Targeted probe for nuclide labeling and preparation method and application of targeted probe

A nuclide and targeting technology, applied in the field of medical imaging, can solve problems such as enlightenment or teaching, and no design ideas are given, and achieve the effects of increasing radioactivity concentration, improving pharmacokinetic properties, and strong labeling ability

Active Publication Date: 2015-08-12
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such a design method has not been reported in the prior art, and at the same time, no design inspiration or teaching has been given for such a design method in the prior art

Method used

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  • Targeted probe for nuclide labeling and preparation method and application of targeted probe
  • Targeted probe for nuclide labeling and preparation method and application of targeted probe
  • Targeted probe for nuclide labeling and preparation method and application of targeted probe

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1 - Synthesis of Folate-Targeted HYNIC Monomers

[0056]

[0057] 1)FA-N 3 Synthesis

[0058] I) Synthesis of FA-NHS: Dissolve folic acid in dimethyl sulfoxide, add N-hydroxysuccinimide (NHS) and dicyclohexylcarbodiimide (DCC), activate in the dark and filter.

[0059] II) FA-N 3 Synthesis of : add 3-azidopropylamine dropwise to the above-mentioned FA-NHS filtrate, add N,N-diisopropylethylamine (DIPEA), after the reaction is complete, drop into diethyl ether to precipitate a precipitate, collect the precipitate and dry it to obtain FA-N 3 .

[0060] 3)D 0 -Synthesis of HYNIC

[0061] I) Synthesis of HYNIC-NHS: Add 6-chloro-nicotine acid to an appropriate amount of 85% hydrazine hydrate, heat at high temperature to make it completely react, then cool and concentrate to obtain a light yellow solid. Dissolve the solid in water, adjust the pH to be weakly acidic with acid, filter after precipitation, wash the obtained solid with 95% ethanol and ether, and ...

Embodiment 2

[0065] Example 2 - Synthesis of PEG-modified folic acid targeting HYNIC monomer

[0066]

[0067] 1) FA-PEG-N 3 Synthesis

[0068] I) Synthesis of FA-NHS: Refer to Example 1 for the synthesis of FA-NHS.

[0069] II) Synthesis of FA-PEG: slowly drop the filtrate of FA-NHS into DMSO of 2,2'-(ethylene dioxy)bis(ethylamine), add N,N-diisopropylethylamine (DIPEA ), reaction 2d at room temperature. Add the reaction solution dropwise to a large amount of dichloromethane to produce a large amount of yellow precipitate, centrifuge or filter with a sand core funnel to obtain a solid, wash with dichloromethane and ether, and dry in a vacuum oven to obtain FA-PEG as a yellow powder solid.

[0070] III) Synthesis of FA-PEG-COOH: Dissolve 1 eq. FA-PEG in DMSO, add 2 eq. succinic anhydride and 0.5 eq. 4-dimethylaminopyridine (DMAP), react at room temperature for 2 d. Add the reaction solution dropwise to a large amount of dichloromethane to produce a large amount of yellow precipitate...

Embodiment 3

[0077] Example 3 - Synthesis of folic acid-targeted HYNIC polymers

[0078] 1) Molecular skeleton D n Synthesis

[0079]

[0080] I)D 0.5 The synthesis of: in ice-water bath, will be dissolved with propargylamine (D 0 ,) methanol solution was slowly added dropwise to excess methyl acrylate methanol solution, reacted at room temperature for 3d under nitrogen protection, concentrated under reduced pressure to obtain a yellow liquid (D 0.5 ).

[0081] II) D 1 Synthesis: In an ice-water bath, the D 0.5 Dissolved in methanol, slowly added dropwise to the methanol solution containing excess ethylenediamine under the protection of nitrogen, then stirred at room temperature for 3 days, concentrated to obtain light yellow liquid D 1 .

[0082] III) D 1.5 Synthesis: In an ice-water bath, D will be dissolved 1 Slowly added dropwise the methanol solution of excess methyl acrylate in the methanol solution, reacted at room temperature under nitrogen protection for 4d, and concentr...

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PUM

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Abstract

The invention discloses a targeted probe for nuclide labeling and a preparation method and an application of the targeted probe. A general structural formula of a complex is as shown in the specification, wherein R' is a nuclide chelating group; R is a targeted group; Dn is a molecular skeleton which is formed by repeated michael addition reaction and amidation reaction employing propargylamine as an initial reactant, the peripheral group is amino, n represents different algebras, and the numerical value of n is an integer greater than or equal to 0; and m is equal to 2n. A polymer in the targeted probe for nuclide labeling is beneficial to improvement of the specific activity; a high-quality developing result can be obtained by instrument scanning; the targeted probe can play a role in effectively monitoring tumors or inflammatory diseases; meanwhile, carrying of relatively many nuclides on a molecule is facilitated by the formed polymer; the nuclide concentration of focus location is improved; and the targeted probe plays a relatively good treatment role.

Description

technical field [0001] The invention belongs to the technical field of medical imaging, and in particular relates to a targeting probe for nuclide labeling, a preparation method and application thereof. Background technique [0002] Molecular imaging is known as medical imaging in the 21st century, because it can provide a strong guarantee for early detection, early diagnosis, and early treatment of diseases. Imaging probes with good targeting and specificity are the key to molecular imaging. Only by obtaining imaging agents with good performance can we better diagnose and treat diseases. [0003] In general, imaging probes consist of two main parts: a targeting group and a labeling group. The targeting group and the labeling group are linked in some chemical form. A good targeting group can smoothly bring the molecule to the disease site, which can achieve the desired effect. Taking folic acid as an example, many recent studies have used folic acid as a targeting molecul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C09K11/06C07D475/04C08G83/00A61K51/04A61K51/06
Inventor 张现忠郭志德宋曼莉高梦娜许多尤林怡
Owner XIAMEN UNIV
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