKey: AVKOBIYTNUGRTE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  25
• 可旋转键数：
  17
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  83.5
• 氢给体数：
  0
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  N-methoxyethyl-N,N-bis(2-diethoxyphosphorylethyl)amine 在 lithium aluminium tetrahydride 作用下， 以 乙醚 为溶剂， 反应 0.8h， 以88%的产率得到N,N-bis(phosphinoethyl)methoxyethylamine
  参考文献：
  名称：

  INTERMEDIATE COMPOUND OF TECHNETIUM NITRIDE COMPLEX FOR RADIODIAGNOSTIC IMAGING

  摘要：

  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。

  公开号：

  US20100160615A1
• 作为产物：
  描述：

  乙烯基磷酸二乙酯 、 2-甲氧基乙胺 在 lithium perchlorate 作用下， 反应 24.0h， 以87%的产率得到N-methoxyethyl-N,N-bis(2-diethoxyphosphorylethyl)amine
  参考文献：
  名称：

  [EN] METHOD FOR LABELING OF SENSITIVE AND THERMOSENSITIVE TARGETING BIOMOLECULES WITH TECHNETIUM BASED COMPOUNDS
  [FR] PROCÉDÉ DE MARQUAGE DE BIOMOLÉCULES DE CIBLAGE SENSIBLES ET THERMOSENSIBLES À L'AIDE DE COMPOSÉS À BASE DE TECHNÉTIUM

  摘要：

  本发明涉及一种标签程序，用于在温和的反应条件下，将敏感和热敏感的靶向分子引入适用于试剂盒配方的基于[99mTc(N)(PNP)]的化合物中。

  公开号：

  WO2018109164A1

文献信息

• Method for labeling of sensitive and thermosensitive targeting biomolecules with technetium based compounds
  申请人：BRACCO IMAGING SPA

  公开号：US11160886B2

  公开（公告）日：2021-11-02

  The present invention relates to a labeling procedure for the incorporation, in mild reaction conditions, of sensitive and thermosensitive targeting molecules into a [99m Tc(N)(PNP)]-based compound suitable for a kit formulation.

  本发明涉及一种标记程序，用于在温和的反应条件下，将敏感的和热敏的靶向分子掺入适用于试剂盒配方的[99m Tc(N)(PNP)]基化合物中。
• WO2007/83395
  申请人：——

  公开号：——

  公开（公告）日：——
• WO2006/80993
  申请人：——

  公开号：——

  公开（公告）日：——
• 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.
• Water-Soluble [Tc(N)(PNP)] Moiety for Room-Temperature ^99mTc Labeling of Sensitive Target Vectors
  作者：Cristina Bolzati、Nicola Salvarese、Barbara Spolaore、Andrea Vittadini、Daniel Forrer、Sara Brunello、Simona Ghiani、Alessandro Maiocchi

  DOI：10.1021/acs.molpharmaceut.1c00816

  日期：2022.3.7