Technetium-99m-labeled isonitrile-containing ferrichomide derivative as well as preparation method and application thereof

A technology for ferrioxamine and its derivatives, which is applied in the field of technetium-99m-labeled isocyanide-containing ferrioxamine derivatives and its preparation, achieving the effects of good stability, good inflammation/muscle ratio, and easy preparation

Active Publication Date: 2022-04-15
BEIJING NORMAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Technetium-99m-labeled ferrioxamine has not been reported as a radiopharmaceutical for the diagnosis of bacterial

Method used

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  • Technetium-99m-labeled isonitrile-containing ferrichomide derivative as well as preparation method and application thereof
  • Technetium-99m-labeled isonitrile-containing ferrichomide derivative as well as preparation method and application thereof
  • Technetium-99m-labeled isonitrile-containing ferrichomide derivative as well as preparation method and application thereof

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Embodiment Construction

[0045] Describe the present invention in detail below by embodiment: a kind of 99m Tc-CNFO complex, its structural formula is as follows:

[0046]

[0047] In the structural formula: with 99m Tc + The core is the central core, and the carbon atom of the isonitrile in the CNFO ligand molecule and 99m Tc coordinates to form a hexacoordinated 99m Tc-CNFO complex. However, n represents an integer of 2 or more.

[0048] a. Synthesis of Ligand CNFO:

[0049] Weigh 6.4mg (0.16mmol) of sodium hydroxide in a round bottom flask, add 10mL of methanol to dissolve, then add 104mg (0.16mmol) of deferoxamine mesylate, after the dissolution is complete, dropwise add 69mg (0.24mmol) of the compound 1 (n=5) in dichloromethane solution, react overnight at room temperature, after the reaction, concentrate the mother liquor, precipitate out after cooling, filter to obtain a filter cake, wash with an appropriate amount of dichloromethane, and dry to obtain a white solid compound 2 (55mg) ...

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Abstract

The invention discloses a < 99m > Tc-labeled isonitrile-containing ferricyanide derivative and a preparation method and application thereof, ferricyanide with bacterial specificity (Ferrioxamine B) is converted into isonitrile ferricyanide (CNFO) capable of being complexed with < 99m > Tc, and a < 99m > Tc-CNFO complex is obtained through a preparation process that isonitrile groups in a CNFO ligand are coordinated with < 99m > Tc. The complex is a hydrophilic substance, is high in radiochemical purity, good in stability, simple and convenient to prepare, high in uptake and good in retention at bacterial inflammation parts, good in inflammation/muscle ratio, capable of distinguishing bacterial inflammation and non-bacterial inflammation, and capable of serving as a novel bacterial inflammation imaging agent to be popularized and applied.

Description

Technical field: [0001] The invention relates to the technical fields of radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a technetium-99m-labeled isonitrile-containing ferrioxamine derivative, a preparation method and an application. Background technique: [0002] In recent years, nuclear medicine imaging such as Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET) has been fully developed, and nuclear medicine imaging can accurately locate the lesion area , reflecting the pathophysiological changes of inflammation, it is helpful to find out the etiology and make a targeted treatment plan, with high sensitivity and strong specificity. With the development of nuclear medicine imaging, the preparation and development of safe and effective bacterial inflammation imaging agents has become an urgent need for current clinical research. Bacteria and other microorganisms have specific iron metabolism, and will secre...

Claims

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Application Information

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IPC IPC(8): C07F19/00C07B59/00A61K51/04A61K103/10
CPCY02P20/55
Inventor 张俊波江雨豪王倩娜王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY
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