bis[(diethoxypropylphosphanyl)ethyl]ethoxyethylamine | 395653-16-4

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: bis[(diethoxypropylphosphanyl)ethyl]ethoxyethylamine
• 英文别名: N,N-bis[2-[bis(3-ethoxypropyl)phosphanyl]ethyl]-2-ethoxyethanamine
• CAS: 395653-16-4
• 化学式: C₂₈H₆₁NO₅P₂
• 分子量: 553.744
• InChiKey: STECUQBEWMGSEJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  36
• 可旋转键数：
  30
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  49.4
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  bis[(diethoxypropylphosphanyl)ethyl]ethoxyethylamine 、 、 反应 0.5h， 生成
  参考文献：
  名称：

  Preparation and evaluation of a 99mTcN–PNP complex of sanazole analogue for detecting tumor hypoxia

  摘要：

  A sanazole derivative, having a favorable single electron reduction potential (SERP) value compared to that of misonidazole, was synthesized and radiolabeled with [(TcN)-Tc-99m(PNP)] precursor to evaluate its potential as a hypoxia imaging agent. The complex, which was lipophilic, could be prepared in good yields and challenging studies with cysteine showed stability of the complex against trans-chelation. However, despite being lipophilic as well as possessing favorable SERP value, biodistribution studies of this complex in fibrosarcoma tumor bearing Swiss mice showed low uptake in tumor. This observation is possibly attributed to fast clearance of the complex from blood, whereby the complex spends insufficient time in tumor to get reduced and trapped. Though uptake in tumor was low, slow clearance of activity from tumor suggests reduction and trapping of the complex in hypoxic cells. The present Tc-99m-complex demonstrated acceptable values of tumor to blood (TBR) and tumor to muscle (TMR) ratios. However, low uptake in tumor which may not be indicative of the actual hypoxic status of the tumor, limit the utility of the complex to detect tumor hypoxia. (c) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.12.079

文献信息

• RADIOPHARMACEUTICAL FOR DIAGNOSTIC IMAGING CONTAINING A TECHNETIUM-99M NITRIDE HETEROCOMPLEX
  申请人：NIHON MEDI-PHYSICS CO., LTD.

  公开号：EP1307239B1

  公开（公告）日：2008-10-08
• Novel cationic metal complex radiopharmaceuticals
  申请人：Liu Shuang

  公开号：US20080124273A1

  公开（公告）日：2008-05-29

  This invention relates to novel cationic crown-ether containing metal complexes, methods of preparing the cationic crown-ether containing metal complexes, and radiopharmaceutical compositions comprising the cationic crown-ether containing metal complexes. This invention relates particularly to cationic crown-ether containing 99m Tc complex radiopharmaceuticals for diagnosis of cardiovascular disorders and cancer. This invention further relates to cationic crown-ether containing 186/188 Re complex radiopharmaceuticals for radiotherapy of cardiovascular disorders and cancer.
• [EN] NOVEL CATIONIC METAL COMPLEX RADIOPHARMACEUTICALS<br/>[FR] RADIOPHARMACEUTIQUES A COMPLEXES METALLIQUES CATIONIQUES
  申请人：PURDUE RESEARCH FOUNDATION

  公开号：WO2006080993A1

  公开（公告）日：2006-08-03

  [EN] This invention relates to novel cationic crown-ether containing metal complexes, methods of preparing the cationic crown-ether containing metal complexes, and radiopharmaceutical compositions comprising the cationic crown-ether containing metal complexes. This invention relates to cationic crown-ether containing ^99m Tc complex radiopharmaceuticals for diagnosis of cardiovascular disorders and cancer. This invention further relates to cationic crown-ether containing ^186/188 Re complex radiopharmaceuticals for radiotherapy of cardiovascular disorders and cancer.
  [FR] L'invention concerne de nouveaux complexes métalliques contenant un éther couronne cationique, des procédés pour préparer ces complexes métalliques contenant un éther couronne cationique et des compositions radiopharmaceutiques comportant des complexes métalliques contenant un éther couronne cationique. La présente invention porte également sur des radiopharmaceutiques complexes ^99m Tc contenant un éther couronne cationique pour le diagnostic de troubles cardio-vasculaires et du cancer, ainsi que sur des radiopharmaceutiques complexes ^186/188 Re contenant un éther couronne cationique pour la radiothérapie de troubles cardio-vasculaires et du cancer.
• Preparation and evaluation of a 99mTcN–PNP complex of sanazole analogue for detecting tumor hypoxia
  作者：Anupam Mathur、Madhava B. Mallia、Sharmila Banerjee、H.D. Sarma、M.R.A. Pillai

  DOI：10.1016/j.bmcl.2012.12.079

  日期：2013.3

  A sanazole derivative, having a favorable single electron reduction potential (SERP) value compared to that of misonidazole, was synthesized and radiolabeled with [(TcN)-Tc-99m(PNP)] precursor to evaluate its potential as a hypoxia imaging agent. The complex, which was lipophilic, could be prepared in good yields and challenging studies with cysteine showed stability of the complex against trans-chelation. However, despite being lipophilic as well as possessing favorable SERP value, biodistribution studies of this complex in fibrosarcoma tumor bearing Swiss mice showed low uptake in tumor. This observation is possibly attributed to fast clearance of the complex from blood, whereby the complex spends insufficient time in tumor to get reduced and trapped. Though uptake in tumor was low, slow clearance of activity from tumor suggests reduction and trapping of the complex in hypoxic cells. The present Tc-99m-complex demonstrated acceptable values of tumor to blood (TBR) and tumor to muscle (TMR) ratios. However, low uptake in tumor which may not be indicative of the actual hypoxic status of the tumor, limit the utility of the complex to detect tumor hypoxia. (c) 2013 Elsevier Ltd. All rights reserved.