Technetium-99m labeled hydrazine-based nicouramido-containing FAPI derivative as well as preparation method and application thereof

A nicotinamide group and derivative technology, which is applied in the field of FAPI derivatives and preparation, can solve the problems that the uptake value of tumors needs to be improved and the uptake is high.

Pending Publication Date: 2021-04-09
BEIJING NORMAL UNIVERSITY
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Problems solved by technology

In 2020, our research group developed a technetium-99m-labeled isocyanide-containing FAPI derivative (patent application number: 202011382815.2), but the drug has high uptake in non-target organs such as l

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  • Technetium-99m labeled hydrazine-based nicouramido-containing FAPI derivative as well as preparation method and application thereof
  • Technetium-99m labeled hydrazine-based nicouramido-containing FAPI derivative as well as preparation method and application thereof
  • Technetium-99m labeled hydrazine-based nicouramido-containing FAPI derivative as well as preparation method and application thereof

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[0029] The present invention is described in detail below by way of examples: a technetium-99m labeled FAPI derivative containing hydrazine-nicotinamide group, the general structural formula is 99m Tc(HYNIC-FAPI)(tricine / TPPTS), its structural formula is as follows:

[0030]

[0031] In the structural formula: the nitrogen atom on the hydrazine group in the HYNIC-FAPI molecule, the phosphorus atom in the co-ligand TPPTS, the oxygen atom and the nitrogen atom in the tricine and 99m Tc coordinates to get 99mTc(HYNIC-FAPI)(tricine / TPPTS) complex.

[0032] 99m The preparation method of Tc (HYNIC-FAPI) (tricine / TPPTS) complex, its preparation steps are as follows:

[0033] a. Synthesis of HYNIC-FAPI

[0034] Weigh 70 mg (0.15 mmol) of FAPI into a round bottom flask, add 1 mL of DMF to dissolve, then add 0.120 mL (0.90 mmol) of triethylamine and 70 mg (0.16 mmol) of compound 1, and react at 60°C for 24 hours. After the reaction, the solvent was distilled off under reduced pr...

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Abstract

The invention discloses a compound with a general formula of 99mTc (HYNIC-FAPI) (tricine/TPPTS) technetium-99 m labeled FAPI derivative containing hydrazino-nicotinamide, and a preparation method and application thereof. By two steps of synthesis of ligand HYNIC-FAPI and 99mtc (HYNIC-FAPI) (tricine/TPPTS) preparation, the 99mTc (HYNIC-FAPI) (tricine/TPPTS) complex is obtained. The complex has the advantages of simple preparation, high radiochemical purity and good stability, has high uptake and good detention at tumor parts of tumor-bearing mice, has specific uptake in tumors, and is a novel tumor radiopharmaceutical with clinical application value.

Description

technical field [0001] The invention belongs to the field of radiopharmaceuticals, in particular to a technetium-99m-labeled FAPI derivative containing hydrazino-nicotamide group, a preparation method and an application. Background technique [0002] Fibroblast activating protein (FAP) is a potential target for tumor detection and treatment. Radionuclide-labeled fibroblast activating protein inhibitor (FAPI) and its derivatives are used as tumor imaging agents and become the focus of current international radiopharmaceutical research. A big hit. In 2020, our research group developed a technetium-99m-labeled isocyanide-containing FAPI derivative (patent application number: 202011382815.2), but the drug has high uptake in non-target organs such as liver and kidney, and the uptake value of the tumor needs to be improved. Insufficient, so the development of better performance 99m Tc-labeled FAPI tumor imaging agent has important practical significance. [0003] In recent year...

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Application Information

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IPC IPC(8): C07F13/00C07B59/00A61K51/04A61K103/10
CPCA61K51/0482C07B59/004C07B2200/05C07F13/005
Inventor 张俊波阮晴张旭冉冯俊红江雨豪王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY
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