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18F labeled quinazoline class EGFR (Epidermal Growth Factor Receptor) positron tracer agent and preparation method and application thereof

A positron tracer and quinazoline technology, which is applied in the field of 18F-labeled small molecule aniline quinazoline EGFR positron tracers, and achieves the improvement of tumor uptake rate, convenient synthesis process, and improved hydrophilicity. Effect

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 EGFR positron tracer;

Method used

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  • 18F labeled quinazoline class EGFR (Epidermal Growth Factor Receptor) positron tracer agent and preparation method and application thereof
  • 18F labeled quinazoline class EGFR (Epidermal Growth Factor Receptor) positron tracer agent and preparation method and application thereof
  • 18F labeled quinazoline class EGFR (Epidermal Growth Factor Receptor) positron tracer agent and preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0075] Example 1: [ 18 Synthesis of F] FH41 (shown in formula II)

[0076]

[0077] Formula I

[0078]

[0079] Formula II

[0080] Synthetic steps:

[0081] 1. Precursor (N-(3-chloro-4-fluorophenyl)-6-methoxy-7-(Tso-polyethyleneglycol(4))quinazolin-4-amine, N-(3-chloro-4-fluorophenyl) -6-methoxy-7-(p-methylbenzenesulfonyl-polyethylene glycol 4)-quinazolin-4-amine, represented by formula I), the compound was sent to Jiangsu Huayi Co., Ltd. for synthesis;

[0082] 2. Will transmit from the medical cyclotron 18 F ions and water are passed to the receiving bottle (1-4Ci);

[0083] 3. will 18 F ions and water pass to the anion exchange column QMA;

[0084] 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, 3mg precursor (formula I) was dissolved in 0.5mL DMSO solution and then added to the reaction bottle; heated at 65°C for 3.5 minutes under the protection of nitrogen or helium, microwave ...

Embodiment 218

[0090] Example 2 [ 18 F] Application of FH41 (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 class EGFR (Epidermal Growth Factor Receptor) positron tracer agent and a preparation method and application thereof and belongs to the field of chemical synthesis. The 18F labeled quinazoline class EGFR positron tracer agent has a chemical structure as shown in a formula II. The synthesized 18F labeled micro-molecular EGFR class positron tracer agent has the clinic values of diagnosis and therapeutic effect monitoring and particularly plays an important role in promoting personalized treatment. Besides, the invention further provides a one-step method, namely a method for fully-automatically synthesizing the 18F labeled quinazoline class EGFR positron 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 the requirements of large-scale production. The formula II is shown below.

Description

[0001] Cross References to Related Applications [0002] This application requires application on January 5, 2013, the application number is 201310002892.4, 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-labeled ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/00C07D239/94C12Q1/06A61K101/02
Inventor 申宝忠
Owner HARBIN MEDICAL UNIVERSITY
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