[18F]MEL6 | 1186533-85-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: [18F]MEL6
• 英文别名: N-[2-(diethylamino)ethyl]-2-(18F)fluoranylpyridine-3-carboxamide
• CAS: 1186533-85-6
• 化学式: C₁₂H₁₈FN₃O
• 分子量: 238.294
• InChiKey: QPKCGDHDEXCQNP-HSGWXFLFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  17
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  45.2
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-chloro-N-[2-(diethylamino)ethyl]nicotinamide 在 K[18F]-K_2.2.2 complex 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以55%的产率得到[18F]MEL6
  参考文献：
  名称：

  Discovery of [¹⁸F]N-(2-(Diethylamino)ethyl)-6-fluoronicotinamide: A Melanoma Positron Emission Tomography Imaging Radiotracer with High Tumor to Body Contrast Ratio and Rapid Renal Clearance

  摘要：

  The high melanoma uptake and rapid body clearance displayed by our series of [I-123]liodonicotinamides prompted the development of [F-18]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide ([F-18]2), a novel radiotracer for PET melanoma imaging. Significantly, unlike fluorobenzoates, [F-18]fluorine incorporation on the nicotinamide ring is one step, facile, and high yielding. [F-18]2 displayed high tumor uptake, rapid body clearance via predominantly renal excretion, and is currently being evaluated in preclinical studies for progression into clinical trials to assess the responsiveness of therapeutic agents.

  DOI：

  10.1021/jm9008423

文献信息

• Nicotinamide Derivatives
  申请人：Katsifis Andrew

  公开号：US20110178396A1

  公开（公告）日：2011-07-21

  A compound comprising a pyridine carboxamide structure, for use in imaging or treating melanoma, is described. An aromatic ring in the structure is substituted with a radiohalogen atom and the substitution on the amide nitrogen atom is such that the compound binds to melanin.

  描述了一种含有吡啶羧酰胺结构的化合物，用于成像或治疗黑色素瘤。结构中的芳香环被取代为一个放射性卤原子，酰胺氮原子上的取代使得该化合物与黑色素结合。
• Discovery of [¹⁸F]<i>N</i>-(2-(Diethylamino)ethyl)-6-fluoronicotinamide: A Melanoma Positron Emission Tomography Imaging Radiotracer with High Tumor to Body Contrast Ratio and Rapid Renal Clearance
  作者：Ivan Greguric、Stephen R. Taylor、Delphine Denoyer、Patrice Ballantyne、Paula Berghofer、Peter Roselt、Tien Q. Pham、Filomena Mattner、Thomas Bourdier、Oliver C. Neels、Donna S. Dorow、Christian Loc’h、Rodney J. Hicks、Andrew Katsifis

  DOI：10.1021/jm9008423

  日期：2009.9.10

  The high melanoma uptake and rapid body clearance displayed by our series of [I-123]liodonicotinamides prompted the development of [F-18]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide ([F-18]2), a novel radiotracer for PET melanoma imaging. Significantly, unlike fluorobenzoates, [F-18]fluorine incorporation on the nicotinamide ring is one step, facile, and high yielding. [F-18]2 displayed high tumor uptake, rapid body clearance via predominantly renal excretion, and is currently being evaluated in preclinical studies for progression into clinical trials to assess the responsiveness of therapeutic agents.