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A sort of 99m tco-tyrdtc complex and its preparation method and application

A 99mtco-gh, 99mtco-tyrdtc technology, applied in the field of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems that hinder wide application and high price

Inactive Publication Date: 2016-08-24
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

So far, radiolabeled amino acids and their derivatives, such as S-( 11 C-methyl)-L-methionine ( 11 C-MET), O-(2- 18 F-fluoroethyl)-L-tyrosine ( 18 F-FET), has been used in clinical tumor imaging research, but 11 C and 18 F needs to be produced by an accelerator, which is expensive, which to some extent hinders its wide application in clinical diagnosis, especially in economically underdeveloped countries and regions

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  • A sort of <sup>99m</sup> tco-tyrdtc complex and its preparation method and application
  • A sort of <sup>99m</sup> tco-tyrdtc complex and its preparation method and application
  • A sort of <sup>99m</sup> tco-tyrdtc complex and its preparation method and application

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Embodiment Construction

[0041] The present invention will be described in detail in the following examples:

[0042] A kind 99m TcO-TYRDTC complex preparation method, its representative general formula is 99m TcO-TYRDTC, the structural formula of its ligand TYRDTC is as follows:

[0043]

[0044] The preparation method is as follows:

[0045] a. Synthesis of ligand TYRDTC:

[0046] Add 1025mg (5.70mmol) of L-tyrosine and 456mg (11.4mmol) of NaOH to the reaction flask, use 10mL of anhydrous methanol as the solvent, stir to dissolve in an ice water bath, and add 5mL dropwise to dissolve 1mL (17.4mmol) of C8 2 After the dropwise addition is completed, react in an ice-water bath for 3 hours, filter with a sand core funnel and take the filtrate, add a small amount of water to the filtrate to separate layers, take the lower aqueous phase and extract three times with ethyl ether and ethyl acetate, and take water The phase rotation is evaporated and dried to obtain 0.81g of light yellow solid tyrosine dithiocarbamat...

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Abstract

The invention discloses a 99mTcO-TYRDTC complex with a representative general formula: 99mTcO-TYRDTC. The 99mTcO-TYRDTC complex is prepared through two process steps of synthesizing ligand TYRDTC and preparing 99mTcO-TYRDTC. The 99mTcO-TYRDTC complex is high in radiochemical purity, good in stability, favorable in tumor affinity, simple and convenient in preparation and wide in application to tumor imaging of human bodies and animals, thereby being a novel amino acid tumor imaging agent with popularization and application values.

Description

Technical field [0001] The invention relates to 99m Tc-labeled radiopharmaceutical chemistry and clinical nuclear medicine technology, specifically related to a 99m TcO-TYRDTC complex and its preparation method and application. Background technique [0002] Malignant tumors are currently one of the main diseases that endanger human health. The annual tumor morbidity and mortality are still on the rise. Early tumor diagnosis and personalized treatment are of great significance to saving patients' lives and prolonging their survival. Traditional non-invasive tumor detection and imaging methods such as X-ray, CT, MRI, etc., are mainly imaging the morphology and structure of organs under pathological conditions, while radionuclide molecular imaging technologies such as positron emission tomography (PET) ) And single photon emission tomography (SPECT) can reflect the changes in tumor physiology, pathology, metabolism and function. At present, with the organic fusion of PET / CT, SPECT / ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F13/00A61K51/04A61K103/10
Inventor 张俊波朱菁菁胡其然杜进陆洁王学斌唐志刚
Owner BEIJING NORMAL UNIVERSITY