18F-labelled quinazolines irreversible EGFR (epidermal growth factor receptor) positive electron tracer agent, as well as preparation method and application thereof

A positron tracer, quinazoline technology, which is applied in the directions of biochemical equipment and methods, radioactive carriers, and the determination/inspection of microorganisms to simplify the synthesis process, improve the yield, and overcome the long synthesis time.

Active Publication Date: 2015-06-24
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 irreversible EGFR positron tracer;

Method used

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  • 18F-labelled quinazolines irreversible EGFR (epidermal growth factor receptor) positive electron tracer agent, as well as preparation method and application thereof
  • 18F-labelled quinazolines irreversible EGFR (epidermal growth factor receptor) positive electron tracer agent, as well as preparation method and application thereof
  • 18F-labelled quinazolines irreversible EGFR (epidermal growth factor receptor) positive electron tracer agent, as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0077] Example 1: [ 18 F] Synthesis of FH411 (shown in formula II)

[0078]

[0079] [ 18 F] Synthetic steps of FH411:

[0080] 1. Precursor (N-[4-(3-Chloro-4-fluorophenylamino)-7-(Tso-PEG(4))quinazoline-6-yl]-4-(dimethylamino)-2(E)-butenamide; (2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-(p-toluenesulfonyl-polyethylene glycol 4)quinazolin-6-yl]-4-( Dimethylamino)-2-butenamide, shown in formula I), this compound is delivered to Jiangsu Huayi Co., Ltd. for synthesis;

[0081] 2. Will transmit from the medical cyclotron 18 F ions and water are passed to the receiving bottle (1-4Ci);

[0082] 3. will 18 F ions and water pass to the anion exchange column QMA;

[0083] 4. 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, 3 mg precursor dissolved in 0.5 mL DMSO or DMF mixture was added to the reaction bottle; under the protection of nitrogen or helium, heated at 65 ° C for 3.5 minutes, and heated ...

Embodiment 218

[0089] Example 2 [ 18 F] Application of FH411 (shown in formula II) in detecting the expression level of epidermal growth factor receptor

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Abstract

The invention discloses an 18F-labelled quinazolines irreversible EGFR (epidermal growth factor receptor) positive electron tracer agent, as well as a preparation method and application thereof. The 18F-labelled quinazolines irreversible EGFR positive electron tracer agent has a chemical structure represented by the formula II. The synthesized 18F-labelled small-molecular irreversible EGFR positive electron tracer agent has a clinical value for diagnosing and monitoring a treating effect and particularly plays an important role in pushing individual-based treatment. Furthermore, the invention further provides a one-step method for synthesizing the 18F-labelled small-molecular irreversible EGFR positive electron tracer agent. The method has the characteristics of multiple purposes, high yield, high efficiency, short synthesis time, low cost and the like and can meet a requirement on large-scale production.

Description

[0001] Cross References to Related Applications [0002] This application requires an application on January 5, 2013, the application number is 201310002893.9, and the title of the invention is "a 18 F-labeled quinazoline-based irreversible EGFR positron tracers and their preparation methods and applications” is the 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/04C07D239/94C12Q1/06A61K101/02
Inventor 申宝忠
Owner HARBIN MEDICAL UNIVERSITY
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