Thymidine derivates as well as preparation method and applications thereof in preparing tumor developing agents as ligand

A technology of thymidine derivatives and thymidine, which is applied in the field of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of high price and short half-life

Active Publication Date: 2011-10-19
JIANGSU INST OF NUCLEAR MEDICINE
View PDF2 Cites 8 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However 18 F-FLT is a positron tracer that requires an accelerator to generate fluorine (18), which is expensive; in contrast, 99m Tc has significant advantages such as short half-life (6.02 hours), suitable gamma-ray energy (140 keV), convenient acquisition from molybdenum-t

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
  • Thymidine derivates as well as preparation method and applications thereof in preparing tumor developing agents as ligand
  • Thymidine derivates as well as preparation method and applications thereof in preparing tumor developing agents as ligand
  • Thymidine derivates as well as preparation method and applications thereof in preparing tumor developing agents as ligand

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0029] The chemical structural formula of NHT:

[0030]

[0031] The reaction equation of NHT is as follows:

[0032] The preparation method of NHT is as follows:

[0033] (1) Synthesis of 3’,5’-bis(p-methylbenzoyl)-thymidine (product 1):

[0034] Add 8g of β-thymidine (33mmol) and 10g of DMAP (4.9mmol) into a 500mL three-neck flask, add 250mL of dichloromethane, and add 10mL of p-toluyl chloride dropwise under stirring conditions. After dropping, heat to reflux , continue to stir the reaction until the reaction solution becomes clear. After the reaction is complete, the reaction solution is cooled to room temperature, washed with water and dilute acetic acid respectively, and the organic layer is separated. After the organic layer is dried and concentrated with anhydrous sodium sulfate, it is washed with an equal volume of The mixed solvent of dichloromethane and ethyl acetate was recrystallized at room temperature for 3-4 hours to obtain 13.8 g of product 1 in the for...

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 thymidine derivates, belonging to the technical field of radiopharmaceutical chemistry and clinical nuclear medicine. A molecular formula of the derivates is N<3>-{N'-[(2-mercaptoethylamine)acetyl]-2-aminoethylsulphydryl-1-hexoamide}-thymidine (short for NHT). The invention further provides a preparation method for the thymidine derivates, as well as applications of the thymidine derivates in preparing tumor developing agents as ligand with <99m>Tc to form complex. Marker <99m>Tc in <99m>Tc-NHT has high radiochemical purity; lipd/water partition coefficient logP is 0.76; the stability is good; the safety of animal experiment is higher; and the ratios of radioactivity absorbed by tumor with radioactivity absorbed by muscle, radioactivity absorbed by bone and radioactivity absorbed by blood according to ID/g by percent are respectively 4.41, 2.45 and 1.51, therefore, the thymidine derivates can be used as a novel tumor developer for tumor diagnosis.

Description

technical field [0001] The invention relates to the technical fields of radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a thymidine derivative, its preparation method and its use as a ligand in the preparation of a tumor imaging agent. Background technique [0002] Tumor is one of the diseases that seriously threaten human life. Radionuclide imaging can reflect changes in the physiology, pathology, metabolism and function of tumors, and radionuclide imaging is a non-invasive detection method. Many advantages make radionuclide Imaging has become the main method of tumor diagnosis. [0003] Among them, radionuclide-labeled nucleosides are a class of molecular probes that develop rapidly, such as 18 F-labeled thymidines 18 F-FLT, 18 F-FLT indirectly reflects cell proliferation by reflecting DNA synthesis. Clinical studies have shown that 18 F-FLT has unique application prospects in the detection of tumor cell proliferation, such as chest tumor...

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): C07H19/073C07H1/00A61K51/04A61K103/10
Inventor 陆春雄蒋泉福
Owner JIANGSU INST OF NUCLEAR MEDICINE
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