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Carbonyl-technetium-labeled chlorambucil complex as well as preparation method and application thereof

A technology of chlorambucil and complexes, which is applied in the field of radionuclide-labeled compounds, can solve the problems of high cost, limitation, and short half-life of FDG synthesis, and achieve good tumor uptake and retention effects

Inactive Publication Date: 2012-01-11
LANZHOU UNIVERSITY
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Problems solved by technology

but,[ 18 F] FDG is a non-specific tumor diagnostic drug, and there are "false positive" and "false negative" imaging results; 18 F is an accelerator-produced nuclide with a short half-life (109.8min), [ 18 F] FDG is expensive to synthesize; these limit [ 18 F] Application of FDG PET imaging in the diagnosis of tumor

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  • Carbonyl-technetium-labeled chlorambucil complex as well as preparation method and application thereof
  • Carbonyl-technetium-labeled chlorambucil complex as well as preparation method and application thereof
  • Carbonyl-technetium-labeled chlorambucil complex as well as preparation method and application thereof

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Embodiment Construction

[0022] The present invention will be further described below through specific embodiments, but it does not mean to limit the protection scope of the present invention.

[0023] Synthesis of L-Histidine-Coupled Chlorambucil Ligand

[0024] Compound 2: Compound 1, chlorambucil (500mg, 1.64mmol), NHS (227.7mg, 1.98mmol) and DCC (407.9mg, 1.98mmol) were dissolved in 10mL acetonitrile, stirred at room temperature for 24h, and the white solid was removed by suction filtration , the solvent was removed under reduced pressure and purified by silica gel column to obtain 571 mg (1.42 mmol, 86.6%) of light yellow oil. 1 H NMR (400MHz, CDCl 3 ): δ=2.04(m, 2H), 2.62(m, 4H), 2.85(d, 4H), 3.63(t, 4H), 3.72(t, 4H), 6.66(d, 2H), 7.10(d, 2H), ppm.ESI-MS: 401.6 ([M+H] + )

[0025] Ligand His-CB: Dissolve L-histidine (38.8 mg, 0.25 mmol) in 1 mL of water, adjust the pH to 9 with 1N NaOH solution, add compound 2 (93.7 mg, 0.234 mmol) in 1 mL of DMF, Mix evenly, add an appropriate amount of ly...

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Abstract

The invention discloses a radioactive-nuclide-labeled compound, namely a carbonyl-technetium-labeled chlorambucil complex as well as a preparation method and an application thereof. The preparation method of the carbonyl-technetium-labeled chlorambucil complex comprises chlorambucil (CB) and L-histidine (L-His) are coupled so as to obtain novel ligand His-CB, and then the ligand and [<99m>Tc(CO)3(H2O)]<+> intermediate are reacted, thereby obtaining the carbonyl-technetium-labeled chlorambucil complex. The carbonyl-technetium-labeled chlorambucil complex disclosed by the invention has the advantages of better tumor ingestion and detention effects, rapid removal of normal tissues and organs and good target / non-target ratio, and can be used for SPECT (single photon emission computed tomography) imaging diagnosis of tumor.

Description

technical field [0001] The present invention relates to a compound labeled with radionuclide, as well as the preparation method and application of the compound, specifically, the present invention relates to carbonyl technetium-labeled chlorambucil complex. Background technique [0002] Malignant tumor is one of the main diseases that lead to abnormal death of human beings. Early diagnosis and treatment of cancer are crucial to improving the cure rate and quality of life of patients. The most important application value of radiopharmaceuticals is the study of physiological and chemical changes in the life process; PET or SPECT imaging using radionuclide-labeled biological functional molecules can non-invasively diagnose various diseases in vivo, and is the most active molecular imaging in recent years. research field. [ 18 F] FDG (fluorodeoxyglucose) is currently the most successful molecular probe used in clinical nuclear medicine for tumor diagnosis, and has the advanta...

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Application Information

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IPC IPC(8): C07F13/00A61K51/04A61P35/00A61K103/10
Inventor 汪建军杨晶
Owner LANZHOU UNIVERSITY
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