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Technetium-99m labeled isonitrile-containing FAPI derivative and preparation method and application thereof

A technology containing isonitriles and derivatives, which is applied in the field of FAPI derivatives and its preparation, and can solve problems such as short half-life

Active Publication Date: 2021-02-26
BEIJING NORMAL UNIVERSITY
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Problems solved by technology

[0003] Currently, a 68 Ga-labeled FAPI imaging agent [ 68 Ga]Ga-FAPI-04 has received extensive attention, and preclinical studies have shown that it has a high tumor-non-target tissue ratio and rapid clearance, but it is due to 68 The half-life of Ga is short (68min), which limits its clinical application to a certain extent

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  • Technetium-99m labeled isonitrile-containing FAPI derivative and preparation method and application thereof
  • Technetium-99m labeled isonitrile-containing FAPI derivative and preparation method and application thereof

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Embodiment Construction

[0035] The present invention is described in detail below by way of examples: a technetium-99m labeled isonitrile-containing FAPI derivative, the general structural formula of which is [ 99m Tc-(CN-FAPI) 6 ] + , its structural formula is as follows:

[0036]

[0037] In the structural formula: with 99m Tc + The core is the central core, and the carbon atoms of the isonitrile in the CN-FAPI ligand molecule and 99m Tc(I) coordinates to form a six-coordinated [ 99m Tc-(CN-FAPI) 6 ] + Complexes. n is an integer greater than or equal to 2.

[0038] The preparation method of the FAPI derivative containing isocyanide of technetium-99m label, its preparation steps are as follows:

[0039] a: Synthesis of ligand CN-FAPI:

[0040] 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. After the reaction, the solvent was distil...

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Abstract

The invention discloses a technetium-99m labeled isocyanide-containing FAPI derivative with a structural general formula of [99mTc-(CN-FAPI) 6] < + > and a preparation method and an application thereof. The [99mTc (CNFAPI) 6] < + > complex is obtained through two steps of synthesis of a ligand CN-FAPI and preparation of [99mTc-(CNFAPI) 6] < + >. The complex is simple and convenient to prepare, high in radiochemical purity and good in stability, has relatively high uptake and good retention at tumor parts of tumor-bearing mice, has specificity in tumor uptake, and is a novel tumor imaging agentwith popularization and application values.

Description

technical field [0001] The invention belongs to the field of radiopharmaceuticals, in particular to a technetium-99m-labeled isonitrile-containing FAPI derivative, a preparation method and application. Background technique [0002] The tumor microenvironment plays an extremely important role in the occurrence and development of tumors. Tumor-associated fibroblasts are an important part of the tumor microenvironment. They have strong proliferation, migration, secretion and synthesis capabilities, and play an important role in the proliferation, migration, immune escape, radiochemotherapy resistance and energy metabolism of tumor cells. Role. Fibroblast activation protein (FAP) is an important molecular marker on the surface of tumor-associated fibroblasts, because it is selectively expressed on the cell membrane of fibroblasts in most solid tumor stroma, and it can promote the proliferation of tumor cells, cell The degradation and reconstruction of extracellular matrix, the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00A61K51/04A61K103/10
CPCA61K51/0482C07B2200/05C07F13/00
Inventor 张俊波阮晴张旭冉冯俊红王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY
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