Technetium-99m-labeled isonitrile-containing PEG chain-modified fapi derivatives, preparation method and application

A technology of CN-PEG-FAPI and derivatives, which is applied in the field of FAPI derivatives and preparation, and can solve the problem of low uptake value

Active Publication Date: 2022-05-20
BEIJING NORMAL UNIVERSITY
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  • Abstract
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Problems solved by technology

Our research group developed a technetium-99m-labeled isocyanide-containing FAPI derivative in 2020 (patent application number: 202011382815.2), but the uptake of the drug in tumors is low and it is taken up in non-target organs such as liver and kidney Higher, so the performance is more excellent 99m Tc-labeled FAPI tumor imaging agent is worth developing

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  • Technetium-99m-labeled isonitrile-containing PEG chain-modified fapi derivatives, preparation method and application
  • Technetium-99m-labeled isonitrile-containing PEG chain-modified fapi derivatives, preparation method and application
  • Technetium-99m-labeled isonitrile-containing PEG chain-modified fapi derivatives, preparation method and application

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Embodiment Construction

[0029] The present invention is described in detail below through the examples: a technetium-99m-labeled isonitrile-containing PEG chain-modified FAPI derivative, the general structural formula of which is [ 99m Tc-(CN-PEG-FAPI) 6 ] + , its structural formula is as follows:

[0030]

[0031] In the structural formula: with 99m Tc +The core is the central core, and the carbon atom of the isonitrile in the ligand molecule of CN-PEG-FAPI and 99m Tc(I) coordinates to form a six-coordinated [ 99m Tc-(CN-PEG-FAPI) 6 ] + Complexes. n is an integer greater than 0.

[0032] A method for preparing FAPI derivatives modified by technetium-99m-labeled PEG chains containing isocyanides, the preparation steps are as follows:

[0033] a: Synthesis of ligand CN-PEG-FAPI:

[0034] Weigh an appropriate amount of FAPI into a round bottom flask, add an appropriate amount of DMF to dissolve, then add an appropriate amount of triethylamine and compound 1, and react at room temperature. ...

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Abstract

The invention discloses a general structural formula of [ 99m Tc‑(CN‑PEG‑FAPI) 6 ] + Technetium-99m-labeled isonitrile-containing PEG chain-modified FAPI derivatives, preparation method and application. Through the synthesis of ligand CN‑PEG‑FAPI and [ 99m Tc‑(CN‑PEG‑FAPI) 6 ] + The preparation of two steps, get [ 99m Tc‑(CN‑PEG‑FAPI) 6 ] + Complexes. The complex is easy to prepare, has high radiochemical purity and good stability, and has low non-target organ uptake in tumor-bearing mice, high uptake and good retention in tumor sites, and specific uptake in tumors. It is a new type of tumor imaging agent with popularization and application value.

Description

technical field [0001] The invention belongs to the field of radiopharmaceuticals, in particular to a technetium-99m labeled isonitrile-containing PEG chain-modified FAPI derivative, a preparation method and an application. Background technique [0002] Fibroblast activating protein (FAP) is an important target in tumor diagnosis and treatment in recent years, and the use of radionuclide-labeled fibroblast activating protein inhibitor (FAPI) and its derivatives as tumor radiopharmaceuticals has become a current research hotspot. Our research group developed a technetium-99m-labeled isocyanide-containing FAPI derivative in 2020 (patent application number: 202011382815.2), but the uptake of the drug in tumors is low and it is taken up in non-target organs such as liver and kidney Higher, so the performance is more excellent 99m Tc-labeled FAPI tumor imaging agent is worth developing. [0003] Polyethylene glycol (PEG) is a neutral, non-toxic high molecular polymer with uniq...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/12C07F13/00A61K51/06C08G65/333
CPCC07D401/12C07F13/005A61K51/065C08G65/33396Y02P20/55
Inventor 张俊波阮晴江雨豪冯俊红王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY
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