1-amidino-4-(4-iodophenyl)piperazine | 96530-60-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-amidino-4-(4-iodophenyl)piperazine
• 英文别名: 4-(4-Iodophenyl)-1-piperazinecarboximidamide；4-(4-iodophenyl)piperazine-1-carboximidamide
• CAS: 96530-60-8
• 化学式: C₁₁H₁₅IN₄
• 分子量: 330.171
• InChiKey: UICUEJBIRBOWHR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  56.4
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  N-苯基哌嗪 在 一氯化碘 作用下， 以 水 、 溶剂黄146 、 二甲基亚砜 为溶剂， 反应 2.0h， 生成 1-amidino-4-(4-iodophenyl)piperazine
  参考文献：
  名称：

  4-（4-碘苯基）哌嗪和1-羧酰胺基衍生物的合成

  摘要：

  以70％的产率合成了先前未报道的4-（4-碘苯基）哌嗪（2）并对其进行了表征。2与S-甲基硫脲硫酸盐的反应以61％的收率得到相应的羧酰胺基衍生物4。4的tlc特性与已制备并评估为潜在心肌成像放射性药物的放射性碘标记材料的tlc特性相同。

  DOI：

  10.1002/jhet.5570220112

文献信息

• Ligands for imaging cardiac innervation
  申请人：Lantheus Medical Imaging, Inc.

  公开号：US10010631B2

  公开（公告）日：2018-07-03

  Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

  本研究公开了在核医学应用（PET 成像）中用作心脏神经支配成像剂的新型化合物。这些基于 PET 的放射性racer 与之前的放射性racer 相比，可表现出更高的稳定性、更少的 NE 释放（从而减少副作用）、更好的定量数据和/或对 VMAT 的高亲和力。还提供了使用这些化合物对心脏神经支配进行成像的方法。在某些情况下，这些化合物是通过在芳基、烷基、酮基、苄基、β-烷基醚、γ-丙基烷基醚和β-丙烯基烷基醚等不同位置上用 18F 对某些化合物进行衍生而得到的。另外，还可以在胺中加入甲基，和/或消除或掩盖儿茶酚官能团，使这些化合物更加稳定。
• HANSON, R. N.;HARIHARAN, SHANKAR;ASTIK, RAMESH, J. HETEROCYCL. CHEM., 1985, 22, N 1, 47-48
  作者：HANSON, R. N.、HARIHARAN, SHANKAR、ASTIK, RAMESH

  DOI：——

  日期：——
• NEURONAL IMAGING AND TREATMENT
  申请人：Tylerton International Holdings Inc.

  公开号：EP2948188B1

  公开（公告）日：2021-09-08
• [EN] NEURONAL IMAGING AND TREATMENT<br/>[FR] IMAGERIE NEURONALE ET TRAITEMENT
  申请人：TYLERTON INTERNAT HOLDINGS INC

  公开号：WO2014115152A1

  公开（公告）日：2014-07-31

  A method is disclosed herein for imaging at least one autonomic nervous system synaptic center in a subject, as well as a method of diagnosing and/or monitoring a medical condition or disease associated with an autonomic nervous system, and a method of guiding a therapy of such a medical condition or disease. The methods comprise administering to the subject a radioactive tracer which selectively binds to autonomic nervous system synapses; measuring radioactive emission of the tracer to obtain data describing a distribution of the tracer in the body; and analyzing the data in order to identify at least one region exhibiting a high concentration of the tracer. Further disclosed herein are radioactive tracers, uses thereof, and an apparatus, for use in a method disclosed herein.