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
View PDF3 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

Examples

Experimental program
Comparison scheme
Effect test

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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C07F13/00A61K51/04A61P35/00A61K103/10
Inventor 汪建军杨晶
Owner LANZHOU UNIVERSITY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap