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18F-labeled quinazoline type EGFR (epidermal growth factor receptor) positron tracer, as well as preparation method and application thereof

A technology of positron tracers and quinazolines, which is applied in biochemical equipment and methods, measurement/testing of microorganisms, organic chemistry, etc., to overcome long synthesis time, reduce uptake rate, and improve synthesis efficiency

Active Publication Date: 2014-04-02
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0023] For the existing problems, one of the technical problems to be solved by the present invention is to provide a [ 18 F] labeled EGFR positron tracer;

Method used

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  • 18F-labeled quinazoline type EGFR (epidermal growth factor receptor) positron tracer, as well as preparation method and application thereof
  • 18F-labeled quinazoline type EGFR (epidermal growth factor receptor) positron tracer, as well as preparation method and application thereof
  • 18F-labeled quinazoline type EGFR (epidermal growth factor receptor) positron tracer, as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Example 1: [ 18 F] Synthesis of FH42 (shown in formula II)

[0074]

[0075] Synthetic steps:

[0076] 1. Precursor (N-(3-chloro-4-fluorophenyl)-7-(Tso-PEG(4))-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine, N-(3- Chloro-4-fluorophenyl)-7-(p-toluenesulfonyl-polyethylene glycol 4)-6-(3-morpholine-4-propoxy)quinazolin-4-amine, shown in formula I ), the compound was sent to Jiangsu Huayi Co., Ltd. for synthesis;

[0077] 2. Will transmit from the medical cyclotron 18 F ions and water are passed to the receiving bottle (1-4Ci);

[0078] 2. Will 18 F ions and water pass to the anion exchange column QMA;

[0079] 3. Using 0.15mL K 2 CO 3 (0.9mg) + 0.5mL acetonitrile was eluted from the QMA column 18 F ion and sent to the reaction bottle, the mixture of 5mg precursor dissolved in 0.5mL DMSO was added to the reaction bottle; under the protection of nitrogen or helium, heated at 65°C for 3.5 minutes, and microwaved at 90°C for 10 minutes;

[0080] 4. Cool the tempera...

Embodiment 2

[0085] Example 2[ 18 F] Application of FH42 (shown in formula II) in detecting the expression level of epidermal growth factor receptor

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Abstract

The invention discloses an 18F-labeled quinazoline type EGFR (epidermal growth factor receptor) positron tracer, as well as a preparation method and an application thereof and belongs to the field of chemical synthesis. The 18F-labeled quinazoline type EGFR positron tracer disclosed by the invention has a chemical structure as shown in a formula II. The synthesized 18F-labeled small molecular EGFR type positron tracer has clinical value of diagnosis and monitoring of treatment curative effect and particularly plays an important role in promoting personalized treatment. In addition, the invention further provides the method for full-automatic synthesis of the 18F-labeled quinazoline type EGFR positron tracer by one step, the method has the characteristics of multiple purposes, large yield, high efficiency, short synthesis time, low cost and the like, and the requirements of large-scale production can be further met.

Description

[0001] Cross References to Related Applications [0002] This application requires an application on January 5, 2013, the application number is 201310002891.X, and the title of the invention is " 18 F-labeled quinazoline EGFR positron tracer and its preparation method and application” priority of the Chinese patent application, the description of which is incorporated herein by reference in its entirety. technical field [0003] The present invention relates to a kind of fluorination substitution reaction synthesis 18 F-labeled small molecule aniline quinazoline EGFR positron tracer and its preparation method and application. The invention belongs to the field of chemical synthesis. Background technique [0004] Positron nuclides produced by medical cyclotrons are currently used clinically 15 O. 13 N. 11 C. 18 F 18 F has a half-life of 110 minutes and has become the most clinically valued positron nuclide. 11 C due to the half-life of only 20 minutes. so 11 C-label...

Claims

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Application Information

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IPC IPC(8): A61K51/04C07D239/94C12Q1/06A61K101/02
Inventor 申宝忠
Owner HARBIN MEDICAL UNIVERSITY
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